Basic Description

Product Name	Recombinant p38 alpha/MAPK14 Antibody - Primary antibody, specific to p38 alpha/MAPK14, Rabbit IgG
Synonyms	CSAID-binding protein antibody; Csaids binding protein antibody; CSBP antibody; CSBP1 antibody; CSBP2 antibody; CSPB1 antibody; Cytokine suppressive anti-inflammatory drug-binding protein antibody; EXIP antibody; MAP kinase 14 antibody; MAP kinase MXI2 an
Specifications & Purity	ExactAb™, Validated, Recombinant, 0.3 mg/mL
Host species	Rabbit
Specificity	p38 alpha/MAPK14
Immunogen	A synthetic peptide derived from human p38 (AA 337-3550).
Positive Control	WB: HeLa, Jurkat, MCF7 and HEK293 cell lysates.
Conjugation	Unconjugated
Grade	ExactAb™, Recombinant, Validated
Product Description	Rabbit anti Human p38 alpha/MAPK14 Antibody, Recombinant, could be used for WB and so on. Application: WB: 1/500-1/1000 Protein Function : Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK14 is one of the four p38 MAPKs which play an important role in the cascades of cellular responses evoked by extracellular stimuli such as proinflammatory cytokines or physical stress leading to direct activation of transcription factors. Accordingly, p38 MAPKs phosphorylate a broad range of proteins and it has been estimated that they may have approximately 200 to 300 substrates each. Some of the targets are downstream kinases which are activated through phosphorylation and further phosphorylate additionnal targets. RPS6KA5/MSK1 and RPS6KA4/MSK2 can directly phosphorylate and activate transcription factors such as CREB1, ATF1, the NF-kappa-B isoform RELA/NFKB3, STAT1 and STAT3, but can also phosphorylate histone H3 and the nucleosomal protein HMGN1. RPS6KA5/MSK1 and RPS6KA4/MSK2 play important roles in the rapid induction of immediate-early genes in response to stress or mitogenic stimuli, either by inducing chromatin remodeling or by recruiting the transcription machinery. On the other hand, two other kinase targets, MAPKAPK2/MK2 and MAPKAPK3/MK3, participate in the control of gene expression mostly at the post-transcriptional level, by phosphorylating ZFP36 (tristetraprolin) and ELAVL1, and by regulating EEF2K, which is important for the elongation of mRNA during translation. MKNK1/MNK1 and MKNK2/MNK2, two other kinases activated by p38 MAPKs, regulate protein synthesis by phosphorylating the initiation factor EIF4E2. MAPK14 interacts also with casein kinase II, leading to its activation through autophosphorylation and further phosphorylation of TP53/p53. In the cytoplasm, the p38 MAPK pathway is an important regulator of protein turnover. For example, CFLAR is an inhibitor of TNF-induced apoptosis whose proteasome-mediated degradation is regulated by p38 MAPK phosphorylation. In a similar way, MAPK14 phosphorylates the ubiquitin ligase SIAH2, regulating its activity towards EGLN3. MAPK14 may also inhibit the lysosomal degradation pathway of autophagy by interfering with the intracellular trafficking of the transmembrane protein ATG9. Another function of MAPK14 is to regulate the endocytosis of membrane receptors by different mechanisms that impinge on the small GTPase RAB5A. In addition, clathrin-mediated EGFR internalization induced by inflammatory cytokines and UV irradiation depends on MAPK14-mediated phosphorylation of EGFR itself as well as of RAB5A effectors. Ectodomain shedding of transmembrane proteins is regulated by p38 MAPKs as well. In response to inflammatory stimuli, p38 MAPKs phosphorylate the membrane-associated metalloprotease ADAM17. Such phosphorylation is required for ADAM17-mediated ectodomain shedding of TGF-alpha family ligands, which results in the activation of EGFR signaling and cell proliferation. Another p38 MAPK substrate is FGFR1. FGFR1 can be translocated from the extracellular space into the cytosol and nucleus of target cells, and regulates processes such as rRNA synthesis and cell growth. FGFR1 translocation requires p38 MAPK activation. In the nucleus, many transcription factors are phosphorylated and activated by p38 MAPKs in response to different stimuli. Classical examples include ATF1, ATF2, ATF6, ELK1, PTPRH, DDIT3, TP53/p53 and MEF2C and MEF2A. The p38 MAPKs are emerging as important modulators of gene expression by regulating chromatin modifiers and remodelers. The promoters of several genes involved in the inflammatory response, such as IL6, IL8 and IL12B, display a p38 MAPK-dependent enrichment of histone H3 phosphorylation on 'Ser-10' (H3S10ph) in LPS-stimulated myeloid cells. This phosphorylation enhances the accessibility of the cryptic NF-kappa-B-binding sites marking promoters for increased NF-kappa-B recruitment. Phosphorylates CDC25B and CDC25C which is required for binding to 14-3-3 proteins and leads to initiation of a G2 delay after ultraviolet radiation. Phosphorylates TIAR following DNA damage, releasing TIAR from GADD45A mRNA and preventing mRNA degradation. The p38 MAPKs may also have kinase-independent roles, which are thought to be due to the binding to targets in the absence of phosphorylation. Protein O-Glc-N-acylation catalyzed by the OGT is regulated by MAPK14, and, although OGT does not seem to be phosphorylated by MAPK14, their interaction increases upon MAPK14 activation induced by glucose deprivation. This interaction may regulate OGT activity by recruiting it to specific targets such as neurofilament H, stimulating its O-Glc-N-acylation. Required in mid-fetal development for the growth of embryo-derived blood vessels in the labyrinth layer of the placenta. Also plays an essential role in developmental and stress-induced erythropoiesis, through regulation of EPO gene expression. Isoform MXI2 activation is stimulated by mitogens and oxidative stress and only poorly phosphorylates ELK1 and ATF2. Isoform EXIP may play a role in the early onset of apoptosis.

Product Properties

Isotype	Rabbit IgG
SDS-PAGE	150 kDa
Purification Method	Antigen affinity purified
Form	Liquid
Concentration	0.3 mg/mL
Storage Temp	Store at -20°C,Avoid repeated freezing and thawing
Shipped In	Ice chest + Ice pads
Stability And Storage	Store at 4°C short term (1-2 weeks). Store at -20°C long term (24 months). Upon delivery aliquot. Avoid freeze/thaw cycle.

Images

Recombinant p38 alpha/MAPK14 Antibody (Ab119717) - Western Blot
All lanes: Recombinant p38 alpha/MAPK14 Antibody (Ab119717) at 1/1000 dilution
Samples: Lysates at 20 µg per lane
Secondary: Goat Anti-Rabbit IgG H&L (HRP) (Ab170144) at 1/20000 dilution

Predicted band size: 41 kDa
Observed band size: 41 kDa
Exposure time: 60.5 s

Associated Targets(Human)

MAPK14 Tchem Mitogen-activated protein kinase 14 (0 Activities)

Discover Target: MAPK14

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)

Discover Target: MAPK14

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Application

Application	Dilution info
WB	1/500-1/1000

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

2 results found

Lot Number	Certificate Type	Date	Item
ZJ24F0202797	Certificate of Analysis	Feb 23, 2024	Ab119717
ZJ24F0202798	Certificate of Analysis	Feb 23, 2024	Ab119717

Citations of This Product

1. Zhu P,Qian J,Xu Z,Meng C,Liu J,Shan W,Zhu W,Wang Y,Yang Y,Zhang W,Zhang Y,Ling Y. (2020) Piperlonguminine and Piperine Analogues as TrxR Inhibitors that Promote ROS and Autophagy and Regulate p38 and Akt/mTOR Signaling.. J Nat Prod, 83 (10.0): (3041-3049). [PMID:33026807]

References

1. Lee JC, Laydon JT, McDonnell PC, Gallagher TF, Kumar S, Green D, McNulty D, Blumenthal MJ, Heys JR, Landvatter SW. (1994) A protein kinase involved in the regulation of inflammatory cytokine biosynthesis.. Nature, 372 (6508): (739-46). [PMID:7997261]
2. Huber K, Brault L, Fedorov O, Gasser C, Filippakopoulos P, Bullock AN, Fabbro D, Trappe J, Schwaller J, Knapp S et al.. (2012) 7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.. J Med Chem, 55 (1): (403-13). [PMID:22136433]
3. Soth M, Hermann JC, Yee C, Alam M, Barnett JW, Berry P, Browner MF, Frank K, Frauchiger S, Harris S et al.. (2013) 3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.. J Med Chem, 56 (1): (345-56). [PMID:23214979]
4. Alevy YG, Patel AC, Romero AG, Patel DA, Tucker J, Roswit WT, Miller CA, Heier RF, Byers DE, Brett TJ et al.. (2012) IL-13-induced airway mucus production is attenuated by MAPK13 inhibition.. J Clin Invest, 122 (12): (4555-68). [PMID:23187130]
5. Adrián FJ, Ding Q, Sim T, Velentza A, Sloan C, Liu Y, Zhang G, Hur W, Ding S, Manley P et al.. (2006) Allosteric inhibitors of Bcr-abl-dependent cell proliferation.. Nat Chem Biol, 2 (2): (95-102). [PMID:16415863]
6. Greenman C, Stephens P, Smith R, Dalgliesh GL, Hunter C, Bignell G, Davies H, Teague J, Butler A, Stevens C et al.. (2007) Patterns of somatic mutation in human cancer genomes.. Nature, 446 (7132): (153-8). [PMID:17344846]
7. Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM et al.. (2004) Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.. J Med Chem, 47 (27): (6658-61). [PMID:15615512]
8. Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Müller A, Baumgartner C, Valent P, Augustin M et al.. (2009) Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.. Leukemia, 23 (3): (477-85). [PMID:19039322]
9. Mirzoeva S, Sawkar A, Zasadzki M, Guo L, Velentza AV, Dunlap V, Bourguignon JJ, Ramstrom H, Haiech J, Van Eldik LJ et al.. (2002) Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound.. J Med Chem, 31 (45): (563-6). [PMID:11806708]
10. Ballou LM, Selinger ES, Choi JY, Drueckhammer DG, Lin RZ. (2007) Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.. J Biol Chem, 282 (33): (24463-70). [PMID:17562705]
11. Davis T, Bagley MC, Dix MC, Murziani PG, Rokicki MJ, Widdowson CS, Zayed JM, Bachler MA, Kipling D. (2007) Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells.. Bioorg Med Chem Lett, 17 (24): (6832-5). [PMID:17964780]
12. Oyarzabal J, Zarich N, Albarran MI, Palacios I, Urbano-Cuadrado M, Mateos G, Reymundo I, Rabal O, Salgado A, Corrionero A et al.. (2010) Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.. J Med Chem, 53 (18): (6618-28). [PMID:20722422]
13. Gavrin LK, Green N, Hu Y, Janz K, Kaila N, Li HQ, Tam SY, Thomason JR, Gopalsamy A, Ciszewski G et al.. (2005) Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.. Bioorg Med Chem Lett, 15 (23): (5288-92). [PMID:16165349]
14. Goldstein DM, Kuglstatter A, Lou Y, Soth MJ. (2010) Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.. J Med Chem, 53 (6): (2345-53). [PMID:19950901]
15. Chen F, Hancock CN, Macias AT, Joh J, Still K, Zhong S, MacKerell Jr AD, Shapiro P. (2006) Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure.. Bioorg Med Chem Lett, 16 (24): (6281-7). [PMID:17000106]
16. Selness SR, Devraj RV, Devadas B, Walker JK, Boehm TL, Durley RC, Shieh H, Xing L, Rucker PV, Jerome KD et al.. (2011) Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.. Bioorg Med Chem Lett, 21 (13): (4066-71). [PMID:21641211]
17. Devadas B, Selness SR, Xing L, Madsen HM, Marrufo LD, Shieh H, Messing DM, Yang JZ, Morgan HM, Anderson GD et al.. (2011) Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.. Bioorg Med Chem Lett, 21 (13): (3856-60). [PMID:21620699]
18. Aston NM, Bamborough P, Buckton JB, Edwards CD, Holmes DS, Jones KL, Patel VK, Smee PA, Somers DO, Vitulli G et al.. (2009) p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.. J Med Chem, 52 (20): (6257-69). [PMID:19772287]
19. Liu C, Lin J, Wrobleski ST, Lin S, Hynes J, Wu H, Dyckman AJ, Li T, Wityak J, Gillooly KM et al.. (2010) Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.. J Med Chem, 53 (18): (6629-39). [PMID:20804198]
20. Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H et al.. (2011) Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.. J Med Chem, 54 (20): (7066-83). [PMID:21936542]
21. Reinhardt HC, Aslanian AS, Lees JA, Yaffe MB. (2007) p53-deficient cells rely on ATM- and ATR-mediated checkpoint signaling through the p38MAPK/MK2 pathway for survival after DNA damage.. Cancer Cell, 11 (2): (175-89). [PMID:17292828]
22. Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P et al.. (2006) 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.. J Med Chem, 49 (24): (7247-51). [PMID:17125279]
23. Engler TA, Henry JR, Malhotra S, Cunningham B, Furness K, Brozinick J, Burkholder TP, Clay MP, Clayton J, Diefenbacher C et al.. (2004) Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.. J Med Chem, 47 (16): (3934-7). [PMID:15267232]
24. Mader M, de Dios A, Shih C, Bonjouklian R, Li T, White W, López de Uralde B, Sánchez-Martinez C, del Prado M, Jaramillo C et al.. (2008) Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38alpha MAP kinase inhibitors with excellent in vivo antiinflammatory properties.. Bioorg Med Chem Lett, 18 (1): (179-83). [PMID:18039577]
25. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.. Nat Chem Biol, 4 (11): (691-9). [PMID:18849971]
26. Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q et al.. (2009) AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).. Blood, 114 (14): (2984-92). [PMID:19654408]
27. Changelian PS, Flanagan ME, Ball DJ, Kent CR, Magnuson KS, Martin WH, Rizzuti BJ, Sawyer PS, Perry BD, Brissette WH et al.. (2003) Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.. Science, 302 (5646): (875-8). [PMID:14593182]
28. Conway JG, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM et al.. (2005) Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.. Proc Natl Acad Sci USA, 102 (44): (16078-83). [PMID:16249345]
29. Raingeaud J, Gupta S, Rogers JS, Dickens M, Han J, Ulevitch RJ, Davis RJ. (1995) Pro-inflammatory cytokines and environmental stress cause p38 mitogen-activated protein kinase activation by dual phosphorylation on tyrosine and threonine.. J Biol Chem, 270 (13): (7420-6). [PMID:7535770]
30. Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O et al.. (2013) Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.. J Med Chem, 56 (20): (8032-48). [PMID:24044867]
31. Hall MD, Salam NK, Hellawell JL, Fales HM, Kensler CB, Ludwig JA, Szakács G, Hibbs DE, Gottesman MM. (2009) Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.. J Med Chem, 52 (10): (3191-204). [PMID:19397322]
32. Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C. (2009) Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).. J Med Chem, 52 (20): (6433-46). [PMID:19788238]
33. Li X, Zuo Y, Tang G, Wang Y, Zhou Y, Wang X, Guo T, Xia M, Ding N, Pan Z. (2014) Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.. J Med Chem, 57 (12): (5112-28). [PMID:24915291]
34. Pandey A, Volkots DL, Seroogy JM, Rose JW, Yu JC, Lambing JL, Hutchaleelaha A, Hollenbach SJ, Abe K, Giese NA et al.. (2002) Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.. J Med Chem, 45 (17): (3772-93). [PMID:12166950]
35. Anderson DR, Meyers MJ, Vernier WF, Mahoney MW, Kurumbail RG, Caspers N, Poda GI, Schindler JF, Reitz DB, Mourey RJ. (2007) Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).. J Med Chem, 50 (11): (2647-54). [PMID:17480064]
36. Millan DS, Bunnage ME, Burrows JL, Butcher KJ, Dodd PG, Evans TJ, Fairman DA, Hughes SJ, Kilty IC, Lemaitre A et al.. (2011) Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.. J Med Chem, 54 (22): (7797-814). [PMID:21888439]
37. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM. (2009) Inhibitor hijacking of Akt activation.. Nat Chem Biol, 5 (7): (484-93). [PMID:19465931]
38. Papeo G, Posteri H, Borghi D, Busel AA, Caprera F, Casale E, Ciomei M, Cirla A, Corti E, D'Anello M et al.. (2015) Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.. J Med Chem, 58 (17): (6875-98). [PMID:26222319]
39. Li B, Cociorva OM, Nomanbhoy T, Weissig H, Li Q, Nakamura K, Liyanage M, Zhang MC, Shih AY, Aban A et al.. (2013) Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a]quinoxalin-4-amine derived JNK1 inhibitors.. Bioorg Med Chem Lett, 23 (18): (5217-22). [PMID:23916259]
40. Brown DS, Belfield AJ, Brown GR, Campbell D, Foubister A, Masters DJ, Pike KG, Snelson WL, Wells SL. (2004) A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis.. Bioorg Med Chem Lett, 14 (21): (5383-7). [PMID:15454231]
41. Haile PA, Votta BJ, Marquis RW, Bury MJ, Mehlmann JF, Singhaus Jr R, Charnley AK, Lakdawala AS, Convery MA, Lipshutz DB et al.. (2016) The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.. J Med Chem, 59 (10): (4867-80). [PMID:27109867]
42. Uckun FM, Dibirdik I, Qazi S, Vassilev A, Ma H, Mao C, Benyumov A, Emami KH. (2007) Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).. Bioorg Med Chem, 15 (2): (800-14). [PMID:17098432]
43. Miwatashi S, Arikawa Y, Kotani E, Miyamoto M, Naruo K, Kimura H, Tanaka T, Asahi S, Ohkawa S. (2005) Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.. J Med Chem, 48 (19): (5966-79). [PMID:16162000]
44. Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J et al.. (2009) Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.. J Med Chem, 52 (20): (6362-8). [PMID:19827834]
45. Kim KH, Maderna A, Schnute ME, Hegen M, Mohan S, Miyashiro J, Lin L, Li E, Keegan S, Lussier J et al.. (2011) Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.. Bioorg Med Chem Lett, 21 (21): (6258-63). [PMID:21958547]
46. Albrecht W, Unger A, Bauer SM, Laufer SA. (2017) Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases.. J Med Chem, 60 (13): (5290-5305). [PMID:28613871]
47. He X, Da Ros S, Nelson J, Zhu X, Jiang T, Okram B, Jiang S, Michellys PY, Iskandar M, Espinola S et al.. (2017) Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.. ACS Med Chem Lett, 8 (10): (1048-1053). [PMID:29057049]
48. Tan L, Gurbani D, Weisberg EL, Jones DS, Rao S, Singer WD, Bernard FM, Mowafy S, Jenney A, Du G et al.. (2017) Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors.. Bioorg Med Chem, 25 (4): (1320-1328). [PMID:28038940]
49. Burger MT, Nishiguchi G, Han W, Lan J, Simmons R, Atallah G, Ding Y, Tamez V, Zhang Y, Mathur M et al.. (2015) Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.. J Med Chem, 58 (21): (8373-86). [PMID:26505898]
50. Goldstein DM, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, Chen J, Bingenheimer W, Dalrymple SA, Dunn J et al.. (2011) Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.. J Med Chem, 54 (7): (2255-65). [PMID:21375264]
51. Bachegowda L, Morrone K, Winski SL, Mantzaris I, Bartenstein M, Ramachandra N, Giricz O, Sukrithan V, Nwankwo G, Shahnaz S et al.. (2016) Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia.. Cancer Res, 76 (16): (4841-4849). [PMID:27287719]
52. Laleu B, Gaggini F, Orchard M, Fioraso-Cartier L, Cagnon L, Houngninou-Molango S, Gradia A, Duboux G, Merlot C, Heitz F et al.. (2010) First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis.. J Med Chem, 53 (21): (7715-30). [PMID:20942471]
53. Pippione AC, Sainas S, Federico A, Lupino E, Piccinini M, Kubbutat M, Contreras JM, Morice C, Barge A, Ducime A et al.. (2018) N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK.. Medchemcomm, 9 (6): (963-968). [PMID:30108985]
54. Patel S, Harris SF, Gibbons P, Deshmukh G, Gustafson A, Kellar T, Lin H, Liu X, Liu Y, Liu Y et al.. (2015) Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).. J Med Chem, 58 (20): (8182-99). [PMID:26431428]
55. Zhang H, Xu L, Qin X, Chen X, Cong H, Hu L, Chen L, Miao Z, Zhang W, Cai Z et al.. (2019) N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure-Activity Relationships, and in Vivo Efficacy.. J Med Chem, 62 (14): (6665-6681). [PMID:31095385]
56. Roy SM, Grum-Tokars VL, Schavocky JP, Saeed F, Staniszewski A, Teich AF, Arancio O, Bachstetter AD, Webster SJ, Van Eldik LJ et al.. (2015) Targeting human central nervous system protein kinases: An isoform selective p38αMAPK inhibitor that attenuates disease progression in Alzheimer's disease mouse models.. ACS Chem Neurosci, 6 (4): (666-80). [PMID:25676389]
57. Pomel V, Klicic J, Covini D, Church DD, Shaw JP, Roulin K, Burgat-Charvillon F, Valognes D, Camps M, Chabert C et al.. (2006) Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.. J Med Chem, 49 (13): (3857-71). [PMID:16789742]
58. De SK, Stebbins JL, Chen LH, Riel-Mehan M, Machleidt T, Dahl R, Yuan H, Emdadi A, Barile E, Chen V et al.. (2009) Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase.. J Med Chem, 52 (7): (1943-52). [PMID:19271755]
59. Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E et al.. (2020) Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.. J Med Chem, 129 (3): (589-97). [PMID:32787110]
60. Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD et al.. (2019) 3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.. J Med Chem, 62 (15): (6876-6893). [PMID:31282155]
61. Cabrera DG, Horatscheck A, Wilson CR, Basarab G, Eyermann CJ, Chibale K. (2018) Plasmodial Kinase Inhibitors: License to Cure?. J Med Chem, 61 (18): (8061-8077). [PMID:29771541]
62. Peng T, Qi B, He J, Ke H, Shi J. (2020) Advances in the Development of Phosphodiesterase-4 Inhibitors.. J Med Chem, 63 (19): (10594-10617). [PMID:32255344]
63. Yin L, Li H, Liu W, Yao Z, Cheng Z, Zhang H, Zou H. (2018) A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.. Eur J Med Chem, 144 (3): (1-28). [PMID:29247857]
64. Erik Rytter Ottosen,Morten Dahl Sørensen,Fredrik Björkling,Tine Skak-Nielsen,Marianne Scheel Fjording,Helle Aaes,Lise Binderup. (2003-12-12) Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.. Journal of medicinal chemistry, 46 ((26)): (5651-5662). [PMID:14667219]
65. Erki Enkvist, Darja Lavogina, Gerda Raidaru, Angela Vaasa, Indrek Viil, Marje Lust, Kaido Viht, Asko Uri,. (2006-11-28) Conjugation of adenosine and hexa-(D-arginine) leads to a nanomolar bisubstrate-analog inhibitor of basophilic protein kinases.. Journal of medicinal chemistry, 49 ((24)): ( 7150-7159 ). [PMID:17125267]
66. Robert M Rzasa,Matthew R Kaller,Gang Liu,Ella Magal,Thomas T Nguyen,Timothy D Osslund,David Powers,Vincent J Santora,Vellarkad N Viswanadhan,Hui-Ling Wang,Xiaoling Xiong,Wenge Zhong,Mark H Norman. (2007-08-19) Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.. Bioorganic & medicinal chemistry, 15 ((20)): (6574-6595). [PMID:17697781]
67. Thomas M Ehrman,David J Barlow,Peter J Hylands. (2010-03-02) In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.. Bioorganic & medicinal chemistry, 18 ((6)): (2204-2218). [PMID:20188577]
68. Seunghee Hong,Jinhee Kim,Sun-Mi Yun,Hyunseung Lee,Yoonsu Park,Soon-Sun Hong,Sungwoo Hong. (2013-04-23) Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant.. Journal of medicinal chemistry, 56 ((9)): (3531-3545). [PMID:23600806]
69. Pratistha Ranjitkar,Amanda M Brock,Dustin J Maly. (2010-03-02) Affinity reagents that target a specific inactive form of protein kinases.. Chemistry & biology, 17 ((2)): (195-206). [PMID:20189109]
70. Anand Divakaran,Siva K Talluri,Alex M Ayoub,Neeraj K Mishra,Huarui Cui,John C Widen,Norbert Berndt,Jin-Yi Zhu,Angela S Carlson,Joseph J Topczewski,Ernst K Schonbrunn,Daniel A Harki,William C K Pomerantz. (2018-09-27) Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.. Journal of medicinal chemistry, 61 ((20)): (9316-9334). [PMID:30253095]
71. Henry JR, Rupert KC, Dodd JH, Turchi IJ, Wadsworth SA, Cavender DE, Schafer PH, Siekierka JJ.. (1998) Potent inhibitors of the MAP kinase p38.. Bioorg Med Chem Lett, 8 (23): (3335-3340). [PMID:9873730]
72. Dumas J, Hatoum-Mokdad H, Sibley RN, Smith RA, Scott WJ, Khire U, Lee W, Wood J, Wolanin D, Cooley J, Bankston D, Redman AM, Schoenleber R, Caringal Y, Gunn D, Romero R, Osterhout M, Paulsen H, Housley TJ, Wilhelm SM, Pirro J, Chien DS, Ranges GE, Shrikhande A, Muzsi A, Bortolon E, Wakefield J, Gianpaolo Ostravage C, Bhargava A, Chau T.. (2002) Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.. Bioorg Med Chem Lett, 12 (12): (1559-1562). [PMID:12039561]
73. Mavunkel BJ, Chakravarty S, Perumattam JJ, Luedtke GR, Liang X, Lim D, Xu YJ, Laney M, Liu DY, Schreiner GF, Lewicki JA, Dugar S.. (2003) Indole-based heterocyclic inhibitors of p38alpha MAP kinase: designing a conformationally restricted analogue.. Bioorg Med Chem Lett, 13 (18): (3087-3090). [PMID:12941340]
74. Rupert KC, Henry JR, Dodd JH, Wadsworth SA, Cavender DE, Olini GC, Fahmy B, Siekierka JJ.. (2003) Imidazopyrimidines, potent inhibitors of p38 MAP kinase.. Bioorg Med Chem Lett, 13 (3): (347-350). [PMID:12565927]
75. Boehm JC, Smietana JM, Sorenson ME, Garigipati RS, Gallagher TF, Sheldrake PL, Bradbeer J, Badger AM, Laydon JT, Lee JC, Hillegass LM, Griswold DE, Breton JJ, Chabot-Fletcher MC, Adams JL.. (1996) 1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency.. J Med Chem, 39 (20): (3929-3937). [PMID:8831759]
76. Liverton NJ, Butcher JW, Claiborne CF, Claremon DA, Libby BE, Nguyen KT, Pitzenberger SM, Selnick HG, Smith GR, Tebben A, Vacca JP, Varga SL, Agarwal L, Dancheck K, Forsyth AJ, Fletcher DS, Frantz B, Hanlon WA, Harper CF, Hofsess SJ, Kostura M, Lin J, Luell S, O'Neill EA, O'Keefe SJ.. (1999) Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.. J Med Chem, 42 (12): (2180-2190). [PMID:10377223]
77. McKenna JM, Halley F, Souness JE, McLay IM, Pickett SD, Collis AJ, Page K, Ahmed I.. (2002) An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors.. J Med Chem, 45 (11): (2173-2184). [PMID:12014955]
78. Trejo A, Arzeno H, Browner M, Chanda S, Cheng S, Comer DD, Dalrymple SA, Dunten P, Lafargue J, Lovejoy B, Freire-Moar J, Lim J, Mcintosh J, Miller J, Papp E, Reuter D, Roberts R, Sanpablo F, Saunders J, Song K, Villasenor A, Warren SD, Welch M, Weller P, Whiteley PE, Zeng L, Goldstein DM.. (2003) Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase.. J Med Chem, 46 (22): (4702-4713). [PMID:14561090]
79. Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA.. (2004) 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.. J Med Chem, 47 (13): (3367-3380). [PMID:15189033]
80. Laughlin SK, Clark MP, Djung JF, Golebiowski A, Brugel TA, Sabat M, Bookland RG, Laufersweiler MJ, VanRens JC, Townes JA, De B, Hsieh LC, Xu SC, Walter RL, Mekel MJ, Janusz MJ.. (2005) The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.. Bioorg Med Chem Lett, 15 (9): (2399-2403). [PMID:15837333]
81. Tamayo N, Liao L, Goldberg M, Powers D, Tudor YY, Yu V, Wong LM, Henkle B, Middleton S, Syed R, Harvey T, Jang G, Hungate R, Dominguez C.. (2005) Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase.. Bioorg Med Chem Lett, 15 (9): (2409-2413). [PMID:15837335]
82. Gellibert F, Woolven J, Fouchet MH, Mathews N, Goodland H, Lovegrove V, Laroze A, Nguyen VL, Sautet S, Wang R, Janson C, Smith W, Krysa G, Boullay V, De Gouville AC, Huet S, Hartley D.. (2004) Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors.. J Med Chem, 47 (18): (4494-4506). [PMID:15317461]
83. de Dios A, Shih C, López de Uralde B, Sánchez C, del Prado M, Martín Cabrejas LM, Pleite S, Blanco-Urgoiti J, Lorite MJ, Nevill CR, Bonjouklian R, York J, Vieth M, Wang Y, Magnus N, Campbell RM, Anderson BD, McCann DJ, Giera DD, Lee PA, Schultz RM, Li LC, Johnson LM, Wolos JA.. (2005) Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy.. J Med Chem, 48 (7): (2270-2273). [PMID:15801819]
84. VanderWel SN, Harvey PJ, McNamara DJ, Repine JT, Keller PR, Quin J, Booth RJ, Elliott WL, Dobrusin EM, Fry DW, Toogood PL.. (2005) Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.. J Med Chem, 48 (7): (2371-2387). [PMID:15801830]
85. Bao J, Hunt JA, Miao S, Rupprecht KM, Stelmach JE, Liu L, Ruzek RD, Sinclair PJ, Pivnichny JV, Hop CE, Kumar S, Zaller DM, Shoop WL, O'neill EA, O'keefe SJ, Thompson CM, Cubbon RM, Wang R, Zhang WX, Thompson JE, Doherty JB.. (2006) p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones.. Bioorg Med Chem Lett, 16 (1): (64-68). [PMID:16242322]
86. Gellibert F, de Gouville AC, Woolven J, Mathews N, Nguyen VL, Bertho-Ruault C, Patikis A, Grygielko ET, Laping NJ, Huet S.. (2006) Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.. J Med Chem, 49 (7): (2210-2221). [PMID:16570917]
87. Borzilleri RM, Bhide RS, Barrish JC, D'Arienzo CJ, Derbin GM, Fargnoli J, Hunt JT, Jeyaseelan R, Kamath A, Kukral DW, Marathe P, Mortillo S, Qian L, Tokarski JS, Wautlet BS, Zheng X, Lombardo LJ.. (2006) Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.. J Med Chem, 49 (13): (3766-3769). [PMID:16789733]
88. Kim ND, Yoon J, Kim JH, Lee JT, Chon YS, Hwang MK, Ha I, Song WJ.. (2006) Putative therapeutic agents for the learning and memory deficits of people with Down syndrome.. Bioorg Med Chem Lett, 16 (14): (3772-3776). [PMID:16698266]
89. DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Buchanan JL, Buckner WH, Cee VJ, Chai L, Deak HL, Epstein LF, Faust T, Gallant P, Geuns-Meyer SD, Gore A, Gu Y, Henkle B, Hodous BL, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, Masse CE, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, White RD, Zhao H, Zhu L, Zhu X.. (2006) Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.. J Med Chem, 49 (19): (5671-5686). [PMID:16970394]
90. Krystof V, Cankar P, Frysová I, Slouka J, Kontopidis G, Dzubák P, Hajdúch M, Srovnal J, de Azevedo WF, Orság M, Paprskárová M, Rolcík J, Látr A, Fischer PM, Strnad M.. (2006) 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.. J Med Chem, 49 (22): (6500-6509). [PMID:17064068]
91. Natarajan SR, Liu L, Levorse M, Thompson JE, O'Neill EA, O'Keefe SJ, Vora KA, Cvetovich R, Chung JY, Carballo-Jane E, Visco DM.. (2006) p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold.. Bioorg Med Chem Lett, 16 (20): (5468-5471). [PMID:16945534]
92. Hu Y, Green N, Gavrin LK, Janz K, Kaila N, Li HQ, Thomason JR, Cuozzo JW, Hall JP, Hsu S, Nickerson-Nutter C, Telliez JB, Lin LL, Tam S.. (2006) Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.. Bioorg Med Chem Lett, 16 (23): (6067-6072). [PMID:16973359]
93. Cee VJ, Albrecht BK, Geuns-Meyer S, Hughes P, Bellon S, Bready J, Caenepeel S, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hodous BL, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, McGowan D, Morrison M, Olivieri PR, Patel VF, Polverino A, Powers D, Rose P, Wang L, Zhao H.. (2007) Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.. J Med Chem, 50 (4): (627-640). [PMID:17253679]
94. Aronov AM, Baker C, Bemis GW, Cao J, Chen G, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Martinez-Botella G, Namchuk MN, Straub J, Tang Q, Xie X.. (2007) Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.. J Med Chem, 50 (6): (1280-1287). [PMID:17300186]
95. Leftheris K, Ahmed G, Chan R, Dyckman AJ, Hussain Z, Ho K, Hynes J, Letourneau J, Li W, Lin S, Metzger A, Moriarty KJ, Riviello C, Shimshock Y, Wen J, Wityak J, Wrobleski ST, Wu H, Wu J, Desai M, Gillooly KM, Lin TH, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Zhang R, Diller D, Doweyko A, Sack J, Baldwin J, Barrish J, Dodd J, Henderson I, Kanner S, Schieven GL, Webb M.. (2004) The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.. J Med Chem, 47 (25): (6283-6291). [PMID:15566298]
96. Bruno O, Brullo C, Bondavalli F, Schenone S, Ranise A, Arduino N, Bertolotto MB, Montecucco F, Ottonello L, Dallegri F, Tognolini M, Ballabeni V, Bertoni S, Barocelli E.. (2007) Synthesis and biological evaluation of N-pyrazolyl-N'-alkyl/benzyl/phenylureas: a new class of potent inhibitors of interleukin 8-induced neutrophil chemotaxis.. J Med Chem, 50 (15): (3618-3626). [PMID:17608466]
97. Potashman MH, Bready J, Coxon A, DeMelfi TM, DiPietro L, Doerr N, Elbaum D, Estrada J, Gallant P, Germain J, Gu Y, Harmange JC, Kaufman SA, Kendall R, Kim JL, Kumar GN, Long AM, Neervannan S, Patel VF, Polverino A, Rose P, Plas Sv, Whittington D, Zanon R, Zhao H.. (2007) Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors.. J Med Chem, 50 (18): (4351-4373). [PMID:17696416]
98. Green N, Hu Y, Janz K, Li HQ, Kaila N, Guler S, Thomason J, Joseph-McCarthy D, Tam SY, Hotchandani R, Wu J, Huang A, Wang Q, Leung L, Pelker J, Marusic S, Hsu S, Telliez JB, Hall JP, Cuozzo JW, Lin LL.. (2007) Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.. J Med Chem, 50 (19): (4728-4745). [PMID:17715908]
99. Cincinelli R, Dallavalle S, Nannei R, Merlini L, Penco S, Giannini G, Pisano C, Vesci L, Ferrara FF, Zuco V, Zanchi C, Zunino F.. (2007) Synthesis and structure-activity relationships of new antiproliferative and proapoptotic retinoid-related biphenyl-4-yl-acrylic acids.. Bioorg Med Chem, 15 (14): (4863-4875). [PMID:17512204]
100. Bagley MC, Davis T, Dix MC, Rokicki MJ, Kipling D.. (2007) Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells.. Bioorg Med Chem Lett, 17 (18): (5107-5110). [PMID:17659871]
101. Singh RK, Lange TS, Kim K, Zou Y, Lieb C, Sholler GL, Brard L.. (2007) Effect of indole ethyl isothiocyanates on proliferation, apoptosis, and MAPK signaling in neuroblastoma cell lines.. Bioorg Med Chem Lett, 17 (21): (5846-5852). [PMID:17855093]
102. Graneto MJ, Kurumbail RG, Vazquez ML, Shieh HS, Pawlitz JL, Williams JM, Stallings WC, Geng L, Naraian AS, Koszyk FJ, Stealey MA, Xu XD, Weier RM, Hanson GJ, Mourey RJ, Compton RP, Mnich SJ, Anderson GD, Monahan JB, Devraj R.. (2007) Synthesis, crystal structure, and activity of pyrazole-based inhibitors of p38 kinase.. J Med Chem, 50 (23): (5712-5719). [PMID:17948975]
103. Hynes J, Dyckman AJ, Lin S, Wrobleski ST, Wu H, Gillooly KM, Kanner SB, Lonial H, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Yang X, Zhang R, Behnia K, Zhang H, Marathe PH, Doweyko AM, Tokarski JS, Sack JS, Pokross M, Kiefer SE, Newitt JA, Barrish JC, Dodd J, Schieven GL, Leftheris K.. (2008) Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.. J Med Chem, 51 (1): (4-16). [PMID:18072718]
104. Martin MW, Newcomb J, Nunes JJ, Boucher C, Chai L, Epstein LF, Faust T, Flores S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Kim JL, Middleton S, Morgenstern K, Oliveira-dos-Santos A, Patel VF, Powers D, Rose P, Tudor Y, Turci SM, Welcher AA, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Ermann M, Johnston D, Saluste CG.. (2008) Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.. J Med Chem, 51 (6): (1637-1648). [PMID:18278858]
105. Angell RM, Angell TD, Bamborough P, Brown D, Brown M, Buckton JB, Cockerill SG, Edwards CD, Jones KL, Longstaff T, Smee PA, Smith KJ, Somers DO, Walker AL, Willson M.. (2008) Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.. Bioorg Med Chem Lett, 18 (1): (324-328). [PMID:17981461]
106. DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Chai L, Chaffee SC, Deak HL, Epstein LF, Faust T, Gallant P, Gore A, Gu Y, Henkle B, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, Zhao H, Zhu L, Zhu X.. (2008) Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.. J Med Chem, 51 (6): (1681-1694). [PMID:18321037]
107. Varma H, Cheng R, Voisine C, Hart AC, Stockwell BR.. (2007) Inhibitors of metabolism rescue cell death in Huntington's disease models.. Proc Natl Acad Sci U S A, 104 (36): (14525-14530). [PMID:17726098]
108. McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, Lamb J, Archibald H, Raudales R, Tam A, Lee D, Rothenberg SM, Supko JG, Sordella R, Ulkus LE, Iafrate AJ, Maheswaran S, Njauw CN, Tsao H, Drew L, Hanke JH, Ma XJ, Erlander MG, Gray NS, Haber DA, Settleman J.. (2007) Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.. Proc Natl Acad Sci U S A, 104 (50): (19936-19941). [PMID:18077425]
109. Feng R, Ni HM, Wang SY, Tourkova IL, Shurin MR, Harada H, Yin XM.. (2007) Cyanidin-3-rutinoside, a natural polyphenol antioxidant, selectively kills leukemic cells by induction of oxidative stress.. J Biol Chem, 282 (18): (13468-13476). [PMID:17360708]
110. O'Keefe SJ, Mudgett JS, Cupo S, Parsons JN, Chartrain NA, Fitzgerald C, Chen SL, Lowitz K, Rasa C, Visco D, Luell S, Carballo-Jane E, Owens K, Zaller DM.. (2007) Chemical genetics define the roles of p38alpha and p38beta in acute and chronic inflammation.. J Biol Chem, 282 (48): (34663-34671). [PMID:17855341]
111. Angell R, Aston NM, Bamborough P, Buckton JB, Cockerill S, deBoeck SJ, Edwards CD, Holmes DS, Jones KL, Laine DI, Patel S, Smee PA, Smith KJ, Somers DO, Walker AL.. (2008) Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.. Bioorg Med Chem Lett, 18 (15): (4428-4432). [PMID:18614366]
112. Bagley MC, Davis T, Dix MC, Murziani PG, Rokicki MJ, Kipling D.. (2008) Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.. Bioorg Med Chem Lett, 18 (13): (3745-3748). [PMID:18539026]
113. Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P.. (2008) Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.. J Med Chem, 51 (21): (6642-6645). [PMID:18834107]
114. Hirabayashi A, Mukaiyama H, Kobayashi H, Shiohara H, Nakayama S, Ozawa M, Miyazawa K, Misawa K, Ohnota H, Isaji M.. (2009) Structure-activity relationship studies of 5-benzylaminoimidazo[1,2-c]pyrimidine-8-carboxamide derivatives as potent, highly selective ZAP-70 kinase inhibitors.. Bioorg Med Chem, 17 (1): (284-294). [PMID:19010686]
115. Xia Z, Knaak C, Ma J, Beharry ZM, McInnes C, Wang W, Kraft AS, Smith CD.. (2009) Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases.. J Med Chem, 52 (1): (74-86). [PMID:19072652]
116. Pettus LH, Xu S, Cao GQ, Chakrabarti PP, Rzasa RM, Sham K, Wurz RP, Zhang D, Middleton S, Henkle B, Plant MH, Saris CJ, Sherman L, Wong LM, Powers DA, Tudor Y, Yu V, Lee MR, Syed R, Hsieh F, Tasker AS.. (2008) 3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.. J Med Chem, 51 (20): (6280-6292). [PMID:18817364]
117. De SK, Chen LH, Stebbins JL, Machleidt T, Riel-Mehan M, Dahl R, Chen V, Yuan H, Barile E, Emdadi A, Murphy R, Pellecchia M.. (2009) Discovery of 2-(5-nitrothiazol-2-ylthio)benzo[d]thiazoles as novel c-Jun N-terminal kinase inhibitors.. Bioorg Med Chem, 17 (7): (2712-2717). [PMID:19282190]
118. Laufer S, Lehmann F.. (2009) Investigations of SCIO-469-like compounds for the inhibition of p38 MAP kinase.. Bioorg Med Chem Lett, 19 (5): (1461-1464). [PMID:19195885]
119. Lumeras W, Caturla F, Vidal L, Esteve C, Balagué C, Orellana A, Domínguez M, Roca R, Huerta JM, Godessart N, Vidal B.. (2009) Design, synthesis, and structure-activity relationships of aminopyridine N-oxides, a novel scaffold for the potent and selective inhibition of p38 mitogen activated protein kinase.. J Med Chem, 52 (17): (5531-5545). [PMID:19678708]
120. Park BS, El-Deeb IM, Yoo KH, Oh CH, Cho SJ, Han DK, Lee HS, Lee JY, Lee SH.. (2009) Design, synthesis and biological evaluation of new potent and highly selective ROS1-tyrosine kinase inhibitor.. Bioorg Med Chem Lett, 19 (16): (4720-4723). [PMID:19596575]
121. Li Q, Al-Ayoubi A, Guo T, Zheng H, Sarkar A, Nguyen T, Eblen ST, Grant S, Kellogg GE, Zhang S.. (2009) Structure-activity relationship (SAR) studies of 3-(2-amino-ethyl)-5-(4-ethoxy-benzylidene)-thiazolidine-2,4-dione: development of potential substrate-specific ERK1/2 inhibitors.. Bioorg Med Chem Lett, 19 (21): (6042-6046). [PMID:19796943]
122. Li J, Kaoud TS, Laroche C, Dalby KN, Kerwin SM.. (2009) Synthesis and biological evaluation of p38alpha kinase-targeting dialkynylimidazoles.. Bioorg Med Chem Lett, 19 (22): (6293-6297). [PMID:19822424]
123. Antczak C, Veach DR, Ramirez CN, Minchenko MA, Shum D, Calder PA, Frattini MG, Clarkson B, Djaballah H.. (2009) Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.. Bioorg Med Chem Lett, 19 (24): (6872-6876). [PMID:19889540]
124. Shomin CD, Meyer SC, Ghosh I.. (2009) Staurosporine tethered peptide ligands that target cAMP-dependent protein kinase (PKA): optimization and selectivity profiling.. Bioorg Med Chem, 17 (17): (6196-6202). [PMID:19674907]
125. Wee XK, Yeo WK, Zhang B, Tan VB, Lim KM, Tay TE, Go ML.. (2009) Synthesis and evaluation of functionalized isoindigos as antiproliferative agents.. Bioorg Med Chem, 17 (21): (7562-7571). [PMID:19783149]
126. Dietrich J, Gokhale V, Wang X, Hurley LH, Flynn GA.. (2010) Application of a novel [3+2] cycloaddition reaction to prepare substituted imidazoles and their use in the design of potent DFG-out allosteric B-Raf inhibitors.. Bioorg Med Chem, 18 (1): (292-304). [PMID:19962319]
127. De SK, Chen V, Stebbins JL, Chen LH, Cellitti JF, Machleidt T, Barile E, Riel-Mehan M, Dahl R, Yang L, Emdadi A, Murphy R, Pellecchia M.. (2010) Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.. Bioorg Med Chem, 18 (2): (590-596). [PMID:20045647]
128. Qiao L, Choi S, Case A, Gainer TG, Seyb K, Glicksman MA, Lo DC, Stein RL, Cuny GD.. (2009) Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors.. Bioorg Med Chem Lett, 19 (21): (6122-6126). [PMID:19783434]
129. Pettus LH, Wurz RP, Xu S, Herberich B, Henkle B, Liu Q, McBride HJ, Mu S, Plant MH, Saris CJ, Sherman L, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS.. (2010) Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.. J Med Chem, 53 (7): (2973-2985). [PMID:20218619]
130. Walker JK, Selness SR, Devraj RV, Hepperle ME, Naing W, Shieh H, Kurambail R, Yang S, Flynn DL, Benson AG, Messing DM, Dice T, Kim T, Lindmark RJ, Monahan JB, Portanova J.. (2010) Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase.. Bioorg Med Chem Lett, 20 (8): (2634-2638). [PMID:20227876]
131. Deng X, Lim SM, Zhang J, Gray NS.. (2010) Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.. Bioorg Med Chem Lett, 20 (14): (4196-4200). [PMID:20541934]
132. Nakao A, Ohkawa N, Nagasaki T, Kagari T, Doi H, Shimozato T, Ushiyama S, Aoki K.. (2010) Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 3.. Bioorg Med Chem Lett, 20 (16): (4774-4778). [PMID:20637613]
133. Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T.. (2010) A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.. J Med Chem, 53 (15): (5439-5448). [PMID:20604564]
134. Dietrich J, Hulme C, Hurley LH.. (2010) The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796.. Bioorg Med Chem, 18 (15): (5738-5748). [PMID:20621496]
135. Terazawa R, Garud DR, Hamada N, Fujita Y, Itoh T, Nozawa Y, Nakane K, Deguchi T, Koketsu M, Ito M.. (2010) Identification of organoselenium compounds that possess chemopreventive properties in human prostate cancer LNCaP cells.. Bioorg Med Chem, 18 (19): (7001-7008). [PMID:20805033]
136. Ye P, Kuhn C, Juan M, Sharma R, Connolly B, Alton G, Liu H, Stanton R, Kablaoui NM.. (2011) Potent and selective thiophene urea-templated inhibitors of S6K.. Bioorg Med Chem Lett, 21 (2): (849-852). [PMID:21185721]
137. Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I.. (2011) Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.. Bioorg Med Chem Lett, 21 (1): (315-319). [PMID:21112785]
138. Gould AE, Adams R, Adhikari S, Aertgeerts K, Afroze R, Blackburn C, Calderwood EF, Chau R, Chouitar J, Duffey MO, England DB, Farrer C, Forsyth N, Garcia K, Gaulin J, Greenspan PD, Guo R, Harrison SJ, Huang SC, Iartchouk N, Janowick D, Kim MS, Kulkarni B, Langston SP, Liu JX, Ma LT, Menon S, Mizutani H, Paske E, Renou CC, Rezaei M, Rowland RS, Sintchak MD, Smith MD, Stroud SG, Tregay M, Tian Y, Veiby OP, Vos TJ, Vyskocil S, Williams J, Xu T, Yang JJ, Yano J, Zeng H, Zhang DM, Zhang Q, Galvin KM.. (2011) Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.. J Med Chem, 54 (6): (1836-1846). [PMID:21341678]
139. Charrier JD, Miller A, Kay DP, Brenchley G, Twin HC, Collier PN, Ramaya S, Keily SB, Durrant SJ, Knegtel RM, Tanner AJ, Brown K, Curnock AP, Jimenez JM.. (2011) Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.. J Med Chem, 54 (7): (2341-2350). [PMID:21391610]
140. De SK, Barile E, Chen V, Stebbins JL, Cellitti JF, Machleidt T, Carlson CB, Yang L, Dahl R, Pellecchia M.. (2011) Design, synthesis, and structure-activity relationship studies of thiophene-3-carboxamide derivatives as dual inhibitors of the c-Jun N-terminal kinase.. Bioorg Med Chem, 19 (8): (2582-2588). [PMID:21458276]
141. Mandal PK, Gao F, Lu Z, Ren Z, Ramesh R, Birtwistle JS, Kaluarachchi KK, Chen X, Bast RC, Liao WS, McMurray JS.. (2011) Potent and selective phosphopeptide mimetic prodrugs targeted to the Src homology 2 (SH2) domain of signal transducer and activator of transcription 3.. J Med Chem, 54 (10): (3549-3563). [PMID:21486047]
142. Ravindra GK, Achaiah G, Sastry GN.. (2008) Molecular modeling studies of phenoxypyrimidinyl imidazoles as p38 kinase inhibitors using QSAR and docking.. Eur J Med Chem, 43 (4): (830-838). [PMID:17706839]
143. Stebbins JL, De SK, Pavlickova P, Chen V, Machleidt T, Chen LH, Kuntzen C, Kitada S, Karin M, Pellecchia M.. (2011) Design and characterization of a potent and selective dual ATP- and substrate-competitive subnanomolar bidentate c-Jun N-terminal kinase (JNK) inhibitor.. J Med Chem, 54 (18): (6206-6214). [PMID:21815634]
144. Lumeras W, Vidal L, Vidal B, Balagué C, Orellana A, Maldonado M, Domínguez M, Segarra V, Caturla F.. (2011) 1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.. J Med Chem, 54 (22): (7899-7910). [PMID:21999461]
145. Kim H, Kim M, Lee J, Yu H, Hah JM.. (2011) Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.. Bioorg Med Chem, 19 (22): (6760-6767). [PMID:22014755]
146. Ishikawa T, Seto M, Banno H, Kawakita Y, Oorui M, Taniguchi T, Ohta Y, Tamura T, Nakayama A, Miki H, Kamiguchi H, Tanaka T, Habuka N, Sogabe S, Yano J, Aertgeerts K, Kamiyama K.. (2011) Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.. J Med Chem, 54 (23): (8030-8050). [PMID:22003817]
147. Festa M, Capasso A, D'Acunto CW, Masullo M, Rossi AG, Pizza C, Piacente S.. (2011) Xanthohumol induces apoptosis in human malignant glioblastoma cells by increasing reactive oxygen species and activating MAPK pathways.. J Nat Prod, 74 (12): (2505-2513). [PMID:22111577]
148. Yang T, Lu Z, Meng L, Wei S, Hong K, Zhu W, Huang C.. (2012) The novel agent ophiobolin O induces apoptosis and cell cycle arrest of MCF-7 cells through activation of MAPK signaling pathways.. Bioorg Med Chem Lett, 22 (1): (579-585). [PMID:22130129]
149. Caruso M, Valsasina B, Ballinari D, Bertrand J, Brasca MG, Caldarelli M, Cappella P, Fiorentini F, Gianellini LM, Scolaro A, Beria I.. (2012) 5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.. Bioorg Med Chem Lett, 22 (1): (96-101). [PMID:22154349]
150. Cuny GD, Ulyanova NP, Patnaik D, Liu JF, Lin X, Auerbach K, Ray SS, Xian J, Glicksman MA, Stein RL, Higgins JM.. (2012) Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors.. Bioorg Med Chem Lett, 22 (5): (2015-2019). [PMID:22335895]
151. Zhang J, Deng X, Choi HG, Alessi DR, Gray NS.. (2012) Characterization of TAE684 as a potent LRRK2 kinase inhibitor.. Bioorg Med Chem Lett, 22 (5): (1864-1869). [PMID:22335897]
152. Innocenti P, Cheung KM, Solanki S, Mas-Droux C, Rowan F, Yeoh S, Boxall K, Westlake M, Pickard L, Hardy T, Baxter JE, Aherne GW, Bayliss R, Fry AM, Hoelder S.. (2012) Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.. J Med Chem, 55 (7): (3228-3241). [PMID:22404346]
153. Andreani A, Granaiola M, Locatelli A, Morigi R, Rambaldi M, Varoli L, Calonghi N, Cappadone C, Farruggia G, Stefanelli C, Masotti L, Nguyen TL, Hamel E, Shoemaker RH.. (2012) Substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and analogues: synthesis, cytotoxic activity, and study of the mechanism of action.. J Med Chem, 55 (5): (2078-2088). [PMID:22283430]
154. Lo Monte F, Kramer T, Gu J, Anumala UR, Marinelli L, La Pietra V, Novellino E, Franco B, Demedts D, Van Leuven F, Fuertes A, Dominguez JM, Plotkin B, Eldar-Finkelman H, Schmidt B.. (2012) Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-3α.. J Med Chem, 55 (9): (4407-4424). [PMID:22533818]
155. Kwon OW, Moon E, Chari MA, Kim TW, Kim AJ, Lee P, Ahn KH, Kim SY.. (2012) A substituted 3,4-dihydropyrimidinone derivative (compound D22) prevents inflammation mediated neurotoxicity; role in microglial activation in BV-2 cells.. Bioorg Med Chem Lett, 22 (16): (5199-5203). [PMID:22819763]
156. Johnson SM, Murphy RC, Geiger JA, DeRocher AE, Zhang Z, Ojo KK, Larson ET, Perera BG, Dale EJ, He P, Reid MC, Fox AM, Mueller NR, Merritt EA, Fan E, Parsons M, Van Voorhis WC, Maly DJ.. (2012) Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.. J Med Chem, 55 (5): (2416-2426). [PMID:22320388]
157. Song H, Lee YS, Roh EJ, Seo JH, Oh KS, Lee BH, Han H, Shin KJ.. (2012) Discovery of potent and selective rhodanine type IKKβ inhibitors by hit-to-lead strategy.. Bioorg Med Chem Lett, 22 (17): (5668-5674). [PMID:22858099]
158. Malmström J, Viklund J, Slivo C, Costa A, Maudet M, Sandelin C, Hiller G, Olsson LL, Aagaard A, Geschwindner S, Xue Y, Vasänge M.. (2012) Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors.. Bioorg Med Chem Lett, 22 (18): (5919-5923). [PMID:22889803]
159. Kaoud TS, Yan C, Mitra S, Tseng CC, Jose J, Taliaferro JM, Tuohetahuntila M, Devkota A, Sammons R, Park J, Park H, Shi Y, Hong J, Ren P, Dalby KN.. (2012) From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules.. ACS Med Chem Lett, 3 (9): (721-725). [PMID:23002419]
160. Srivatsan A, Wang Y, Joshi P, Sajjad M, Chen Y, Liu C, Thankppan K, Missert JR, Tracy E, Morgan J, Rigual N, Baumann H, Pandey RK.. (2011) In vitro cellular uptake and dimerization of signal transducer and activator of transcription-3 (STAT3) identify the photosensitizing and imaging-potential of isomeric photosensitizers derived from chlorophyll-a and bacteriochlorophyll-a.. J Med Chem, 54 (19): (6859-6873). [PMID:21842893]
161. Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE.. (2011) Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).. J Med Chem, 54 (22): (7860-7883). [PMID:22039836]
162. Park EJ, Kiselev E, Conda-Sheridan M, Cushman M, Pezzuto JM.. (2012) Induction of apoptosis by 3-amino-6-(3-aminopropyl)-5,6-dihydro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline via modulation of MAPKs (p38 and c-Jun N-terminal kinase) and c-Myc in HL-60 human leukemia cells.. J Nat Prod, 75 (3): (378-384). [PMID:22148260]
163. Huh JE, Kang JW, Nam D, Baek YH, Choi DY, Park DS, Lee JD.. (2012) Melittin suppresses VEGF-A-induced tumor growth by blocking VEGFR-2 and the COX-2-mediated MAPK signaling pathway.. J Nat Prod, 75 (11): (1922-1929). [PMID:23110475]
164. Sunose M, Bell K, Ellard K, Bergamini G, Neubauer G, Werner T, Ramsden N.. (2012) Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.. Bioorg Med Chem Lett, 22 (14): (4613-4618). [PMID:22726925]
165. Reith AD, Bamborough P, Jandu K, Andreotti D, Mensah L, Dossang P, Choi HG, Deng X, Zhang J, Alessi DR, Gray NS.. (2012) GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.. Bioorg Med Chem Lett, 22 (17): (5625-5629). [PMID:22863203]
166. Amombo GM, Kramer T, Lo Monte F, Göring S, Fach M, Smith S, Kolb S, Schubenel R, Baumann K, Schmidt B.. (2012) Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3.. Bioorg Med Chem Lett, 22 (24): (7634-7640). [PMID:23107479]
167. Dolečková I, Cesnek M, Dračinský M, Brynda J, Voller J, Janeba Z, Kryštof V.. (2013) Synthesis and biological evaluation of guanidino analogues of roscovitine.. Eur J Med Chem, 62 (443-452). [PMID:23399722]
168. Brown A, Shi Q, Moore TW, Yoon Y, Prussia A, Maddox C, Liotta DC, Shim H, Snyder JP.. (2013) Monocarbonyl curcumin analogues: heterocyclic pleiotropic kinase inhibitors that mediate anticancer properties.. J Med Chem, 56 (9): (3456-3466). [PMID:23550937]
169. Yin Y, Lin L, Ruiz C, Khan S, Cameron MD, Grant W, Pocas J, Eid N, Park H, Schröter T, Lograsso PV, Feng Y.. (2013) Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.. J Med Chem, 56 (9): (3568-3581). [PMID:23570561]
170. Mortensen DS, Sapienza J, Lee BG, Perrin-Ninkovic SM, Harris R, Shevlin G, Parnes JS, Whitefield B, Hickman M, Khambatta G, Bisonette RR, Peng S, Gamez JC, Leisten J, Narla RK, Fultz KE, Sankar S.. (2013) Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.. Bioorg Med Chem Lett, 23 (6): (1588-1591). [PMID:23414803]
171. Olajide OA, Bhatia HS, de Oliveira AC, Wright CW, Fiebich BL.. (2013) Anti-neuroinflammatory properties of synthetic cryptolepine in human neuroblastoma cells: possible involvement of NF-κB and p38 MAPK inhibition.. Eur J Med Chem, 63 (333-339). [PMID:23507189]
172. Jiang R, Frackowiak B, Shin Y, Song X, Chen W, Lin L, Cameron MD, Duckett DR, Kamenecka TM.. (2013) Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.. Bioorg Med Chem Lett, 23 (9): (2683-2687). [PMID:23518277]
173. Lin WH, Hsu JT, Hsieh SY, Chen CT, Song JS, Yen SC, Hsu T, Lu CT, Chen CH, Chou LH, Yang YN, Chiu CH, Chen CP, Tseng YJ, Yen KJ, Yeh CF, Chao YS, Yeh TK, Jiaang WT.. (2013) Discovery of 3-phenyl-1H-5-pyrazolylamine derivatives containing a urea pharmacophore as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).. Bioorg Med Chem, 21 (11): (2856-2867). [PMID:23618709]
174. Wright LE, Frye JB, Lukefahr AL, Timmermann BN, Mohammad KS, Guise TA, Funk JL.. (2013) Curcuminoids block TGF-β signaling in human breast cancer cells and limit osteolysis in a murine model of breast cancer bone metastasis.. J Nat Prod, 76 (3): (316-321). [PMID:23145932]
175. Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Pandya D, Diep L, Fitzgerald K, Artis DR, Anderson JP, Bergeron M.. (2013) Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.. Bioorg Med Chem Lett, 23 (9): (2743-2749). [PMID:23522834]
176. Akama T, Dong C, Virtucio C, Freund YR, Chen D, Orr MD, Jacobs RT, Zhang YK, Hernandez V, Liu Y, Wu A, Bu W, Liu L, Jarnagin K, Plattner JJ.. (2013) Discovery and structure-activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents.. Bioorg Med Chem Lett, 23 (21): (5870-5873). [PMID:24075731]
177. Hanke T, Dehm F, Liening S, Popella SD, Maczewsky J, Pillong M, Kunze J, Weinigel C, Barz D, Kaiser A, Wurglics M, Lämmerhofer M, Schneider G, Sautebin L, Schubert-Zsilavecz M, Werz O.. (2013) Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.. J Med Chem, 56 (22): (9031-9044). [PMID:24171493]
178. Huang H, Guzman-Perez A, Acquaviva L, Berry V, Bregman H, Dovey J, Gunaydin H, Huang X, Huang L, Saffran D, Serafino R, Schneider S, Wilson C, DiMauro EF.. (2013) Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.. ACS Med Chem Lett, 4 (12): (1218-1223). [PMID:24900633]
179. He Y, Duckett D, Chen W, Ling YY, Cameron MD, Lin L, Ruiz CH, Lograsso PV, Kamenecka TM, Koenig M.. (2014) Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.. Bioorg Med Chem Lett, 24 (1): (161-164). [PMID:24332487]
180. Maciag AE, Holland RJ, Kim Y, Kumari V, Luthers CE, Sehareen WS, Biswas D, Morris NL, Ji X, Anderson LM, Saavedra JE, Keefer LK.. (2014) Nitric oxide (NO) releasing poly ADP-ribose polymerase 1 (PARP-1) inhibitors targeted to glutathione S-transferase P1-overexpressing cancer cells.. J Med Chem, 57 (6): (2292-2302). [PMID:24521039]
181. Park CH, Lee C, Yang JS, Joe BY, Chun K, Kim H, Kim HY, Kang JS, Lee JI, Kim MH, Han G.. (2014) Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors.. Bioorg Med Chem Lett, 24 (12): (2655-2660). [PMID:24813730]
182. Menet CJ, Fletcher SR, Van Lommen G, Geney R, Blanc J, Smits K, Jouannigot N, Deprez P, van der Aar EM, Clement-Lacroix P, Lepescheux L, Galien R, Vayssiere B, Nelles L, Christophe T, Brys R, Uhring M, Ciesielski F, Van Rompaey L.. (2014) Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.. J Med Chem, 57 (22): (9323-9342). [PMID:25369270]
183. Cho N, Yang H, Kim JW, Kim YC, Sung SH.. (2014) Chemical constituents isolated from Disporum viridescens leaves and their inhibitory effect on nitric oxide production in BV2 microglial cells.. Bioorg Med Chem Lett, 24 (24): (5675-5678). [PMID:25467159]
184. Tseng CH, Tzeng CC, Chiu CC, Hsu CY, Chou CK, Chen YL.. (2015) Discovery of 2-[2-(5-nitrofuran-2-yl)vinyl]quinoline derivatives as a novel type of antimetastatic agents.. Bioorg Med Chem, 23 (1): (141-148). [PMID:25467291]
185. Hasumi K, Sato S, Saito T, Kato JY, Shirota K, Sato J, Suzuki H, Ohta S.. (2014) Design and synthesis of 5-[(2-chloro-6-fluorophenyl)acetylamino]-3-(4-fluorophenyl)-4-(4-pyrimidinyl)isoxazole (AKP-001), a novel inhibitor of p38 MAP kinase with reduced side effects based on the antedrug concept.. Bioorg Med Chem, 22 (15): (4162-4176). [PMID:24938496]
186. Cumming JG, Debreczeni JÉ, Edfeldt F, Evertsson E, Harrison M, Holdgate GA, James MJ, Lamont SG, Oldham K, Sullivan JE, Wells SL.. (2015) Discovery and characterization of MAPK-activated protein kinase-2 prevention of activation inhibitors.. J Med Chem, 58 (1): (278-293). [PMID:25255283]
187. Carry JC, Clerc F, Minoux H, Schio L, Mauger J, Nair A, Parmantier E, Le Moigne R, Delorme C, Nicolas JP, Krick A, Abécassis PY, Crocq-Stuerga V, Pouzieux S, Delarbre L, Maignan S, Bertrand T, Bjergarde K, Ma N, Lachaud S, Guizani H, Lebel R, Doerflinger G, Monget S, Perron S, Gasse F, Angouillant-Boniface O, Filoche-Rommé B, Murer M, Gontier S, Prévost C, Monteiro ML, Combeau C.. (2015) SAR156497, an exquisitely selective inhibitor of aurora kinases.. J Med Chem, 58 (1): (362-375). [PMID:25369539]
188. Koch P, Gehringer M, Laufer SA.. (2015) Inhibitors of c-Jun N-terminal kinases: an update.. J Med Chem, 58 (1): (72-95). [PMID:25415535]
189. Muth F, Günther M, Bauer SM, Döring E, Fischer S, Maier J, Drückes P, Köppler J, Trappe J, Rothbauer U, Koch P, Laufer SA.. (2015) Tetra-substituted pyridinylimidazoles as dual inhibitors of p38α mitogen-activated protein kinase and c-Jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases.. J Med Chem, 58 (1): (443-456). [PMID:25475894]
190. Chen WY, Chen FY, Lee AS, Ting KH, Chang CM, Hsu JF, Lee WS, Sheu JR, Chen CH, Shen MY.. (2015) Sesamol reduces the atherogenicity of electronegative L5 LDL in vivo and in vitro.. J Nat Prod, 78 (2): (225-233). [PMID:25692815]
191. Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, Zhang X, Zhang Y, Kays L, Hipskind PA, Wrobleski AD, Lobb KL, Clay JM, Cohen JD, Walgren JL, McCann D, Patel P, Clawson DK, Guo S, Manglicmot D, Groshong C, Logan C, Starling JJ, Flynn DL.. (2015) Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.. J Med Chem, 58 (10): (4165-4179). [PMID:25965804]
192. Chen CT, Hsu JT, Lin WH, Lu CT, Yen SC, Hsu T, Huang YL, Song JS, Chen CH, Chou LH, Yen KJ, Chen CP, Kuo PC, Huang CL, Liu HE, Chao YS, Yeh TK, Jiaang WT.. (2015) Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.. Eur J Med Chem, 100 (151-161). [PMID:26081023]
193. Zhou X, Wang Y, Lee WY, Or PM, Wan DC, Kwan YW, Yeung JH.. (2015) Miltirone Is a Dual Inhibitor of P-Glycoprotein and Cell Growth in Doxorubicin-Resistant HepG2 Cells.. J Nat Prod, 78 (9): (2266-2275). [PMID:26339922]
194. Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L.. (2015) Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.. Bioorg Med Chem, 23 (21): (7000-7006). [PMID:26455654]
195. Elkamhawy A, Farag AK, Viswanath AN, Bedair TM, Leem DG, Lee KT, Pae AN, Roh EJ.. (2015) Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.. Bioorg Med Chem Lett, 25 (22): (5147-5154). [PMID:26475520]
196. Sestito S, Nesi G, Daniele S, Martelli A, Digiacomo M, Borghini A, Pietra D, Calderone V, Lapucci A, Falasca M, Parrella P, Notarangelo A, Breschi MC, Macchia M, Martini C, Rapposelli S.. (2015) Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme.. Eur J Med Chem, 105 (274-288). [PMID:26498573]
197. Nakano H, Hasegawa T, Saito N, Furukawa K, Mukaida N, Kojima H, Okabe T, Nagano T.. (2015) Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent.. Bioorg Med Chem Lett, 25 (24): (5687-5693). [PMID:26547690]
198. Lee NY, Chung KS, Jin JS, Bang KS, Eom YJ, Hong CH, Nugroho A, Park HJ, An HJ.. (2015) Effect of Chicoric Acid on Mast Cell-Mediated Allergic Inflammation in Vitro and in Vivo.. J Nat Prod, 78 (12): (2956-2962). [PMID:26593037]
199. Aman W, Lee J, Kim M, Yang S, Jung H, Hah JM.. (2016) Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.. Bioorg Med Chem Lett, 26 (4): (1188-1192). [PMID:26810260]
200. Huard K, Gosset JR, Montgomery JI, Gilbert A, Hayward MM, Magee TV, Cabral S, Uccello DP, Bahnck K, Brown J, Purkal J, Gorgoglione M, Lanba A, Futatsugi K, Herr M, Genung NE, Aspnes G, Polivkova J, Garcia-Irizarry CN, Li Q, Canterbury D, Niosi M, Vera NB, Li Z, Khunte B, Siderewicz J, Rolph T, Erion DM.. (2016) Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family.. J Med Chem, 59 (3): (1165-1175). [PMID:26734723]
201. Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J.. (2016) 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.. J Med Chem, 59 (4): (1388-1409). [PMID:26741168]
202. Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J.. (2016) Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.. Bioorg Med Chem Lett, 26 (5): (1443-1451). [PMID:26852363]
203. Mariano M, Hartmann RW, Engel M.. (2016) Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.. Eur J Med Chem, 112 (209-216). [PMID:26896709]
204. Juszczak M, Walczak K, Matysiak J, Lemieszek MK, Langner E, Karpińska MM, Pożarowski P, Niewiadomy A, Rzeski W.. (2016) New derivative of 2-(2,4-dihydroxyphenyl)thieno-1,3-thiazin-4-one (BChTT) elicits antiproliferative effect via p38-mediated cell cycle arrest in cancer cells.. Bioorg Med Chem, 24 (6): (1356-1361). [PMID:26897091]
205. Liang X, Liu X, Wang B, Zou F, Wang A, Qi S, Chen C, Zhao Z, Wang W, Qi Z, Lv F, Hu Z, Wang L, Zhang S, Liu Q, Liu J.. (2016) Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.. J Med Chem, 59 (5): (1984-2004). [PMID:26789553]
206. Fiore M, Forli S, Manetti F.. (2016) Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.. J Med Chem, 59 (8): (3609-3634). [PMID:26502061]
207. Daydé-Cazals B, Fauvel B, Singer M, Feneyrolles C, Bestgen B, Gassiot F, Spenlinhauer A, Warnault P, Van Hijfte N, Borjini N, Chevé G, Yasri A.. (2016) Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.. J Med Chem, 59 (8): (3886-3905). [PMID:27010810]
208. Schroeder RL, Goyal N, Bratton M, Townley I, Pham NA, Tram P, Stone T, Geathers J, Nguyen K, Sridhar J.. (2016) Identification of quinones as novel PIM1 kinase inhibitors.. Bioorg Med Chem Lett, 26 (13): (3187-3191). [PMID:27173800]
209. Laufer R, Li SW, Liu Y, Ng G, Lang Y, Feher M, Brokx R, Beletskaya I, Hodgson R, Mao G, Plotnikova O, Awrey DE, Mason JM, Wei X, Lin DC, Che Y, Kiarash R, Madeira B, Fletcher GC, Mak TW, Bray MR, Pauls HW.. (2016) Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.. Bioorg Med Chem Lett, 26 (15): (3562-3566). [PMID:27335255]
210. Kumar V, Guru SK, Jain SK, Joshi P, Gandhi SG, Bharate SB, Bhushan S, Bharate SS, Vishwakarma RA.. (2016) A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties.. Bioorg Med Chem Lett, 26 (15): (3457-3463). [PMID:27363938]
211. Kim H, Lee C, Yang JS, Choi S, Park CH, Kang JS, Oh SJ, Yun J, Kim MH, Han G.. (2016) Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia.. Eur J Med Chem, 120 (74-85). [PMID:27187860]
212. Zhang L, Zhang Z, Chen F, Chen Y, Lin Y, Wang J.. (2016) Aromatic heterocyclic esters of podophyllotoxin exert anti-MDR activity in human leukemia K562/ADR cells via ROS/MAPK signaling pathways.. Eur J Med Chem, 123 (226-235). [PMID:27484511]
213. Klaeger S, Heinzlmeir S and Wilhelm M et al. (2017) The target landscape of clinical kinase drugs.. Science, 358 (6367): [PMID:29191878]
214. Chen Y, Zheng Y, Jiang Q, Qin F, Zhang Y, Fu L, He G.. (2017) Integrated bioinformatics, computational and experimental methods to discover novel Raf/extracellular-signal regulated kinase (ERK) dual inhibitors against breast cancer cells.. Eur J Med Chem, 127 (997-1011). [PMID:27839788]
215. Fu DJ, Zhang L, Song J, Mao RW, Zhao RH, Liu YC, Hou YH, Li JH, Yang JJ, Jin CY, Li P, Zi XL, Liu HM, Zhang SY, Zhang YB.. (2017) Design and synthesis of formononetin-dithiocarbamate hybrids that inhibit growth and migration of PC-3 cells via MAPK/Wnt signaling pathways.. Eur J Med Chem, 127 (87-99). [PMID:28038329]
216. Hoemann M, Wilson N, Argiriadi M, Banach D, Burchat A, Calderwood D, Clapham B, Cox P, Duignan DB, Konopacki D, Somal G, Vasudevan A.. (2016) Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.. Bioorg Med Chem Lett, 26 (22): (5562-5567). [PMID:27789138]
217. Cai Y, Li W, Tu H, Chen N, Zhong Z, Yan P, Dong J.. (2017) Curcumolide reduces diabetic retinal vascular leukostasis and leakage partly via inhibition of the p38MAPK/NF-κ B signaling.. Bioorg Med Chem Lett, 27 (8): (1835-1839). [PMID:28274631]
218. Hamed MM, Darwish SS, Herrmann J, Abadi AH, Engel M.. (2017) First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents.. J Med Chem, 60 (7): (2853-2868). [PMID:28291344]
219. Amin KM, Syam YM, Anwar MM, Ali HI, Abdel-Ghani TM, Serry AM.. (2017) Synthesis and molecular docking studies of new furochromone derivatives as p38α MAPK inhibitors targeting human breast cancer MCF-7 cells.. Bioorg Med Chem, 25 (8): (2423-2436). [PMID:28291685]
220. Wang Y, Sun Y, Cao R, Liu D, Xie Y, Li L, Qi X, Huang N.. (2017) In Silico Identification of a Novel Hinge-Binding Scaffold for Kinase Inhibitor Discovery.. J Med Chem, 60 (20): (8552-8564). [PMID:28945083]
221. Lim WC, Kim H, Kim YJ, Choi KC, Lee IH, Lee KH, Kim MK, Ko H.. (2017) Dioscin suppresses TGF-β1-induced epithelial-mesenchymal transition and suppresses A549 lung cancer migration and invasion.. Bioorg Med Chem Lett, 27 (15): (3342-3348). [PMID:28610976]
222. Lechtenberg BC, Mace PD, Sessions EH, Williamson R, Stalder R, Wallez Y, Roth GP, Riedl SJ, Pasquale EB.. (2017) Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.. ACS Med Chem Lett, 8 (7): (726-731). [PMID:28740606]
223. Liu Z, Wang P, Chen H, Wold EA, Tian B, Brasier AR, Zhou J.. (2017) Drug Discovery Targeting Bromodomain-Containing Protein 4.. J Med Chem, 60 (11): (4533-4558). [PMID:28195723]
224. Smith GP, Badolo L, Chell V, Chen IJ, Christensen KV, David L, Daechsel JA, Hentzer M, Herzig MC, Mikkelsen GK, Watson SP, Williamson DS.. (2017) The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors.. Bioorg Med Chem Lett, 27 (18): (4500-4505). [PMID:28802631]
225. Gouda AM, Abdelazeem AH, Omar HA, Abdalla AN, Abourehab MAS, Ali HI.. (2017) Pyrrolizines: Design, synthesis, anticancer evaluation and investigation of the potential mechanism of action.. Bioorg Med Chem, 25 (20): (5637-5651). [PMID:28916158]
226. Juchum M, Günther M, Döring E, Sievers-Engler A, Lämmerhofer M, Laufer S.. (2017) Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping.. J Med Chem, 60 (11): (4636-4656). [PMID:28482151]
227. Fukuda T, Goto R, Kiho T, Ueda K, Muramatsu S, Hashimoto M, Aki A, Watanabe K, Tanaka N.. (2017) Discovery of DS79182026: A potent orally active hepcidin production inhibitor.. Bioorg Med Chem Lett, 27 (16): (3716-3722). [PMID:28705644]
228. Fukuda T, Goto R, Kiho T, Ueda K, Muramatsu S, Hashimoto M, Aki A, Watanabe K, Tanaka N.. (2017) Discovery of DS28120313 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4,6-disubstituted indazole derivatives.. Bioorg Med Chem Lett, 27 (23): (5252-5257). [PMID:29079471]
229. Diab S, Abdelaziz AM, Li P, Teo T, Basnet SKC, Noll B, Rahaman MH, Lu J, Hou J, Yu M, Le BT, Albrecht H, Milne RW, Wang S.. (2017) Dual Inhibition of Mnk2 and FLT3 for potential treatment of acute myeloid leukaemia.. Eur J Med Chem, 139 (762-772). [PMID:28863357]
230. Bistrović A, Krstulović L, Harej A, Grbčić P, Sedić M, Koštrun S, Pavelić SK, Bajić M, Raić-Malić S.. (2018) Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer.. Eur J Med Chem, 143 (1616-1634). [PMID:29133046]
231. Liang C, Wu X, Li Z, Zhu J, Lu C, Shen Y.. (2018) Design, synthesis and pharmacological evaluation of N-(5-chloro-2,4-dihydroxybenzoyl)-(R)-N-arylmethyl-1,2,3,4-tetrahydro-3-isoquinolinecarboxamides as potent Hsp90 inhibitors.. Eur J Med Chem, 143 (85-96). [PMID:29172085]
232. Pu SY, Wouters R, Schor S, Rozenski J, Barouch-Bentov R, Prugar LI, O'Brien CM, Brannan JM, Dye JM, Herdewijn P, De Jonghe S, Einav S.. (2018) Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity.. J Med Chem, 61 (14): (6178-6192). [PMID:29953812]
233. Farag AK, Elkamhawy A, Londhe AM, Lee KT, Pae AN, Roh EJ.. (2017) Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.. Eur J Med Chem, 141 (657-675). [PMID:29107425]
234. Reiersølmoen AC, Han J, Sundby E, Hoff BH.. (2018) Identification of fused pyrimidines as interleukin 17 secretion inhibitors.. Eur J Med Chem, 155 (562-578). [PMID:29909341]
235. Thakkar M, Bhuniya D, Kaduskar R, Mengawade T, Naik K, Salunkhe V, Bhalerao A, Kurhade S, Mavinahalli J, Jain V, Petla R, Avaragolla S, Ray S, Rouduri S, Dhanave A, De S, Pathade V, Tambe A, Raje AA, Madgula V, Joshi S, Nadeem A, Bala M, Umrani D, Hariharan N, Kulkarni B, Mookhtiar KA.. (2017) Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.. Bioorg Med Chem Lett, 27 (8): (1867-1873). [PMID:28279528]
236. Kim SM, Park YJ, Shin MS, Kim HR, Kim MJ, Lee SH, Yun SP, Kwon SH.. (2017) Acacetin inhibits neuronal cell death induced by 6-hydroxydopamine in cellular Parkinson's disease model.. Bioorg Med Chem Lett, 27 (23): (5207-5212). [PMID:29089232]
237. Malínková V, Řezníčková E, Jorda R, Gucký T, Kryštof V.. (2017) Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.. Bioorg Med Chem, 25 (24): (6523-6535). [PMID:29089259]
238. Monastyrskyi A, Nilchan N, Quereda V, Noguchi Y, Ruiz C, Grant W, Cameron M, Duckett D, Roush W.. (2018) Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.. Bioorg Med Chem, 26 (3): (590-602). [PMID:29289448]
239. Li Q, Zhu ZX, Zhang X, Luo W, Chang LP, Chen S, Wang YX, Xie SQ, Chang CC, Wang CJ.. (2018) The lead optimization of the polyamine conjugate of flavonoid with a naphthalene motif: Synthesis and biological evaluation.. Eur J Med Chem, 146 (564-576). [PMID:29407981]
240. Cho H, Shin I, Ju E, Choi S, Hur W, Kim H, Hong E, Kim ND, Choi HG, Gray NS, Sim T.. (2018) First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.. J Med Chem, 61 (18): (8353-8373). [PMID:30153003]
241. Kaieda A, Takahashi M, Takai T, Goto M, Miyazaki T, Hori Y, Unno S, Kawamoto T, Tanaka T, Itono S, Takagi T, Hamada T, Shirasaki M, Okada K, Snell G, Bragstad K, Sang BC, Uchikawa O, Miwatashi S.. (2018) Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.. Bioorg Med Chem, 26 (3): (647-660). [PMID:29291937]
242. Assadieskandar A, Yu C, Maisonneuve P, Liu X, Chen YC, Prakash GKS, Kurinov I, Sicheri F, Zhang C.. (2018) Effects of rigidity on the selectivity of protein kinase inhibitors.. Eur J Med Chem, 146 (519-528). [PMID:29407977]
243. Wang Q, Liu F, Qi S, Qi Z, Yan XE, Wang B, Wang A, Wang W, Chen C, Liu X, Jiang Z, Hu Z, Wang L, Wang W, Ren T, Zhang S, Yun CH, Liu Q, Liu J.. (2018) Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia.. Eur J Med Chem, 150 (366-384). [PMID:29544149]
244. He LJ, Yang DL, Li SQ, Zhang YJ, Tang Y, Lei J, Frett B, Lin HK, Li HY, Chen ZZ, Xu ZG.. (2018) Facile construction of fused benzimidazole-isoquinolinones that induce cell-cycle arrest and apoptosis in colorectal cancer cells.. Bioorg Med Chem, 26 (14): (3899-3908). [PMID:29921474]
245. Lovering F, Morgan P, Allais C, Aulabaugh A, Brodfuehrer J, Chang J, Coe J, Ding W, Dowty H, Fleming M, Frisbie R, Guzova J, Hepworth D, Jasti J, Kortum S, Kurumbail R, Mohan S, Papaioannou N, Strohbach JW, Vincent F, Lee K, Zapf CW.. (2018) Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors.. Eur J Med Chem, 145 (606-621). [PMID:29348070]
246. Fearon D, Westwood IM, van Montfort RLM, Bayliss R, Jones K, Bavetsias V.. (2018) Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.. Bioorg Med Chem, 26 (11): (3021-3029). [PMID:29764757]
247. Liu H, Liang H, Meng H, Deng X, Zhang X, Lai L.. (2018) A novel allosteric inhibitor that prevents IKKβ activation.. Medchemcomm, 9 (2): (239-243). [PMID:30108917]
248. Jiang JK, Huang X, Shamim K, Patel PR, Lee A, Wang AQ, Nguyen K, Tawa G, Cuny GD, Yu PB, Zheng W, Xu X, Sanderson P, Huang W.. (2018) Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.. Bioorg Med Chem Lett, 28 (20): (3356-3362). [PMID:30227946]
249. Wang B, Wu J, Wu Y, Chen C, Zou F, Wang A, Wu H, Hu Z, Jiang Z, Liu Q, Wang W, Zhang Y, Liu F, Zhao M, Hu J, Huang T, Ge J, Wang L, Ren T, Wang Y, Liu J, Liu Q.. (2018) Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.. Eur J Med Chem, 158 (896-916). [PMID:30253346]
250. Melo TRF, Kumkhaek C, Fernandes GFDS, Lopes Pires ME, Chelucci RC, Barbieri KP, Coelho F, Capote TSO, Lanaro C, Carlos IZ, Marcondes S, Chegaev K, Guglielmo S, Fruttero R, Chung MC, Costa FF, Rodgers GP, Dos Santos JL.. (2018) Discovery of phenylsulfonylfuroxan derivatives as gamma globin inducers by histone acetylation.. Eur J Med Chem, 154 (341-353). [PMID:29852459]
251. Dodo K, Kuboki E, Shimizu T, Imamura R, Magarisawa M, Takahashi M, Tokuhiro T, Yotsumoto S, Asano K, Nakao S, Terayama N, Suda T, Tanaka M, Sodeoka M.. (2019) Development of a Water-Soluble Indolylmaleimide Derivative IM-93 Showing Dual Inhibition of Ferroptosis and NETosis.. ACS Med Chem Lett, 10 (9): (1272-1278). [PMID:31531196]
252. Zhang Q, Hu X, Wan G, Wang J, Li L, Wu X, Liu Z, Yu L.. (2019) Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.. Eur J Med Chem, 184 (111728-111728). [PMID:31610375]
253. Rana S, Sonawane YA, Taylor MA, Kizhake S, Zahid M, Natarajan A.. (2018) Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.. Bioorg Med Chem Lett, 28 (23-24): (3736-3740). [PMID:30343954]
254. Narayan S, Ramisetti S, Jaiswal AS, Law BK, Singh-Pillay A, Singh P, Amin S, Sharma AK.. (2019) ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.. Eur J Med Chem, 161 (456-467). [PMID:30384048]
255. Osborne J, Birchall K, Tsagris DJ, Lewis SJ, Smiljanic-Hurley E, Taylor DL, Levy A, Alessi DR, McIver EG.. (2019) Discovery of potent and selective 5-azaindazole inhibitors of leucine-rich repeat kinase 2 (LRRK2) - Part 1.. Bioorg Med Chem Lett, 29 (4): (668-673). [PMID:30554956]
256. Michalak B, Piwowarski JP, Granica S, Waltenberger B, Atanasov AG, Khan SY, Breuss JM, Uhrin P, Żyżyńska-Granica B, Stojakowska A, Stuppner H, Kiss AK.. (2019) Eupatoriopicrin Inhibits Pro-inflammatory Functions of Neutrophils via Suppression of IL-8 and TNF-alpha Production and p38 and ERK 1/2 MAP Kinases.. J Nat Prod, 82 (2): (375-385). [PMID:30653318]
257. Wang Y, Dou X, Jiang L, Jin H, Zhang L, Zhang L, Liu Z.. (2019) Discovery of novel glycogen synthase kinase-3α inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia.. Eur J Med Chem, 171 (221-234). [PMID:30925338]
258. Huang JM, Huang FI, Yang CR.. (2019) Moscatilin Ameliorates Tau Phosphorylation and Cognitive Deficits in Alzheimer's Disease Models.. J Nat Prod, 82 (7): (1979-1988). [PMID:31291099]
259. Liang X, Zang J, Li X, Tang S, Huang M, Geng M, Chou CJ, Li C, Cao Y, Xu W, Liu H, Zhang Y.. (2019) Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.. J Med Chem, 62 (8): (3898-3923). [PMID:30901208]
260. Tang G, Liu L, Wang X, Pan Z.. (2019) Discovery of 7H-pyrrolo[2,3-d]pyrimidine derivatives as selective covalent irreversible inhibitors of interleukin-2-inducible T-cell kinase (Itk).. Eur J Med Chem, 173 (167-183). [PMID:30999237]
261. Abdelaziz AM, Basnet SKC, Islam S, Li M, Tadesse S, Albrecht H, Gerber C, Yu M, Wang S.. (2019) Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors.. Bioorg Med Chem Lett, 29 (18): (2650-2654). [PMID:31362920]
262. Heng H, Wang Z, Li H, Huang Y, Lan Q, Guo X, Zhang L, Zhi Y, Cai J, Qin T, Xiang L, Wang S, Chen Y, Lu T, Lu S.. (2019) Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model.. Eur J Med Chem, 176 (248-267). [PMID:31103903]
263. Huang MR, Hsu YL, Lin TC, Cheng TJ, Li LW, Tseng YW, Chou YS, Liu JH, Pan SH, Fang JM, Wong CH.. (2019) Structure-guided development of purine amide, hydroxamate, and amidoxime for the inhibition of non-small cell lung cancer.. Eur J Med Chem, 181 (111551-111551). [PMID:31376567]
264. Carlson AS, Cui H, Divakaran A, Johnson JA, Brunner RM, Pomerantz WCK, Topczewski JJ.. (2019) Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors.. ACS Med Chem Lett, 10 (9): (1296-1301). [PMID:31531200]
265. Wang X, Yu C, Wang C, Ma Y, Wang T, Li Y, Huang Z, Zhou M, Sun P, Zheng J, Yang S, Fan Y, Xiang R.. (2019) Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.. Eur J Med Chem, 181 (111535-111535). [PMID:31376566]
266. Zhao L, Li Y, Wang Y, Qiao Z, Miao Z, Yang J, Huang L, Tian C, Li L, Chen D, Yang S.. (2019) Discovery of 4H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models.. J Med Chem, 62 (23): (10691-10710). [PMID:31693351]
267. Jang J, Son JB, To C, Bahcall M, Kim SY, Kang SY, Mushajiang M, Lee Y, Jänne PA, Choi HG, Gray NS.. (2017) Discovery of a potent dual ALK and EGFR T790M inhibitor.. Eur J Med Chem, 136 (497-510). [PMID:28528303]
268. Oukoloff K, Coquelle N, Bartolini M, Naldi M, Le Guevel R, Bach S, Josselin B, Ruchaud S, Catto M, Pisani L, Denora N, Iacobazzi RM, Silman I, Sussman JL, Buron F, Colletier JP, Jean L, Routier S, Renard PY.. (2019) Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3.. Eur J Med Chem, 168 (58-77). [PMID:30798053]
269. Heider F, Ansideri F, Tesch R, Pantsar T, Haun U, Döring E, Kudolo M, Poso A, Albrecht W, Laufer SA, Koch P.. (2019) Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors.. Eur J Med Chem, 175 (309-329). [PMID:31096153]
270. Yueh C, Rettenmaier J, Xia B, Hall DR, Alekseenko A, Porter KA, Barkovich K, Keseru G, Whitty A, Wells JA, Vajda S, Kozakov D.. (2019) Kinase Atlas: Druggability Analysis of Potential Allosteric Sites in Kinases.. J Med Chem, 62 (14): (6512-6524). [PMID:31274316]
271. Andrews LD, Kane TR, Dozzo P, Haglund CM, Hilderbrandt DJ, Linsell MS, Machajewski T, McEnroe G, Serio AW, Wlasichuk KB, Neau DB, Pakhomova S, Waldrop GL, Sharp M, Pogliano J, Cirz RT, Cohen F.. (2019) Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase.. J Med Chem, 62 (16): (7489-7505). [PMID:31306011]
272. Kang SJ, Lee JW, Chung SH, Jang SY, Choi J, Suh KH, Kim YH, Ham YJ, Min KH.. (2019) Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors.. Eur J Med Chem, 163 (660-670). [PMID:30576901]
273. Ikegashira K, Ikenogami T, Yamasaki T, Oka T, Hase Y, Miyagawa N, Inagaki K, Kawahara I, Koga Y, Hashimoto H.. (2019) Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.. Bioorg Med Chem Lett, 29 (7): (873-877). [PMID:30755337]
274. Jung O, Lee J, Lee YJ, Yun JM, Son YJ, Cho JY, Ryou C, Lee SY.. (2016) Timosaponin AIII inhibits migration and invasion of A549 human non-small-cell lung cancer cells via attenuations of MMP-2 and MMP-9 by inhibitions of ERK1/2, Src/FAK and β-catenin signaling pathways.. Bioorg Med Chem Lett, 26 (16): (3963-3967). [PMID:27422337]
275. Jnawali HN, Jeon D, Jeong MC, Lee E, Jin B, Ryoo S, Yoo J, Jung ID, Lee SJ, Park YM, Kim Y.. (2016) Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.. J Nat Prod, 79 (4): (961-969). [PMID:26974691]
276. Piala AT, Akella R, Potts MB, Dudics-Giagnocavo SA, He H, Wei S, White MA, Posner BA, Goldsmith EJ.. (2016) Discovery of novel TAOK2 inhibitor scaffolds from high-throughput screening.. Bioorg Med Chem Lett, 26 (16): (3923-3927). [PMID:27426302]
277. Abdelhafez OM, Ahmed EY, Abdel Latif NA, Arafa RK, Abd Elmageed ZY, Ali HI.. (2019) Design and molecular modeling of novel P38α MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds.. Bioorg Med Chem, 27 (7): (1308-1319). [PMID:30792101]
278. Li YW, Li XY, Li S, Zhao LM, Ma J, Piao HR, Jiang Z, Jin CH, Jin X.. (2020) Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5.. Bioorg Med Chem Lett, 30 (2): (126822-126822). [PMID:31810777]
279. Zak M,Hanan EJ,Lupardus P,Brown DG,Robinson C,Siu M,Lyssikatos JP,Romero FA,Zhao G,Kellar T,Mendonca R,Ray NC,Goodacre SC,Crackett PH,McLean N,Hurley CA,Yuen PW,Cheng YX,Liu X,Liimatta M,Kohli PB,Nonomiya J,Salmon G,Buckley G,Lloyd J,Gibbons P,Ghilardi N,Kenny JR,Johnson A. (2019) Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.. Bioorg Med Chem Lett, 29 (12.0): (1522-1531). [PMID:30981576]
280. Hamilton GL,Chen H,Deshmukh G,Eigenbrot C,Fong R,Johnson A,Kohli PB,Lupardus PJ,Liederer BM,Ramaswamy S,Wang H,Wang J,Xu Z,Zhu Y,Vucic D,Patel S. (2019) Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.. Bioorg Med Chem Lett, 29 (12.0): (1497-1501). [PMID:31000154]
281. Zhu P,Qian J,Xu Z,Meng C,Liu J,Shan W,Zhu W,Wang Y,Yang Y,Zhang W,Zhang Y,Ling Y. (2020) Piperlonguminine and Piperine Analogues as TrxR Inhibitors that Promote ROS and Autophagy and Regulate p38 and Akt/mTOR Signaling.. J Nat Prod, 83 (10.0): (3041-3049). [PMID:33026807]
282. Panknin O,Wagenfeld A,Bone W,Bender E,Nowak-Reppel K,Fernández-Montalván AE,Nubbemeyer R,Bäurle S,Ring S,Schmees N,Prien O,Schäfer M,Friedrich C,Zollner TM,Steinmeyer A,Mueller T,Langer G. (2020) Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.. J Med Chem, 63 (20): (11854-11881). [PMID:32960053]
283. Matheson, Christopher J., Coxon, Christopher R., Bayliss, Richard, Boxall, Kathy, Carbain, Benoit, Fry, Andrew M., Hardcastle, Ian R., Harnor, Suzannah J., Mas-Droux, Corine, Newell, David R., Richards, Mark W., Sivaprakasam, Mangaleswaran, Turner, David, Griffin, Roger J., Golding, Bernard T., Cano, Celine. (2020) 2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase. RSC Med Chem, 11 (6): (707-731). [PMID:33479670]
284. Jiang X,Zhou J,Wang Y,Chen L,Duan Y,Huang J,Liu C,Chen Y,Liu W,Sun H,Feng F,Qu W. (2020) Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.. Eur J Med Chem, 207 (112751-112751). [PMID:32950908]
285. Ding X,Stasi LP,Ho MH,Zhao B,Wang H,Long K,Xu Q,Sang Y,Sun C,Hu H,Yu H,Wan Z,Wang L,Edge C,Liu Q,Li Y,Dong K,Guan X,Tattersall FD,Reith AD,Ren F. (2018) Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors.. Bioorg Med Chem Lett, 28 (9.0): (1615-1620). [PMID:29588215]
286. Dart ML,Machleidt T,Jost E,Schwinn MK,Robers MB,Shi C,Kirkland TA,Killoran MP,Wilkinson JM,Hartnett JR,Zimmerman K,Wood KV. (2018) Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift.. ACS Med Chem Lett, 9 (6.0): (546-551). [PMID:29937980]
287. Elwaie TA,Abbas SE,Aly EI,George RF,Ali H,Kraiouchkine N,Abdelwahed KS,Fandy TE,El Sayed KA,Abd Elmageed ZY,Ali HI. (2020) HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability.. J Med Chem, 63 (24.0): (15906-15945). [PMID:33314925]
288. Jiang X,Zhou J,Wang Y,Liu X,Xu K,Xu J,Feng F,Sun H. (2021) PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.. Eur J Med Chem, 210 (112949-112949). [PMID:33097303]
289. Tabti R,Lamoureux F,Charrier C,Ory B,Heymann D,Bentouhami E,Désaubry L. (2021) Development of prohibitin ligands against osteoporosis.. Eur J Med Chem, 210 (112961-112961). [PMID:33129591]
290. Ali EMH,El-Telbany RFA,Abdel-Maksoud MS,Ammar UM,Mersal KI,Zaraei SO,El-Gamal MI,Choi SI,Lee KT,Kim HK,Lee KH,Oh CH. (2021) Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAF/p38α inhibitors.. Eur J Med Chem, 215 (113277-113277). [PMID:33601311]
291. Yang J,Chen K,Zhang G,Yang QY,Li YS,Huang SZ,Wang YL,Yang W,Jiang XJ,Yan HX,Zhu JQ,Xiang R,Luo YF,Li WM,Wei YQ,Li LL,Yang SY. (2018) Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.. Eur J Med Chem, 143 (1148-1164). [PMID:29133048]
292. Xu G,Zhang Y,Wang H,Guo Z,Wang X,Li X,Chang S,Sun T,Yu Z,Xu T,Zhao L,Wang Y,Yu W. (2020) Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors.. Eur J Med Chem, 198 (112354-112354). [PMID:32387837]
293. Liang X, Tang S, Liu X, Liu Y, Xu Q, Wang X, Saidahmatov A, Li C, Wang J, Zhou Y, Zhang Y, Geng M, Huang M, Liu H.. (2022) Discovery of Novel Pyrrolo[2,3-d]pyrimidine-based Derivatives as Potent JAK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors.. J Med Chem, 65 (2.0): (1243-1264). [PMID:33586434]
294. Zervos, A S AS, Faccio, L L, Gatto, J P JP, Kyriakis, J M JM and Brent, R R.. (1995) Mxi2, a mitogen-activated protein kinase that recognizes and phosphorylates Max protein.. Proceedings of the National Academy of Sciences of the United States of America, (7): [PMID:7479834]
295. Han, J J, Richter, B B, Li, Z Z, Kravchenko, V V and Ulevitch, R J RJ.. (1995) Molecular cloning of human p38 MAP kinase.. Biochimica et biophysica acta, (16): [PMID:7696354]
296. Freshney, N W NW and 6 more authors.. (1994) Interleukin-1 activates a novel protein kinase cascade that results in the phosphorylation of Hsp27.. Cell, (23): [PMID:7923354]
297. Raingeaud, J J, Whitmarsh, A J AJ, Barrett, T T, Dérijard, B B and Davis, R J RJ.. (1996) MKK3- and MKK6-regulated gene expression is mediated by the p38 mitogen-activated protein kinase signal transduction pathway.. Molecular and cellular biology, [PMID:8622669]
298. Wilson, K P KP and 7 more authors.. (1996) Crystal structure of p38 mitogen-activated protein kinase.. The Journal of biological chemistry, (1): [PMID:8910361]
299. Tong, L L and 7 more authors.. (1997) A highly specific inhibitor of human p38 MAP kinase binds in the ATP pocket.. Nature structural biology, [PMID:9095200]
300. Wilson, K P KP and 9 more authors.. (1997) The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase.. Chemistry & biology, [PMID:9224565]
301. Enslen, H H, Raingeaud, J J and Davis, R J RJ.. (1998) Selective activation of p38 mitogen-activated protein (MAP) kinase isoforms by the MAP kinase kinases MKK3 and MKK6.. The Journal of biological chemistry, (16): [PMID:9430721]
302. Deak, M M, Clifton, A D AD, Lucocq, L M LM and Alessi, D R DR.. (1998) Mitogen- and stress-activated protein kinase-1 (MSK1) is directly activated by MAPK and SAPK2/p38, and may mediate activation of CREB.. The EMBO journal, (3): [PMID:9687510]
303. Wang, Z Z and 8 more authors.. (1998) Structural basis of inhibitor selectivity in MAP kinases.. Structure (London, England : 1993), (15): [PMID:9753691]
304. Pierrat, B B, Correia, J S JS, Mary, J L JL, Tomás-Zuber, M M and Lesslauer, W W.. (1998) RSK-B, a novel ribosomal S6 kinase family member, is a CREB kinase under dominant control of p38alpha mitogen-activated protein kinase (p38alphaMAPK).. The Journal of biological chemistry, (6): [PMID:9792677]
305. Zhao, M M and 8 more authors.. (1999) Regulation of the MEF2 family of transcription factors by p38.. Molecular and cellular biology, [PMID:9858528]
306. Yang, S H SH, Galanis, A A and Sharrocks, A D AD.. (1999) Targeting of p38 mitogen-activated protein kinases to MEF2 transcription factors.. Molecular and cellular biology, [PMID:10330143]
307. Tanoue, T T, Moriguchi, T T and Nishida, E E.. (1999) Molecular cloning and characterization of a novel dual specificity phosphatase, MKP-5.. The Journal of biological chemistry, (9): [PMID:10391943]
308. Herbison, C E CE and 5 more authors.. (1999) Structure and polymorphism of two stress-activated protein kinase genes centromeric of the MHC: SAPK2a and SAPK4.. DNA sequence : the journal of DNA sequencing and mapping, [PMID:10727080]
309. Sayed, M M, Kim, S O SO, Salh, B S BS, Issinger, O G OG and Pelech, S L SL.. (2000) Stress-induced activation of protein kinase CK2 by direct interaction with p38 mitogen-activated protein kinase.. The Journal of biological chemistry, (2): [PMID:10747897]
310. Sanz, V V, Arozarena, I I and Crespo, P P.. (2000) Distinct carboxy-termini confer divergent characteristics to the mitogen-activated protein kinase p38alpha and its splice isoform Mxi2.. FEBS letters, (2): [PMID:10838079]
311. Tamura, K K and 5 more authors.. (2000) Requirement for p38alpha in erythropoietin expression: a role for stress kinases in erythropoiesis.. Cell, (21): [PMID:10943842]
312. Scheper, G C GC, Morrice, N A NA, Kleijn, M M and Proud, C G CG.. (2001) The mitogen-activated protein kinase signal-integrating kinase Mnk2 is a eukaryotic initiation factor 4E kinase with high levels of basal activity in mammalian cells.. Molecular and cellular biology, [PMID:11154262]
313. Slack, D N DN, Seternes, O M OM, Gabrielsen, M M and Keyse, S M SM.. (2001) Distinct binding determinants for ERK2/p38alpha and JNK map kinases mediate catalytic activation and substrate selectivity of map kinase phosphatase-1.. The Journal of biological chemistry, (11): [PMID:11278799]
314. Bulavin, D V DV and 7 more authors.. (2001) Initiation of a G2/M checkpoint after ultraviolet radiation requires p38 kinase.. Nature, (3): [PMID:11333986]
315. Tanoue, T T, Yamamoto, T T, Maeda, R R and Nishida, E E.. (2001) A Novel MAPK phosphatase MKP-7 acts preferentially on JNK/SAPK and p38 alpha and beta MAPKs.. The Journal of biological chemistry, (13): [PMID:11359773]
316. Ge, Baoxue B and 7 more authors.. (2002) MAPKK-independent activation of p38alpha mediated by TAB1-dependent autophosphorylation of p38alpha.. Science (New York, N.Y.), (15): [PMID:11847341]
317. Sudo, Tatsuhiko T, Yagasaki, Yuki Y, Hama, Hiroshi H, Watanabe, Naoko N and Osada, Hiroyuki H.. (2002) Exip, a new alternative splicing variant of p38 alpha, can induce an earlier onset of apoptosis in HeLa cells.. Biochemical and biophysical research communications, (8): [PMID:11866441]
318. Zhu, Shan S and 14 more authors.. (2002) Minocycline inhibits cytochrome c release and delays progression of amyotrophic lateral sclerosis in mice.. Nature, (2): [PMID:11986668]
319. Gevaert, Kris K and 6 more authors.. (2003) Exploring proteomes and analyzing protein processing by mass spectrometric identification of sorted N-terminal peptides.. Nature biotechnology, [PMID:12665801]
320. Patel, Sangita B SB and 5 more authors.. (2004) Lattice stabilization and enhanced diffraction in human p38 alpha crystals by protein engineering.. Biochimica et biophysica acta, (14): [PMID:14726206]
321. Diskin, Ron R, Askari, Nadav N, Capone, Ricardo R, Engelberg, David D and Livnah, Oded O.. (2004) Active mutants of the human p38alpha mitogen-activated protein kinase.. The Journal of biological chemistry, (5): [PMID:15284239]
322. Rush, John J and 9 more authors.. (2005) Immunoaffinity profiling of tyrosine phosphorylation in cancer cells.. Nature biotechnology, [PMID:15592455]
323. Salvador, Jesus M JM, Mittelstadt, Paul R PR, Belova, Galina I GI, Fornace, Albert J AJ and Ashwell, Jonathan D JD.. (2005) The autoimmune suppressor Gadd45alpha inhibits the T cell alternative p38 activation pathway.. Nature immunology, [PMID:15735649]
324. Lominadze, George G and 5 more authors.. (2005) Myeloid-related protein-14 is a p38 MAPK substrate in human neutrophils.. Journal of immunology (Baltimore, Md. : 1950), (1): [PMID:15905572]
325. Sullivan, Jane E JE and 13 more authors.. (2005) Prevention of MKK6-dependent activation by binding to p38alpha MAP kinase.. Biochemistry, (20): [PMID:16342939]
326. Fu, Jing J, Yang, Ziqiang Z, Wei, Jinxue J, Han, Jiahuai J and Gu, Jun J.. (2006) Nuclear protein NP60 regulates p38 MAPK activity.. Journal of cell science, (1): [PMID:16352664]
327. Zohn, Irene E IE and 5 more authors.. (2006) p38 and a p38-interacting protein are critical for downregulation of E-cadherin during mouse gastrulation.. Cell, (2): [PMID:16751104]
328. Khurana, Ashwani A and 5 more authors.. (2006) Regulation of the ring finger E3 ligase Siah2 by p38 MAPK.. The Journal of biological chemistry, (17): [PMID:17003045]
329. ter Haar, Ernst E, Prabhakar, Prakash P, Prabakhar, Prakash P, Liu, Xun X and Lepre, Christopher C.. (2007) Crystal structure of the p38 alpha-MAPKAP kinase 2 heterodimer.. The Journal of biological chemistry, (30): [PMID:17255097]
330. Matsuoka, Shuhei S and 12 more authors.. (2007) ATM and ATR substrate analysis reveals extensive protein networks responsive to DNA damage.. Science (New York, N.Y.), (25): [PMID:17525332]
331. Qi, Xiaomei X and 7 more authors.. (2007) p38alpha antagonizes p38gamma activity through c-Jun-dependent ubiquitin-proteasome pathways in regulating Ras transformation and stress response.. The Journal of biological chemistry, (26): [PMID:17724032]
332. Zahedi, René P RP and 8 more authors.. (2008) Phosphoproteome of resting human platelets.. Journal of proteome research, [PMID:18088087]
333. Kneidinger, Michael M and 17 more authors.. (2008) The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils.. Blood, (15): [PMID:18180381]
334. Daub, Henrik H and 9 more authors.. (2008) Kinase-selective enrichment enables quantitative phosphoproteomics of the kinome across the cell cycle.. Molecular cell, (8): [PMID:18691976]
335. Mayya, Viveka V and 7 more authors.. (2009) Quantitative phosphoproteomic analysis of T cell receptor signaling reveals system-wide modulation of protein-protein interactions.. Science signaling, (18): [PMID:19690332]
336. Webber, Jemma L JL and Tooze, Sharon A SA.. (2010) Coordinated regulation of autophagy by p38alpha MAPK through mAtg9 and p38IP.. The EMBO journal, (6): [PMID:19893488]
337. Wang, Pingzhang P, Yu, Peng P, Gao, Peng P, Shi, Taiping T and Ma, Dalong D.. (2009) Discovery of novel human transcript variants by analysis of intronic single-block EST with polyadenylation site.. BMC genomics, (12): [PMID:19906316]
338. Xu, Pinglong P and Derynck, Rik R.. (2010) Direct activation of TACE-mediated ectodomain shedding by p38 MAP kinase regulates EGF receptor-dependent cell proliferation.. Molecular cell, (26): [PMID:20188673]
339. Cuadrado, Ana A and Nebreda, Angel R AR.. (2010) Mechanisms and functions of p38 MAPK signalling.. The Biochemical journal, (1): [PMID:20626350]
340. Reinhardt, H Christian HC and 10 more authors.. (2010) DNA damage activates a spatially distinct late cytoplasmic cell-cycle checkpoint network controlled by MK2-mediated RNA stabilization.. Molecular cell, (8): [PMID:20932473]
341. Cariolato, Luca L, Cavin, Sabrina S and Diviani, Dario D.. (2011) A-kinase anchoring protein (AKAP)-Lbc anchors a PKN-based signaling complex involved in α1-adrenergic receptor-induced p38 activation.. The Journal of biological chemistry, (11): [PMID:21224381]
342. An, Hanbing H, Lu, Xinyuan X, Liu, Dan D and Yarbrough, Wendell G WG.. (2011) LZAP inhibits p38 MAPK (p38) phosphorylation and activity by facilitating p38 association with the wild-type p53 induced phosphatase 1 (WIP1).. PloS one, (24): [PMID:21283629]
343. Peng, Hui H and 5 more authors.. (2011) The Mycobacterium tuberculosis early secreted antigenic target of 6 kDa inhibits T cell interferon-γ production through the p38 mitogen-activated protein kinase pathway.. The Journal of biological chemistry, (8): [PMID:21586573]
344. Zhou, Houjiang H and 6 more authors.. (2013) Toward a comprehensive characterization of a human cancer cell phosphoproteome.. Journal of proteome research, (4): [PMID:23186163]
345. Li, Cong C and 9 more authors.. (2019) MicroRNA-143-3p promotes human cardiac fibrosis via targeting sprouty3 after myocardial infarction.. Journal of molecular and cellular cardiology, [PMID:30878395]
346. May-Dracka TL,Arduini R,Bertolotti-Ciarlet A,Bhisetti G,Brickelmaier M,Cahir-McFarland E,Enyedy I,Fontenot JD,Hesson T,Little K,Lyssikatos J,Marcotte D,McKee T,Murugan P,Patterson T,Peng H,Rushe M,Silvian L,Spilker K,Wu P,Xin Z,Burkly LC. (2018) Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity.. Bioorg Med Chem Lett, 28 (10): (1964-1971). [PMID:29636220]

Solution Calculators

Molarity Calculator

Determine the necessary mass, volume, or concentration for preparing a solution.

Dilution Calculator

Determine the dilution needed to prepare a stock solution.

SKU	Size	Availability	Price
Ab119717-10μl	10μl	In stock	$66.90
Ab119717-50μl	50μl	In stock	$189.90
Ab119717-100μl	100μl	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$299.90
Ab119717-1ml	1ml	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$2,809.90

Recombinant p38 alpha/MAPK14 Antibody - Primary antibody, specific to p38 alpha/MAPK14, Rabbit IgG