Call +1 (833) 552-7181 or Contact us Earn $25 in coupons on your first order with Aladdin!
Toggle Nav
My Cart
Search
Advanced Search
Menu
Sign In
྾
main product photo

Recombinant PDGFR alpha Antibody - Primary antibody, specific to PDGFRA, Rabbit IgG

    Application:
  • WB
Features and benefits
  • Host species: Rabbit
  • Species reactivity(Reacts with): Human,Mouse,Rat
  • Isotype: Rabbit IgG
  • Conjugation: Unconjugated
Item Number
Ab120914
Grouped product items
SKUSizeAvailabilityPrice Qty
Ab120914-10μl
10μl
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$76.90
Ab120914-50μl
50μl
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$229.90
Ab120914-100μl
100μl
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$329.90
Ab120914-1ml
1ml
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,699.90
Add to Wish List Compare
Bulk Order  DATASHEET

Recombinant; Rabbit anti Human PDGFR alpha Antibody; WB; Unconjugated

View related series
Click to view target information: PDGFRA
Accession#:P16234 Gene ID:5156 PDGFR alpha PDGFRA

Basic Description

Product NameRecombinant PDGFR alpha Antibody - Primary antibody, specific to PDGFRA, Rabbit IgG
SynonymsPDGFRA | PDGFR2 | RHEPDGFRA | Platelet-derived growth factor receptor alpha | PDGF-R-alpha | PDGFR-alpha | Alpha platelet-derived growth factor receptor | Alpha-type platelet-derived growth factor receptor | CD140 antigen-like family member A | CD140a ant
Specifications & PurityExactAb™, Validated, Recombinant, 0.3 mg/mL
Host speciesRabbit
SpecificityPDGFRA
ImmunogenA synthetic peptide derived from human PDGF Receptor alpha (AA 1074-1089).
Positive ControlWB: C6, 3T3 lysates.
ConjugationUnconjugated
GradeExactAb™, Recombinant, Validated
Product Description

Rabbit anti Human PDGFR alpha Antibody, Recombinant, could be used for WB and so on.
Application:
WB: 1/500-1/1000
Protein Function
Receptor that binds both PDGFA and PDGFB and has a tyrosine-protein kinase activity.

Product Properties

IsotypeRabbit IgG
SDS-PAGE150 kDa
Purification MethodImmunogen affinity purified
FormLiquid
Concentration0.3 mg/mL
Storage TempStore at -20°C,Avoid repeated freezing and thawing
Shipped InIce chest + Ice pads
Stability And StorageStore 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 PDGFR alpha Antibody (Ab120914) - Western Blot
All lanes: Recombinant PDGFR alpha Antibody (Ab120914) 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: 195 kDa
Observed band size: 173 kDa
Exposure time: 28.8 s

Associated Targets(Human)

PDGFRA Tclin Platelet-derived growth factor receptor alpha (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PDGFRA Tclin Platelet-derived growth factor receptor alpha (5682 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Application

ApplicationDilution info
WB1/500-1/1000

">

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 NumberCertificate TypeDateItem
ZJ23F0901086Certificate of AnalysisSep 18, 2023 Ab120914
ZJ23F0901087Certificate of AnalysisSep 18, 2023 Ab120914

Related Documents

 SDS

 Specification Sheet

FAQs and Articles

FAQ
Guidelines of Primary Antibodies for Western Blotting
Categories: Protocols
Tags:
Western blotting Monoclonal antibodies Recombinant Antibodies Polyclonal Antibodies Primary Antibodies Selection Loading Controls
Protocol of Western Blotting For High Molecular Weights
Categories: Protocols
Tags:
Western blotting Biological buffer Immunoblotting Protein Electrophoresis High Molecular Weights large molecular proteins WB antibody

References

1. Kraker AJ, Hartl BG, Amar AM, Barvian MR, Showalter HD, Moore CW..  (2000)  Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors..  Biochem Pharmacol,  60  (7): (885-898).  [PMID:10974196] [10.1016/s0006-2952(00)00405-6]
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] [10.1021/op500134e]
3. Kubo K, Shimizu T, Ohyama S, Murooka H, Iwai A, Nakamura K, Hasegawa K, Kobayashi Y, Takahashi N, Takahashi K et al..  (2005)  Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas..  J Med Chem,  48  (5): (1359-66).  [PMID:15743179] [10.1021/op500134e]
4. Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S et al..  (2010)  Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant..  J Med Chem,  53  (12): (4701-19).  [PMID:20513156] [10.1021/op500134e]
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] [10.1021/op500134e]
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] [10.1021/op500134e]
7. 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] [10.1021/op500134e]
8. Dubreuil P, Letard S, Ciufolini M, Gros L, Humbert M, Castéran N, Borge L, Hajem B, Lermet A, Sippl W et al..  (2009)  Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT..  PLoS ONE,  4  (9): (e7258).  [PMID:19789626] [10.1021/op500134e]
9. Zhou Y, Chen Y, Tong L, Xie H, Wen W, Zhang J, Xi Y, Shen Y, Geng M, Wang Y et al..  (2012)  AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR..  J Cell Mol Med,  16  (10): (2321-30).  [PMID:22304225] [10.1021/op500134e]
10. Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A et al..  (2006)  N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor..  J Med Chem,  49  (22): (6465-88).  [PMID:17064066] [10.1021/op500134e]
11. Klutchko SR, Zhou H, Winters RT, Tran TP, Bridges AJ, Althaus IW, Amato DM, Elliott WL, Ellis PA, Meade MA et al..  (2006)  Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors..  J Med Chem,  49  (4): (1475-85).  [PMID:16480284] [10.1021/op500134e]
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] [10.1021/op500134e]
13. 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] [10.1021/op500134e]
14. Heinrich MC, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M.  (2012)  Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors..  Clin Cancer Res,  18  (16): (4375-84).  [PMID:22745105] [10.1021/op500134e]
15. 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] [10.1021/op500134e]
16. 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] [10.1021/op500134e]
17. Roberts WG, Whalen PM, Soderstrom E, Moraski G, Lyssikatos JP, Wang HF, Cooper B, Baker DA, Savage D, Dalvie D et al..  (2005)  Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451..  Cancer Res,  65  (3): (957-66).  [PMID:15705896] [10.1021/op500134e]
18. Trudel S, Li ZH, Wei E, Wiesmann M, Chang H, Chen C, Reece D, Heise C, Stewart AK.  (2005)  CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma..  Blood,  105  (7): (2941-8).  [PMID:15598814] [10.1021/op500134e]
19. 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] [10.1021/op500134e]
20. 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] [10.1021/op500134e]
21. Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K et al..  (2012)  Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent..  J Med Chem,  55  (2): (903-13).  [PMID:22148921] [10.1021/op500134e]
22. 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] [10.1021/op500134e]
23. Fraser C, Dawson JC, Dowling R, Houston DR, Weiss JT, Munro AF, Muir M, Harrington L, Webster SP, Frame MC et al..  (2016)  Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase..  J Med Chem,  59  (10): (4697-710).  [PMID:27115835] [10.1021/op500134e]
24. 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] [10.1021/op500134e]
25. 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] [10.1021/op500134e]
26. 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] [10.1021/op500134e]
27. Lam B, Arikawa Y, Cramlett J, Dong Q, de Jong R, Feher V, Grimshaw CE, Farrell PJ, Hoffman ID, Jennings A et al..  (2016)  Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK)..  Bioorg Med Chem Lett,  26  (24): (5947-5950).  [PMID:27839918] [10.1021/op500134e]
28. Huang Z, Li H, Zhang Q, Lu F, Hong M, Zhang Z, Guo X, Zhu Y, Li S, Liu H.  (2017)  Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis..  ACS Med Chem Lett,  8  (11): (1142-1147).  [PMID:29152045] [10.1021/op500134e]
29. 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] [10.1021/op500134e]
30. 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] [10.1021/op500134e]
31. Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH et al..  (2012)  Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families..  J Pharmacol Exp Ther,  343  (3): (617-27).  [PMID:22935731] [10.1021/op500134e]
32. Patwardhan PP, Ivy KS, Musi E, de Stanchina E, Schwartz GK.  (2016)  Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma..  Oncotarget,  7  (4): (4093-109).  [PMID:26675259] [10.1021/op500134e]
33. Gucký T, Řezníčková E, Radošová Muchová T, Jorda R, Klejová Z, Malínková V, Berka K, Bazgier V, Ajani H, Lepšík M et al..  (2018)  Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations..  J Med Chem,  61  (9): (3855-3869).  [PMID:29672049] [10.1021/op500134e]
34. 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] [10.1039/C8MD00068A]
35. Reich SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B, Ernst JT, Han Q, Goel VK et al..  (2018)  Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition..  J Med Chem,  61  (8): (3516-3540).  [PMID:29526098] [10.1021/op500134e]
36. 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] [10.1021/op500134e]
37. Wu Y, Wang B, Wang J, Qi S, Zou F, Qi Z, Liu F, Liu Q, Chen C, Hu C et al..  (2019)  Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors..  J Med Chem,  62  (13): (6083-6101).  [PMID:31250638] [10.1021/op500134e]
38. Fensome A, Ambler CM, Arnold E, Banker ME, Brown MF, Chrencik J, Clark JD, Dowty ME, Efremov IV, Flick A et al..  (2018)  Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)..  J Med Chem,  61  (19): (8597-8612).  [PMID:30113844] [10.1021/op500134e]
39. Zhou Y, Shan S, Li ZB, Xin LJ, Pan DS, Yang QJ, Liu YP, Yue XP, Liu XR, Gao JZ et al..  (2017)  CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency..  Cancer Sci,  108  (3): (469-477).  [PMID:28004478] [10.1021/op500134e]
40. 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] [10.1021/op500134e]
41. Mazzocca A, Napolitano A, Silletta M, Spalato Ceruso M, Santini D, Tonini G, Vincenzi B.  (2019)  New frontiers in the medical management of gastrointestinal stromal tumours..  Ther Adv Med Oncol,  11  (13): (1755-70).  [PMID:31205499] [10.1177/1758835919841946]
42. Ren X, Pan X, Zhang Z, Wang D, Lu X, Li Y, Wen D, Long H, Luo J, Feng Y et al..  (2013)  Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib..  J Med Chem,  56  (3): (879-94).  [PMID:23301703] [10.1021/op500134e]
43. 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,  71  (13): (1755-70).  [PMID:32787110] [10.1021/acs.jmedchem.0c00936]
44. Liao AT, Chien MB, Shenoy N, Mendel DB, McMahon G, Cherrington JM, London CA.  (2002)  Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors..  Blood,  100  (2): (585-93).  [PMID:12091352] [10.1021/op500134e]
45. Yang H, Chennamaneni LR, Ho MWT, Ang SH, Tan ESW, Jeyaraj DA, Yeap YS, Liu B, Ong EH, Joy JK et al..  (2018)  Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia..  J Med Chem,  61  (10): (4348-4369).  [PMID:29683667] [10.1021/op500134e]
46. 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]
47. Sung Hee Hwang, Aaron T Wecksler, Guodong Zhang, Christophe Morisseau, Long V Nguyen, Samuel H Fu, Bruce D Hammock,.  (2013-06-04)  Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors..  Bioorganic & medicinal chemistry letters,  23  ((13)): ( 3732-3737 ).  [PMID:23726028]
48. Ajit Dhananjay Jagtap,Pei-Teh Chang,Jia-Rong Liu,Hsiao-Chun Wang,Nagendra B Kondekar,Li-Jiuan Shen,Hsiang-Wen Tseng,Grace Shiahuy Chen,Ji-Wang Chern.  (2014-08-05)  Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia..  European journal of medicinal chemistry,  85  (268-288).  [PMID:25089810]
49. Bing Yu,Li-da Tang,Yi-Liang Li,Shu-Hui Song,Xiao-Liang Ji,Mu-Sen Lin,Chun-Fu Wu.  (2011-12-16)  Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase..  Bioorganic & medicinal chemistry letters,  22  ((1)): (110-114).  [PMID:22169262]
50. 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] [10.1021/jm031145u]
51. Kuo GH, Wang A, Emanuel S, Deangelis A, Zhang R, Connolly PJ, Murray WV, Gruninger RH, Sechler J, Fuentes-Pesquera A, Johnson D, Middleton SA, Jolliffe L, Chen X..  (2005)  Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors..  J Med Chem,  48  (6): (1886-1900).  [PMID:15771433] [10.1021/jm040099a]
52. 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] [10.1021/jm049355+]
53. Vendôme J, Letard S, Martin F, Svinarchuk F, Dubreuil P, Auclair C, Le Bret M..  (2005)  Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases..  J Med Chem,  48  (20): (6194-6201).  [PMID:16190746] [10.1021/jm050231m]
54. McDermott LA, Higgins B, Simcox M, Luk KC, Nevins T, Kolinsky K, Smith M, Yang H, Li JK, Chen Y, Ke J, Mallalieu N, Egan T, Kolis S, Railkar A, Gerber L, Liu JJ, Konzelmann F, Zhang Z, Flynn T, Morales O, Chen Y..  (2006)  Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis..  Bioorg Med Chem Lett,  16  (7): (1950-1953).  [PMID:16460940] [10.1016/j.bmcl.2005.12.092]
55. 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] [10.1021/jm061112p]
56. Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ..  (2007)  1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel..  J Med Chem,  50  (9): (2011-2029).  [PMID:17425296] [10.1021/jm061223o]
57. Weiss MM, Harmange JC, Polverino AJ, Bauer D, Berry L, Berry V, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Whittington DA, Zanon R..  (2008)  Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors..  J Med Chem,  51  (6): (1668-1680).  [PMID:18324759] [10.1021/jm701098w]
58. 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] [10.1073/pnas.0707498104]
59. Kunz RK, Rumfelt S, Chen N, Zhang D, Tasker AS, Bürli R, Hungate R, Yu V, Nguyen Y, Whittington DA, Meagher KL, Plant M, Tudor Y, Schrag M, Xu Y, Ng GY, Hu E..  (2008)  Discovery of amido-benzisoxazoles as potent c-Kit inhibitors..  Bioorg Med Chem Lett,  18  (18): (5115-5117).  [PMID:18723346] [10.1016/j.bmcl.2008.07.111]
60. 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] [10.1021/jm800986w]
61. 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] [10.1021/jm800937p]
62. Golubovskaya VM, Nyberg C, Zheng M, Kweh F, Magis A, Ostrov D, Cance WG..  (2008)  A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the y397 site of focal adhesion kinase decreases tumor growth..  J Med Chem,  51  (23): (7405-7416).  [PMID:18989950] [10.1021/jm800483v]
63. Cha MY, Lee KO, Kim JW, Lee CG, Song JY, Kim YH, Lee GS, Park SB, Kim MS..  (2009)  Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer..  J Med Chem,  52  (21): (6880-6888).  [PMID:19888761] [10.1021/jm901146p]
64. 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] [10.1016/j.bmcl.2009.10.085]
65. 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] [10.1016/j.bmc.2009.07.056]
66. 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] [10.1016/j.bmc.2009.09.008]
67. 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] [10.1016/j.bmcl.2009.09.010]
68. 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] [10.1021/jm100095x]
69. Yu H, Jung Y, Kim H, Lee J, Oh CH, Yoo KH, Sim T, Hah JM..  (2010)  1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives: a novel type II Raf kinase inhibitors..  Bioorg Med Chem Lett,  20  (12): (3805-3808).  [PMID:20466542] [10.1016/j.bmcl.2010.04.039]
70. 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] [10.1016/j.bmcl.2010.05.043]
71. 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] [10.1021/jm901808w]
72. Barile E, De SK, Carlson CB, Chen V, Knutzen C, Riel-Mehan M, Yang L, Dahl R, Chiang G, Pellecchia M..  (2010)  Design, synthesis, and structure-activity relationships of 3-ethynyl-1H-indazoles as inhibitors of the phosphatidylinositol 3-kinase signaling pathway..  J Med Chem,  53  (23): (8368-8375).  [PMID:21062009] [10.1021/jm100825h]
73. 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] [10.1016/j.bmcl.2010.11.010]
74. 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] [10.1021/jm101499u]
75. Okamoto M, Kojima H, Saito N, Okabe T, Masuda Y, Furuya T, Nagano T..  (2011)  Virtual screening and further development of novel ALK inhibitors..  Bioorg Med Chem,  19  (10): (3086-3095).  [PMID:21515061] [10.1016/j.bmc.2011.04.008]
76. Shallal HM, Russu WA..  (2011)  Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives..  Eur J Med Chem,  46  (6): (2043-2057).  [PMID:21429632] [10.1016/j.ejmech.2011.02.057]
77. Lin WH, Hsieh SY, Yen SC, Chen CT, Yeh TK, Hsu T, Lu CT, Chen CP, Chen CW, Chou LH, Huang YL, Cheng AH, Chang YI, Tseng YJ, Yen KR, Chao YS, Hsu JT, Jiaang WT..  (2011)  Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3)..  Bioorg Med Chem,  19  (14): (4173-4182).  [PMID:21708468] [10.1016/j.bmc.2011.06.016]
78. 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] [10.1021/jm2008634]
79. 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] [10.1016/j.bmcl.2012.01.028]
80. Li WW, Wang XY, Zheng RL, Yan HX, Cao ZX, Zhong L, Wang ZR, Ji P, Yang LL, Wang LJ, Xu Y, Liu JJ, Yang J, Zhang CH, Ma S, Feng S, Sun QZ, Wei YQ, Yang SY..  (2012)  Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo..  J Med Chem,  55  (8): (3852-3866).  [PMID:22452518] [10.1021/jm300042x]
81. Nakano H, Saito N, Parker L, Tada Y, Abe M, Tsuganezawa K, Yokoyama S, Tanaka A, Kojima H, Okabe T, Nagano T..  (2012)  Rational evolution of a novel type of potent and selective proviral integration site in Moloney murine leukemia virus kinase 1 (PIM1) inhibitor from a screening-hit compound..  J Med Chem,  55  (11): (5151-5164).  [PMID:22540945] [10.1021/jm3001289]
82. 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] [10.1021/jm200900q]
83. 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] [10.1016/j.bmcl.2012.06.104]
84. Duveau DY, Hu X, Walsh MJ, Shukla S, Skoumbourdis AP, Boxer MB, Ambudkar SV, Shen M, Thomas CJ..  (2013)  Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors..  Bioorg Med Chem Lett,  23  (3): (682-686).  [PMID:23273517] [10.1016/j.bmcl.2012.11.111]
85. Garofalo AW, Adler M, Aubele DL, Bowers S, Franzini M, Goldbach E, Lorentzen C, Neitz RJ, Probst GD, Quinn KP, Santiago P, Sham HL, Tam D, Truong AP, Ye XM, Ren Z..  (2013)  Novel cinnoline-based inhibitors of LRRK2 kinase activity..  Bioorg Med Chem Lett,  23  (1): (71-74).  [PMID:23219325] [10.1016/j.bmcl.2012.11.021]
86. Yang LL, Li GB, Ma S, Zou C, Zhou S, Sun QZ, Cheng C, Chen X, Wang LJ, Feng S, Li LL, Yang SY..  (2013)  Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo..  J Med Chem,  56  (4): (1641-1655).  [PMID:23362959] [10.1021/jm301537p]
87. 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] [10.1016/j.bmcl.2013.01.110]
88. Garofalo AW, Adler M, Aubele DL, Brigham EF, Chian D, Franzini M, Goldbach E, Kwong GT, Motter R, Probst GD, Quinn KP, Ruslim L, Sham HL, Tam D, Tanaka P, Truong AP, Ye XM, Ren Z..  (2013)  Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors..  Bioorg Med Chem Lett,  23  (7): (1974-1977).  [PMID:23453068] [10.1016/j.bmcl.2013.02.041]
89. Franzini M, Ye XM, Adler M, Aubele DL, Garofalo AW, Gauby S, Goldbach E, Probst GD, Quinn KP, Santiago P, Sham HL, Tam D, Truong A, Ren Z..  (2013)  Triazolopyridazine LRRK2 kinase inhibitors..  Bioorg Med Chem Lett,  23  (7): (1967-1973).  [PMID:23454015] [10.1016/j.bmcl.2013.02.043]
90. 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] [10.1016/j.bmc.2013.03.083]
91. Pauwels D, Klaassen H, Lahortiga I, Kilonda A, Jacobs K, Sweron B, Corbau R, Chaltin P, Marchand A, Cools J..  (2013)  Identification of novel FLT3 kinase inhibitors..  Eur J Med Chem,  63  (713-721).  [PMID:23567961] [10.1016/j.ejmech.2013.03.024]
92. 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] [10.1016/j.bmcl.2013.02.065]
93. Troxler T, Greenidge P, Zimmermann K, Desrayaud S, Drückes P, Schweizer T, Stauffer D, Rovelli G, Shimshek DR..  (2013)  Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2..  Bioorg Med Chem Lett,  23  (14): (4085-4090).  [PMID:23768909] [10.1016/j.bmcl.2013.05.054]
94. Gogate PN, Ethirajan M, Kurenova EV, Magis AT, Pandey RK, Cance WG..  (2014)  Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction..  Eur J Med Chem,  80  (154-166).  [PMID:24780592] [10.1016/j.ejmech.2014.04.041]
95. Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB..  (2014)  Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2..  Bioorg Med Chem Lett,  24  (12): (2635-2639).  [PMID:24813737] [10.1016/j.bmcl.2014.04.068]
96. Xie F, Zhu H, Zhang H, Lang Q, Tang L, Huang Q, Yu L..  (2015)  In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor..  Eur J Med Chem,  89  (310-319).  [PMID:25462247] [10.1016/j.ejmech.2014.10.044]
97. Zhang P, Li S, Gao Y, Lu W, Huang K, Ye D, Li X, Chu Y..  (2014)  Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake..  Bioorg Med Chem Lett,  24  (24): (5639-5643).  [PMID:25467150] [10.1016/j.bmcl.2014.10.078]
98. Song Z, Yang Y, Liu Z, Peng X, Guo J, Yang X, Wu K, Ai J, Ding J, Geng M, Zhang A..  (2015)  Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases..  J Med Chem,  58  (1): (197-211).  [PMID:24785465] [10.1021/jm5005144]
99. 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] [10.1021/jm501557a]
100. Roth GJ, Binder R, Colbatzky F, Dallinger C, Schlenker-Herceg R, Hilberg F, Wollin SL, Kaiser R..  (2015)  Nintedanib: from discovery to the clinic..  J Med Chem,  58  (3): (1053-1063).  [PMID:25474320] [10.1021/jm501562a]
101. Lawrence HR, Mahajan K, Luo Y, Zhang D, Tindall N, Huseyin M, Gevariya H, Kazi S, Ozcan S, Mahajan NP, Lawrence NJ..  (2015)  Development of novel ACK1/TNK2 inhibitors using a fragment-based approach..  J Med Chem,  58  (6): (2746-2763).  [PMID:25699576] [10.1021/jm501929n]
102. Kovackova S, Chang L, Bekerman E, Neveu G, Barouch-Bentov R, Chaikuad A, Heroven C, Šála M, De Jonghe S, Knapp S, Einav S, Herdewijn P..  (2015)  Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents..  J Med Chem,  58  (8): (3393-3410).  [PMID:25822739] [10.1021/jm501759m]
103. Zhang CH, Zheng MW, Li YP, Lin XD, Huang M, Zhong L, Li GB, Zhang RJ, Lin WT, Jiao Y, Wu XA, Yang J, Xiang R, Chen LJ, Zhao YL, Cheng W, Wei YQ, Yang SY..  (2015)  Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer..  J Med Chem,  58  (9): (3957-3974).  [PMID:25835317] [10.1021/acs.jmedchem.5b00270]
104. 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] [10.1016/j.ejmech.2015.05.008]
105. Lin XD, Yang HW, Ma S, Li WW, Zhang CH, Wang WJ, Xiang R, Li LL, Yang SY..  (2015)  Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors..  Bioorg Med Chem Lett,  25  (20): (4534-4538).  [PMID:26342867] [10.1016/j.bmcl.2015.08.068]
106. Carta D, Bortolozzi R, Hamel E, Basso G, Moro S, Viola G, Ferlin MG..  (2015)  Novel 3-Substituted 7-Phenylpyrrolo[3,2-f]quinolin-9(6H)-ones as Single Entities with Multitarget Antiproliferative Activity..  J Med Chem,  58  (20): (7991-8010).  [PMID:26418966] [10.1021/acs.jmedchem.5b00805]
107. 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] [10.1016/j.bmc.2015.09.038]
108. Ravez S, Arsenlis S, Barczyk A, Dupont A, Frédérick R, Hesse S, Kirsch G, Depreux P, Goossens L..  (2015)  Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors..  Bioorg Med Chem,  23  (22): (7340-7347).  [PMID:26526740] [10.1016/j.bmc.2015.10.035]
109. 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] [10.1016/j.bmcl.2015.10.098]
110. Meredith EL, Mainolfi N, Poor S, Qiu Y, Miranda K, Powers J, Liu D, Ma F, Solovay C, Rao C, Johnson L, Ji N, Artman G, Hardegger L, Hanks S, Shen S, Woolfenden A, Fassbender E, Sivak JM, Zhang Y, Long D, Cepeda R, Liu F, Hosagrahara VP, Lee W, Tarsa P, Anderson K, Elliott J, Jaffee B..  (2015)  Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration..  J Med Chem,  58  (23): (9273-9286).  [PMID:26568411] [10.1021/acs.jmedchem.5b01227]
111. Han W, Menezes DL, Xu Y, Knapp MS, Elling R, Burger MT, Ni ZJ, Smith A, Lan J, Williams TE, Verhagen J, Huh K, Merritt H, Chan J, Kaufman S, Voliva CF, Pecchi S..  (2016)  Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model..  Bioorg Med Chem Lett,  26  (3): (742-746).  [PMID:26774655] [10.1016/j.bmcl.2016.01.003]
112. 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] [10.1016/j.bmcl.2016.01.062]
113. Simov V, Deshmukh SV, Dinsmore CJ, Elwood F, Fernandez RB, Garcia Y, Gibeau C, Gunaydin H, Jung J, Katz JD, Kraybill B, Lapointe B, Patel SB, Siu T, Su H, Young JR..  (2016)  Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors..  Bioorg Med Chem Lett,  26  (7): (1803-1808).  [PMID:26927423] [10.1016/j.bmcl.2016.02.035]
114. Cherian J, Nacro K, Poh ZY, Guo S, Jeyaraj DA, Wong YX, Ho M, Yang HY, Joy JK, Kwek ZP, Liu B, Wee JL, Ong EH, Choong ML, Poulsen A, Lee MA, Pendharkar V, Ding LJ, Manoharan V, Chew YS, Sangthongpitag K, Lim S, Ong ST, Hill J, Keller TH..  (2016)  Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells..  J Med Chem,  59  (7): (3063-3078).  [PMID:27011159] [10.1021/acs.jmedchem.5b01712]
115. 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] [10.1021/acs.jmedchem.6b00087]
116. Wang Q, Liu F, Wang B, Zou F, Chen C, Liu X, Wang A, Qi S, Wang W, Qi Z, Zhao Z, Hu Z, Wang W, Wang L, Zhang S, Wang Y, Liu J, Liu Q..  (2016)  Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs)..  J Med Chem,  59  (8): (3964-3979).  [PMID:27077705] [10.1021/acs.jmedchem.6b00200]
117. 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] [10.1016/j.bmcl.2016.04.079]
118. 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] [10.1016/j.ejmech.2016.05.022]
119. 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] [10.1016/j.ejmech.2016.11.009]
120. Cheeseman MD, Chessum NE, Rye CS, Pasqua AE, Tucker MJ, Wilding B, Evans LE, Lepri S, Richards M, Sharp SY, Ali S, Rowlands M, O'Fee L, Miah A, Hayes A, Henley AT, Powers M, Te Poele R, De Billy E, Pellegrino L, Raynaud F, Burke R, van Montfort RL, Eccles SA, Workman P, Jones K..  (2017)  Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen..  J Med Chem,  60  (1): (180-201).  [PMID:28004573] [10.1021/acs.jmedchem.6b01055]
121. Ma F, Liu P, Lei M, Liu J, Wang H, Zhao S, Hu L..  (2017)  Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3)..  Eur J Med Chem,  127  (72-86).  [PMID:28038328] [10.1016/j.ejmech.2016.12.038]
122. Lu Y, Mao F, Li X, Zheng X, Wang M, Xu Q, Zhu J, Li J..  (2017)  Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs)..  J Med Chem,  60  (12): (5099-5119).  [PMID:28541695] [10.1021/acs.jmedchem.7b00468]
123. Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S..  (2017)  Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers..  J Med Chem,  60  (12): (4869-4881).  [PMID:28557458] [10.1021/acs.jmedchem.6b01862]
124. Zhu W, Chen H, Wang Y, Wang J, Peng X, Chen X, Gao Y, Li C, He Y, Ai J, Geng M, Zheng M, Liu H..  (2017)  Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer..  J Med Chem,  60  (14): (6018-6035).  [PMID:28714692] [10.1021/acs.jmedchem.7b00076]
125. Zhao F, Zhang LD, Hao Y, Chen N, Bai R, Wang YJ, Zhang CC, Li GS, Hao LJ, Shi C, Zhang J, Mao Y, Fan Y, Xia GX, Yu JX, Liu YJ..  (2017)  Identification of 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives as highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitors via metabolite profiling-based structural optimization..  Eur J Med Chem,  134  (147-158).  [PMID:28411455] [10.1016/j.ejmech.2017.03.085]
126. Zhang H, Wu W, Feng C, Liu Z, Bai E, Wang X, Lei M, Cheng H, Feng H, Shi J, Wang J, Zhang Z, Jin T, Chen S, Hu S, Zhu Y..  (2017)  Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants..  Eur J Med Chem,  135  (12-23).  [PMID:28426996] [10.1016/j.ejmech.2017.04.036]
127. 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] [10.1016/j.bmcl.2017.07.004]
128. He L, Li D, Zhang C, Bai P, Chen L..  (2017)  Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC..  Bioorg Med Chem Lett,  27  (17): (4171-4175).  [PMID:28734581] [10.1016/j.bmcl.2017.07.009]
129. Adams CM, Anderson K, Artman G, Bizec JC, Cepeda R, Elliott J, Fassbender E, Ghosh M, Hanks S, Hardegger LA, Hosagrahara VP, Jaffee B, Jendza K, Ji N, Johnson L, Lee W, Liu D, Liu F, Long D, Ma F, Mainolfi N, Meredith EL, Miranda K, Peng Y, Poor S, Powers J, Qiu Y, Rao C, Shen S, Sivak JM, Solovay C, Tarsa P, Woolfenden A, Zhang C, Zhang Y..  (2018)  The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration..  J Med Chem,  61  (4): (1622-1635).  [PMID:29400470] [10.1021/acs.jmedchem.7b01731]
130. 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] [10.1016/j.bmcl.2017.10.031]
131. 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] [10.1016/j.ejmech.2017.10.003]
132. Czarna A, Wang J, Zelencova D, Liu Y, Deng X, Choi HG, Zhang T, Zhou W, Chang JW, Kildalsen H, Seternes OM, Gray NS, Engh RA, Rothweiler U..  (2018)  Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors..  J Med Chem,  61  (17): (7560-7572).  [PMID:30095246] [10.1021/acs.jmedchem.7b01847]
133. 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] [10.1016/j.ejmech.2018.06.019]
134. 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] [10.1016/j.bmc.2017.10.032]
135. 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] [10.1016/j.bmc.2017.12.020]
136. Myers SH, Temps C, Houston DR, Brunton VG, Unciti-Broceta A..  (2018)  Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening..  J Med Chem,  61  (5): (2104-2110).  [PMID:29466002] [10.1021/acs.jmedchem.7b01605]
137. 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] [10.1021/acs.jmedchem.8b00882]
138. Kettle JG, Anjum R, Barry E, Bhavsar D, Brown C, Boyd S, Campbell A, Goldberg K, Grondine M, Guichard S, Hardy CJ, Hunt T, Jones RDO, Li X, Moleva O, Ogg D, Overman RC, Packer MJ, Pearson S, Schimpl M, Shao W, Smith A, Smith JM, Stead D, Stokes S, Tucker M, Ye Y..  (2018)  Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors..  J Med Chem,  61  (19): (8797-8810).  [PMID:30204441] [10.1021/acs.jmedchem.8b00938]
139. 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] [10.1016/j.ejmech.2018.01.053]
140. 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] [10.1016/j.ejmech.2018.03.003]
141. 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] [10.1016/j.bmc.2018.06.010]
142. Li X, Huang Y, Cheng J, Zhang L, Mao F, Zhu J, Sheng C, Li J..  (2018)  Discovery of novel Syk/PDGFR-α/c-Kit inhibitors as multi-targeting drugs to treat rheumatoid arthritis..  Bioorg Med Chem,  26  (15): (4375-4381).  [PMID:30078608] [10.1016/j.bmc.2018.06.029]
143. Hudson L, Mui J, Vázquez S, Carvalho DM, Williams E, Jones C, Bullock AN, Hoelder S..  (2018)  Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept..  J Med Chem,  61  (16): (7261-7272).  [PMID:30085668] [10.1021/acs.jmedchem.8b00782]
144. 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] [10.1016/j.bmcl.2018.09.006]
145. 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] [10.1016/j.ejmech.2018.09.025]
146. Zhang Y, Lv H, Luo L, Xu Y, Pan Y, Wang Y, Lin H, Xiong J, Guo P, Zhang J, Li X, Ye F..  (2018)  Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer..  Eur J Med Chem,  157  (1300-1325).  [PMID:30195240] [10.1016/j.ejmech.2018.08.031]
147. Liu X, Wang B, Chen C, Qi Z, Zou F, Wang J, Hu C, Wang A, Ge J, Liu Q, Yu K, Hu Z, Jiang Z, Wang W, Wang L, Wang W, Ren T, Bai M, Liu Q, Liu J..  (2019)  Discovery of ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs)..  J Med Chem,  62  (10): (5006-5024).  [PMID:31046271] [10.1021/acs.jmedchem.9b00176]
148. 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] [10.1021/acsmedchemlett.9b00142]
149. 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] [10.1016/j.ejmech.2019.111728]
150. Baska F, Sipos A, Őrfi Z, Nemes Z, Dobos J, Szántai-Kis C, Szabó E, Szénási G, Dézsi L, Hamar P, Cserepes MT, Tóvári J, Garamvölgyi R, Krekó M, Őrfi L..  (2019)  Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases..  Eur J Med Chem,  184  (111710-111710).  [PMID:31614258] [10.1016/j.ejmech.2019.111710]
151. 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] [10.1016/j.ejmech.2018.10.052]
152. 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] [10.1016/j.ejmech.2019.03.039]
153. Martínez-González S, Rodríguez-Arístegui S, Gómez de la Oliva CA, Hernández AI, González Cantalapiedra E, Varela C, García AB, Rabal O, Oyarzabal J, Bischoff JR, Klett J, Albarrán MI, Cebriá A, Ajenjo N, García-Serelde B, Gómez-Casero E, Cuadrado-Urbano M, Cebrián D, Blanco-Aparicio C, Pastor J..  (2019)  Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors..  Eur J Med Chem,  168  (87-109).  [PMID:30802730] [10.1016/j.ejmech.2019.02.022]
154. Nan X, Jiang YF, Li HJ, Wang JH, Wu YC..  (2019)  Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors..  Bioorg Med Chem,  27  (13): (2801-2812).  [PMID:31079967] [10.1016/j.bmc.2019.05.007]
155. 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] [10.1021/acs.jmedchem.8b01597]
156. 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] [10.1016/j.bmcl.2019.07.043]
157. 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] [10.1016/j.ejmech.2019.05.021]
158. 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] [10.1016/j.ejmech.2019.07.038]
159. 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] [10.1021/acs.jmedchem.9b01143]
160. Lin WH, Wu SY, Yeh TK, Chen CT, Song JS, Shiao HY, Kuo CC, Hsu T, Lu CT, Wang PC, Wu TS, Peng YH, Lin HY, Chen CP, Weng YL, Kung FC, Wu MH, Su YC, Huang KW, Chou LH, Hsueh CC, Yen KJ, Kuo PC, Huang CL, Chen LT, Shih C, Tsai HJ, Jiaang WT..  (2019)  Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia..  J Med Chem,  62  (24): (11135-11150).  [PMID:31721578] [10.1021/acs.jmedchem.9b01229]
161. 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] [10.1016/j.ejmech.2017.04.079]
162. Wang Y, Li L, Fan J, Dai Y, Jiang A, Geng M, Ai J, Duan W..  (2018)  Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors..  J Med Chem,  61  (20): (9085-9104).  [PMID:29522671] [10.1021/acs.jmedchem.7b01843]
163. Farag AK, Hassan AHE, Jeong H, Kwon Y, Choi JG, Oh MS, Park KD, Kim YK, Roh EJ..  (2019)  First-in-class DAPK1/CSF1R dual inhibitors: Discovery of 3,5-dimethoxy-N-(4-(4-methoxyphenoxy)-2-((6-morpholinopyridin-3-yl)amino)pyrimidin-5-yl)benzamide as a potential anti-tauopathies agent..  Eur J Med Chem,  162  (161-175).  [PMID:30445265] [10.1016/j.ejmech.2018.10.057]
164. 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] [10.1016/j.ejmech.2018.12.063]
165. Bensinger D, Stubba D, Cremer A, Kohl V, Waßmer T, Stuckert J, Engemann V, Stegmaier K, Schmitz K, Schmidt B..  (2019)  Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations..  J Med Chem,  62  (5): (2428-2446).  [PMID:30742435] [10.1021/acs.jmedchem.8b01714]
166. Colombano G, Caldwell JJ, Matthews TP, Bhatia C, Joshi A, McHardy T, Mok NY, Newbatt Y, Pickard L, Strover J, Hedayat S, Walton MI, Myers SM, Jones AM, Saville H, McAndrew C, Burke R, Eccles SA, Davies FE, Bayliss R, Collins I..  (2019)  Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease..  J Med Chem,  62  (5): (2447-2465).  [PMID:30779566] [10.1021/acs.jmedchem.8b01721]
167. Sever B, Altıntop MD, Radwan MO, Özdemir A, Otsuka M, Fujita M, Ciftci HI..  (2019)  Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors..  Eur J Med Chem,  182  (111648-111648).  [PMID:31493743] [10.1016/j.ejmech.2019.111648]
168. Wang Q, Dai Y, Ji Y, Shi H, Guo Z, Chen D, Chen Y, Peng X, Gao Y, Wang X, Chen L, Jiang Y, Geng M, Shen J, Ai J, Xiong B..  (2019)  Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma..  Eur J Med Chem,  163  (671-689).  [PMID:30572178] [10.1016/j.ejmech.2018.12.015]
169. 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] [10.1016/j.ejmech.2018.12.025]
170. 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] [10.1016/j.bmcl.2019.02.006]
171. Kaiser TM, Dentmon ZW, Dalloul CE, Sharma SK, Liotta DC..  (2020)  Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease..  ACS Med Chem Lett,  11  (4): (491-496).  [PMID:32292555] [10.1021/acsmedchemlett.9b00612]
172. Mathison CJN, Chianelli D, Rucker PV, Nelson J, Roland J, Huang Z, Yang Y, Jiang J, Xie YF, Epple R, Bursulaya B, Lee C, Gao MY, Shaffer J, Briones S, Sarkisova Y, Galkin A, Li L, Li N, Li C, Hua S, Kasibhatla S, Kinyamu-Akunda J, Kikkawa R, Molteni V, Tellew JE..  (2020)  Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma..  ACS Med Chem Lett,  11  (4): (558-565).  [PMID:32292564] [10.1021/acsmedchemlett.0c00015]
173. Liu J, Wang Y, Chen C, Tu Z, Zhu S, Zhou F, Si H, Zheng C, Zhang Z, Cai Q..  (2020)  Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors..  ACS Med Chem Lett,  11  (8): (1567-1572).  [PMID:32832025] [10.1021/acsmedchemlett.0c00216]
174. 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] [10.1016/j.bmcl.2019.04.014]
175. Zhou Y,Xu X,Wang F,He H,Gong G,Xiong L,Qi B.  (2020)  Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer..  Eur J Med Chem,  204  (112643-112643).  [PMID:32731184] [10.1016/j.ejmech.2020.112643]
176. 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] [10.1021/acsmedchemlett.8b00081]
177. 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] [10.1021/acs.jmedchem.0c01647]
178. Rojas-Prats E,Martinez-Gonzalez L,Gonzalo-Consuegra C,Liachko NF,Perez C,Ramírez D,Kraemer BC,Martin-Requero Á,Perez DI,Gil C,de Lago E,Martinez A.  (2021)  Targeting nuclear protein TDP-43 by cell division cycle kinase 7 inhibitors: A new therapeutic approach for amyotrophic lateral sclerosis..  Eur J Med Chem,  210  (112968-112968).  [PMID:33139113] [10.1016/j.ejmech.2020.112968]
179. Sbenati RM,Zaraei SO,El-Gamal MI,Anbar HS,Tarazi H,Zoghbor MM,Mohamood NA,Khakpour MM,Zaher DM,Omar HA,Alach NN,Shehata MK,El-Gamal R.  (2021)  Design, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells..  Eur J Med Chem,  210  (113081-113081).  [PMID:33310290] [10.1016/j.ejmech.2020.113081]
180. 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] [10.1016/j.ejmech.2017.09.018]
181. Jeong P,Moon Y,Lee JH,Lee SD,Park J,Lee J,Kim J,Lee HJ,Kim NY,Choi J,Heo JD,Shin JE,Park HW,Kim YG,Han SY,Kim YC.  (2020)  Discovery of orally active indirubin-3'-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia..  Eur J Med Chem,  195  (112205-112205).  [PMID:32272419] [10.1016/j.ejmech.2020.112205]
182. Cao DS,Jiang SL,Guan YD,Chen XS,Zhang LX,Zhang Y,Chen AF,Yang JM,Cheng Y.  (2020)  A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone..  Eur J Med Chem,  199  (112421-112421).  [PMID:32428794] [10.1016/j.ejmech.2020.112421]
183. Wang B,Zhang W,Liu X,Zou F,Wang J,Liu Q,Wang A,Hu Z,Chen Y,Qi S,Jiang Z,Chen C,Hu C,Wang L,Wang W,Liu Q,Liu J.  (2020)  Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants..  Eur J Med Chem,  207  (112744-112744).  [PMID:32949955] [10.1016/j.ejmech.2020.112744]
184. 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] [10.1021/acs.jmedchem.0c02111]
185. Yu, J C JC and 6 more authors..  (1991)  Tyrosine mutations within the alpha platelet-derived growth factor receptor kinase insert domain abrogate receptor-associated phosphatidylinositol-3 kinase activity without affecting mitogenic or chemotactic signal transduction..  Molecular and cellular biology,      [PMID:1646396]
186. Anderson, D D and 5 more authors..  (1990)  Binding of SH2 domains of phospholipase C gamma 1, GAP, and Src to activated growth factor receptors..  Science (New York, N.Y.),    (16):   [PMID:2173144]
187. Matsui, T T and 7 more authors..  (1989)  Isolation of a novel receptor cDNA establishes the existence of two PDGF receptor genes..  Science (New York, N.Y.),    (10):   [PMID:2536956]
188. Claesson-Welsh, L L, Eriksson, A A, Westermark, B B and Heldin, C H CH..  (1989)  cDNA cloning and expression of the human A-type platelet-derived growth factor (PDGF) receptor establishes structural similarity to the B-type PDGF receptor..  Proceedings of the National Academy of Sciences of the United States of America,      [PMID:2544881]
189. Matsui, T T and 6 more authors..  (1989)  Independent expression of human alpha or beta platelet-derived growth factor receptor cDNAs in a naive hematopoietic cell leads to functional coupling with mitogenic and chemotactic signaling pathways..  Proceedings of the National Academy of Sciences of the United States of America,      [PMID:2554309]
190. Eriksson, A A and 8 more authors..  (1995)  Demonstration of functionally different interactions between phospholipase C-gamma and the two types of platelet-derived growth factor receptors..  The Journal of biological chemistry,    (31):   [PMID:7535778]
191. Ebert, M M and 5 more authors..  (1995)  Induction of platelet-derived growth factor A and B chains and over-expression of their receptors in human pancreatic cancer..  International journal of cancer,    (4):   [PMID:7665222]
192. Fretto, L J LJ and 6 more authors..  (1993)  Mechanism of platelet-derived growth factor (PDGF) AA, AB, and BB binding to alpha and beta PDGF receptor..  The Journal of biological chemistry,    (15):   [PMID:7679113]
193. Craven, R J RJ and 8 more authors..  (1995)  Receptor tyrosine kinases expressed in metastatic colon cancer..  International journal of cancer,    (16):   [PMID:7896447]
194. Vassbotn, F S FS, Havnen, O K OK, Heldin, C H CH and Holmsen, H H..  (1994)  Negative feedback regulation of human platelets via autocrine activation of the platelet-derived growth factor alpha-receptor..  The Journal of biological chemistry,    (13):   [PMID:8188664]
195. Kawagishi, J J, Kumabe, T T, Yoshimoto, T T and Yamamoto, T T..  (1995)  Structure, organization, and transcription units of the human alpha-platelet-derived growth factor receptor gene, PDGFRA..  Genomics,    (20):   [PMID:8586421]
196. Yokote, K K and 6 more authors..  (1996)  Structural determinants in the platelet-derived growth factor alpha-receptor implicated in modulation of chemotaxis..  The Journal of biological chemistry,    (1):   [PMID:8617789]
197. Yokote, K K, Margolis, B B, Heldin, C H CH and Claesson-Welsh, L L..  (1996)  Grb7 is a downstream signaling component of platelet-derived growth factor alpha- and beta-receptors..  The Journal of biological chemistry,    (29):   [PMID:8940081]
198. Bazenet, C E CE, Gelderloos, J A JA and Kazlauskas, A A..  (1996)  Phosphorylation of tyrosine 720 in the platelet-derived growth factor alpha receptor is required for binding of Grb2 and SHP-2 but not for activation of Ras or cell proliferation..  Molecular and cellular biology,      [PMID:8943348]
199. Heldin, C H CH, Ostman, A A and Rönnstrand, L L..  (1998)  Signal transduction via platelet-derived growth factor receptors..  Biochimica et biophysica acta,    (19):   [PMID:9739761]
200. Abdiu, A A and 5 more authors..  (1998)  Human malignant fibrous histiocytomas in vitro: growth characteristics and their association with expression of mRNA for platelet-derived growth factor, transforming growth factor-alpha and their receptors..  European journal of cancer (Oxford, England : 1990),      [PMID:10070317]
201. Matsumoto, T T and 8 more authors..  (2000)  Differential interaction of CrkII adaptor protein with platelet-derived growth factor alpha- and beta-receptors is determined by its internal tyrosine phosphorylation..  Biochemical and biophysical research communications,    (2):   [PMID:10733900]
202. Rosenkranz, S S and 6 more authors..  (2000)  Src family kinases negatively regulate platelet-derived growth factor alpha receptor-dependent signaling and disease progression..  The Journal of biological chemistry,    (31):   [PMID:10734113]
203. Lindholm, C K CK, Frantz, J D JD, Shoelson, S E SE and Welsh, M M..  (2000)  Shf, a Shb-like adapter protein, is involved in PDGF-alpha-receptor regulation of apoptosis..  Biochemical and biophysical research communications,    (30):   [PMID:11095946]
204. Gilbertson, D G DG and 13 more authors..  (2001)  Platelet-derived growth factor C (PDGF-C), a novel growth factor that binds to PDGF alpha and beta receptor..  The Journal of biological chemistry,    (20):   [PMID:11297552]
205. Karthikeyan, Subramanian S, Leung, Teli T and Ladias, John A A JA..  (2002)  Structural determinants of the Na+/H+ exchanger regulatory factor interaction with the beta 2 adrenergic and platelet-derived growth factor receptors..  The Journal of biological chemistry,    (24):   [PMID:11882663]
206. Heinrich, Michael C MC and 12 more authors..  (2003)  PDGFRA activating mutations in gastrointestinal stromal tumors..  Science (New York, N.Y.),    (31):   [PMID:12522257]
207. Miller-Kasprzak, Ewa E, Niemir, Zofia I ZI and Czekalski, Stanisław S..  (2002)  [Structure and function of PDGF-R-alpha and its expression in normal kidney and kidney diseases]..  Przeglad lekarski,      [PMID:12632922]
208. Cools, Jan J and 25 more authors..  (2003)  A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome..  The New England journal of medicine,    (27):   [PMID:12660384]
209. Griffin, John H JH, Leung, Joey J, Bruner, Rebecca J RJ, Caligiuri, Michael A MA and Briesewitz, Roger R..  (2003)  Discovery of a fusion kinase in EOL-1 cells and idiopathic hypereosinophilic syndrome..  Proceedings of the National Academy of Sciences of the United States of America,    (24):   [PMID:12808148]
210. Chompret, Agnès A and 7 more authors..  (2004)  PDGFRA germline mutation in a family with multiple cases of gastrointestinal stromal tumor..  Gastroenterology,      [PMID:14699510]
211. Hillier, Ladeana W LW and 121 more authors..  (2005)  Generation and annotation of the DNA sequences of human chromosomes 2 and 4..  Nature,    (7):   [PMID:15815621]
212. Yi, Eunhee S ES, Strong, Curtis R CR, Piao, Zhe Z, Perucho, Manuel M and Weidner, Noel N..  (2005)  Epithelioid gastrointestinal stromal tumor with PDGFRA activating mutation and immunoreactivity..  Applied immunohistochemistry & molecular morphology : AIMM,      [PMID:15894928]
213. and Borbényi, Zita Z..  (2005)  [Disorders with eosinophilia, treatment of hypereosinophilic syndrome]..  Orvosi hetilap,    (1):   [PMID:15921304]
214. Corless, Christopher L CL and 9 more authors..  (2005)  PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib..  Journal of clinical oncology : official journal of the American Society of Clinical Oncology,    (10):   [PMID:15928335]
215. Chen, Lei L LL and 9 more authors..  (2005)  Imatinib resistance in gastrointestinal stromal tumors..  Current oncology reports,      [PMID:15946589]
216. and Tefferi, A A..  (2005)  Modern diagnosis and treatment of primary eosinophilia..  Acta haematologica,      [PMID:15995325]
217. Prenen, Hans H and 8 more authors..  (2006)  Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate..  Clinical cancer research : an official journal of the American Association for Cancer Research,    (15):   [PMID:16638875]
218. Millward, M J MJ and 11 more authors..  (2006)  The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study..  British journal of cancer,    (9):   [PMID:16969355]
219. de Raedt, Thomas T and 10 more authors..  (2006)  Intestinal neurofibromatosis is a subtype of familial GIST and results from a dominant activating mutation in PDGFRA..  Gastroenterology,      [PMID:17087943]
220. Vantler, Marius M and 5 more authors..  (2006)  PI3-kinase/Akt-dependent antiapoptotic signaling by the PDGF alpha receptor is negatively regulated by Src family kinases..  FEBS letters,    (22):   [PMID:17141222]
221. Sonpavde, Guru G and Hutson, Thomas E TE..  (2007)  Pazopanib: a novel multitargeted tyrosine kinase inhibitor..  Current oncology reports,      [PMID:17288876]
222. Stock, Peggy P and 5 more authors..  (2007)  Platelet-derived growth factor receptor-alpha: a novel therapeutic target in human hepatocellular cancer..  Molecular cancer therapeutics,      [PMID:17604334]
223. Matsui, Junji J and 7 more authors..  (2008)  E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition..  International journal of cancer,    (1):   [PMID:17943726]
224. Feire, Adam L AL, Roy, René M RM, Manley, Kate K and Compton, Teresa T..  (2010)  The glycoprotein B disintegrin-like domain binds beta 1 integrin to mediate cytomegalovirus entry..  Journal of virology,      [PMID:20660204]
225. von Bubnoff, N N and 7 more authors..  (2011)  The low frequency of clinical resistance to PDGFR inhibitors in myeloid neoplasms with abnormalities of PDGFRA might be related to the limited repertoire of possible PDGFRA kinase domain mutations in vitro..  Oncogene,    (24):   [PMID:20972453]
226. Elling, Christian C and 13 more authors..  (2011)  Novel imatinib-sensitive PDGFRA-activating point mutations in hypereosinophilic syndrome induce growth factor independence and leukemia-like disease..  Blood,    (10):   [PMID:21224473]
227. Sévère, Nicolas N, Miraoui, Hichem H and Marie, Pierre J PJ..  (2011)  The Casitas B lineage lymphoma (Cbl) mutant G306E enhances osteogenic differentiation in human mesenchymal stromal cells in part by decreased Cbl-mediated platelet-derived growth factor receptor alpha and fibroblast growth factor receptor 2 ubiquitination..  The Journal of biological chemistry,    (8):   [PMID:21596750]
228. Doi, Toshihiko and 5 more authors..  (2014)  Phase I study of olaratumab in Japanese patients with advanced solid tumors..  Cancer science,      [PMID:24816152]
229. Ricci, Riccardo R and 10 more authors..  (2015)  PDGFRA-mutant syndrome..  Modern pathology : an official journal of the United States and Canadian Academy of Pathology, Inc,      [PMID:25975287]
230. Qi, Wei W and 39 more authors..  (2017)  An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED..  Nature chemical biology,      [PMID:28135235]
231. Wu, Yiquan and 8 more authors..  (2017)  Human cytomegalovirus glycoprotein complex gH/gL/gO uses PDGFR-α as a key for entry..  PLoS pathogens,      [PMID:28403202]
232. Wind, Sven and 7 more authors..  (2019)  Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib..  Clinical pharmacokinetics,      [PMID:31016670]
233. 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] [10.1016/j.bmcl.2018.03.032]

Solution Calculators

Privacy Policy Website Terms of Use Return policy Terms and Conditions of Sale Cookie Policy Sales Policy
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Copyright © 2023-present Aladdin Scientific Corp . All rights reserved.