Click Here for 5% Off Your First Aladdin Purchase!

CD117/c-Kit Mouse mAb - Primary antibody, specific to c-Kit, Mouse IgG1

  • Carrier Free
  • ExactAb™
  • Validated
  • Lot by Lot
Features and benefits
  • Short Overview:

    mAb (104D2); Mouse anti Human CD117/c-Kit Antibody; Flow; Unconjugated

  • Species reactivity(Reacts with): Human
  • Isotype: Mouse IgG1
    Application:
  • Flow Cyt
Item Number
Ab096639
Grouped product items
SKUSizeAvailabilityPrice Qty
Ab096639-10μg
10μg
In stock
$36.90
Ab096639-50μg
50μg
In stock
$99.90
Ab096639-100μg
100μg
In stock
$169.90
Ab096639-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,499.90

mAb (104D2); Mouse anti Human CD117/c-Kit Antibody; Flow; Unconjugated

Basic Description

Product NameCD117/c-Kit Mouse mAb - Primary antibody, specific to c-Kit, Mouse IgG1
SynonymsCD117 antigen; CD117; ckit; c-kit; EC 2.7.10; EC 2.7.10.1; KIT; PBT; piebald trait; Proto-oncogene c-Kit; proto-oncogene tyrosine-protein kinase Kit; SCF R; SCFR; SCFRmast/stem cell growth factor receptor; soluble KIT variant 1; Tyrosine-protein kinase Ki
Specifications & PurityExactAb™, Validated, Carrier Free, Lot by Lot
Host speciesMouse
Specificityc-Kit
ConjugationUnconjugated
GradeCarrier Free, ExactAb™, Validated
Product Description

Mouse anti Human c-Kit Antibody, Monoclonal (104D2), could be used for Flow and so on.

Application

Flow: < 0.5 μg/100w cells

Protein Function

Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and

Function

, and in melanogenesis. In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1, SH2B2/APS and CBL. Activates the AKT1 signaling pathway by phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase. Activated KIT also transmits signals via GRB2 and activation of RAS, RAF1 and the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1. Promotes activation of STAT family members STAT1, STAT3, STAT5A and STAT5B. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. KIT signaling is modulated by protein phosphatases, and by rapid internalization and degradation of the receptor. Activated KIT promotes phosphorylation of the protein phosphatases PTPN6/SHP-1 and PTPRU, and of the transcription factors STAT1, STAT3, STAT5A and STAT5B. Promotes phosphorylation of PIK3R1, CBL, CRK (isoform Crk-II), LYN, MAPK1/ERK2 and/or MAPK3/ERK1, PLCG1, SRC and SHC1.

Product Properties

IsotypeMouse IgG1
Light Chain Typekappa
SDS-PAGE150 kDa
Purification MethodProtein A purified
FormLiquid
ConcentrationLot by Lot
Storage TempStore at 2-8°C
Shipped InWet ice
Stability And StorageShipped at 4°C. Store at 4°C long term (36 months). Upon delivery aliquot.

Images

CD117/c-Kit Mouse mAb (Ab096639) - Flow Cytometry
Flow Cytometry analysis of K562 cells labelling CD117/c-Kit (red) with CD117/c-Kit Mouse mAb (Ab096639) at 0.1 μg/mL for 1 hour at 4°C. Goat Anti-Mouse IgG (PE) (Ab179006) at a dilution of 1/1000 was used as the secondary antibody. Blue - Isotype control, mouse IgG (Ab170221). Black - Unlabelled control, cells without incubation with primary antibody.

Associated Targets

KIT Tclin Mast/stem cell growth factor receptor Kit 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Application

ApplicationDilution info
Flow

< 0.5µg/100w cells

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

3 results found

Lot NumberCertificate TypeDateItem
ZJ24F0404004Certificate of AnalysisApr 01, 2024 Ab096639
ZJ24F0404003Certificate of AnalysisApr 01, 2024 Ab096639
ZJ24F0404002Certificate of AnalysisApr 01, 2024 Ab096639

Related Documents

References

1. 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]
2. Yuzawa S, Opatowsky Y, Zhang Z, Mandiyan V, Lax I, Schlessinger J.  (2007)  Structural basis for activation of the receptor tyrosine kinase KIT by stem cell factor..  Cell,  130  (2): (323-34).  [PMID:17662946]
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]
4. Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M et al..  (2010)  A structure-guided approach to creating covalent FGFR inhibitors..  Chem Biol,  17  (3): (285-95).  [PMID:20338520]
5. 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]
6. 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): (95-102).  [PMID:16415863]
7. 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]
8. 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]
9. 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. Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS et al..  (2006)  Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor..  Mol Cancer Ther,  (4): (995-1006).  [PMID:16648571]
11. 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,  (9): (e7258).  [PMID:19789626]
12. Manley PW, Furet P, Bold G, Brüggen J, Mestan J, Meyer T, Schnell CR, Wood J, Haberey M, Huth A et al..  (2002)  Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors..  J Med Chem,  45  (26): (5687-93).  [PMID:12477352]
13. Bold G, Altmann KH, Frei J, Lang M, Manley PW, Traxler P, Wietfeld B, Brüggen J, Buchdunger E, Cozens R et al..  (2000)  New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis..  J Med Chem,  43  (12): (2310-23).  [PMID:10882357]
14. 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]
15. 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]
16. 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]
17. Mahboobi S, Uecker A, Sellmer A, Cénac C, Höcher H, Pongratz H, Eichhorn E, Hufsky H, Trümpler A, Sicker M et al..  (2006)  Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase..  J Med Chem,  49  (11): (3101-15).  [PMID:16722630]
18. Murata K, Kumagai H, Kawashima T, Tamitsu K, Irie M, Nakajima H, Suzu S, Shibuya M, Kamihira S, Nosaka T et al..  (2003)  Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosine kinase 3 (FLT3)..  J Biol Chem,  278  (35): (32892-8).  [PMID:12815052]
19. Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ et al..  (2006)  Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity..  J Med Chem,  49  (12): (3563-80).  [PMID:16759099]
20. 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]
21. 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]
22. Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L et al..  (2012)  Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E..  J Med Chem,  55  (3): (1082-105).  [PMID:22168626]
23. 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]
24. Mahadevan D, Cooke L, Riley C, Swart R, Simons B, Della Croce K, Wisner L, Iorio M, Shakalya K, Garewal H et al..  (2007)  A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors..  Oncogene,  26  (27): (3909-19).  [PMID:17325667]
25. 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]
26. Eriksson A, Hermanson M, Wickström M, Lindhagen E, Ekholm C, Jenmalm Jensen A, Löthgren A, Lehmann F, Larsson R, Parrow V et al..  (2012)  The novel tyrosine kinase inhibitor AKN-028 has significant antileukemic activity in cell lines and primary cultures of acute myeloid leukemia..  Blood Cancer J,  (3): (e81).  [PMID:22864397]
27. 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,  (11): (691-9).  [PMID:18849971]
28. 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]
29. 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]
30. 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]
31. Akeno-Stuart N, Croyle M, Knauf JA, Malaguarnera R, Vitagliano D, Santoro M, Stephan C, Grosios K, Wartmann M, Cozens R et al..  (2007)  The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells..  Cancer Res,  67  (14): (6956-64).  [PMID:17638907]
32. Ohno H, Kubo K, Murooka H, Kobayashi Y, Nishitoba T, Shibuya M, Yoneda T, Isoe T.  (2006)  A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model..  Mol Cancer Ther,  (11): (2634-43).  [PMID:17121910]
33. Manthey CL, Johnson DL, Illig CR, Tuman RW, Zhou Z, Baker JF, Chaikin MA, Donatelli RR, Franks CF, Zeng L et al..  (2009)  JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia..  Mol Cancer Ther,  (11): (3151-61).  [PMID:19887542]
34. 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]
35. Kelly LM, Yu JC, Boulton CL, Apatira M, Li J, Sullivan CM, Williams I, Amaral SM, Curley DP, Duclos N et al..  (2002)  CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML)..  Cancer Cell,  (5): (421-32).  [PMID:12124172]
36. Wilhelm SM, Carter C, Tang L, Wilkie D, McNabola A, Rong H, Chen C, Zhang X, Vincent P, McHugh M et al..  (2004)  BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis..  Cancer Res,  64  (19): (7099-109).  [PMID:15466206]
37. 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]
38. Lee SL, Hsu EC, Chou CC, Chuang HC, Bai LY, Kulp SK, Chen CS.  (2011)  Identification and characterization of a novel integrin-linked kinase inhibitor..  J Med Chem,  54  (18): (6364-74).  [PMID:21823616]
39. 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]
40. 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]
41. Coombs TC, Tanega C, Shen M, Wang JL, Auld DS, Gerritz SW, Schoenen FJ, Thomas CJ, Aubé J.  (2013)  Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315..  Bioorg Med Chem Lett,  23  (12): (3654-61).  [PMID:23642479]
42. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM.  (2009)  Inhibitor hijacking of Akt activation..  Nat Chem Biol,  (7): (484-93).  [PMID:19465931]
43. Weinberg LR, Albom MS, Angeles TS, Husten J, Lisko JG, McHugh RJ, Milkiewicz KL, Murthy S, Ott GR, Theroff JP et al..  (2011)  Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors..  Bioorg Med Chem Lett,  21  (1): (164-7).  [PMID:21123062]
44. Milkiewicz KL, Aimone LD, Albom MS, Angeles TS, Chang H, Grobelny JV, Husten J, Losardo C, Miknyoczki S, Murthy S et al..  (2011)  Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group..  Bioorg Med Chem,  19  (21): (6274-84).  [PMID:21967808]
45. Ott GR, Tripathy R, Cheng M, McHugh R, Anzalone AV, Underiner TL, Curry MA, Quail MR, Lu L, Wan W et al..  (2010)  Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity..  ACS Med Chem Lett,  (9): (493-8).  [PMID:24900237]
46. Strachan DC, Ruffell B, Oei Y, Bissell MJ, Coussens LM, Pryer N, Daniel D.  (2013)  CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8(+) T cells..  Oncoimmunology,  (12): (e26968).  [PMID:24498562]
47. 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]
48. Bode CM, Boezio AA, Albrecht BK, Bellon SF, Berry L, Broome MA, Choquette D, Dussault I, Lewis RT, Lin MH et al..  (2012)  Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors..  Bioorg Med Chem Lett,  22  (12): (4089-93).  [PMID:22595176]
49. Tap WD, Wainberg ZA, Anthony SP, Ibrahim PN, Zhang C, Healey JH, Chmielowski B, Staddon AP, Cohn AL, Shapiro GI et al..  (2015)  Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor..  N Engl J Med,  373  (5): (428-37).  [PMID:26222558]
50. Genovese MC, Hsia E, Belkowski SM, Chien C, Masterson T, Thurmond RL, Manthey CL, Yan XD, Ge T, Franks C et al..  (2015)  Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy..  J Rheumatol,  42  (10): (1752-60).  [PMID:26233509]
51. 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]
52. 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]
53. 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]
54. Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS.  (2012)  Brain Penetrant LRRK2 Inhibitor..  ACS Med Chem Lett,  (8): (658-662).  [PMID:23066449]
55. Hobson AD, Harris CM, van der Kam EL, Turner SC, Abibi A, Aguirre AL, Bousquet P, Kebede T, Konopacki DB, Gintant G et al..  (2015)  Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders..  J Med Chem,  58  (23): (9154-70).  [PMID:26509640]
56. 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,  (11): (1142-1147).  [PMID:29152045]
57. 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]
58. 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]
59. 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]
60. 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,  (4): (4093-109).  [PMID:26675259]
61. 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]
62. 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]
63. Li Y, Xiong Y, Zhang G, Zhang L, Yang W, Yang J, Huang L, Qiao Z, Miao Z, Lin G et al..  (2018)  Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model..  J Med Chem,  61  (24): (11398-11414).  [PMID:30480444]
64. Qi B, Yang Y, Gong G, He H, Yue X, Xu X, Hu Y, Li J, Chen T, Wan X et al..  (2019)  Discovery of N1-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)-N3-(2-(2,6-difluorophenyl)-4-oxothiazolidin-3-yl)urea as a multi-tyrosine kinase inhibitor for drug-sensitive and drug-resistant cancers treatment..  Eur J Med Chem,  163  (3): (10-27).  [PMID:30503936]
65. You WK, Sennino B, Williamson CW, Falcón B, Hashizume H, Yao LC, Aftab DT, McDonald DM.  (2011)  VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer..  Cancer Res,  71  (14): (4758-68).  [PMID:21613405]
66. Evans EK, Gardino AK, Kim JL, Hodous BL, Shutes A, Davis A, Zhu XJ, Schmidt-Kittler O, Wilson D, Wilson K et al..  (2017)  A precision therapy against cancers driven by KIT/PDGFRA mutations..  Sci Transl Med,  (414): (589-97).  [PMID:29093181]
67. 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]
68. Zhang J, Jiang X, Jiang Y, Guo M, Zhang S, Li J, He J, Liu J, Wang J, Ouyang L.  (2016)  Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs..  Eur J Med Chem,  108  (3): (495-504).  [PMID:26717201]
69. 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]
70. 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]
71. Ma B, Bohnert T, Otipoby KL, Tien E, Arefayene M, Bai J, Bajrami B, Bame E, Chan TR, Humora M et al..  (2020)  Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases..  J Med Chem,  63  (21): (12526-12541).  [PMID:32696648]
72. 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]
73. 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]
74. 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]
75. 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]
76. Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Rucklin G..  (2004)  Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis..  Bioorg Med Chem Lett,  14  (13): (3595-3599).  [PMID:15177482]
77. Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Rucklin G..  (2004)  SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity..  Bioorg Med Chem Lett,  14  (13): (3601-3605).  [PMID:15177483]
78. 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]
79. 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]
80. Revesz L, Blum E, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Neumann U, Rucklin G..  (2006)  Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity..  Bioorg Med Chem Lett,  16  (2): (262-266).  [PMID:16249085]
81. Zhao H, Serby MD, Xin Z, Szczepankiewicz BG, Liu M, Kosogof C, Liu B, Nelson LT, Johnson EF, Wang S, Pederson T, Gum RJ, Clampit JE, Haasch DL, Abad-Zapatero C, Fry EH, Rondinone C, Trevillyan JM, Sham HL, Liu G..  (2006)  Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors..  J Med Chem,  49  (15): (4455-4458).  [PMID:16854050]
82. 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]
83. 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]
84. 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]
85. 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]
86. Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Diaz G, Glaser KB, Guo J, Harris CM, Li J, Marcotte PA, Moskey MD, Oie T, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR..  (2008)  3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases..  J Med Chem,  51  (5): (1231-1241).  [PMID:18260617]
87. 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]
88. 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]
89. 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]
90. Chu JJ, Yang PL..  (2007)  c-Src protein kinase inhibitors block assembly and maturation of dengue virus..  Proc Natl Acad Sci U S A,  104  (9): (3520-3525).  [PMID:17360676]
91. Slack-Davis JK, Martin KH, Tilghman RW, Iwanicki M, Ung EJ, Autry C, Luzzio MJ, Cooper B, Kath JC, Roberts WG, Parsons JT..  (2007)  Cellular characterization of a novel focal adhesion kinase inhibitor..  J Biol Chem,  282  (20): (14845-14852).  [PMID:17395594]
92. Kim KS, Zhang L, Schmidt R, Cai ZW, Wei D, Williams DK, Lombardo LJ, Trainor GL, Xie D, Zhang Y, An Y, Sack JS, Tokarski JS, Darienzo C, Kamath A, Marathe P, Zhang Y, Lippy J, Jeyaseelan R, Wautlet B, Henley B, Gullo-Brown J, Manne V, Hunt JT, Fargnoli J, Borzilleri RM..  (2008)  Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities..  J Med Chem,  51  (17): (5330-5341).  [PMID:18690676]
93. 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]
94. 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]
95. 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]
96. Huang H, Hutta DA, Rinker JM, Hu H, Parsons WH, Schubert C, DesJarlais RL, Crysler CS, Chaikin MA, Donatelli RR, Chen Y, Cheng D, Zhou Z, Yurkow E, Manthey CL, Player MR..  (2009)  Pyrido[2,3-d]pyrimidin-5-ones: a novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors..  J Med Chem,  52  (4): (1081-1099).  [PMID:19193011]
97. Gunaratnam M, Swank S, Haider SM, Galesa K, Reszka AP, Beltran M, Cuenca F, Fletcher JA, Neidle S..  (2009)  Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule..  J Med Chem,  52  (12): (3774-3783).  [PMID:19469547]
98. Li R, Pourpak A, Morris SW..  (2009)  Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach..  J Med Chem,  52  (16): (4981-5004).  [PMID:19610618]
99. 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]
100. 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]
101. 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]
102. 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]
103. 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]
104. 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]
105. 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]
106. 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]
107. 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]
108. 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]
109. 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]
110. Deng X, Yang Q, Kwiatkowski N, Sim T, McDermott U, Settleman JE, Lee JD, Gray NS..  (2011)  Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1..  ACS Med Chem Lett,  (3): (195-200).  [PMID:21412406]
111. Ren X, Duan L, He Q, Zhang Z, Zhou Y, Wu D, Pan J, Pei D, Ding K, Ding K..  (2010)  Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway..  ACS Med Chem Lett,  (9): (454-459).  [PMID:24900231]
112. 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]
113. 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]
114. 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]
115. Davies RJ, Pierce AC, Forster C, Grey R, Xu J, Arnost M, Choquette D, Galullo V, Tian SK, Henkel G, Chen G, Heidary DK, Ma J, Stuver-Moody C, Namchuk M..  (2011)  Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia..  J Med Chem,  54  (20): (7184-7192).  [PMID:21970471]
116. 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]
117. 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]
118. 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]
119. 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]
120. Heidary DK, Huang G, Boucher D, Ma J, Forster C, Grey R, Xu J, Arnost M, Choquette D, Chen G, Zhou JH, Yao YM, Ball ED, Namchuk M, Davies RJ, Henkel G..  (2012)  VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia..  J Med Chem,  55  (2): (725-734).  [PMID:22221201]
121. 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]
122. 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]
123. Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Lorenzo M, Rodríguez A, Rivero V, Martín JI, Saluste CG, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán M, Alfonso P, García-Serelde B, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Pastor J..  (2012)  Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor..  Bioorg Med Chem Lett,  22  (10): (3460-3466).  [PMID:22520259]
124. 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]
125. Lin X, Huang XP, Chen G, Whaley R, Peng S, Wang Y, Zhang G, Wang SX, Wang S, Roth BL, Huang N..  (2012)  Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors..  J Med Chem,  55  (12): (5749-5759).  [PMID:22694093]
126. 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]
127. 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]
128. 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]
129. 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]
130. 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]
131. 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]
132. 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]
133. Richters A, Ketzer J, Getlik M, Grütter C, Schneider R, Heuckmann JM, Heynck S, Sos ML, Gupta A, Unger A, Schultz-Fademrecht C, Thomas RK, Bauer S, Rauh D..  (2013)  Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design..  J Med Chem,  56  (14): (5757-5772).  [PMID:23773153]
134. Peng Z, Maxwell DS, Sun D, Bhanu Prasad BA, Schuber PT, Pal A, Ying Y, Han D, Gao L, Wang S, Levitzki A, Kapuria V, Talpaz M, Young M, Showalter HD, Donato NJ, Bornmann WG..  (2014)  Degrasyn-like symmetrical compounds: possible therapeutic agents for multiple myeloma (MM-I)..  Bioorg Med Chem,  22  (4): (1450-1458).  [PMID:24457091]
135. Szokol B, Gyulavári P, Kurkó I, Baska F, Szántai-Kis C, Greff Z, Orfi Z, Peták I, Pénzes K, Torka R, Ullrich A, Orfi L, Vántus T, Kéri G..  (2014)  Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors..  ACS Med Chem Lett,  (4): (298-303).  [PMID:24900830]
136. 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]
137. 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]
138. Park BS, Al-Sanea MM, Abdelazem AZ, Park HM, Roh EJ, Park HM, Yoo KH, Sim T, Tae JS, Lee SH..  (2014)  Structure-based optimization and biological evaluation of trisubstituted pyrazole as a core structure of potent ROS1 kinase inhibitors..  Bioorg Med Chem,  22  (15): (3871-3878).  [PMID:24997577]
139. Zeng LF, Zhang RY, Yu ZH, Li S, Wu L, Gunawan AM, Lane BS, Mali RS, Li X, Chan RJ, Kapur R, Wells CD, Zhang ZY..  (2014)  Therapeutic potential of targeting the oncogenic SHP2 phosphatase..  J Med Chem,  57  (15): (6594-6609).  [PMID:25003231]
140. Horbert R, Pinchuk B, Johannes E, Schlosser J, Schmidt D, Cappel D, Totzke F, Schächtele C, Peifer C..  (2015)  Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorβ (PDGF-Rβ) guided by water thermodynamics..  J Med Chem,  58  (1): (170-182).  [PMID:25007344]
141. Zhang W, DeRyckere D, Hunter D, Liu J, Stashko MA, Minson KA, Cummings CT, Lee M, Glaros TG, Newton DL, Sather S, Zhang D, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X..  (2014)  UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor..  J Med Chem,  57  (16): (7031-7041).  [PMID:25068800]
142. Unzue A, Dong J, Lafleur K, Zhao H, Frugier E, Caflisch A, Nevado C..  (2014)  Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: structure-based design, synthesis, and in vivo validation..  J Med Chem,  57  (15): (6834-6844).  [PMID:25076195]
143. 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]
144. 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]
145. Tintori C, La Sala G, Vignaroli G, Botta L, Fallacara AL, Falchi F, Radi M, Zamperini C, Dreassi E, Dello Iacono L, Orioli D, Biamonti G, Garbelli M, Lossani A, Gasparrini F, Tuccinardi T, Laurenzana I, Angelucci A, Maga G, Schenone S, Brullo C, Musumeci F, Desogus A, Crespan E, Botta M..  (2015)  Studies on the ATP Binding Site of Fyn Kinase for the Identification of New Inhibitors and Their Evaluation as Potential Agents against Tauopathies and Tumors..  J Med Chem,  58  (11): (4590-4609).  [PMID:25923950]
146. Choi HS, Rucker PV, Wang Z, Fan Y, Albaugh P, Chopiuk G, Gessier F, Sun F, Adrian F, Liu G, Hood T, Li N, Jia Y, Che J, McCormack S, Li A, Li J, Steffy A, Culazzo A, Tompkins C, Phung V, Kreusch A, Lu M, Hu B, Chaudhary A, Prashad M, Tuntland T, Liu B, Harris J, Seidel HM, Loren J, Molteni V..  (2015)  (R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors..  ACS Med Chem Lett,  (5): (562-567).  [PMID:26005534]
147. 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]
148. 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]
149. 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]
150. 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]
151. 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]
152. 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]
153. Li X, Wang A, Yu K, Qi Z, Chen C, Wang W, Hu C, Wu H, Wu J, Zhao Z, Liu J, Zou F, Wang L, Wang B, Wang W, Zhang S, Liu J, Liu Q..  (2015)  Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia..  J Med Chem,  58  (24): (9625-9638).  [PMID:26630553]
154. Simon-Szabó L, Kokas M, Greff Z, Boros S, Bánhegyi P, Zsákai L, Szántai-Kis C, Vantus T, Mandl J, Bánhegyi G, Vályi-Nagy I, Őrfi L, Ullrich A, Csala M, Kéri G..  (2016)  Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes..  Bioorg Med Chem Lett,  26  (2): (424-428).  [PMID:26704265]
155. 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]
156. 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]
157. 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]
158. Park H, Lee S, Hong S..  (2016)  Discovery of Dual Inhibitors for Wild Type and D816V Mutant of c-KIT Kinase through Virtual and Biochemical Screening of Natural Products..  J Nat Prod,  79  (2): (293-299).  [PMID:26807861]
159. 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]
160. 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]
161. 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]
162. 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]
163. 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]
164. Klaeger S, Heinzlmeir S and Wilhelm M et al.  (2017)  The target landscape of clinical kinase drugs..  Science,  358  (6367):   [PMID:29191878]
165. Musumeci F, Fallacara AL, Brullo C, Grossi G, Botta L, Calandro P, Chiariello M, Kissova M, Crespan E, Maga G, Schenone S..  (2017)  Identification of new pyrrolo[2,3-d]pyrimidines as Src tyrosine kinase inhibitors in vitro active against Glioblastoma..  Eur J Med Chem,  127  (369-378).  [PMID:28076826]
166. 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]
167. Ma X, Zhou J, Wang C, Carter-Cooper B, Yang F, Larocque E, Fine J, Tsuji G, Chopra G, Lapidus RG, Sintim HO..  (2017)  Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach..  ACS Med Chem Lett,  (5): (492-497).  [PMID:28523099]
168. 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]
169. Argyros O, Lougiakis N, Kouvari E, Papafotika A, Raptopoulou CP, Psycharis V, Christoforidis S, Pouli N, Marakos P, Tamvakopoulos C..  (2017)  Design and synthesis of novel 7-aminosubstituted pyrido[2,3-b]pyrazines exhibiting anti-breast cancer activity..  Eur J Med Chem,  126  (954-968).  [PMID:28006668]
170. 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]
171. 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]
172. 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]
173. Kaitsiotou H, Keul M, Hardick J, Mühlenberg T, Ketzer J, Ehrt C, Krüll J, Medda F, Koch O, Giordanetto F, Bauer S, Rauh D..  (2017)  Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT..  J Med Chem,  60  (21): (8801-8815).  [PMID:28991465]
174. 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]
175. Patel HM, Pawara R, Ansari A, Noolvi M, Surana S..  (2017)  Design and synthesis of quinazolinones as EGFR inhibitors to overcome EGFR resistance obstacle..  Bioorg Med Chem,  25  (10): (2713-2723).  [PMID:28366268]
176. Mah S, Park JH, Jung HY, Ahn K, Choi S, Tae HS, Jung KH, Rho JK, Lee JC, Hong SS, Hong S..  (2017)  Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design..  J Med Chem,  60  (22): (9205-9221).  [PMID:29091425]
177. Bharate SB, Kumar V, Jain SK, Mintoo MJ, Guru SK, Nuthakki VK, Sharma M, Bharate SS, Gandhi SG, Mondhe DM, Bhushan S, Vishwakarma RA..  (2018)  Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor..  J Med Chem,  61  (4): (1664-1687).  [PMID:29370702]
178. 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]
179. 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]
180. 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]
181. Patel S, Meilandt WJ, Erickson RI, Chen J, Deshmukh G, Estrada AA, Fuji RN, Gibbons P, Gustafson A, Harris SF, Imperio J, Liu W, Liu X, Liu Y, Lyssikatos JP, Ma C, Yin J, Lewcock JW, Siu M..  (2017)  Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease..  J Med Chem,  60  (19): (8083-8102).  [PMID:28929759]
182. 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]
183. 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]
184. Malki WH, Gouda AM, Ali HEA, Al-Rousan R, Samaha D, Abdalla AN, Bustamante J, Abd Elmageed ZY, Ali HI..  (2018)  Structural-based design, synthesis, and antitumor activity of novel alloxazine analogues with potential selective kinase inhibition..  Eur J Med Chem,  152  (31-52).  [PMID:29684708]
185. Zhi Y, Li B, Yao C, Li H, Chen P, Bao J, Qin T, Wang Y, Lu T, Lu S..  (2018)  Discovery of the selective and efficacious inhibitors of FLT3 mutations..  Eur J Med Chem,  155  (303-315).  [PMID:29894944]
186. 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]
187. 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]
188. 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]
189. 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]
190. Zang J, Liang X, Huang Y, Jia Y, Li X, Xu W, Chou CJ, Zhang Y..  (2018)  Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously..  J Med Chem,  61  (12): (5304-5322).  [PMID:29787262]
191. 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]
192. Philip S, Kumarasiri M, Teo T, Yu M, Wang S..  (2018)  Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?.  J Med Chem,  61  (12): (5073-5092).  [PMID:29266937]
193. 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]
194. 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]
195. La Pietra V, Sartini S, Botta L, Antonelli A, Ferrari SM, Fallahi P, Moriconi A, Coviello V, Quattrini L, Ke YY, Hsing-Pang H, Da Settimo F, Novellino E, La Motta C, Marinelli L..  (2018)  Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors..  Eur J Med Chem,  150  (491-505).  [PMID:29549836]
196. 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]
197. 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]
198. 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]
199. Pan Z, Chen Y, Liu J, Jiang Q, Yang S, Guo L, He G..  (2018)  Design, synthesis, and biological evaluation of polo-like kinase 1/eukaryotic elongation factor 2 kinase (PLK1/EEF2K) dual inhibitors for regulating breast cancer cells apoptosis and autophagy..  Eur J Med Chem,  144  (517-528).  [PMID:29288948]
200. 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]
201. 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]
202. 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]
203. 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]
204. 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]
205. 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]
206. 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]
207. Choi MJ, Roh EJ, Hur W, Lee SH, Sim T, Oh CH, Lee SH, Kim JS, Yoo KH..  (2018)  Design, synthesis, and biological evaluation of novel aminopyrimidinylisoindolines as AXL kinase inhibitors..  Bioorg Med Chem Lett,  28  (23-24): (3761-3765).  [PMID:30340900]
208. 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]
209. 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]
210. 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]
211. 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]
212. Mo C, Zhang Z, Li Y, Huang M, Zou J, Luo J, Tu ZC, Xu Y, Ren X, Ding K, Lu X..  (2020)  Design and Optimization of 3'-(Imidazo[1,2-a]pyrazin-3-yl)-[1,1'-biphenyl]-3-carboxamides as Selective DDR1 Inhibitors..  ACS Med Chem Lett,  11  (3): (379-384).  [PMID:32184973]
213. 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]
214. 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]
215. Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW..  (2019)  Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase..  J Med Chem,  62  (10): (5096-5110).  [PMID:31013427]
216. 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]
217. Szabadkai I, Torka R, Garamvölgyi R, Baska F, Gyulavári P, Boros S, Illyés E, Choidas A, Ullrich A, Őrfi L..  (2018)  Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as Novel AXL Kinase Inhibitors..  J Med Chem,  61  (14): (6277-6292).  [PMID:29928803]
218. 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]
219. 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]
220. 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]
221. 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]
222. Yuan X, Chen Y, Zhang W, He J, Lei L, Tang M, Liu J, Li M, Dou C, Yang T, Yang L, Yang S, Wei Y, Peng A, Niu T, Xiang M, Ye H, Chen L..  (2019)  Identification of Pyrrolo[2,3- d]pyrimidine-Based Derivatives as Potent and Orally Effective Fms-like Tyrosine Receptor Kinase 3 (FLT3) Inhibitors for Treating Acute Myelogenous Leukemia..  J Med Chem,  62  (8): (4158-4173).  [PMID:30939008]
223. Wu TS, Lin WH, Tsai HJ, Hsueh CC, Hsu T, Wang PC, Lin HY, Peng YH, Lu CT, Lee LC, Tu CH, Kung FC, Shiao HY, Yeh TK, Song JS, Chang JY, Su YC, Chen LT, Chen CT, Jiaang WT, Wu SY..  (2019)  Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants..  J Med Chem,  62  (8): (3940-3957).  [PMID:30968693]
224. Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, Shen X, Aubert-Nicol S, Chen YC, Cheong J, Crawford JJ, Hafner M, Haghshenas P, Jakalian A, Leclerc JP, Lim NK, O'Brien T, Plise EG, Shalan H, Sturino C, Wai J, Xiao Y, Yin J, Zhao L, Gould S, Olivero A, Heffron TP..  (2019)  Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma..  Bioorg Med Chem Lett,  29  (16): (2294-2301).  [PMID:31307887]
225. 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]
226. 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]
227. 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]
228. Zhu D, Huang H, Pinkas DM, Luo J, Ganguly D, Fox AE, Arner E, Xiang Q, Tu ZC, Bullock AN, Brekken RA, Ding K, Lu X..  (2019)  2-Amino-2,3-dihydro-1H-indene-5-carboxamide-Based Discoidin Domain Receptor 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Antipancreatic Cancer Efficacy..  J Med Chem,  62  (16): (7431-7444).  [PMID:31310125]
229. Moslin R, Zhang Y, Wrobleski ST, Lin S, Mertzman M, Spergel S, Tokarski JS, Strnad J, Gillooly K, McIntyre KW, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Heimrich E, Yang X, Muckelbauer JK, Chang C, Tredup J, Mulligan D, Xie D, Aranibar N, Chiney M, Burke JR, Lombardo L, Carter PH, Weinstein DS..  (2019)  Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2)..  J Med Chem,  62  (20): (8953-8972).  [PMID:31314518]
230. 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]
231. 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]
232. 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]
233. Nair S, Kumar SR, Paidi VR, Sistla R, Kantheti D, Polimera SR, Thangavel S, Mukherjee AJ, Das M, Bhide RS, Pitts WJ, Murugesan N, Dudhgoankar S, Nagar J, Subramani S, Mazumder D, Carman JA, Holloway DA, Li X, Fereshteh MP, Ruepp S, Palanisamy K, Mariappan TT, Maddi S, Saxena A, Elzinga P, Chimalakonda A, Ruan Q, Ghosh K, Bose S, Sack J, Yan C, Kiefer SE, Xie D, Newitt JA, Saravanakumar SP, Rampulla RA, Barrish JC, Carter PH, Hynes J..  (2020)  Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis..  ACS Med Chem Lett,  11  (7): (1402-1409).  [PMID:32676146]
234. 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]
235. Nan X,Li HJ,Fang SB,Li QY,Wu YC.  (2020)  Structure-based discovery of novel 4-(2-fluorophenoxy)quinoline derivatives as c-Met inhibitors using isocyanide-involved multicomponent reactions..  Eur J Med Chem,  193  (112241-112241).  [PMID:32200199]
236. 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]
237. 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]
238. 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]
239. Srour AM,Ahmed NS,Abd El-Karim SS,Anwar MM,El-Hallouty SM.  (2020)  Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors..  Bioorg Med Chem,  28  (18): (115657-115657).  [PMID:32828424]
240. 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]
241. 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]
242. Chen Y,Bai G,Ning Y,Cai S,Zhang T,Song P,Zhou J,Duan W,Ding J,Xie H,Zhang H.  (2020)  Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma..  Eur J Med Chem,  190  (112092-112092).  [PMID:32014679]
243. 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]
244. Lakkaniga NR,Zhang L,Belachew B,Gunaganti N,Frett B,Li HY.  (2020)  Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression..  Eur J Med Chem,  203  (112589-112589).  [PMID:32717530]
245. 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]
246. 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]
247. Giebel, L B LB, Strunk, K M KM, Holmes, S A SA and Spritz, R A RA..  (1992)  Organization and nucleotide sequence of the human KIT (mast/stem cell growth factor receptor) proto-oncogene..  Oncogene,      [PMID:1279499]
248. Spritz, R A RA, Giebel, L B LB and Holmes, S A SA..  (1992)  Dominant negative and loss of function mutations of the c-kit (mast/stem cell growth factor receptor) proto-oncogene in human piebaldism..  American journal of human genetics,      [PMID:1370874]
249. and Fleischman, R A RA..  (1992)  Human piebald trait resulting from a dominant negative mutant allele of the c-kit membrane receptor gene..  The Journal of clinical investigation,      [PMID:1376329]
250. Giebel, L B LB and Spritz, R A RA..  (1991)  Mutation of the KIT (mast/stem cell growth factor receptor) protooncogene in human piebaldism..  Proceedings of the National Academy of Sciences of the United States of America,    (1):   [PMID:1717985]
251. Yarden, Y Y and 9 more authors..  (1987)  Human proto-oncogene c-kit: a new cell surface receptor tyrosine kinase for an unidentified ligand..  The EMBO journal,      [PMID:2448137]
252. Toyota, M M and 5 more authors..  (1994)  Complementary DNA cloning and characterization of truncated form of c-kit in human colon carcinoma cells..  Cancer research,    (1):   [PMID:7505199]
253. Yamamoto, K K, Tojo, A A, Aoki, N N and Shibuya, M M..  (1993)  Characterization of the promoter region of the human c-kit proto-oncogene..  Japanese journal of cancer research : Gann,      [PMID:7506248]
254. Blume-Jensen, P P, Rönnstrand, L L, Gout, I I, Waterfield, M D MD and Heldin, C H CH..  (1994)  Modulation of Kit/stem cell factor receptor-induced signaling by protein kinase C..  The Journal of biological chemistry,    (26):   [PMID:7520444]
255. Blume-Jensen, P P, Wernstedt, C C, Heldin, C H CH and Rönnstrand, L L..  (1995)  Identification of the major phosphorylation sites for protein kinase C in kit/stem cell factor receptor in vitro and in intact cells..  The Journal of biological chemistry,    (9):   [PMID:7539802]
256. Spritz, R A RA, Holmes, S A SA, Itin, P P and Küster, W W..  (1993)  Novel mutations of the KIT (mast/stem cell growth factor receptor) proto-oncogene in human piebaldism..  The Journal of investigative dermatology,      [PMID:7687267]
257. Furitsu, T T and 9 more authors..  (1993)  Identification of mutations in the coding sequence of the proto-oncogene c-kit in a human mast cell leukemia cell line causing ligand-independent activation of c-kit product..  The Journal of clinical investigation,      [PMID:7691885]
258. Riva, P P, Milani, N N, Gandolfi, P P and Larizza, L L..  (1995)  A 12-bp deletion (7818del12) in the c-kit protooncogene in a large Italian kindred with piebaldism..  Human mutation,      [PMID:8680409]
259. Andre, C C and 7 more authors..  (1997)  Sequence analysis of two genomic regions containing the KIT and the FMS receptor tyrosine kinase genes..  Genomics,    (15):   [PMID:9027509]
260. Pignon, J M JM and 7 more authors..  (1997)  A new c-kit mutation in a case of aggressive mast cell disease..  British journal of haematology,      [PMID:9029028]
261. Price, D J DJ and 5 more authors..  (1997)  Direct association of Csk homologous kinase (CHK) with the diphosphorylated site Tyr568/570 of the activated c-KIT in megakaryocytes..  The Journal of biological chemistry,    (28):   [PMID:9038210]
262. Linnekin, D D, DeBerry, C S CS and Mou, S S..  (1997)  Lyn associates with the juxtamembrane region of c-Kit and is activated by stem cell factor in hematopoietic cell lines and normal progenitor cells..  The Journal of biological chemistry,    (24):   [PMID:9341198]
263. Hirota, S S and 14 more authors..  (1998)  Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors..  Science (New York, N.Y.),    (23):   [PMID:9438854]
264. Spritz, R A RA and Beighton, P P..  (1998)  Piebaldism with deafness: molecular evidence for an expanded syndrome..  American journal of medical genetics,    (6):   [PMID:9450866]
265. Kozlowski, M M and 5 more authors..  (1998)  SHP-1 binds and negatively modulates the c-Kit receptor by interaction with tyrosine 569 in the c-Kit juxtamembrane domain..  Molecular and cellular biology,      [PMID:9528781]
266. Beghini, A A, Larizza, L L, Cairoli, R R and Morra, E E..  (1998)  c-kit activating mutations and mast cell proliferation in human leukemia..  Blood,    (15):   [PMID:9657776]
267. Nishida, T T and 10 more authors..  (1998)  Familial gastrointestinal stromal tumours with germline mutation of the KIT gene..  Nature genetics,      [PMID:9697690]
268. Nomura, K K, Hatayama, I I, Narita, T T, Kaneko, T T and Shiraishi, M M..  (1998)  A novel KIT gene missense mutation in a Japanese family with piebaldism..  The Journal of investigative dermatology,      [PMID:9699740]
269. Longley, B J BJ and 7 more authors..  (1999)  Activating and dominant inactivating c-KIT catalytic domain mutations in distinct clinical forms of human mastocytosis..  Proceedings of the National Academy of Sciences of the United States of America,    (16):   [PMID:9990072]
270. Tian, Q Q, Frierson, H F HF, Krystal, G W GW and Moskaluk, C A CA..  (1999)  Activating c-kit gene mutations in human germ cell tumors..  The American journal of pathology,      [PMID:10362788]
271. Thömmes, K K, Lennartsson, J J, Carlberg, M M and Rönnstrand, L L..  (1999)  Identification of Tyr-703 and Tyr-936 as the primary association sites for Grb2 and Grb7 in the c-Kit/stem cell factor receptor..  The Biochemical journal,    (1):   [PMID:10377264]
272. Taniguchi, Y Y, London, R R, Schinkmann, K K, Jiang, S S and Avraham, H H..  (1999)  The receptor protein tyrosine phosphatase, PTP-RO, is upregulated during megakaryocyte differentiation and Is associated with the c-Kit receptor..  Blood,    (15):   [PMID:10397721]
273. Mancini, A A, Koch, A A, Stefan, M M, Niemann, H H and Tamura, T T..  (2000)  The direct association of the multiple PDZ domain containing proteins (MUPP-1) with the human c-Kit C-terminus is regulated by tyrosine kinase activity..  FEBS letters,    (29):   [PMID:11018522]
274. Syrris, P P and 6 more authors..  (2000)  Three novel mutations of the proto-oncogene KIT cause human piebaldism..  American journal of medical genetics,    (6):   [PMID:11074500]
275. Beghini, A A and 6 more authors..  (2001)  Germline mutation in the juxtamembrane domain of the kit gene in a family with gastrointestinal stromal tumors and urticaria pigmentosa..  Cancer,    (1):   [PMID:11505412]
276. Chen, X X, Ji, Z L ZL and Chen, Y Z YZ..  (2002)  TTD: Therapeutic Target Database..  Nucleic acids research,    (1):   [PMID:11752352]
277. Liang, Xiquan X and 5 more authors..  (2002)  Phosphatidylinositol 3-kinase and Src family kinases are required for phosphorylation and membrane recruitment of Dok-1 in c-Kit signaling..  The Journal of biological chemistry,    (19):   [PMID:11825908]
278. Wollberg, Patrik P, Lennartsson, Johan J, Gottfridsson, Eva E, Yoshimura, Akihiko A and Rönnstrand, Lars L..  (2003)  The adapter protein APS associates with the multifunctional docking sites Tyr-568 and Tyr-936 in c-Kit..  The Biochemical journal,    (15):   [PMID:12444928]
279. Voytyuk, Olexandr O and 6 more authors..  (2003)  Src family kinases are involved in the differential signaling from two splice forms of c-Kit..  The Journal of biological chemistry,    (14):   [PMID:12511554]
280. Abrams, Tinya J TJ, Lee, Leslie B LB, Murray, Lesley J LJ, Pryer, Nancy K NK and Cherrington, Julie M JM..  (2003)  SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer..  Molecular cancer therapeutics,      [PMID:12748309]
281. Mol, Clifford D CD and 9 more authors..  (2003)  Structure of a c-kit product complex reveals the basis for kinase transactivation..  The Journal of biological chemistry,    (22):   [PMID:12824176]
282. Schueneman, Aaron J AJ and 7 more authors..  (2003)  SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models..  Cancer research,    (15):   [PMID:12873999]
283. Lennartsson, Johan J, Wernstedt, Christer C, Engström, Ulla U, Hellman, Ulf U and Rönnstrand, Lars L..  (2003)  Identification of Tyr900 in the kinase domain of c-Kit as a Src-dependent phosphorylation site mediating interaction with c-Crk..  Experimental cell research,    (1):   [PMID:12878163]
284. Paronetto, Maria Paola MP and 7 more authors..  (2004)  Expression of a truncated form of the c-Kit tyrosine kinase receptor and activation of Src kinase in human prostatic cancer..  The American journal of pathology,      [PMID:15039213]
285. Mol, Clifford D CD and 9 more authors..  (2004)  Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase..  The Journal of biological chemistry,    (23):   [PMID:15123710]
286. Rönnstrand, L L..  (2004)  Signal transduction via the stem cell factor receptor/c-Kit..  Cellular and molecular life sciences : CMLS,      [PMID:15526160]
287. Lennartsson, Johan J, Jelacic, Tanya T, Linnekin, Diana D and Shivakrupa, R R..  (2005)  Normal and oncogenic forms of the receptor tyrosine kinase kit..  Stem cells (Dayton, Ohio),      [PMID:15625120]
288. 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]
289. Chen, Lei L LL and 5 more authors..  (2005)  A mutation-created novel intra-exonic pre-mRNA splice site causes constitutive activation of KIT in human gastrointestinal stromal tumors..  Oncogene,    (16):   [PMID:15824741]
290. Carter, Todd A and 21 more authors..  (2005)  Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases..  Proceedings of the National Academy of Sciences of the United States of America,    (2):   [PMID:16046538]
291. Dy, G K GK and 8 more authors..  (2005)  A phase II trial of imatinib (ST1571) in patients with c-kit expressing relapsed small-cell lung cancer: a CALGB and NCCTG study..  Annals of oncology : official journal of the European Society for Medical Oncology,      [PMID:16087693]
292. Roskoski, Robert R..  (2005)  Signaling by Kit protein-tyrosine kinase--the stem cell factor receptor..  Biochemical and biophysical research communications,    (11):   [PMID:16129412]
293. Bignell, Graham G and 52 more authors..  (2006)  Sequence analysis of the protein kinase gene family in human testicular germ-cell tumors of adolescents and adults..  Genes, chromosomes & cancer,      [PMID:16175573]
294. Liu, Tao T and 6 more authors..  ()  Human plasma N-glycoproteome analysis by immunoaffinity subtraction, hydrazide chemistry, and mass spectrometry..  Journal of proteome research,      [PMID:16335952]
295. Schittenhelm, Marcus M MM and 9 more authors..  (2006)  Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies..  Cancer research,    (1):   [PMID:16397263]
296. Shah, Neil P NP and 5 more authors..  (2006)  Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis..  Blood,    (1):   [PMID:16434489]
297. Lee, Jae-Lyun JL and 10 more authors..  (2006)  Response to imatinib in KIT- and PDGFRA-wild type gastrointestinal stromal associated with neurofibromatosis type 1..  Digestive diseases and sciences,      [PMID:16865565]
298. 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]
299. Koch, Christian A CA and 8 more authors..  (2006)  Does the expression of c-kit (CD117) in neuroendocrine tumors represent a target for therapy?.  Annals of the New York Academy of Sciences,      [PMID:17102120]
300. Liu, Li L and 8 more authors..  (2006)  Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5..  Cancer research,    (15):   [PMID:17178882]
301. Lierman, Els E and 5 more authors..  (2007)  The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors..  Haematologica,      [PMID:17229632]
302. Cascone, Tina T, Gridelli, Cesare C and Ciardiello, Fortunato F..  (2007)  Combined targeted therapies in non-small cell lung cancer: a winner strategy?.  Current opinion in oncology,      [PMID:17272980]
303. Sonpavde, Guru G and Hutson, Thomas E TE..  (2007)  Pazopanib: a novel multitargeted tyrosine kinase inhibitor..  Current oncology reports,      [PMID:17288876]
304. Roskoski, Robert R..  (2007)  Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor..  Biochemical and biophysical research communications,    (4):   [PMID:17367763]
305. Rutkowski, Piotr P and 11 more authors..  (2007)  Predictive factors for long-term effects of imatinib therapy in patients with inoperable/metastatic CD117(+) gastrointestinal stromal tumors (GISTs)..  Journal of cancer research and clinical oncology,      [PMID:17458563]
306. Guida, Teresa T and 7 more authors..  (2007)  Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants..  Clinical cancer research : an official journal of the American Association for Cancer Research,    (1):   [PMID:17545544]
307. Posadas, Edwin M EM and 10 more authors..  (2007)  A prospective analysis of imatinib-induced c-KIT modulation in ovarian cancer: a phase II clinical study with proteomic profiling..  Cancer,    (15):   [PMID:17559139]
308. Voisset, Edwige E, Lopez, Sophie S, Dubreuil, Patrice P and De Sepulveda, Paulo P..  (2007)  The tyrosine kinase FES is an essential effector of KITD816V proliferation signal..  Blood,    (1):   [PMID:17595334]
309. Sun, Jianmin J, Pedersen, Malin M, Bengtsson, Susanne S and Rönnstrand, Lars L..  (2007)  Grb2 mediates negative regulation of stem cell factor receptor/c-Kit signaling by recruitment of Cbl..  Experimental cell research,    (1):   [PMID:17904548]
310. 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]
311. Jin, Pei P and 9 more authors..  (2008)  Novel splice variants derived from the receptor tyrosine kinase superfamily are potential therapeutics for rheumatoid arthritis..  Arthritis research & therapy,      [PMID:18593464]
312. Sun, Jianmin J, Pedersen, Malin M and Rönnstrand, Lars L..  (2009)  The D816V mutation of c-Kit circumvents a requirement for Src family kinases in c-Kit signal transduction..  The Journal of biological chemistry,    (24):   [PMID:19265199]
313. Oppermann, Felix S FS and 7 more authors..  (2009)  Large-scale proteomics analysis of the human kinome..  Molecular & cellular proteomics : MCP,      [PMID:19369195]
314. Bodemer, Christine C and 26 more authors..  (2010)  Pediatric mastocytosis is a clonal disease associated with D816V and other activating c-KIT mutations..  The Journal of investigative dermatology,      [PMID:19865100]
315. DiNitto, Jonathan P JP and 8 more authors..  (2010)  Function of activation loop tyrosine phosphorylation in the mechanism of c-Kit auto-activation and its implication in sunitinib resistance..  Journal of biochemistry,      [PMID:20147452]
316. Muciaccia, Barbara B and 9 more authors..  (2010)  Expression of a truncated form of KIT tyrosine kinase in human spermatozoa correlates with sperm DNA integrity..  Human reproduction (Oxford, England),      [PMID:20601678]
317. Neumann, Ingo I and 6 more authors..  (2010)  Retinoic acid enhances sensitivity of neuroblastoma cells for imatinib mesylate..  Pediatric blood & cancer,      [PMID:20658618]
318. Zadjali, Fahad F and 9 more authors..  (2011)  Structural basis for c-KIT inhibition by the suppressor of cytokine signaling 6 (SOCS6) ubiquitin ligase..  The Journal of biological chemistry,    (7):   [PMID:21030588]
319. Pittoni, P P, Piconese, S S, Tripodo, C C and Colombo, M P MP..  (2011)  Tumor-intrinsic and -extrinsic roles of c-Kit: mast cells as the primary off-target of tyrosine kinase inhibitors..  Oncogene,    (17):   [PMID:21057534]
320. Chaix, Amandine A and 5 more authors..  (2011)  Mechanisms of STAT protein activation by oncogenic KIT mutants in neoplastic mast cells..  The Journal of biological chemistry,    (25):   [PMID:21135090]
321. Kim, Soo Young SY and 7 more authors..  (2011)  Mechanism of activation of human c-KIT kinase by internal tandem duplications of the juxtamembrane domain and point mutations at aspartic acid 816..  Biochemical and biophysical research communications,    (1):   [PMID:21640708]
322. Wasag, Bartosz B and 8 more authors..  (2011)  Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis..  Experimental hematology,      [PMID:21689725]
323. Gleixner, Karoline V KV and 7 more authors..  (2013)  Synergistic growth-inhibitory effects of ponatinib and midostaurin (PKC412) on neoplastic mast cells carrying KIT D816V..  Haematologica,      [PMID:23539538]
324. Wang, H J HJ, Lin, Z M ZM, Zhang, J J, Yin, J H JH and Yang, Y Y..  (2014)  A new germline mutation in KIT associated with diffuse cutaneous mastocytosis in a Chinese family..  Clinical and experimental dermatology,      [PMID:24289326]
325. Cannarile, Michael A MA and 5 more authors..  (2017)  Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy..  Journal for immunotherapy of cancer,    (18):   [PMID:28716061]
326. Yalcin, Suayib and Lacin, Sahin..  (2019)  Impact of tivozanib on patient outcomes in treatment of advanced renal cell carcinoma..  Cancer management and research,      [PMID:31496820]
327. Nemunaitis, John and 11 more authors..  (2020)  Intrigue: Phase III study of ripretinib versus sunitinib in advanced gastrointestinal stromal tumor after imatinib..  Future oncology (London, England),      [PMID:31755321]
328. Liu, Peng and 5 more authors..  (2020)  The Use of Molecular Subtypes for Precision Therapy of Recurrent and Metastatic Gastrointestinal Stromal Tumor..  OncoTargets and therapy,      [PMID:32273716]

Solution Calculators