Therapeutic Targets Database
BIDD Pharmainformatics Databases


Target Validation Information
Target NameProto-oncogene tyrosine-protein kinase LCK    
Type of TargetSuccessful target    
Drug Potency against TargetVX-680Ki = 520 nM[1]
AZD-0530IC50 < 4 nM[2]
PD-0166326;PD-166326IC50 < 5 nM[3]
PD-0173952IC50 < 5 nM[3]
PD-0173955;PD-17395IC50 < 5 nM[3]
PD-0173958IC50 < 5 nM[3]
PD-0180970IC50 < 5 nM[3]
PD-0179483IC50 < 5 nM[3]
PD-0173956IC50 < 5 nM[3]
(4-Phenoxy-phenyl)-quinazolin-4-yl-amineIC50 < 8 nM[4]
JNJ-10198409IC50 = 100 nM[5]
4-(3-Chloro-phenoxy)-6,7-dimethoxy-quinazolineIC50 = 1000 nM[6]
Y-c[D-Pen-(3,5-diI)Tyr-GSFC]KR-NH2IC50 = 11000 nM[7]
Y-c[D-Pen-(3-I)Tyr-GSFC]KR-NH2IC50 = 11000 nM[7]
A-770041IC50 = 147 nM[8]
SU 6656IC50 = 150 nM[9]
A-641359IC50 = 20 nM[8]
CGP-57380IC50 = 2500 nM[9]
2-(3,4,5-Trihydroxy-benzylidene)-malononitrileIC50 = 3000 nM[10]
AG-1879IC50 = 31 nM[9]
BMS-536924IC50 = 341 nM[11]
A-420983IC50 = 37 nM[12]
NM-PP1IC50 = 460 nM[9]
RPR-108518AIC50 = 500 nM[6]
ZM-336372IC50 = 570 nM[9]
CEP-5104IC50 = 6400 nM[13]
LAVENDUSTIN AIC50 = 8000 nM[14]
3-(4-(o-toluidino)pyrimidin-2-ylamino)benzamideIC50 = 89 nM[15]
6-o-tolylquinazolin-2-amineIC50 = 94 nM[16]
AZD-1152-HQPA;BarasertibKi = 170 nM[17]
TG-100435Ki = 29.4 nM[18]
Ref 1Nat Med. 2004 Mar;10(3):262-7. Epub 2004 Feb 22.VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. To Reference
Ref 2J Med Chem. 2006 Nov 2;49(22):6465-88.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. To Reference
Ref 3Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. To Reference
Ref 4Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70.Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. To Reference
Ref 5J Med Chem. 2005 Dec 29;48(26):8163-73.(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. To Reference
Ref 6Bioorg. Med. Chem. Lett. 7(4):417-420 (1997) To Reference
Ref 7J Med Chem. 1998 Jun 18;41(13):2252-60.Discovery of a novel series of potent and selective substrate-based inhibitors of p60c-src protein tyrosine kinase: conformational and topographical constraints in peptide design. To Reference
Ref 8Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10.Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. To Reference
Ref 9Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update. To Reference
Ref 10J Med Chem. 1993 Nov 12;36(23):3556-64.Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins. To Reference
Ref 11J Med Chem. 2005 Sep 8;48(18):5639-43.Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. To Reference
Ref 12Bioorg Med Chem Lett. 2004 May 17;14(10):2613-6.A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection. To Reference
Ref 13J Med Chem. 2008 Sep 25;51(18):5680-9. Epub 2008 Aug 21.Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. To Reference
Ref 14J Med Chem. 1993 Oct 1;36(20):3010-4.Non-amine based analogues of lavendustin A as protein-tyrosine kinase inhibitors. To Reference
Ref 15Bioorg Med Chem Lett. 2007 Aug 1;17(15):4363-8. Epub 2007 Apr 13.N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics. To Reference
Ref 16J Med Chem. 2006 Sep 21;49(19):5671-86.Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. To Reference
Ref 17J Med Chem. 2007 May 3;50(9):2213-24. Epub 2007 Mar 21.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. To Reference
Ref 18Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. To Reference


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