Target Validation Information
Target ID T12499
Target Name Lck tyrosine kinase
Target Type
Successful
Drug Potency against Target 4-(3-Chloro-phenoxy)-6,7-dimethoxy-quinazoline Drug Info IC50 = 1000 nM
CEP-5104 Drug Info IC50 = 6400 nM [529647]
AZD-1152-HQPA Drug Info Ki = 170 nM [528741]
PD-0173958 Drug Info IC50 < 5 nM [525862]
RPR-108518A Drug Info IC50 = 500 nM
JNJ-10198409 Drug Info IC50 = 100 nM [527932]
TG-100435 Drug Info Ki = 29.4 nM [528527]
3-(4-(o-toluidino)pyrimidin-2-ylamino)benzamide Drug Info IC50 = 89 nM [528928]
BMS-536924 Drug Info IC50 = 341 nM [527711]
PD-0180970 Drug Info IC50 < 5 nM [525862]
VX-680 Drug Info Ki = 520 nM [526974]
A-420983 Drug Info IC50 = 37 nM [527057]
PD-0173952 Drug Info IC50 < 5 nM [525862]
SU 6656 Drug Info IC50 = 150 nM [529039]
A-641359 Drug Info IC50 = 20 nM [527790]
A-770041 Drug Info IC50 = 147 nM [527790]
6-o-tolylquinazolin-2-amine Drug Info IC50 = 94 nM [528429]
(4-Phenoxy-phenyl)-quinazolin-4-yl-amine Drug Info IC50 < 8 nM [525876]
CGP-57380 Drug Info IC50 = 2500 nM [529039]
PD-0166326 Drug Info IC50 < 5 nM [525862]
PD-0173956 Drug Info IC50 < 5 nM [525862]
ZM-336372 Drug Info IC50 = 570 nM [529039]
LAVENDUSTIN A Drug Info IC50 = 8000 nM [533899]
PD-0179483 Drug Info IC50 < 5 nM [525862]
PD-0173955 Drug Info IC50 < 5 nM [525862]
AG-1879 Drug Info IC50 = 31 nM [529039]
Y-c[D-Pen-(3-I)Tyr-GSFC]KR-NH2 Drug Info IC50 = 11000 nM [534651]
Y-c[D-Pen-(3,5-diI)Tyr-GSFC]KR-NH2 Drug Info IC50 = 11000 nM [534651]
NM-PP1 Drug Info IC50 = 460 nM [529039]
2-(3,4,5-Trihydroxy-benzylidene)-malononitrile Drug Info IC50 = 3000 nM [533795]
References
Ref 529647J 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.
Ref 528741J 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.
Ref 525862Biochem 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.
Ref 527932J 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.
Ref 528527Bioorg 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.
Ref 528928Bioorg 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.
Ref 527711J 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.
Ref 525862Biochem 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.
Ref 526974Nat 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.
Ref 527057Bioorg 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.
Ref 525862Biochem 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.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 527790Bioorg 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.
Ref 527790Bioorg 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.
Ref 528429J 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.
Ref 525876Bioorg 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.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 525862Biochem 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.
Ref 525862Biochem 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.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 533899J Med Chem. 1993 Oct 1;36(20):3010-4.Non-amine based analogues of lavendustin A as protein-tyrosine kinase inhibitors.
Ref 525862Biochem 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.
Ref 525862Biochem 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.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 534651J 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 constraintsin peptide design.
Ref 534651J 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 constraintsin peptide design.
Ref 529039Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update.
Ref 533795J Med Chem. 1993 Nov 12;36(23):3556-64.Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins.

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