| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T12499 | ||||
| Target Name | LCK tyrosine protein kinase (LCK) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | VX-680 | Drug Info | Ki = 520 nM | [3] | |
| (4-Phenoxy-phenyl)-quinazolin-4-yl-amine | Drug Info | IC50 < 8 nM | [2] | ||
| 2-(3,4,5-Trihydroxy-benzylidene)-malononitrile | Drug Info | IC50 = 3000 nM | [14] | ||
| 3-(4-(o-toluidino)pyrimidin-2-ylamino)benzamide | Drug Info | IC50 = 89 nM | [11] | ||
| 4-(3-Chloro-phenoxy)-6,7-dimethoxy-quinazoline | Drug Info | IC50 = 1000 nM | |||
| 6-o-tolylquinazolin-2-amine | Drug Info | IC50 = 94 nM | [8] | ||
| A-420983 | Drug Info | IC50 = 37 nM | [4] | ||
| A-641359 | Drug Info | IC50 = 20 nM | [6] | ||
| A-770041 | Drug Info | IC50 = 147 nM | [6] | ||
| AZD-1152-HQPA | Drug Info | Ki = 170 nM | [10] | ||
| BMS-536924 | Drug Info | IC50 = 341 nM | [5] | ||
| CEP-5104 | Drug Info | IC50 = 6400 nM | [13] | ||
| CGP-57380 | Drug Info | IC50 = 2500 nM | [12] | ||
| HKI-9924129 | Drug Info | IC50 < 5 nM | [1] | ||
| ISIS-CRP | Drug Info | IC50 = 31 nM | [12] | ||
| JNJ-10198409 | Drug Info | IC50 = 100 nM | [7] | ||
| LAVENDUSTIN A | Drug Info | IC50 = 8000 nM | [15] | ||
| NM-PP1 | Drug Info | IC50 = 460 nM | [12] | ||
| PD-0166326 | Drug Info | IC50 < 5 nM | [1] | ||
| PD-0173952 | Drug Info | IC50 < 5 nM | [1] | ||
| PD-0173955 | Drug Info | IC50 < 5 nM | [1] | ||
| PD-0173956 | Drug Info | IC50 < 5 nM | [1] | ||
| PD-0173958 | Drug Info | IC50 < 5 nM | [1] | ||
| PD-0179483 | Drug Info | IC50 < 5 nM | [1] | ||
| RPR-108518A | Drug Info | IC50 = 500 nM | |||
| SU 6656 | Drug Info | IC50 = 150 nM | [12] | ||
| TG-100435 | Drug Info | Ki = 29.4 nM | [9] | ||
| Y-c[D-Pen-(3,5-diI)Tyr-GSFC]KR-NH2 | Drug Info | IC50 = 11000 nM | [16] | ||
| Y-c[D-Pen-(3-I)Tyr-GSFC]KR-NH2 | Drug Info | IC50 = 11000 nM | [16] | ||
| ZM-336372 | Drug Info | IC50 = 570 nM | [12] | ||
| References | |||||
| REF 1 | Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. Biochem Pharmacol. 2000 Oct 1;60(7):885-98. | ||||
| REF 2 | Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70. | ||||
| REF 3 | VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med. 2004 Mar;10(3):262-7. | ||||
| REF 4 | A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection. Bioorg Med Chem Lett. 2004 May 17;14(10):2613-6. | ||||
| REF 5 | 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 antitum... J Med Chem. 2005 Sep 8;48(18):5639-43. | ||||
| REF 6 | Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. | ||||
| REF 7 | (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad ant... J Med Chem. 2005 Dec 29;48(26):8163-73. | ||||
| REF 8 | Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. J Med Chem. 2006 Sep 21;49(19):5671-86. | ||||
| REF 9 | 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 kinas... Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. | ||||
| REF 10 | Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. J Med Chem. 2007 May 3;50(9):2213-24. | ||||
| REF 11 | N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4363-8. | ||||
| REF 12 | The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. | ||||
| REF 13 | Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-linea... J Med Chem. 2008 Sep 25;51(18):5680-9. | ||||
| REF 14 | Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins. J Med Chem. 1993 Nov 12;36(23):3556-64. | ||||
| REF 15 | Non-amine based analogues of lavendustin A as protein-tyrosine kinase inhibitors. J Med Chem. 1993 Oct 1;36(20):3010-4. | ||||
| REF 16 | Discovery of a novel series of potent and selective substrate-based inhibitors of p60c-src protein tyrosine kinase: conformational and topographica... J Med Chem. 1998 Jun 18;41(13):2252-60. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.