| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T63505 | ||||
| Target Name | Tyrosine-protein kinase ABL1 (ABL) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Adenosine triphosphate | Drug Info | EC50 = 187000000 nM | [12] | |
| Imatinib | Drug Info | Ki = 38 nM | [16] | ||
| Bosutinib | Drug Info | IC50 = 1.2 nM | [15] | ||
| Nilotinib | Drug Info | Ki = 20~60 nM | [13] | ||
| Saracatinib | Drug Info | IC50 = 5 nM | [14] | ||
| (E)-4-(3,5-dimethoxystyryl)phenol | Drug Info | IC50 = 10000 nM | [2] | ||
| 3'',5''-dimethoxy-[1,1':2',1'']-terphenyl-4-ol | Drug Info | IC50 = 14000 nM | [2] | ||
| 3'',5''-dimethoxy-[1,1':3',1'']-terphenyl-4-ol | Drug Info | IC50 = 14000 nM | [2] | ||
| 4,3'',5''-trimethoxy-[1,1':2',1'']-terphenyl | Drug Info | IC50 = 6000 nM | [2] | ||
| 4,3'',5''-trimethoxy-[1,1':3',1'']-terphenyl | Drug Info | IC50 = 10000 nM | [2] | ||
| AP-24163 | Drug Info | IC50 = 25 nM | [11] | ||
| AP-24226 | Drug Info | IC50 = 20 nM | [11] | ||
| BAS-00387275 | Drug Info | Ki = 2500 nM | [4] | ||
| BAS-00387328 | Drug Info | Ki = 800 nM | [4] | ||
| BAS-00387347 | Drug Info | Ki = 600 nM | [4] | ||
| BAS-00672722 | Drug Info | Ki = 1000 nM | [4] | ||
| BAS-01373578 | Drug Info | Ki = 5000 nM | [4] | ||
| BAS-0338872 | Drug Info | Ki = 1300 nM | [8] | ||
| BAS-0338876 | Drug Info | Ki = 400 nM | [8] | ||
| BAS-09534324 | Drug Info | Ki = 2000 nM | [4] | ||
| Bis-(5-hydroxy-1H-indol-2-yl)-methanone | Drug Info | IC50 = 4200 nM | [3] | ||
| ISIS-CRP | Drug Info | Ki = 500 nM | [9] | ||
| JNJ-10198409 | Drug Info | IC50 = 22 nM | [1] | ||
| PD-0166326 | Drug Info | IC50 = 2.8 nM | [10] | ||
| PD-0173955 | Drug Info | IC50 = 2 nM | [5] | ||
| PD-0173956 | Drug Info | IC50 = 21 nM | [10] | ||
| SKI-758 | Drug Info | IC50 = 0.4 nM | [7] | ||
| TG-100435 | Drug Info | Ki = 19.4 nM | [6] | ||
| TRISMETHOXYRESVERATROL | Drug Info | IC50 = 10000 nM | [2] | ||
| [1,1':2',1'']-terphenyl-4,3'',5''-triol | Drug Info | IC50 = 8000 nM | [2] | ||
| References | |||||
| REF 1 | (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 2 | Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. J Med Chem. 2006 May 18;49(10):3012-8. | ||||
| REF 3 | Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2006 Jun 1;49(11):3101-15. | ||||
| REF 4 | A combination of docking/dynamics simulations and pharmacophoric modeling to discover new dual c-Src/Abl kinase inhibitors. J Med Chem. 2006 Jun 1;49(11):3278-86. | ||||
| REF 5 | Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and hom... J Med Chem. 2006 Sep 21;49(19):5759-68. | ||||
| REF 6 | 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 7 | Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76. | ||||
| REF 8 | Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1207-11. | ||||
| REF 9 | Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines. J Med Chem. 2008 Mar 13;51(5):1252-9. | ||||
| REF 10 | 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. 2009 Dec 15;19(24):6872-6. | ||||
| REF 11 | 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 (AP2453... J Med Chem. 2010 Jun 24;53(12):4701-19. | ||||
| REF 12 | Agonists and antagonists acting at P2X7 receptor. Curr Top Med Chem. 2004;4(16):1707-17. | ||||
| REF 13 | Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell. 2005 Feb;7(2):129-41. | ||||
| REF 14 | Flying under the radar: the new wave of BCR-ABL inhibitors. Nat Rev Drug Discov. 2007 Oct;6(10):834-48. | ||||
| REF 15 | Recent progress of SRC family kinase inhibitors as anticancer agents. Mini Rev Med Chem. 2008 Sep;8(10):1053-63. | ||||
| REF 16 | Towards the optimal antihistamine: studies with ebastine. Inflamm Res. 1998;47 Suppl 1:S36-7. | ||||
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