| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T17980 | ||||
| Target Name | Fyn tyrosine kinase | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | CEP-5104 | Drug Info | IC50 = 3400 nM | [529647] | |
| CEP-6331 | Drug Info | IC50 = 1190 nM | [529647] | ||
| Dasatinib | Drug Info | Kd = 0.79 nM | [552773] | ||
| JNJ-10198409 | Drug Info | IC50 = 378 nM | [527932] | ||
| Ro-4396686 | Drug Info | IC50 = 466 nM | [528018] | ||
| References | |||||
| Ref 529647 | J 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 529647 | J 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 552773 | A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358. | ||||
| Ref 527932 | J 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 528018 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. | ||||
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