| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T90648 | ||||
| Target Name | mRNA of B-Raf | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | 2-(Phenylamino)-6-(3-acetamidophenyl)pyrazine | Drug Info | IC50 = 12000 nM | [527954] | |
| 2-(Benzylamino)-6-(3-acetamidophenyl)pyrazine | Drug Info | IC50 = 18000 nM | [527954] | ||
| Pyrazolo[1,5-a]pyrimidine-3-carboxylate | Drug Info | IC50 = 1540 nM | [530074] | ||
| ZM-336372 | Drug Info | IC50 = 230 nM | [529039] | ||
| L-779450 | Drug Info | IC50 = 10 nM | [527836] | ||
| References | |||||
| Ref 527954 | J Med Chem. 2006 Jan 12;49(1):407-16.Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead. | ||||
| Ref 527954 | J Med Chem. 2006 Jan 12;49(1):407-16.Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead. | ||||
| Ref 530074 | Bioorg Med Chem Lett. 2009 May 15;19(10):2735-8. Epub 2009 Mar 28.Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors. | ||||
| Ref 529039 | Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update. | ||||
| Ref 527836 | Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81. Epub 2005 Nov 2.The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. | ||||
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