Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T90648 | ||||
Target Name | B-Raf messenger RNA (BRAF mRNA) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | 2-(Benzylamino)-6-(3-acetamidophenyl)pyrazine | Drug Info | IC50 = 18000 nM | [2] | |
2-(Phenylamino)-6-(3-acetamidophenyl)pyrazine | Drug Info | IC50 = 12000 nM | [2] | ||
L-779450 | Drug Info | IC50 = 10 nM | [1] | ||
Pyrazolo[1,5-a]pyrimidine-3-carboxylate | Drug Info | IC50 = 1540 nM | [4] | ||
ZM-336372 | Drug Info | IC50 = 230 nM | [3] | ||
References | |||||
REF 1 | The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81. | ||||
REF 2 | Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead. J Med Chem. 2006 Jan 12;49(1):407-16. | ||||
REF 3 | The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. | ||||
REF 4 | Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors. Bioorg Med Chem Lett. 2009 May 15;19(10):2735-8. | ||||
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