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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