| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T45262 | ||||
| Target Name | Corticotropin-releasing factor receptor 1 (CRHR1) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Pexacerfont | Drug Info | IC50 = 6.1 nM | [7] | |
| Drug Info | Ki = 2 nM | [3] | |||
| BMS-561388 | Drug Info | IC50 = 66 nM | [4] | ||
| CP-376395 | Drug Info | IC50 = 5.1 nM | [2] | ||
| DMP-696 | Drug Info | IC50 = 1.2 nM | [5] | ||
| N-mesityl-4,6-dimethyl-3-tosylpyridin-2-amine | Drug Info | Ki = 1778 nM | [1] | ||
| N-mesityl-6-methyl-3-tosylpyridin-2-amine | Drug Info | Ki = 145 nM | [1] | ||
| PD-171729 | Drug Info | Ki = 5 nM | [6] | ||
| Action against Disease Model | GSK561679 | Drug Info | NBI-77860/GSK561679 was identified as a high affinity ligand of CRF1 with a pK(i) value of 8.2 and a functional CRF(1) antagonist with pIC(50) value of 7.0 in the in vitro CRF ACTH production assay | [8] | |
| References | |||||
| REF 1 | Synthesis and evaluation of 2-anilino-3-phenylsulfonyl-6-methylpyridines as corticotropin-releasing factor1 receptor ligands. Bioorg Med Chem Lett. 2006 Feb 15;16(4):934-7. | ||||
| REF 2 | 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J Med Chem. 2008 Mar 13;51(5):1385-92. | ||||
| REF 3 | 2-Arylpyrimidines: novel CRF-1 receptor antagonists. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4486-90. | ||||
| REF 4 | 8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists. J Med Chem. 2009 May 14;52(9):3073-83. | ||||
| REF 5 | In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists. J Med Chem. 2009 Jul 23;52(14):4161-72. | ||||
| REF 6 | Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists. Bioorg Med Chem Lett. 1998 Aug 18;8(16):2067-70. | ||||
| REF 7 | Progress in corticotropin-releasing factor-1 antagonist development. Drug Discov Today. 2010 May;15(9-10):371-83. | ||||
| REF 8 | Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7259-64. | ||||
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