CP 376,395 [Ligand Id: 3496] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL270948 (CP-376395) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CRF1 receptor/Corticotropin releasing factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1800] [GtoPdb: 212] [UniProtKB: P34998] | ||||||||
| ChEMBL | Antagonist activity at human CRF1 receptor assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation counting | F | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2008) 51: 1385-1392 [PMID:18288792] |
| CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353] | ||||||||
| ChEMBL | Antagonist activity at CRF1 receptor in rat cortical membrane assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation | F | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2008) 51: 1385-1392 [PMID:18288792] |
| ChEMBL | Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter | B | 8.29 | pIC50 | 5.13 | nM | IC50 | J Med Chem (2008) 51: 1385-1392 [PMID:18288792] |
| ChEMBL | Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter | B | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (2008) 51: 1385-1392 [PMID:18288792] |
| ChEMBL | Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting | B | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (2011) 54: 4187-4206 [PMID:21618986] |
| GtoPdb | - | - | 8.3 | pIC50 | 5.01 | nM | IC50 | J Med Chem (2008) 51: 1385-92 [PMID:18288792] |
| CRF2 receptor/Corticotropin releasing factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4069] [GtoPdb: 213] [UniProtKB: Q13324] | ||||||||
| ChEMBL | Binding affinity for human CRF2 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2008) 51: 1385-1392 [PMID:18288792] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
