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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
