CP-316,311 [Ligand Id: 10377] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL270738 (CP-316311) |
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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] | ||||||||
| GtoPdb | Antagonism of CRF-stimulated adenylate cyclase activity by the CRF1 receptor endogenously expressed in human IMR32 cells. | - | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2008) 51: 1377-84 [PMID:18260619] |
| ChEMBL | Antagonist activity at human CRF1 receptor endogenously expressed in human IMR32 cells | F | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2008) 51: 1377-1384 [PMID:18260619] |
| ChEMBL | Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells | B | 7.04 | pIC50 | 92 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2365-2371 [PMID:21414781] |
| ChEMBL | Inhibition of CRF1 receptor | B | 8.17 | pIC50 | 6.8 | nM | IC50 | J Med Chem (2008) 51: 1377-1384 [PMID:18260619] |
| CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353] | ||||||||
| ChEMBL | Antagonist activity at rat cortex CRF1 receptor assessed as inhibition of CRF-stimulated adenylate cyclase activity | F | 8.12 | pKi | 7.6 | nM | Ki | J Med Chem (2008) 51: 1377-1384 [PMID:18260619] |
| ChEMBL | Displacement of [125]oCRF from rat cortex CRF1 receptor | B | 8.17 | pIC50 | 6.8 | nM | IC50 | J Med Chem (2008) 51: 1377-1384 [PMID:18260619] |
| ChEMBL | Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter | B | 8.17 | pIC50 | 6.8 | 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 | 8.17 | pIC50 | 6.8 | nM | IC50 | J Med Chem (2011) 54: 4187-4206 [PMID:21618986] |
| ChEMBL | Displacement of [125]oCRF from rat cortex CRF1 receptor | B | 8.17 | pIC50 | 6.76 | nM | IC50 | J Med Chem (2008) 51: 1377-1384 [PMID:18260619] |
| ChEMBL | Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter | B | 8.17 | pIC50 | 6.76 | nM | IC50 | J Med Chem (2008) 51: 1385-1392 [PMID:18288792] |
| GtoPdb | In vitro binding to rat cortex. | - | 8.17 | pIC50 | 6.8 | nM | IC50 | J Med Chem (2008) 51: 1377-84 [PMID:18260619] |
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]
