CP-316,311 [Ligand Id: 10377] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL270738 (CP-316311) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
