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ChEMBL ligand: CHEMBL482950 (Bms562086, BMS-562086, CRF1 ANTAGONIST, Dpc-a69448, Pexacerfont) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Binding affinity to rat adenosine A1 receptor expressed in CHO cells | B | 5.58 | pKi | 2660 | nM | Ki | J Med Chem (2009) 52: 3084-3092 [PMID:19361209] |
Corticotropin-releasing factor-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5930] [UniProtKB: P24387] | ||||||||
ChEMBL | Binding affinity to human recombinant CRF binding protein | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2009) 52: 3084-3092 [PMID:19361209] |
ChEMBL | Binding affinity to CRF-binding protein (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Drug Metab Dispos (2012) 40: 1093-1103 [PMID:22381334] |
CRF1 receptor/Corticotropin releasing factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1800] [GtoPdb: 212] [UniProtKB: P34998] | ||||||||
ChEMBL | Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066] |
ChEMBL | Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066] |
GtoPdb | Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes. | - | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066] |
ChEMBL | Antagonist activity at human CRF1 receptor | B | 8.21 | pIC50 | 6.1 | nM | IC50 | Drug Metab Dispos (2012) 40: 1093-1103 [PMID:22381334] |
ChEMBL | Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells | B | 8.35 | pIC50 | 4.5 | nM | IC50 | J Med Chem (2009) 52: 3084-3092 [PMID:19361209] |
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 pituitary cells assessed as inhibition of CRF-mediated ACTH production | F | 6.89 | pIC50 | 129 | nM | IC50 | J Med Chem (2009) 52: 3084-3092 [PMID:19361209] |
GtoPdb | Antagonism of CRF-mediated ACTH production in rat pituitary cells. | - | 6.89 | pIC50 | 129 | nM | IC50 | Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066] |
ChEMBL | Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting | B | 8.21 | pIC50 | 6.1 | nM | IC50 | J Med Chem (2009) 52: 3084-3092 [PMID:19361209] |
ChEMBL | Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting | B | 8.21 | pIC50 | 6.1 | nM | IC50 | J Med Chem (2011) 54: 4187-4206 [PMID:21618986] |
CRF2 receptor/Corticotropin releasing factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4069] [GtoPdb: 213] [UniProtKB: Q13324] | ||||||||
ChEMBL | Displacement of [125I]Tyr0-sauvagine from CRF2beta receptor expressed in pig choroid plexus membrane | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2009) 52: 3084-3092 [PMID:19361209] |
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
ChEMBL | Binding affinity to human neurokinin 2 receptor | B | 5.31 | pIC50 | 4900 | nM | IC50 | J Med Chem (2009) 52: 3084-3092 [PMID:19361209] |
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]