pexacerfont [Ligand Id: 10379] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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] |
| apelin receptor/Apelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: APLNR | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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] |
| GPR119/Glucose-dependent insulinotropic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in agonist mode with target: GPR119 | F | 5 | pEC50 | >10000 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 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]
