cetrorelix [Ligand Id: 1190] 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: CHEMBL1200490 (Cetrorelix, Cetrotide) |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968] | ||||||||
| ChEMBL | Competitive antagonism of GnRH-induced response in the reporter gene assay | F | 8.9 | pKd | 1.26 | nM | Kd | J Med Chem (2001) 44: 453-467 [PMID:11462984] |
| ChEMBL | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay | B | 9.87 | pKd | 0.14 | nM | Kd | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| GtoPdb | - | - | 10 | pKi | - | - | - |
Endocrinology (2007) 148: 857-67 [PMID:17095587]; Anal Biochem (1997) 251: 17-23 [PMID:9300077]; Eur J Biochem (1995) 231: 535-43 [PMID:7649152] |
| ChEMBL | Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells | F | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2001) 44: 453-467 [PMID:11462984] |
| GtoPdb | - | - | 8.7 | pIC50 | 1.98 | nM | IC50 | Endocrinology (2002) 143: 737-43 [PMID:11861490] |
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]
