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 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]
