degarelix [Ligand Id: 5585] 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: CHEMBL415606 (Degarelix, FE200486 (AS ACETATE SALT), Firmagon) |
|---|
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 | 9.2 | pKd | 0.63 | nM | Kd | J Med Chem (2001) 44: 453-467 [PMID:11462984] |
| GtoPdb | - | - | 8.77 | pKi | 1.7 | nM | Ki | Cancer Manag Res (2010) 2: 39-52 [PMID:21188095] |
| ChEMBL | Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells | F | 8.06 | pIC50 | 8.8 | nM | IC50 | J Med Chem (2001) 44: 453-467 [PMID:11462984] |
| ChEMBL | Antagonism of GnRH response in HEK293 cells expressing human GnRH receptor | F | 8.79 | pIC50 | 1.64 | nM | IC50 | J Med Chem (2005) 48: 4851-4860 [PMID:16033265] |
| ChEMBL | Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay | F | 9.24 | pIC50 | 0.58 | nM | IC50 | J Med Chem (2006) 49: 3536-3543 [PMID:16759096] |
| ChEMBL | Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay | F | 9.24 | pIC50 | 0.58 | nM | IC50 | J Med Chem (2006) 49: 3536-3543 [PMID:16759096] |
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]
