elagolix [Ligand Id: 8362] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1208155 (Elagolix, NBI-56418) |
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| 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] | ||||||||
| GtoPdb | - | - | 9.05 | pKi | 0.9 | nM | Ki |
J Med Chem (2008) 51: 7478-85 [PMID:19006286]; Drugs (2018) 78: 1501-1508 [PMID:30194661] |
| ChEMBL | Antagonist activity at wild type HA-tagged human GnRH1 receptor expressed in HEK293T cells assessed as inhibition of GnRH peptide-stimulated IP1 accumulation by measuring GnRH peptide EC50 at 100 uM pretreated for 1 hr followed by stimulation with GnRH peptide for 1 hr (Rvb = 2.5 nM) | B | 9.22 | pEC50 | 0.6 | nM | EC50 | Eur J Med Chem (2024) 279: 116903-116903 [PMID:39342681] |
ChEMBL data shown on this page come from version 37:
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]
