Assay Detail
Binding
CHEMBL1008934
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 5.50 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468551 | — | — | 1 | 5.92 |
| CHEMBL502182 | ELAGOLIX SODIUM | 4.0 | 1 | 5.36 |
| CHEMBL179691 | — | — | 1 | 5.21 |
| CHEMBL506877 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468551 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL502182 | ELAGOLIX SODIUM | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL179691 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL506877 | — | Ki | > | 10000.0 | nM | - |