Assay Detail
Functional
CHEMBL1008931
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RBL-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| IC50 | 11 | 8.34 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468551 | — | — | 1 | 9.30 |
| CHEMBL502182 | ELAGOLIX SODIUM | 4.0 | 1 | 8.82 |
| CHEMBL179691 | — | — | 1 | 8.55 |
| CHEMBL502341 | — | — | 1 | 8.49 |
| CHEMBL506877 | — | — | 1 | 7.57 |
| CHEMBL509075 | — | — | 1 | 7.33 |
| CHEMBL503705 | — | — | 1 | - |
| CHEMBL510538 | — | — | 1 | - |
| CHEMBL501329 | — | — | 1 | - |
| CHEMBL509440 | — | — | 1 | - |
| CHEMBL510285 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468551 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL502182 | ELAGOLIX SODIUM | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL179691 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL502341 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL506877 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL509075 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL503705 | — | IC50 | - | — | - | |
| CHEMBL510538 | — | IC50 | - | — | - | |
| CHEMBL501329 | — | IC50 | - | — | - | |
| CHEMBL509440 | — | IC50 | - | — | - | |
| CHEMBL510285 | — | IC50 | - | — | - |