Assay Detail
Binding
CHEMBL1008930
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| Ki | 13 | 8.58 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468551 | — | — | 1 | 9.30 |
| CHEMBL179691 | — | — | 1 | 9.25 |
| CHEMBL434936 | — | — | 1 | 9.19 |
| CHEMBL502182 | ELAGOLIX SODIUM | 4.0 | 1 | 9.05 |
| CHEMBL502341 | — | — | 1 | 8.96 |
| CHEMBL509075 | — | — | 1 | 8.92 |
| CHEMBL506877 | — | — | 1 | 8.68 |
| CHEMBL503705 | — | — | 1 | 8.43 |
| CHEMBL510285 | — | — | 1 | 8.38 |
| CHEMBL191817 | — | — | 1 | 8.25 |
| CHEMBL510538 | — | — | 1 | 8.12 |
| CHEMBL501329 | — | — | 1 | 7.92 |
| CHEMBL509440 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468551 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL179691 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL434936 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL502182 | ELAGOLIX SODIUM | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL502341 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL509075 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL506877 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL503705 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL510285 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL191817 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL510538 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL501329 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL509440 | — | Ki | = | 71.0 | nM | 7.15 |