Assay Detail
Binding
CHEMBL865189
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.68 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22055 | SUFUGOLIX | 2.0 | 1 | 9.30 |
| CHEMBL179691 | — | — | 1 | 9.00 |
| CHEMBL3085508 | — | — | 1 | 8.77 |
| CHEMBL436874 | — | — | 1 | 8.51 |
| CHEMBL371722 | — | — | 1 | 7.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22055 | SUFUGOLIX | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL179691 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3085508 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL436874 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL371722 | — | IC50 | = | 14.6 | nM | 7.84 |