Assay Detail
Binding
CHEMBL908389
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.44 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22055 | SUFUGOLIX | 2.0 | 1 | 9.10 |
| CHEMBL435167 | — | — | 1 | 9.05 |
| CHEMBL280212 | — | — | 1 | 8.22 |
| CHEMBL385175 | — | — | 1 | 7.70 |
| CHEMBL332355 | — | — | 1 | 7.54 |
| CHEMBL333518 | — | — | 1 | 7.28 |
| CHEMBL332138 | — | — | 1 | 6.68 |
| CHEMBL387006 | — | — | 1 | 6.62 |
| CHEMBL262557 | — | — | 1 | 6.22 |
| CHEMBL120260 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22055 | SUFUGOLIX | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL435167 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL280212 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL385175 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL332355 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL333518 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL332138 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL387006 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL262557 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL120260 | — | IC50 | = | 1100.0 | nM | 5.96 |