Assay Detail
Binding
CHEMBL907222
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E 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 | 6.95 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL435167 | — | — | 1 | 8.96 |
| CHEMBL22055 | SUFUGOLIX | 2.0 | 1 | 8.92 |
| CHEMBL280212 | — | — | 1 | 7.51 |
| CHEMBL385175 | — | — | 1 | 7.16 |
| CHEMBL332355 | — | — | 1 | 6.64 |
| CHEMBL333518 | — | — | 1 | 6.35 |
| CHEMBL387006 | — | — | 1 | 5.85 |
| CHEMBL332138 | — | — | 1 | 5.82 |
| CHEMBL120260 | — | — | 1 | 5.30 |
| CHEMBL262557 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL435167 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL22055 | SUFUGOLIX | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL280212 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL385175 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL332355 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL333518 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL387006 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL332138 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL120260 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL262557 | — | IC50 | > | 10000.0 | nM | - |