Assay Detail
Binding
CHEMBL907229
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 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 | 6.58 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22055 | SUFUGOLIX | 2.0 | 1 | 8.22 |
| CHEMBL435167 | — | — | 1 | 8.05 |
| CHEMBL280212 | — | — | 1 | 7.00 |
| CHEMBL385175 | — | — | 1 | 6.05 |
| CHEMBL332138 | — | — | 1 | 6.02 |
| CHEMBL332355 | — | — | 1 | 5.96 |
| CHEMBL387006 | — | — | 1 | 5.75 |
| CHEMBL333518 | — | — | 1 | 5.58 |
| CHEMBL262557 | — | — | 1 | - |
| CHEMBL120260 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22055 | SUFUGOLIX | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL435167 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL280212 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL385175 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL332138 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL332355 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL387006 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL333518 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL262557 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL120260 | — | IC50 | > | 10000.0 | nM | - |