Assay Detail
Functional
CHEMBL955062
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RBL |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.12 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL509075 | — | — | 1 | 8.31 |
| CHEMBL450471 | — | — | 1 | 7.96 |
| CHEMBL499588 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL509075 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL450471 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL499588 | — | IC50 | = | 7900.0 | nM | 5.10 |