Assay Detail
Binding
CHEMBL4676183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.97 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740373 | — | — | 2 | 7.57 |
| CHEMBL4749790 | — | — | 2 | 7.54 |
| CHEMBL4756920 | — | — | 2 | 7.40 |
| CHEMBL4798298 | — | — | 1 | 7.14 |
| CHEMBL4740709 | — | — | 4 | 6.14 |
| CHEMBL4787218 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740373 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4740373 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4749790 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4756920 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4756920 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4798298 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4740709 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4740709 | — | IC50 | = | 726.0 | nM | 6.14 |
| CHEMBL4740709 | — | IC50 | = | 1419.0 | nM | 5.85 |
| CHEMBL4749790 | — | IC50 | >= | 20.0 | 10^3nM | - |
| CHEMBL4740709 | — | IC50 | >= | 20.0 | 10^3nM | - |
| CHEMBL4787218 | — | IC50 | - | — | - |