Assay Detail
Binding
CHEMBL4676232
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| Kd | 4 | 9.03 | 9.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1200490 | CETRORELIX | 4.0 | 1 | 9.87 |
| CHEMBL1800159 | RELUGOLIX | 4.0 | 1 | 9.08 |
| CHEMBL502182 | ELAGOLIX SODIUM | 4.0 | 1 | 8.92 |
| CHEMBL4537788 | BAY-784 | — | 1 | 8.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1200490 | CETRORELIX | Kd | = | 0.135 | nM | 9.87 |
| CHEMBL1800159 | RELUGOLIX | Kd | = | 0.84 | nM | 9.08 |
| CHEMBL502182 | ELAGOLIX SODIUM | Kd | = | 1.19 | nM | 8.92 |
| CHEMBL4537788 | BAY-784 | Kd | = | 5.52 | nM | 8.26 |