Assay Detail
Binding
CHEMBL828596
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.03 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL360143 | — | — | 1 | 8.55 |
| CHEMBL179691 | — | — | 1 | 8.52 |
| CHEMBL359894 | — | — | 1 | 8.30 |
| CHEMBL178457 | — | — | 1 | 8.21 |
| CHEMBL326504 | — | — | 1 | 8.19 |
| CHEMBL359754 | — | — | 1 | 8.00 |
| CHEMBL324912 | — | — | 1 | 7.70 |
| CHEMBL179269 | — | — | 1 | 7.47 |
| CHEMBL179429 | — | — | 1 | 7.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL360143 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL179691 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL359894 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL178457 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL326504 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL359754 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL324912 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL179269 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL179429 | — | IC50 | = | 49.0 | nM | 7.31 |