Assay Detail
Binding
CHEMBL839508
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Binding affinity for Rat gonadotropin-releasing hormone receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 |
|---|---|---|---|
| Ki | 8 | 5.11 | 5.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL360143 | — | — | 1 | 5.54 |
| CHEMBL326504 | — | — | 1 | 5.50 |
| CHEMBL359894 | — | — | 1 | 5.12 |
| CHEMBL179269 | — | — | 1 | 5.11 |
| CHEMBL178457 | — | — | 1 | 5.00 |
| CHEMBL179429 | — | — | 1 | 4.96 |
| CHEMBL324912 | — | — | 1 | 4.92 |
| CHEMBL359754 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL360143 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL326504 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL359894 | — | Ki | = | 7600.0 | nM | 5.12 |
| CHEMBL179269 | — | Ki | = | 7700.0 | nM | 5.11 |
| CHEMBL178457 | — | Ki | = | 9900.0 | nM | 5.00 |
| CHEMBL179429 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL324912 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL359754 | — | Ki | = | 18000.0 | nM | 4.75 |