Assay Detail
Binding
CHEMBL828774
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Binding affinity for Monkey gonadotropin-releasing hormone receptor
11
Total Activities
11
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 |
|---|---|---|---|
| Ki | 11 | 7.37 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL179691 | — | — | 1 | 8.46 |
| CHEMBL360143 | — | — | 1 | 8.19 |
| CHEMBL180076 | — | — | 1 | 7.82 |
| CHEMBL178457 | — | — | 1 | 7.38 |
| CHEMBL359894 | — | — | 1 | 7.35 |
| CHEMBL179269 | — | — | 1 | 7.19 |
| CHEMBL359754 | — | — | 1 | 7.13 |
| CHEMBL178281 | — | — | 1 | 7.00 |
| CHEMBL326504 | — | — | 1 | 6.92 |
| CHEMBL179429 | — | — | 1 | 6.92 |
| CHEMBL324912 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL179691 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL360143 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL180076 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL178457 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL359894 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL179269 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL359754 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL178281 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL326504 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL179429 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL324912 | — | Ki | = | 200.0 | nM | 6.70 |