Assay Detail
Binding
CHEMBL685317
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In vivo inhibition of monkey Gonadotropin-releasing hormone receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.03 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22314 | — | — | 1 | 7.82 |
| CHEMBL423291 | — | — | 1 | 7.52 |
| CHEMBL23969 | — | — | 1 | 7.37 |
| CHEMBL22653 | — | — | 1 | 7.30 |
| CHEMBL3085404 | — | — | 1 | 7.06 |
| CHEMBL283381 | — | — | 1 | 7.06 |
| CHEMBL279885 | — | — | 1 | 6.70 |
| CHEMBL23729 | — | — | 1 | 6.26 |
| CHEMBL23830 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22314 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL423291 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL23969 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL22653 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL3085404 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL283381 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL279885 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL23729 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL23830 | — | Ki | = | 610.0 | nM | 6.21 |