Assay Detail
Functional
CHEMBL923764
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
14
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.75 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL256109 | — | — | 2 | 8.82 |
| CHEMBL556355 | — | — | 1 | 8.59 |
| CHEMBL259906 | — | — | 1 | 8.48 |
| CHEMBL403234 | — | — | 2 | 8.27 |
| CHEMBL22653 | — | — | 1 | 8.09 |
| CHEMBL407719 | — | — | 1 | - |
| CHEMBL401807 | — | — | 1 | - |
| CHEMBL257599 | — | — | 1 | - |
| CHEMBL403081 | — | — | 1 | - |
| CHEMBL255242 | — | — | 1 | - |
| CHEMBL401632 | — | — | 1 | - |
| CHEMBL259907 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL256109 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL556355 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL259906 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL403234 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL22653 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL256109 | — | IC50 | = | 385.0 | nM | 6.42 |
| CHEMBL403234 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL407719 | — | IC50 | - | — | - | |
| CHEMBL401807 | — | IC50 | - | — | - | |
| CHEMBL257599 | — | IC50 | - | — | - | |
| CHEMBL403081 | — | IC50 | - | — | - | |
| CHEMBL255242 | — | IC50 | - | — | - | |
| CHEMBL401632 | — | IC50 | - | — | - | |
| CHEMBL259907 | — | IC50 | - | — | - |