Assay Detail
Functional
CHEMBL995202
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RBL |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.32 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL505033 | — | — | 1 | 9.22 |
| CHEMBL454774 | — | — | 1 | 8.59 |
| CHEMBL453441 | — | — | 1 | 8.55 |
| CHEMBL448253 | — | — | 1 | 7.64 |
| CHEMBL449468 | — | — | 1 | 7.58 |
| CHEMBL448656 | — | — | 1 | - |
| CHEMBL509267 | — | — | 1 | - |
| CHEMBL451916 | — | — | 1 | - |
| CHEMBL447592 | — | — | 1 | - |
| CHEMBL452474 | — | — | 1 | - |
| CHEMBL449373 | — | — | 1 | - |
| CHEMBL444989 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL505033 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL454774 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL453441 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL448253 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL449468 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL448656 | — | IC50 | - | — | - | |
| CHEMBL509267 | — | IC50 | - | — | - | |
| CHEMBL451916 | — | IC50 | - | — | - | |
| CHEMBL447592 | — | IC50 | - | — | - | |
| CHEMBL452474 | — | IC50 | - | — | - | |
| CHEMBL449373 | — | IC50 | - | — | - | |
| CHEMBL444989 | — | IC50 | - | — | - |