Assay Detail
Binding
CHEMBL995200
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Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 14 | 7.89 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL454774 | — | — | 1 | 9.00 |
| CHEMBL453441 | — | — | 1 | 8.96 |
| CHEMBL505033 | — | — | 1 | 8.92 |
| CHEMBL449373 | — | — | 1 | 8.33 |
| CHEMBL448253 | — | — | 1 | 8.12 |
| CHEMBL506338 | — | — | 1 | 8.03 |
| CHEMBL452474 | — | — | 1 | 8.00 |
| CHEMBL502967 | — | — | 1 | 7.57 |
| CHEMBL447424 | — | — | 1 | 7.54 |
| CHEMBL450414 | — | — | 1 | 7.46 |
| CHEMBL509347 | — | — | 1 | 7.42 |
| CHEMBL447592 | — | — | 1 | 7.28 |
| CHEMBL452198 | — | — | 1 | 7.01 |
| CHEMBL499442 | — | — | 1 | 6.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL454774 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL453441 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL505033 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL449373 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL448253 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL506338 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL452474 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL502967 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL447424 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL450414 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL509347 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL447592 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL452198 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL499442 | — | Ki | = | 155.0 | nM | 6.81 |