Assay Detail
Binding
CHEMBL995201
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 13 | 8.04 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL434936 | — | — | 1 | 9.22 |
| CHEMBL451916 | — | — | 1 | 8.92 |
| CHEMBL454774 | — | — | 1 | 8.92 |
| CHEMBL509075 | — | — | 1 | 8.92 |
| CHEMBL505033 | — | — | 1 | 8.89 |
| CHEMBL453441 | — | — | 1 | 8.68 |
| CHEMBL449468 | — | — | 1 | 8.39 |
| CHEMBL509267 | — | — | 1 | 7.82 |
| CHEMBL455769 | — | — | 1 | 7.50 |
| CHEMBL444989 | — | — | 1 | 7.48 |
| CHEMBL448656 | — | — | 1 | 7.47 |
| CHEMBL503624 | — | — | 1 | 6.96 |
| CHEMBL499849 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL434936 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL451916 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL454774 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL509075 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL505033 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL453441 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL449468 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL509267 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL455769 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL444989 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL448656 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL503624 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL499849 | — | Ki | = | 3900.0 | nM | 5.41 |