Assay Detail
Binding
CHEMBL684240
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Inhibition of recombinant human Gonadotropin-releasing hormone receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.77 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL48192 | — | — | 1 | 9.52 |
| CHEMBL48165 | — | — | 1 | 9.30 |
| CHEMBL48674 | — | — | 1 | 9.15 |
| CHEMBL49230 | — | — | 1 | 9.15 |
| CHEMBL45883 | — | — | 1 | 9.05 |
| CHEMBL45784 | — | — | 1 | 9.00 |
| CHEMBL416651 | — | — | 1 | 8.96 |
| CHEMBL46177 | — | — | 1 | 8.96 |
| CHEMBL47895 | — | — | 1 | 8.74 |
| CHEMBL46312 | — | — | 1 | 8.70 |
| CHEMBL297269 | — | — | 1 | 8.64 |
| CHEMBL48249 | — | — | 1 | 8.41 |
| CHEMBL295917 | — | — | 1 | 8.00 |
| CHEMBL417189 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL48192 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL48165 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL48674 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL49230 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL45883 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL45784 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL416651 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL46177 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL47895 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL46312 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL297269 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL48249 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL295917 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL417189 | — | IC50 | = | 57.0 | nM | 7.24 |