Assay Detail
Functional
CHEMBL1010962
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
9
Total Activities
9
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
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.53 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513998 | — | — | 1 | 8.13 |
| CHEMBL459215 | — | — | 1 | 8.03 |
| CHEMBL473807 | — | — | 1 | 8.01 |
| CHEMBL446978 | — | — | 1 | 7.85 |
| CHEMBL475650 | — | — | 1 | 7.80 |
| CHEMBL474991 | — | — | 1 | 7.55 |
| CHEMBL474992 | — | — | 1 | 7.19 |
| CHEMBL475660 | — | — | 1 | 6.85 |
| CHEMBL515123 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513998 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL459215 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL473807 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL446978 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL475650 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL474991 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL474992 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL475660 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL515123 | — | IC50 | = | 400.0 | nM | 6.40 |