Assay Detail
Binding
CHEMBL1010963
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 8.04 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473807 | — | — | 1 | 8.74 |
| CHEMBL513998 | — | — | 1 | 8.46 |
| CHEMBL459215 | — | — | 1 | 8.31 |
| CHEMBL446978 | — | — | 1 | 8.25 |
| CHEMBL474991 | — | — | 1 | 7.92 |
| CHEMBL475650 | — | — | 1 | 7.80 |
| CHEMBL474992 | — | — | 1 | 7.68 |
| CHEMBL475660 | — | — | 1 | 7.62 |
| CHEMBL515123 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473807 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL513998 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL459215 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL446978 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL474991 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL475650 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL474992 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL475660 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL515123 | — | IC50 | = | 26.0 | nM | 7.58 |