Assay Detail
Functional
CHEMBL1010964
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | Pituitary gland cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 6.64 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL459215 | — | — | 1 | 7.60 |
| CHEMBL513998 | — | — | 1 | 7.36 |
| CHEMBL446978 | — | — | 1 | 7.16 |
| CHEMBL475650 | — | — | 1 | 6.92 |
| CHEMBL473807 | — | — | 1 | 6.62 |
| CHEMBL474991 | — | — | 1 | 6.50 |
| CHEMBL475660 | — | — | 1 | 6.27 |
| CHEMBL474992 | — | — | 1 | 6.08 |
| CHEMBL515123 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL459215 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL513998 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL446978 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL475650 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL473807 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL474991 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL475660 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL474992 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL515123 | — | IC50 | = | 5900.0 | nM | 5.23 |