Assay Detail
Functional
CHEMBL963642
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
8
Total Activities
8
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
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.15 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL459215 | — | — | 1 | 7.60 |
| CHEMBL516479 | — | — | 1 | 7.39 |
| CHEMBL460480 | — | — | 1 | 7.23 |
| CHEMBL459659 | — | — | 1 | 6.62 |
| CHEMBL517881 | — | — | 1 | 6.32 |
| CHEMBL460892 | — | — | 1 | 5.82 |
| CHEMBL512893 | — | — | 1 | 4.12 |
| CHEMBL472117 | — | — | 1 | 4.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL459215 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL516479 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL460480 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL459659 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL517881 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL460892 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL512893 | — | IC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL472117 | — | IC50 | = | 83000.0 | nM | 4.08 |