Assay Detail
Functional
CHEMBL954343
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: structure-activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.67 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460480 | — | — | 1 | 8.40 |
| CHEMBL493731 | — | — | 1 | 7.89 |
| CHEMBL521674 | — | — | 1 | 7.85 |
| CHEMBL492327 | — | — | 1 | 7.64 |
| CHEMBL493344 | — | — | 1 | 7.37 |
| CHEMBL494400 | — | — | 1 | 7.36 |
| CHEMBL493565 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460480 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL493731 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL521674 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL492327 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL493344 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL494400 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL493565 | — | IC50 | = | 71.0 | nM | 7.15 |