Assay Detail
Functional
CHEMBL1115139
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
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
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.18 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468565 | — | — | 1 | 6.80 |
| CHEMBL521674 | — | — | 1 | 6.70 |
| CHEMBL1091579 | — | — | 1 | 6.58 |
| CHEMBL474991 | — | — | 1 | 6.44 |
| CHEMBL1088866 | — | — | 1 | 6.38 |
| CHEMBL1092638 | — | — | 1 | 6.04 |
| CHEMBL1091580 | — | — | 1 | 5.82 |
| CHEMBL1092245 | — | — | 1 | 5.47 |
| CHEMBL1091209 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468565 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL521674 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1091579 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL474991 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1088866 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL1092638 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL1091580 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1092245 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1091209 | — | IC50 | = | 4400.0 | nM | 5.36 |