Assay Detail
Binding
CHEMBL1115143
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
13
Total Activities
13
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
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.93 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1091579 | — | — | 1 | 8.64 |
| CHEMBL1091209 | — | — | 1 | 8.37 |
| CHEMBL521674 | — | — | 1 | 8.24 |
| CHEMBL1088866 | — | — | 1 | 8.17 |
| CHEMBL1092638 | — | — | 1 | 8.01 |
| CHEMBL468565 | — | — | 1 | 8.00 |
| CHEMBL474991 | — | — | 1 | 7.92 |
| CHEMBL1091580 | — | — | 1 | 7.36 |
| CHEMBL1092245 | — | — | 1 | 7.33 |
| CHEMBL1092626 | — | — | 1 | 7.24 |
| CHEMBL1092627 | — | — | 1 | - |
| CHEMBL1091901 | — | — | 1 | - |
| CHEMBL1088865 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1091579 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL1091209 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL521674 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL1088866 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL1092638 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL468565 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL474991 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1091580 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1092245 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1092626 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1092627 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1091901 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1088865 | — | IC50 | > | 10000.0 | nM | - |