Assay Detail
Binding
CHEMBL963637
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
20
Total Activities
20
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
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.68 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460480 | — | — | 1 | 8.77 |
| CHEMBL459215 | — | — | 1 | 8.31 |
| CHEMBL516479 | — | — | 1 | 8.26 |
| CHEMBL517881 | — | — | 1 | 8.24 |
| CHEMBL459659 | — | — | 1 | 8.21 |
| CHEMBL460892 | — | — | 1 | 8.06 |
| CHEMBL444509 | — | — | 1 | 7.30 |
| CHEMBL515200 | — | — | 1 | 6.92 |
| CHEMBL508898 | — | — | 1 | 6.92 |
| CHEMBL452547 | — | — | 1 | 6.66 |
| CHEMBL527422 | — | — | 1 | 6.24 |
| CHEMBL512893 | — | — | 1 | 6.10 |
| CHEMBL516934 | — | — | 1 | 5.92 |
| CHEMBL507973 | — | — | 1 | 5.89 |
| CHEMBL472117 | — | — | 1 | 5.82 |
| CHEMBL488812 | — | — | 1 | 5.48 |
| CHEMBL488478 | — | — | 1 | 5.35 |
| CHEMBL452044 | — | — | 1 | 5.20 |
| CHEMBL487627 | — | — | 1 | 5.02 |
| CHEMBL452293 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460480 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL459215 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL516479 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL517881 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL459659 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL460892 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL444509 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL515200 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL508898 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL452547 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL527422 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL512893 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL516934 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL507973 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL472117 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL488812 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL488478 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL452044 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL487627 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL452293 | — | IC50 | = | 11000.0 | nM | 4.96 |