Assay Detail
Binding
CHEMBL963639
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Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 15 | 5.90 | 7.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460480 | — | — | 1 | 7.76 |
| CHEMBL516479 | — | — | 1 | 7.50 |
| CHEMBL459215 | — | — | 1 | 7.40 |
| CHEMBL517881 | — | — | 1 | 7.14 |
| CHEMBL459659 | — | — | 1 | 6.96 |
| CHEMBL460892 | — | — | 1 | 6.17 |
| CHEMBL444509 | — | — | 1 | 6.15 |
| CHEMBL515200 | — | — | 1 | 6.00 |
| CHEMBL508898 | — | — | 1 | 5.41 |
| CHEMBL452547 | — | — | 1 | 5.28 |
| CHEMBL452044 | — | — | 1 | 4.82 |
| CHEMBL472117 | — | — | 1 | 4.82 |
| CHEMBL512893 | — | — | 1 | 4.68 |
| CHEMBL527422 | — | — | 1 | 4.29 |
| CHEMBL487627 | — | — | 1 | 4.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460480 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL516479 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL459215 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL517881 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL459659 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL460892 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL444509 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL515200 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL508898 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL452547 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL452044 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL472117 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL512893 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL527422 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL487627 | — | IC50 | = | 64000.0 | nM | 4.19 |