Assay Detail
Functional
CHEMBL963640
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Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 15 | 6.48 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460480 | — | — | 1 | 8.40 |
| CHEMBL459215 | — | — | 1 | 8.03 |
| CHEMBL516479 | — | — | 1 | 7.96 |
| CHEMBL459659 | — | — | 1 | 7.85 |
| CHEMBL517881 | — | — | 1 | 7.62 |
| CHEMBL460892 | — | — | 1 | 7.20 |
| CHEMBL515200 | — | — | 1 | 6.35 |
| CHEMBL508898 | — | — | 1 | 6.19 |
| CHEMBL444509 | — | — | 1 | 5.92 |
| CHEMBL452547 | — | — | 1 | 5.64 |
| CHEMBL507973 | — | — | 1 | 5.55 |
| CHEMBL527422 | — | — | 1 | 5.47 |
| CHEMBL512893 | — | — | 1 | 5.35 |
| CHEMBL472117 | — | — | 1 | 5.04 |
| CHEMBL487627 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460480 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL459215 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL516479 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL459659 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL517881 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL460892 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL515200 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL508898 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL444509 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL452547 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL507973 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL527422 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL512893 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL472117 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL487627 | — | IC50 | = | 21000.0 | nM | 4.68 |