Assay Detail
Binding
CHEMBL815447
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Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.29 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301788 | — | — | 1 | 8.22 |
| CHEMBL299532 | — | — | 1 | 8.15 |
| CHEMBL46295 | — | — | 1 | 8.05 |
| CHEMBL300963 | — | — | 1 | 7.96 |
| CHEMBL297705 | — | — | 1 | 7.52 |
| CHEMBL300946 | — | — | 1 | 7.48 |
| CHEMBL49824 | — | — | 1 | 7.40 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 7.09 |
| CHEMBL300433 | — | — | 1 | 7.09 |
| CHEMBL298911 | — | — | 1 | 7.00 |
| CHEMBL51645 | — | — | 1 | 7.00 |
| CHEMBL296619 | — | — | 1 | 6.58 |
| CHEMBL49657 | — | — | 1 | 6.51 |
| CHEMBL49796 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301788 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL299532 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL46295 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL300963 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL297705 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL300946 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL49824 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL300433 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL298911 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL51645 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL296619 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL49657 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL49796 | — | IC50 | = | 920.0 | nM | 6.04 |