Assay Detail
Binding
CHEMBL817097
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Displacement of P[3H]-AVP from isolated rat kidney medullary V2 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 | 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 | 15 | 7.88 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 9.30 |
| CHEMBL46295 | — | — | 1 | 9.00 |
| CHEMBL301788 | — | — | 1 | 8.96 |
| CHEMBL299532 | — | — | 1 | 8.80 |
| CHEMBL300963 | — | — | 1 | 8.74 |
| CHEMBL49824 | — | — | 1 | 8.40 |
| CHEMBL298911 | — | — | 1 | 8.37 |
| CHEMBL300433 | — | — | 1 | 8.14 |
| CHEMBL297705 | — | — | 1 | 8.08 |
| CHEMBL51645 | — | — | 1 | 7.48 |
| CHEMBL49796 | — | — | 1 | 6.80 |
| CHEMBL49392 | — | — | 1 | 6.68 |
| CHEMBL49657 | — | — | 1 | 6.62 |
| CHEMBL49323 | — | — | 1 | 6.54 |
| CHEMBL296619 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL46295 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL301788 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL299532 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL300963 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL49824 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL298911 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL300433 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL297705 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL51645 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL49796 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL49392 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL49657 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL49323 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL296619 | — | IC50 | = | 480.0 | nM | 6.32 |