Assay Detail
Binding
CHEMBL821341
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Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.44 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL302709 | — | — | 1 | 8.00 |
| CHEMBL418890 | — | — | 1 | 7.64 |
| CHEMBL70981 | — | — | 1 | 7.58 |
| CHEMBL71305 | — | — | 1 | 7.58 |
| CHEMBL304956 | — | — | 1 | 7.51 |
| CHEMBL73286 | — | — | 1 | 7.51 |
| CHEMBL82376 | — | — | 1 | 7.48 |
| CHEMBL310581 | — | — | 1 | 7.48 |
| CHEMBL71797 | — | — | 1 | 7.42 |
| CHEMBL311230 | — | — | 1 | 7.35 |
| CHEMBL310416 | — | — | 1 | 7.27 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL302709 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL418890 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL70981 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL71305 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL304956 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL73286 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL82376 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL310581 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL71797 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL311230 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL310416 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 340.0 | nM | 6.47 |