Assay Detail
Binding
CHEMBL821340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 15 | 7.03 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306970 | — | — | 1 | 8.20 |
| CHEMBL312036 | — | — | 1 | 7.82 |
| CHEMBL418890 | — | — | 1 | 7.82 |
| CHEMBL68085 | — | — | 1 | 7.70 |
| CHEMBL81755 | — | — | 1 | 7.60 |
| CHEMBL81269 | — | — | 1 | 7.50 |
| CHEMBL420031 | — | — | 1 | 7.43 |
| CHEMBL310416 | — | — | 1 | 7.23 |
| CHEMBL81133 | — | — | 1 | 6.92 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 6.64 |
| CHEMBL420216 | — | — | 1 | 6.47 |
| CHEMBL311931 | — | — | 1 | 6.37 |
| CHEMBL80029 | — | — | 1 | 6.27 |
| CHEMBL311230 | — | — | 1 | 6.19 |
| CHEMBL314344 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306970 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL312036 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL418890 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL68085 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL81755 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL81269 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL420031 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL310416 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL81133 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL420216 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL311931 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL80029 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL311230 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL314344 | — | IC50 | = | 4400.0 | nM | 5.36 |