Assay Detail
Binding
CHEMBL880663
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Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
12
Total Activities
12
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
(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.54 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL424663 | — | — | 1 | 8.70 |
| CHEMBL381248 | — | — | 1 | 8.52 |
| CHEMBL196737 | — | — | 1 | 7.92 |
| CHEMBL197616 | — | — | 1 | 7.89 |
| CHEMBL371721 | — | — | 1 | 7.89 |
| CHEMBL194970 | — | — | 1 | 7.68 |
| CHEMBL371055 | — | — | 1 | 7.20 |
| CHEMBL380579 | — | — | 1 | 7.19 |
| CHEMBL372766 | — | — | 1 | 7.07 |
| CHEMBL198931 | — | — | 1 | 7.06 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 6.75 |
| CHEMBL198446 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL424663 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL381248 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL196737 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL197616 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL371721 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL194970 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL371055 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL380579 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL372766 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL198931 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL198446 | — | IC50 | = | 280.0 | nM | 6.55 |