Assay Detail
Binding
CHEMBL817837
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Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.33 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL350576 | — | — | 1 | 8.10 |
| CHEMBL424183 | — | — | 1 | 7.96 |
| CHEMBL166135 | — | — | 1 | 7.92 |
| CHEMBL165554 | — | — | 1 | 7.89 |
| CHEMBL165076 | — | — | 1 | 7.82 |
| CHEMBL165670 | — | — | 1 | 7.70 |
| CHEMBL351453 | — | — | 1 | 7.36 |
| CHEMBL166261 | — | — | 1 | 7.30 |
| CHEMBL349965 | — | — | 1 | 6.77 |
| CHEMBL349062 | — | — | 1 | 6.75 |
| CHEMBL166265 | — | — | 1 | 6.72 |
| CHEMBL165183 | — | — | 1 | 6.68 |
| CHEMBL350792 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL350576 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL424183 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL166135 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL165554 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL165076 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL165670 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL351453 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL166261 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL349965 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL349062 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL166265 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL165183 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL350792 | — | IC50 | = | 550.0 | nM | 6.26 |