Assay Detail
Functional
CHEMBL815214
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Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 | 5 | 7.23 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 2 | 8.30 |
| CHEMBL165670 | — | — | 1 | 7.16 |
| CHEMBL424183 | — | — | 1 | 7.16 |
| CHEMBL166261 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL165670 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL424183 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL166261 | — | IC50 | = | 330.0 | nM | 6.48 |