Assay Detail
Binding
CHEMBL817838
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In vitro binding affinity to human V2 receptor
10
Total Activities
10
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
The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.76 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 8.92 |
| CHEMBL350973 | — | — | 1 | 8.77 |
| CHEMBL159359 | — | — | 1 | 8.57 |
| CHEMBL418890 | — | — | 1 | 8.49 |
| CHEMBL350089 | — | — | 1 | 8.47 |
| CHEMBL350090 | — | — | 1 | 7.15 |
| CHEMBL350383 | — | — | 1 | 6.89 |
| CHEMBL162588 | — | — | 1 | 6.85 |
| CHEMBL349506 | — | — | 1 | 6.82 |
| CHEMBL351587 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL350973 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL159359 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL418890 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL350089 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL350090 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL350383 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL162588 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL349506 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL351587 | — | IC50 | = | 220.0 | nM | 6.66 |