Assay Detail
Binding
CHEMBL820168
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In vitro binding affinity for rat V1a receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 12 | 6.32 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL159823 | — | — | 1 | 8.47 |
| CHEMBL159359 | — | — | 1 | 7.80 |
| CHEMBL418890 | — | — | 1 | 7.64 |
| CHEMBL159831 | — | — | 1 | 6.64 |
| CHEMBL49429 | LIXIVAPTAN | 3.0 | 1 | 6.47 |
| CHEMBL350090 | — | — | 1 | 5.77 |
| CHEMBL351587 | — | — | 1 | 5.70 |
| CHEMBL162588 | — | — | 1 | 5.70 |
| CHEMBL349506 | — | — | 1 | 5.68 |
| CHEMBL350383 | — | — | 1 | 5.68 |
| CHEMBL160029 | — | — | 1 | 5.33 |
| CHEMBL162748 | — | — | 1 | 4.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL159823 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL159359 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL418890 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL159831 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL49429 | LIXIVAPTAN | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL350090 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL351587 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL162588 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL349506 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL350383 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL160029 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL162748 | — | IC50 | = | 12400.0 | nM | 4.91 |