Assay Detail
Binding
CHEMBL3419318
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-vasopressin from mouse vasopressin 1a receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 6.36 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3416884 | — | — | 1 | 7.96 |
| CHEMBL3416883 | — | — | 1 | 7.89 |
| CHEMBL3416881 | — | — | 1 | 7.85 |
| CHEMBL3416885 | RO-5028442 | 1.0 | 1 | 7.41 |
| CHEMBL3416868 | — | — | 1 | 7.39 |
| CHEMBL3416882 | — | — | 1 | 6.90 |
| CHEMBL3416869 | — | — | 1 | 6.75 |
| CHEMBL3416860 | — | — | 1 | 6.68 |
| CHEMBL3416861 | — | — | 1 | 6.00 |
| CHEMBL3416870 | — | — | 1 | 5.99 |
| CHEMBL3416879 | — | — | 1 | 5.83 |
| CHEMBL3416880 | — | — | 1 | 5.71 |
| CHEMBL3416878 | — | — | 1 | 5.62 |
| CHEMBL3416871 | — | — | 1 | 5.53 |
| CHEMBL3416872 | — | — | 1 | 5.32 |
| CHEMBL3416876 | — | — | 1 | 5.23 |
| CHEMBL3416875 | — | — | 1 | 5.23 |
| CHEMBL3416867 | — | — | 1 | 5.18 |
| CHEMBL3416877 | — | — | 1 | - |
| CHEMBL3416874 | — | — | 1 | - |
| CHEMBL3416873 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3416884 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3416883 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3416881 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3416885 | RO-5028442 | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL3416868 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL3416882 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL3416869 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL3416860 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL3416861 | — | Ki | = | 1012.0 | nM | 6.00 |
| CHEMBL3416870 | — | Ki | = | 1018.0 | nM | 5.99 |
| CHEMBL3416879 | — | Ki | = | 1491.0 | nM | 5.83 |
| CHEMBL3416880 | — | Ki | = | 1972.0 | nM | 5.71 |
| CHEMBL3416878 | — | Ki | = | 2395.0 | nM | 5.62 |
| CHEMBL3416871 | — | Ki | = | 2980.0 | nM | 5.53 |
| CHEMBL3416872 | — | Ki | = | 4816.0 | nM | 5.32 |
| CHEMBL3416876 | — | Ki | = | 5886.0 | nM | 5.23 |
| CHEMBL3416875 | — | Ki | = | 5890.0 | nM | 5.23 |
| CHEMBL3416867 | — | Ki | = | 6620.0 | nM | 5.18 |
| CHEMBL3416877 | — | Ki | - | — | - | |
| CHEMBL3416874 | — | Ki | - | — | - | |
| CHEMBL3416873 | — | Ki | - | — | - |