Assay Detail
Functional
CHEMBL4121250
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Antagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition measured for 5 mins by Fluo-4-AM dye based FLIPR assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.44 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126100 | — | — | 1 | 7.85 |
| CHEMBL4127791 | — | — | 1 | 7.46 |
| CHEMBL4129142 | — | — | 1 | 5.36 |
| CHEMBL4128839 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126100 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4127791 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4129142 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4128839 | — | IC50 | = | 7862.0 | nM | 5.10 |