Assay Detail
Functional
CHEMBL4727317
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
39
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | 1321N1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.93 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3416885 | RO-5028442 | 1.0 | 1 | 8.70 |
| CHEMBL4756212 | — | — | 1 | 8.62 |
| CHEMBL4297183 | BALOVAPTAN | 3.0 | 1 | 8.52 |
| CHEMBL4789306 | — | — | 1 | 8.00 |
| CHEMBL4779447 | — | — | 1 | 7.96 |
| CHEMBL4759676 | — | — | 1 | 7.96 |
| CHEMBL4781783 | — | — | 1 | 7.70 |
| CHEMBL4746818 | — | — | 3 | 7.68 |
| CHEMBL4790089 | — | — | 1 | 7.60 |
| CHEMBL4744606 | — | — | 1 | 7.46 |
| CHEMBL4758331 | — | — | 1 | 7.46 |
| CHEMBL4753130 | — | — | 1 | 7.46 |
| CHEMBL4790970 | — | — | 1 | 7.40 |
| CHEMBL4758799 | — | — | 1 | 7.40 |
| CHEMBL4782389 | — | — | 1 | 7.30 |
| CHEMBL4798542 | — | — | 1 | 7.26 |
| CHEMBL4787242 | — | — | 1 | 7.10 |
| CHEMBL4762200 | — | — | 1 | 7.07 |
| CHEMBL4763639 | — | — | 1 | 6.87 |
| CHEMBL4743785 | — | — | 1 | 6.77 |
| CHEMBL4741743 | — | — | 1 | 6.75 |
| CHEMBL4760164 | — | — | 1 | 6.70 |
| CHEMBL4760698 | — | — | 1 | 6.58 |
| CHEMBL4785083 | — | — | 1 | 6.55 |
| CHEMBL4794001 | — | — | 1 | 6.52 |
| CHEMBL4776471 | — | — | 1 | 6.42 |
| CHEMBL4749660 | — | — | 1 | 6.41 |
| CHEMBL4796133 | — | — | 1 | 6.35 |
| CHEMBL4742173 | — | — | 1 | 6.12 |
| CHEMBL4751260 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3416885 | RO-5028442 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4756212 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4297183 | BALOVAPTAN | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4789306 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4759676 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4779447 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4781783 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4746818 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4790089 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4758331 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4744606 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4753130 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4758799 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4790970 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4746818 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4782389 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4798542 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4787242 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4762200 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4763639 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4743785 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4741743 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4760164 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4760698 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4746818 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4785083 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4794001 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4776471 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4749660 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4796133 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4742173 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4751260 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4799501 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4787124 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4757593 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4742335 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4764410 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4742334 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4798616 | — | IC50 | = | 8300.0 | nM | 5.08 |