Assay Detail
Binding
CHEMBL4727316
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]AVP from human V1a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assay
45
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 45 | 8.02 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4756212 | — | — | 1 | 9.22 |
| CHEMBL4297183 | BALOVAPTAN | 3.0 | 1 | 9.15 |
| CHEMBL4790970 | — | — | 1 | 9.05 |
| CHEMBL4759676 | — | — | 1 | 9.00 |
| CHEMBL4798542 | — | — | 1 | 8.70 |
| CHEMBL4796133 | — | — | 1 | 8.70 |
| CHEMBL4790089 | — | — | 1 | 8.64 |
| CHEMBL4779447 | — | — | 1 | 8.59 |
| CHEMBL4762200 | — | — | 1 | 8.52 |
| CHEMBL4758799 | — | — | 1 | 8.52 |
| CHEMBL4776471 | — | — | 1 | 8.52 |
| CHEMBL4758331 | — | — | 1 | 8.52 |
| CHEMBL4789306 | — | — | 1 | 8.48 |
| CHEMBL4746818 | — | — | 3 | 8.40 |
| CHEMBL4785083 | — | — | 1 | 8.40 |
| CHEMBL4760164 | — | — | 1 | 8.40 |
| CHEMBL4744606 | — | — | 1 | 8.40 |
| CHEMBL4787242 | — | — | 1 | 8.39 |
| CHEMBL4759748 | — | — | 1 | 8.30 |
| CHEMBL4749660 | — | — | 1 | 8.30 |
| CHEMBL4741743 | — | — | 3 | 8.30 |
| CHEMBL4763639 | — | — | 1 | 8.30 |
| CHEMBL4781783 | — | — | 1 | 8.28 |
| CHEMBL3416885 | RO-5028442 | 1.0 | 1 | 8.26 |
| CHEMBL4753130 | — | — | 1 | 8.22 |
| CHEMBL4782389 | — | — | 1 | 8.22 |
| CHEMBL4743785 | — | — | 1 | 8.22 |
| CHEMBL4794001 | — | — | 1 | 8.15 |
| CHEMBL4742335 | — | — | 1 | 7.89 |
| CHEMBL4760698 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4756212 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4297183 | BALOVAPTAN | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL4790970 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL4759676 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4796133 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4798542 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4790089 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL4779447 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL4758799 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4776471 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4758331 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4762200 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4789306 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4744606 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4760164 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4746818 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4785083 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4787242 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL4749660 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4741743 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4759748 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4763639 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4746818 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4781783 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL3416885 | RO-5028442 | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL4782389 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4743785 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4753130 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4794001 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4742335 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4760698 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4799501 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4789445 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4741743 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4746818 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4787124 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4764410 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4742173 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4741743 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL4742334 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL4798616 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL4751260 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL4740795 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4743673 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL4757593 | — | Ki | = | 560.0 | nM | 6.25 |