Assay Detail
Binding
CHEMBL907381
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Displacement of [3H]AVP from vasopressin V1a receptor in rat liver membrane
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.39 | 8.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL373742 | VASOPRESSIN | 4.0 | 1 | 8.81 |
| CHEMBL1429 | DESMOPRESSIN | 4.0 | 2 | 7.97 |
| CHEMBL375324 | — | — | 1 | 7.89 |
| CHEMBL385739 | — | — | 1 | 7.60 |
| CHEMBL221436 | — | — | 1 | 7.22 |
| CHEMBL385068 | — | — | 1 | 7.17 |
| CHEMBL375325 | — | — | 1 | 6.89 |
| CHEMBL435323 | — | — | 1 | 6.50 |
| CHEMBL414074 | — | — | 1 | 6.35 |
| CHEMBL375096 | — | — | 1 | 6.05 |
| CHEMBL412973 | — | — | 1 | 6.00 |
| CHEMBL265859 | — | — | 1 | 5.90 |
| CHEMBL219272 | — | — | 1 | 5.89 |
| CHEMBL375188 | — | — | 1 | 5.85 |
| CHEMBL375187 | — | — | 1 | 5.75 |
| CHEMBL265858 | — | — | 1 | 5.64 |
| CHEMBL375323 | — | — | 1 | 5.55 |
| CHEMBL263090 | — | — | 1 | 5.54 |
| CHEMBL373968 | — | — | 1 | 5.48 |
| CHEMBL412972 | — | — | 1 | 5.42 |
| CHEMBL412742 | — | — | 1 | 5.36 |
| CHEMBL221485 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL373742 | VASOPRESSIN | Ki | = | 1.54 | nM | 8.81 |
| CHEMBL1429 | DESMOPRESSIN | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL375324 | — | Ki | = | 12.9 | nM | 7.89 |
| CHEMBL385739 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL221436 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL385068 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL1429 | DESMOPRESSIN | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL375325 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL435323 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL414074 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL375096 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL412973 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL265859 | — | Ki | = | 1252.0 | nM | 5.90 |
| CHEMBL219272 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL375188 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL375187 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL265858 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL375323 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL263090 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL373968 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL412972 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL412742 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL221485 | — | Ki | = | 9100.0 | nM | 5.04 |