Assay Detail
Binding
CHEMBL907380
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Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 7.85 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL375324 | — | — | 1 | 9.70 |
| CHEMBL435323 | — | — | 1 | 9.59 |
| CHEMBL221436 | — | — | 1 | 9.52 |
| CHEMBL1429 | DESMOPRESSIN | 4.0 | 2 | 9.52 |
| CHEMBL373742 | VASOPRESSIN | 4.0 | 1 | 9.35 |
| CHEMBL385739 | — | — | 1 | 8.74 |
| CHEMBL385068 | — | — | 1 | 8.51 |
| CHEMBL265859 | — | — | 1 | 8.51 |
| CHEMBL375096 | — | — | 1 | 8.47 |
| CHEMBL375325 | — | — | 1 | 8.42 |
| CHEMBL265858 | — | — | 1 | 7.90 |
| CHEMBL375323 | — | — | 1 | 7.29 |
| CHEMBL414074 | — | — | 1 | 7.16 |
| CHEMBL219272 | — | — | 1 | 7.12 |
| CHEMBL412972 | — | — | 1 | 7.00 |
| CHEMBL412973 | — | — | 1 | 6.68 |
| CHEMBL373968 | — | — | 1 | 6.62 |
| CHEMBL375188 | — | — | 1 | 6.37 |
| CHEMBL412742 | — | — | 1 | 6.35 |
| CHEMBL263090 | — | — | 1 | 6.35 |
| CHEMBL221485 | — | — | 1 | 6.22 |
| CHEMBL375187 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL375324 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL435323 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL221436 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1429 | DESMOPRESSIN | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL373742 | VASOPRESSIN | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL1429 | DESMOPRESSIN | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL385739 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL385068 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL265859 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL375096 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL375325 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL265858 | — | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL375323 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL414074 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL219272 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL412972 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL412973 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL373968 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL375188 | — | Ki | = | 425.0 | nM | 6.37 |
| CHEMBL412742 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL263090 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL221485 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL375187 | — | Ki | = | 1050.0 | nM | 5.98 |