Assay Detail
Binding
CHEMBL4880932
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Inhibition of Vasopressin V1A at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_287530)
13
Total Activities
11
Compounds Tested
3
Activity Types
14
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Profiling data from Eurofins-Panlabs
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 11 | - | - |
| IC50 | 1 | 8.17 | 8.17 |
| Ki | 1 | 8.88 | 8.88 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Assay protocol publication | Assay protocol publication | - | — | PMID: 8106369 |
| Detection method | Detection method | - | — | Radioligand Binding |
| Incubation temperature | Incubation temperature | - | — | 25 °C |
| Incubation time | Incubation time | - | — | 2 h |
| Ligand | Ligand | - | — | [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr |
| Ligand Bmax | Ligand Bmax | 2.8 | pM/ mg protein | — |
| Ligand concentration | Ligand concentration | 0.03 | nM | — |
| Ligand Kd | Ligand Kd | 0.0074 | nM | — |
| Ligand specific binding | Ligand specific binding | 85.0 | % | — |
| Non-specific ligand with concentration | Non-specific ligand with concentration | - | — | 1 µM (Arg8)-Vasopressin |
| Reference compound | Reference compound | - | — | (Arg8)-Vasopressin |
| reference compound IC50 | reference compound IC50 | 0.33 | nM | — |
| reference compound Ki | reference compound Ki | 0.065 | nM | — |
| Source of protein | Source of protein | - | — | Human recombinant HEK-293 cells |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4594444 | PECAVAPTAN | 2.0 | 3 | 8.88 |
| CHEMBL4537788 | BAY-784 | — | 1 | - |
| CHEMBL4098877 | MLi-2 | — | 1 | - |
| CHEMBL1800685 | PPTN | — | 1 | - |
| CHEMBL2204538 | THPP-1 | — | 1 | - |
| CHEMBL4551635 | BAY-069 | — | 1 | - |
| CHEMBL4643852 | BAY-6672 | — | 1 | - |
| CHEMBL4514203 | BAY-390 | — | 1 | - |
| CHEMBL4802045 | BAY-091 | — | 1 | - |
| CHEMBL5410211 | — | — | 1 | - |
| CHEMBL5465173 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4594444 | PECAVAPTAN | Ki | = | 1.33 | nM | 8.88 |
| CHEMBL4594444 | PECAVAPTAN | IC50 | = | 6.74 | nM | 8.17 |
| CHEMBL4537788 | BAY-784 | Inhibition | = | -11.0 | % | - |
| CHEMBL4098877 | MLi-2 | Inhibition | = | -9.0 | % | - |
| CHEMBL1800685 | PPTN | Inhibition | = | 3.0 | % | - |
| CHEMBL2204538 | THPP-1 | Inhibition | = | 1.0 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | 7.0 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | -18.0 | % | - |
| CHEMBL4514203 | BAY-390 | Inhibition | = | -7.0 | % | - |
| CHEMBL4802045 | BAY-091 | Inhibition | = | -3.0 | % | - |
| CHEMBL5410211 | — | Inhibition | = | -2.3 | % | - |
| CHEMBL4594444 | PECAVAPTAN | Inhibition | = | 65.0 | % | - |
| CHEMBL5465173 | — | Inhibition | = | 28.0 | % | - |