Assay Detail
Binding
CHEMBL4141652
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Displacement of [3H]-vasopressin from human vasopressin V1a receptor expressed in HEK293 cell membranes after 90 mins by radioligand binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.14 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3763342 | — | — | 1 | 7.57 |
| CHEMBL3763951 | — | — | 1 | 7.21 |
| CHEMBL3763823 | — | — | 1 | 7.19 |
| CHEMBL3763174 | — | — | 1 | 6.71 |
| CHEMBL4166008 | — | — | 1 | 6.60 |
| CHEMBL4162565 | — | — | 1 | 6.19 |
| CHEMBL4173250 | — | — | 1 | 6.10 |
| CHEMBL4176616 | — | — | 1 | 6.06 |
| CHEMBL4159182 | — | — | 1 | 5.97 |
| CHEMBL4169435 | — | — | 1 | 5.75 |
| CHEMBL4169830 | — | — | 1 | 5.72 |
| CHEMBL4169825 | — | — | 1 | 5.71 |
| CHEMBL4162568 | — | — | 1 | 5.68 |
| CHEMBL4161507 | — | — | 1 | 5.48 |
| CHEMBL4169437 | — | — | 1 | 5.20 |
| CHEMBL4173255 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3763342 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3763951 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL3763823 | — | Ki | = | 64.1 | nM | 7.19 |
| CHEMBL3763174 | — | Ki | = | 194.7 | nM | 6.71 |
| CHEMBL4166008 | — | Ki | = | 250.7 | nM | 6.60 |
| CHEMBL4162565 | — | Ki | = | 642.8 | nM | 6.19 |
| CHEMBL4173250 | — | Ki | = | 795.1 | nM | 6.10 |
| CHEMBL4176616 | — | Ki | = | 874.1 | nM | 6.06 |
| CHEMBL4159182 | — | Ki | = | 1062.0 | nM | 5.97 |
| CHEMBL4169435 | — | Ki | = | 1756.0 | nM | 5.75 |
| CHEMBL4169830 | — | Ki | = | 1910.0 | nM | 5.72 |
| CHEMBL4169825 | — | Ki | = | 1938.0 | nM | 5.71 |
| CHEMBL4162568 | — | Ki | = | 2095.0 | nM | 5.68 |
| CHEMBL4161507 | — | Ki | = | 3343.0 | nM | 5.48 |
| CHEMBL4169437 | — | Ki | = | 6250.0 | nM | 5.20 |
| CHEMBL4173255 | — | Ki | = | 6807.0 | nM | 5.17 |