Assay Detail
Binding
CHEMBL820278
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Binding affinity against human vasopressin V1a receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 7.45 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2369839 | — | — | 1 | 8.82 |
| CHEMBL2369831 | — | — | 1 | 8.54 |
| CHEMBL1429 | DESMOPRESSIN | 4.0 | 2 | 8.42 |
| CHEMBL221436 | — | — | 1 | 7.94 |
| CHEMBL2369838 | — | — | 1 | 7.89 |
| CHEMBL1790575 | — | — | 1 | 7.78 |
| CHEMBL2369841 | — | — | 1 | 7.71 |
| CHEMBL2369829 | — | — | 1 | 7.71 |
| CHEMBL2369845 | — | — | 1 | 7.65 |
| CHEMBL411148 | — | — | 1 | 7.61 |
| CHEMBL2369830 | — | — | 1 | 7.55 |
| CHEMBL2369834 | — | — | 1 | 7.44 |
| CHEMBL2369842 | — | — | 1 | 7.43 |
| CHEMBL268306 | — | — | 1 | 7.36 |
| CHEMBL2369836 | — | — | 1 | 7.32 |
| CHEMBL375324 | — | — | 1 | 7.27 |
| CHEMBL2369848 | — | — | 1 | 7.20 |
| CHEMBL2369840 | — | — | 1 | 7.12 |
| CHEMBL2369847 | — | — | 1 | 7.10 |
| CHEMBL375096 | — | — | 1 | 7.06 |
| CHEMBL265858 | — | — | 1 | 6.82 |
| CHEMBL80877 | — | — | 1 | 6.56 |
| CHEMBL2369835 | — | — | 1 | 6.36 |
| CHEMBL2369837 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2369839 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2369831 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL1429 | DESMOPRESSIN | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL221436 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL2369838 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1790575 | — | Ki | = | 16.8 | nM | 7.78 |
| CHEMBL2369841 | — | Ki | = | 19.7 | nM | 7.71 |
| CHEMBL2369829 | — | Ki | = | 19.7 | nM | 7.71 |
| CHEMBL2369845 | — | Ki | = | 22.5 | nM | 7.65 |
| CHEMBL411148 | — | Ki | = | 24.8 | nM | 7.61 |
| CHEMBL2369830 | — | Ki | = | 28.1 | nM | 7.55 |
| CHEMBL2369834 | — | Ki | = | 36.3 | nM | 7.44 |
| CHEMBL2369842 | — | Ki | = | 36.9 | nM | 7.43 |
| CHEMBL268306 | — | Ki | = | 44.1 | nM | 7.36 |
| CHEMBL2369836 | — | Ki | = | 48.2 | nM | 7.32 |
| CHEMBL375324 | — | Ki | = | 54.2 | nM | 7.27 |
| CHEMBL1429 | DESMOPRESSIN | Ki | = | 62.4 | nM | 7.21 |
| CHEMBL2369848 | — | Ki | = | 63.3 | nM | 7.20 |
| CHEMBL2369840 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2369847 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL375096 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL265858 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL80877 | — | Ki | = | 276.0 | nM | 6.56 |
| CHEMBL2369835 | — | Ki | = | 436.0 | nM | 6.36 |
| CHEMBL2369837 | — | Ki | = | 463.0 | nM | 6.33 |