Assay Detail
Binding
CHEMBL820469
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Inhibitory activity against arginine vasopressin V1 receptor using [3H]AVP as radioligand in human platelet
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of 5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine derivatives: novel arginine vasopressin antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.19 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430083 | — | — | 1 | 8.52 |
| CHEMBL367323 | — | — | 1 | 8.40 |
| CHEMBL368354 | — | — | 1 | 8.30 |
| CHEMBL177248 | — | — | 1 | 8.30 |
| CHEMBL368353 | — | — | 1 | 8.00 |
| CHEMBL413748 | — | — | 1 | 8.00 |
| CHEMBL177885 | — | — | 1 | 7.30 |
| CHEMBL368818 | — | — | 1 | 7.30 |
| CHEMBL369150 | — | — | 1 | 7.22 |
| CHEMBL435331 | — | — | 1 | 6.40 |
| CHEMBL366790 | — | — | 1 | 6.40 |
| CHEMBL175182 | — | — | 1 | 6.16 |
| CHEMBL176146 | — | — | 1 | 6.10 |
| CHEMBL177285 | — | — | 1 | 6.00 |
| CHEMBL175212 | — | — | 1 | 5.52 |
| CHEMBL366816 | — | — | 1 | - |
| CHEMBL369832 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430083 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL367323 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL368354 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL177248 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL368353 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL413748 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL177885 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL368818 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL369150 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL435331 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL366790 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL175182 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL176146 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL177285 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL175212 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL366816 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL369832 | — | IC50 | < | 1.0 | nM | - |