Assay Detail
Binding
CHEMBL1052804
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Displacement of [3H]Arg8-vasopressin from human vasopressin V1a receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 5.93 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL582857 | NELIVAPTAN | 2.0 | 1 | 7.66 |
| CHEMBL583082 | — | — | 1 | 7.48 |
| CHEMBL572709 | — | — | 1 | 6.73 |
| CHEMBL583083 | — | — | 1 | 6.72 |
| CHEMBL1204126 | — | — | 1 | 6.50 |
| CHEMBL572760 | — | — | 1 | 6.40 |
| CHEMBL572984 | — | — | 1 | 6.31 |
| CHEMBL572754 | — | — | 1 | 6.26 |
| CHEMBL576341 | — | — | 1 | 6.15 |
| CHEMBL583081 | — | — | 1 | 6.14 |
| CHEMBL575796 | — | — | 1 | 6.02 |
| CHEMBL1204403 | — | — | 1 | 5.95 |
| CHEMBL575797 | — | — | 1 | 5.90 |
| CHEMBL575987 | — | — | 1 | 5.90 |
| CHEMBL572983 | — | — | 1 | 5.58 |
| CHEMBL575359 | — | — | 1 | 5.44 |
| CHEMBL567176 | — | — | 1 | 5.34 |
| CHEMBL572835 | — | — | 1 | 5.32 |
| CHEMBL583084 | — | — | 1 | 5.31 |
| CHEMBL575986 | — | — | 1 | 5.30 |
| CHEMBL575972 | — | — | 1 | 5.25 |
| CHEMBL577816 | — | — | 1 | 5.21 |
| CHEMBL575574 | — | — | 1 | 5.16 |
| CHEMBL572921 | — | — | 1 | 5.06 |
| CHEMBL574450 | — | — | 1 | 5.05 |
| CHEMBL577599 | — | — | 1 | - |
| CHEMBL576147 | — | — | 1 | - |
| CHEMBL575773 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL582857 | NELIVAPTAN | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL583082 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL572709 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL583083 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL1204126 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL572760 | — | Ki | = | 395.0 | nM | 6.40 |
| CHEMBL572984 | — | Ki | = | 486.0 | nM | 6.31 |
| CHEMBL572754 | — | Ki | = | 553.0 | nM | 6.26 |
| CHEMBL576341 | — | Ki | = | 709.0 | nM | 6.15 |
| CHEMBL583081 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL575796 | — | Ki | = | 947.0 | nM | 6.02 |
| CHEMBL1204403 | — | Ki | = | 1129.0 | nM | 5.95 |
| CHEMBL575797 | — | Ki | = | 1257.0 | nM | 5.90 |
| CHEMBL575987 | — | Ki | = | 1268.0 | nM | 5.90 |
| CHEMBL572983 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL575359 | — | Ki | = | 3654.0 | nM | 5.44 |
| CHEMBL567176 | — | Ki | = | 4617.0 | nM | 5.34 |
| CHEMBL572835 | — | Ki | = | 4803.0 | nM | 5.32 |
| CHEMBL583084 | — | Ki | = | 4926.0 | nM | 5.31 |
| CHEMBL575986 | — | Ki | = | 4963.0 | nM | 5.30 |
| CHEMBL575972 | — | Ki | = | 5564.0 | nM | 5.25 |
| CHEMBL577816 | — | Ki | = | 6164.0 | nM | 5.21 |
| CHEMBL575574 | — | Ki | = | 6888.0 | nM | 5.16 |
| CHEMBL572921 | — | Ki | = | 8734.0 | nM | 5.06 |
| CHEMBL574450 | — | Ki | = | 8866.0 | nM | 5.05 |
| CHEMBL577599 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL576147 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL575773 | — | Ki | > | 8000.0 | nM | - |