Assay Detail
Binding
CHEMBL885357
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Ability to bind to human cloned B1 receptor in competition binding experiments with [3H][des-Arg10,Leu9]-Kallidin.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.65 | 10.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3085458 | — | — | 1 | 10.64 |
| CHEMBL3142391 | — | — | 1 | 10.46 |
| CHEMBL412824 | — | — | 1 | 9.66 |
| CHEMBL2369827 | — | — | 1 | 9.05 |
| CHEMBL216618 | — | — | 1 | 8.25 |
| CHEMBL2369828 | — | — | 1 | 7.62 |
| CHEMBL408846 | — | — | 1 | 7.08 |
| CHEMBL80472 | — | — | 1 | 6.42 |
| CHEMBL406291 | BRADYKININ | 2.0 | 1 | - |
| CHEMBL3142396 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3085458 | — | Ki | = | 0.023 | nM | 10.64 |
| CHEMBL3142391 | — | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL412824 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL2369827 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL216618 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL2369828 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL408846 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL80472 | — | Ki | = | 382.0 | nM | 6.42 |
| CHEMBL406291 | BRADYKININ | Ki | > | 10.0 | nM | - |
| CHEMBL3142396 | — | Ki | > | 10.0 | nM | - |