Assay Detail
Binding
CHEMBL652641
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Binding affinity towards human cloned Bradykinin receptor B2 expressed in CHO cells by [3H]bradykinin displacement.
18
Total Activities
17
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
Synthesis and characterization of bradykinin B(2) receptor agonists containing constrained dipeptide mimics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.38 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028850 | ICATIBANT | 4.0 | 1 | 10.22 |
| CHEMBL406291 | BRADYKININ | 2.0 | 1 | 10.19 |
| CHEMBL440257 | — | — | 1 | 10.15 |
| CHEMBL428148 | — | — | 1 | 9.15 |
| CHEMBL386697 | — | — | 1 | 8.60 |
| CHEMBL262313 | — | — | 1 | 8.22 |
| CHEMBL384617 | — | — | 1 | 7.85 |
| CHEMBL2370748 | — | — | 1 | 7.72 |
| CHEMBL3350763 | — | — | 2 | 7.07 |
| CHEMBL2111891 | — | — | 1 | 6.85 |
| CHEMBL2112709 | — | — | 1 | 6.80 |
| CHEMBL415032 | — | — | 1 | 6.28 |
| CHEMBL427805 | — | — | 1 | 6.11 |
| CHEMBL436963 | — | — | 1 | 5.99 |
| CHEMBL264712 | — | — | 1 | 5.68 |
| CHEMBL415209 | — | — | 1 | 5.31 |
| CHEMBL407626 | — | — | 1 | 4.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028850 | ICATIBANT | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL406291 | BRADYKININ | Ki | = | 0.065 | nM | 10.19 |
| CHEMBL440257 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL428148 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL386697 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL262313 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL384617 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2370748 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3350763 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL2111891 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL2112709 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL415032 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL427805 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL436963 | — | Ki | = | 1030.0 | nM | 5.99 |
| CHEMBL3350763 | — | Ki | = | 1040.0 | nM | 5.98 |
| CHEMBL264712 | — | Ki | = | 2070.0 | nM | 5.68 |
| CHEMBL415209 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL407626 | — | Ki | = | 18600.0 | nM | 4.73 |