Assay Detail
Binding
CHEMBL876526
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Displacement of [3H]BK (1 nM) from human Bradykinin receptor B2 expressed in Cos-7 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Nonpeptide bradykinin B2 receptor antagonists: conversion of rodent-selective bradyzide analogues into potent, orally-active human bradykinin B2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.24 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2112283 | — | — | 1 | 9.10 |
| CHEMBL2112221 | — | — | 1 | 8.83 |
| CHEMBL2112220 | — | — | 1 | 8.55 |
| CHEMBL1907656 | — | — | 1 | 8.33 |
| CHEMBL1907654 | — | — | 1 | 7.47 |
| CHEMBL1907652 | — | — | 1 | 7.02 |
| CHEMBL1907651 | — | — | 1 | 6.92 |
| CHEMBL303258 | — | — | 1 | 6.62 |
| CHEMBL2112219 | — | — | 1 | 6.60 |
| CHEMBL1907655 | — | — | 1 | 6.52 |
| CHEMBL1907657 | — | — | 1 | 6.19 |
| CHEMBL308468 | — | — | 1 | 6.11 |
| CHEMBL431562 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2112283 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL2112221 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL2112220 | — | Ki | = | 2.79 | nM | 8.55 |
| CHEMBL1907656 | — | Ki | = | 4.67 | nM | 8.33 |
| CHEMBL1907654 | — | Ki | = | 34.1 | nM | 7.47 |
| CHEMBL1907652 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL1907651 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL303258 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL2112219 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL1907655 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL1907657 | — | Ki | = | 645.0 | nM | 6.19 |
| CHEMBL308468 | — | Ki | = | 772.0 | nM | 6.11 |
| CHEMBL431562 | — | Ki | = | 1430.0 | nM | 5.84 |