Assay Detail
Binding
CHEMBL652383
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Inhibition of specific binding of [3H]-BK (1 nM) to rat Bradykinin receptor B2 by 50% in NG108-15 cell membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | NG108-15 |
| Subcellular | Membrane |
| 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 | 11 | 8.27 | 10.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1907651 | — | — | 1 | 10.64 |
| CHEMBL1907652 | — | — | 1 | 9.51 |
| CHEMBL308468 | — | — | 1 | 9.30 |
| CHEMBL431562 | — | — | 1 | 9.22 |
| CHEMBL1907654 | — | — | 1 | 8.26 |
| CHEMBL1907653 | — | — | 1 | 8.14 |
| CHEMBL2112283 | — | — | 1 | 7.97 |
| CHEMBL1907656 | — | — | 1 | 7.84 |
| CHEMBL2112221 | — | — | 1 | 7.19 |
| CHEMBL2112220 | — | — | 1 | 6.75 |
| CHEMBL1907655 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1907651 | — | Ki | = | 0.023 | nM | 10.64 |
| CHEMBL1907652 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL308468 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL431562 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1907654 | — | Ki | = | 5.46 | nM | 8.26 |
| CHEMBL1907653 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL2112283 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL1907656 | — | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL2112221 | — | Ki | = | 64.5 | nM | 7.19 |
| CHEMBL2112220 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL1907655 | — | Ki | = | 654.0 | nM | 6.18 |