Assay Detail
Binding
CHEMBL653423
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Inhibition of [3H]BK (1.0 nM) binding to the human bradykinin receptor B2, expressed in CHO cells
24
Total Activities
24
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
Discovery of the first non-peptide full agonists for the human bradykinin B(2) receptor incorporating 4-(2-picolyloxy)quinoline and 1-(2-picolyl)benzimidazole frameworks.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.62 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430652 | — | — | 1 | 9.44 |
| CHEMBL262507 | — | — | 1 | 9.40 |
| CHEMBL99869 | — | — | 1 | 9.39 |
| CHEMBL98460 | — | — | 1 | 9.25 |
| CHEMBL329762 | — | — | 1 | 9.17 |
| CHEMBL433214 | — | — | 1 | 9.16 |
| CHEMBL98459 | — | — | 1 | 9.08 |
| CHEMBL98292 | — | — | 1 | 9.04 |
| CHEMBL542096 | — | — | 1 | 8.96 |
| CHEMBL98458 | — | — | 1 | 8.92 |
| CHEMBL329701 | — | — | 1 | 8.85 |
| CHEMBL328509 | — | — | 1 | 8.85 |
| CHEMBL98349 | — | — | 1 | 8.62 |
| CHEMBL97393 | — | — | 1 | 8.60 |
| CHEMBL540300 | — | — | 1 | 8.59 |
| CHEMBL329758 | — | — | 1 | 8.46 |
| CHEMBL538020 | — | — | 1 | 8.43 |
| CHEMBL264751 | — | — | 1 | 8.38 |
| CHEMBL538022 | — | — | 1 | 8.09 |
| CHEMBL545255 | — | — | 1 | 7.89 |
| CHEMBL555403 | — | — | 1 | 7.47 |
| CHEMBL553530 | — | — | 1 | 7.21 |
| CHEMBL542911 | — | — | 1 | 7.11 |
| CHEMBL99978 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL430652 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL262507 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL99869 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL98460 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL329762 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL433214 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL98459 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL98292 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL542096 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL98458 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL329701 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL328509 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL98349 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL97393 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL540300 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL329758 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL538020 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL264751 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL538022 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL545255 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL555403 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL553530 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL542911 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL99978 | — | IC50 | > | 1000.0 | nM | - |