Assay Detail
Binding
CHEMBL653424
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In vitro inhibitory activity towards human bradykinin receptor B2 expressed in CHO cells using [3H]BK (1.0 nM) as a radioligand
36
Total Activities
36
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
A new series of highly potent non-peptide bradykinin B2 receptor antagonists incorporating the 4-heteroarylquinoline framework. Improvement of aqueous solubility and new insights into species difference.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.05 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3216880 | — | — | 1 | 9.77 |
| CHEMBL543070 | — | — | 1 | 9.74 |
| CHEMBL3217081 | — | — | 1 | 9.64 |
| CHEMBL542598 | — | — | 1 | 9.64 |
| CHEMBL3217072 | — | — | 1 | 9.59 |
| CHEMBL3215979 | — | — | 1 | 9.55 |
| CHEMBL541805 | — | — | 1 | 9.55 |
| CHEMBL3217085 | — | — | 1 | 9.46 |
| CHEMBL544480 | — | — | 1 | 9.38 |
| CHEMBL543068 | — | — | 1 | 9.37 |
| CHEMBL2028850 | ICATIBANT | 4.0 | 1 | 9.31 |
| CHEMBL544720 | — | — | 1 | 9.00 |
| CHEMBL542096 | — | — | 1 | 8.96 |
| CHEMBL439737 | — | — | 1 | 8.96 |
| CHEMBL3143958 | — | — | 1 | 8.68 |
| CHEMBL44557 | — | — | 1 | 8.66 |
| CHEMBL3143949 | — | — | 1 | 8.49 |
| CHEMBL552986 | — | — | 1 | 8.41 |
| CHEMBL543781 | — | — | 1 | 8.32 |
| CHEMBL554206 | — | — | 1 | 8.28 |
| CHEMBL44087 | — | — | 1 | 8.14 |
| CHEMBL538732 | — | — | 1 | 8.05 |
| CHEMBL542836 | — | — | 1 | 7.66 |
| CHEMBL43746 | — | — | 1 | 7.32 |
| CHEMBL298463 | — | — | 1 | 7.25 |
| CHEMBL288603 | — | — | 1 | 7.17 |
| CHEMBL295428 | — | — | 1 | 7.10 |
| CHEMBL295005 | — | — | 1 | 7.03 |
| CHEMBL240875 | — | — | 1 | 6.80 |
| CHEMBL41446 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3216880 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL543070 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL542598 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL3217081 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL3217072 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL3215979 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL541805 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL3217085 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL544480 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL543068 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL2028850 | ICATIBANT | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL544720 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL542096 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL439737 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3143958 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL44557 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3143949 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL552986 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL543781 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL554206 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL44087 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL538732 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL542836 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL43746 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL298463 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL288603 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL295428 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL295005 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL240875 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL41446 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL288079 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL296865 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL43510 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL290431 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL21311 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL298320 | — | IC50 | = | 9100.0 | nM | 5.04 |