Assay Detail
Binding
CHEMBL653420
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Concentration required to inhibit specific binding of [3H]BK at 1.2 nM to A-431 cells (human epidermoid carcinoma) which express Bradykinin receptor B2 by 50%.
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | A-431 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 2. Overcoming the species difference between guinea pig and man.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.09 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543899 | — | — | 1 | 8.85 |
| CHEMBL538732 | — | — | 1 | 8.82 |
| CHEMBL544134 | — | — | 1 | 8.80 |
| CHEMBL540840 | — | — | 1 | 8.62 |
| CHEMBL555555 | — | — | 1 | 8.59 |
| CHEMBL2028850 | ICATIBANT | 4.0 | 1 | 8.48 |
| CHEMBL539550 | — | — | 1 | 8.43 |
| CHEMBL540828 | — | — | 1 | 8.39 |
| CHEMBL538281 | — | — | 1 | 8.32 |
| CHEMBL553844 | — | — | 1 | 8.04 |
| CHEMBL538531 | — | — | 1 | 7.80 |
| CHEMBL543657 | — | — | 1 | 7.70 |
| CHEMBL544135 | — | — | 1 | 7.70 |
| CHEMBL544132 | — | — | 1 | 7.21 |
| CHEMBL130660 | — | — | 1 | 7.12 |
| CHEMBL543898 | — | — | 1 | 6.92 |
| CHEMBL543188 | — | — | 1 | 6.85 |
| CHEMBL559195 | — | — | 1 | 6.82 |
| CHEMBL422794 | — | — | 1 | 6.82 |
| CHEMBL336209 | — | — | 1 | 6.82 |
| CHEMBL545765 | — | — | 1 | 6.75 |
| CHEMBL555556 | — | — | 1 | 6.72 |
| CHEMBL542473 | — | — | 1 | 6.70 |
| CHEMBL338682 | — | — | 1 | 6.62 |
| CHEMBL542472 | — | — | 1 | 6.58 |
| CHEMBL130452 | — | — | 1 | 6.46 |
| CHEMBL130438 | — | — | 1 | 6.32 |
| CHEMBL130196 | — | — | 1 | 6.29 |
| CHEMBL131380 | — | — | 1 | 6.29 |
| CHEMBL545534 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543899 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL538732 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL544134 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL540840 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL555555 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2028850 | ICATIBANT | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL539550 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL540828 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL538281 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL553844 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL538531 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL543657 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL544135 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL544132 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL130660 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL543898 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL543188 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL336209 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL559195 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL422794 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL545765 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL555556 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL542473 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL338682 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL542472 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL130452 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL130438 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL131380 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL130196 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL545534 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL131517 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL544600 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL132620 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL556816 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL336116 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL558018 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL130379 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL131404 | — | IC50 | > | 1000.0 | nM | - |