Assay Detail
Binding
CHEMBL884128
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Inhibition of the specific binding of [3H]BK to human recombinant Bradykinin receptor B2 expressed in CHO cells.
22
Total Activities
22
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 novel class of orally active non-peptide bradykinin B2 receptor antagonists. 4. Discovery of novel frameworks mimicking the active conformation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.25 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553911 | — | — | 1 | 9.59 |
| CHEMBL555976 | — | — | 1 | 9.43 |
| CHEMBL537683 | — | — | 1 | 9.39 |
| CHEMBL553315 | — | — | 1 | 9.39 |
| CHEMBL357075 | — | — | 1 | 9.29 |
| CHEMBL544623 | — | — | 1 | 9.28 |
| CHEMBL542096 | — | — | 1 | 8.96 |
| CHEMBL130517 | FR-173657 | — | 1 | 8.85 |
| CHEMBL555006 | — | — | 1 | 8.82 |
| CHEMBL140383 | — | — | 1 | 8.59 |
| CHEMBL543685 | — | — | 1 | 8.49 |
| CHEMBL544622 | — | — | 1 | 8.41 |
| CHEMBL538784 | — | — | 1 | 8.34 |
| CHEMBL143697 | — | — | 1 | 8.32 |
| CHEMBL130775 | — | — | 1 | 8.24 |
| CHEMBL342016 | — | — | 1 | 7.85 |
| CHEMBL142015 | — | — | 1 | 6.96 |
| CHEMBL342195 | — | — | 1 | 6.82 |
| CHEMBL344021 | — | — | 1 | 6.68 |
| CHEMBL2111974 | — | — | 1 | 6.15 |
| CHEMBL337555 | — | — | 1 | 5.38 |
| CHEMBL139870 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553911 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL555976 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL537683 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL553315 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL357075 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL544623 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL542096 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL130517 | FR-173657 | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL555006 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL140383 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL543685 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL544622 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL538784 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL143697 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL130775 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL342016 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL142015 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL342195 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL344021 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2111974 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL337555 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL139870 | — | IC50 | > | 10000.0 | nM | - |