Assay Detail
Binding
CHEMBL653418
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition specific binding of [3H]BK (1.0 nM) to human Bradykinin receptor B2 which was expressed in CHO (Chinese hamster ovary) cells by 50%.
55
Total Activities
55
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. 3. Discovering bioisosteres of the imidazo[1,2-a] pyridine moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 55 | 7.57 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028850 | ICATIBANT | 4.0 | 1 | 9.31 |
| CHEMBL130436 | — | — | 1 | 9.29 |
| CHEMBL542096 | — | — | 1 | 8.96 |
| CHEMBL130517 | FR-173657 | — | 1 | 8.85 |
| CHEMBL539294 | — | — | 1 | 8.74 |
| CHEMBL544599 | — | — | 1 | 8.72 |
| CHEMBL543899 | — | — | 1 | 8.66 |
| CHEMBL44557 | — | — | 1 | 8.66 |
| CHEMBL555465 | — | — | 1 | 8.60 |
| CHEMBL543659 | — | — | 1 | 8.60 |
| CHEMBL555202 | — | — | 1 | 8.55 |
| CHEMBL553293 | — | — | 1 | 8.49 |
| CHEMBL552986 | — | — | 1 | 8.41 |
| CHEMBL264751 | — | — | 1 | 8.38 |
| CHEMBL542232 | — | — | 1 | 8.34 |
| CHEMBL543781 | — | — | 1 | 8.32 |
| CHEMBL553614 | — | — | 1 | 8.28 |
| CHEMBL554206 | — | — | 1 | 8.28 |
| CHEMBL44087 | — | — | 1 | 8.14 |
| CHEMBL540819 | — | — | 1 | 8.12 |
| CHEMBL553843 | — | — | 1 | 8.07 |
| CHEMBL132860 | — | — | 1 | 8.07 |
| CHEMBL538732 | — | — | 1 | 8.05 |
| CHEMBL552543 | — | — | 1 | 8.03 |
| CHEMBL133005 | — | — | 1 | 7.96 |
| CHEMBL132510 | — | — | 1 | 7.85 |
| CHEMBL133913 | — | — | 1 | 7.77 |
| CHEMBL542836 | — | — | 1 | 7.66 |
| CHEMBL130782 | — | — | 1 | 7.58 |
| CHEMBL336574 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028850 | ICATIBANT | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL130436 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL542096 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL130517 | FR-173657 | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL539294 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL544599 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL543899 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL44557 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL555465 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL543659 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL555202 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL553293 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL552986 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL264751 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL542232 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL543781 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL553614 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL554206 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL44087 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL540819 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL553843 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL132860 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL538732 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL552543 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL133005 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL132510 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL133913 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL542836 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL130782 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL336574 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL542479 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL335946 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL133339 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL43746 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL298463 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL541590 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL288603 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL295428 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL295005 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL424268 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL334753 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL240875 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL41446 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL544601 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL542958 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL334421 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL288079 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL296865 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL43510 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL133186 | — | IC50 | = | 2000.0 | nM | 5.70 |