Assay Detail
Binding
CHEMBL653278
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In vitro for inhibition of specific binding of [3H]BK (0.06 nM) to bradykinin receptor B2 in guinea pig ileum membrane preparations.
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 1. Construction of the basic framework.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 6.44 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL132620 | — | — | 1 | 8.62 |
| CHEMBL554431 | — | — | 1 | 8.11 |
| CHEMBL336116 | — | — | 1 | 8.05 |
| CHEMBL131517 | — | — | 1 | 8.05 |
| CHEMBL154188 | — | — | 1 | 7.80 |
| CHEMBL558018 | — | — | 1 | 7.80 |
| CHEMBL543700 | — | — | 1 | 7.72 |
| CHEMBL554412 | — | — | 1 | 7.58 |
| CHEMBL156899 | — | — | 1 | 7.38 |
| CHEMBL556176 | — | — | 1 | 7.34 |
| CHEMBL358234 | — | — | 1 | 7.27 |
| CHEMBL155339 | — | — | 1 | 7.14 |
| CHEMBL154625 | — | — | 1 | 6.82 |
| CHEMBL156902 | — | — | 1 | 6.70 |
| CHEMBL154386 | — | — | 1 | 6.64 |
| CHEMBL357530 | — | — | 1 | 6.46 |
| CHEMBL152542 | — | — | 1 | 6.42 |
| CHEMBL154633 | — | — | 1 | 6.39 |
| CHEMBL156847 | — | — | 1 | 6.38 |
| CHEMBL154823 | — | — | 1 | 6.31 |
| CHEMBL154682 | — | — | 1 | 6.30 |
| CHEMBL154465 | — | — | 1 | 6.27 |
| CHEMBL154122 | — | — | 1 | 6.24 |
| CHEMBL545573 | — | — | 1 | 6.24 |
| CHEMBL154130 | — | — | 1 | 6.11 |
| CHEMBL356480 | — | — | 1 | 6.09 |
| CHEMBL350232 | — | — | 1 | 5.92 |
| CHEMBL152650 | — | — | 1 | 5.85 |
| CHEMBL153271 | — | — | 1 | 5.82 |
| CHEMBL539324 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL132620 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL554431 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL131517 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL336116 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL154188 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL558018 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL543700 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL554412 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL156899 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL556176 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL358234 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL155339 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL154625 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL156902 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL154386 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL357530 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL152542 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL154633 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL156847 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL154823 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL154682 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL154465 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL154122 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL545573 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL154130 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL356480 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL350232 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL152650 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL153271 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL539324 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL346718 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL346458 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL346034 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL154558 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL152158 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL156606 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL153890 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL152439 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL345670 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL358232 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL153344 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL154570 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL345704 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL436418 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL152071 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL434667 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL154393 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL154158 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL346803 | — | IC50 | > | 100000.0 | nM | - |