Assay Detail
Binding
CHEMBL653280
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to inhibit specific binding of [3H]BK at 0.06 nM to Bradykinin receptor B2 in guinea pig ileum membrane preparations by 50%.
37
Total Activities
37
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. 2. Overcoming the species difference between guinea pig and man.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 8.59 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028850 | ICATIBANT | 4.0 | 1 | 10.05 |
| CHEMBL553844 | — | — | 1 | 9.44 |
| CHEMBL540840 | — | — | 1 | 9.42 |
| CHEMBL539550 | — | — | 1 | 9.36 |
| CHEMBL538732 | — | — | 1 | 9.30 |
| CHEMBL544134 | — | — | 1 | 9.26 |
| CHEMBL540828 | — | — | 1 | 9.23 |
| CHEMBL543899 | — | — | 1 | 9.18 |
| CHEMBL544135 | — | — | 1 | 9.12 |
| CHEMBL543898 | — | — | 1 | 9.11 |
| CHEMBL544132 | — | — | 1 | 9.10 |
| CHEMBL543657 | — | — | 1 | 9.10 |
| CHEMBL555555 | — | — | 1 | 9.05 |
| CHEMBL538531 | — | — | 1 | 8.96 |
| CHEMBL559195 | — | — | 1 | 8.85 |
| CHEMBL130452 | — | — | 1 | 8.85 |
| CHEMBL555556 | — | — | 1 | 8.85 |
| CHEMBL422794 | — | — | 1 | 8.66 |
| CHEMBL542473 | — | — | 1 | 8.64 |
| CHEMBL132620 | — | — | 1 | 8.62 |
| CHEMBL543188 | — | — | 1 | 8.57 |
| CHEMBL130660 | — | — | 1 | 8.57 |
| CHEMBL556816 | — | — | 1 | 8.42 |
| CHEMBL538281 | — | — | 1 | 8.41 |
| CHEMBL545765 | — | — | 1 | 8.38 |
| CHEMBL130196 | — | — | 1 | 8.38 |
| CHEMBL544600 | — | — | 1 | 8.28 |
| CHEMBL338682 | — | — | 1 | 8.25 |
| CHEMBL131517 | — | — | 1 | 8.05 |
| CHEMBL130438 | — | — | 1 | 8.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028850 | ICATIBANT | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL553844 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL540840 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL539550 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL538732 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL544134 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL540828 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL543899 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL544135 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL543898 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL544132 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL543657 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL555555 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL538531 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL555556 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL559195 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL130452 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL422794 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL542473 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL132620 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL543188 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL130660 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL556816 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL538281 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL545765 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL130196 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL544600 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL338682 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL131517 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL336116 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL130438 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL545534 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL542472 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL131404 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL130379 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL336209 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL131380 | — | IC50 | = | 340.0 | nM | 6.47 |