Assay Detail
Binding
CHEMBL818749
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Inhibition of specific binding of [3H]BK to bradykinin B2 receptors of guinea pig ileum (GPI)
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Novel series of O-substituted 8-quinolines and 4-benzothiazoles as potent antagonists of the bradykinin B2 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.44 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113169 | — | — | 1 | 10.00 |
| CHEMBL113963 | — | — | 1 | 10.00 |
| CHEMBL325255 | — | — | 1 | 9.52 |
| CHEMBL115163 | — | — | 1 | 9.22 |
| CHEMBL112140 | — | — | 1 | 8.89 |
| CHEMBL323693 | — | — | 1 | 8.89 |
| CHEMBL114732 | — | — | 1 | 8.89 |
| CHEMBL114401 | — | — | 1 | 8.74 |
| CHEMBL113465 | — | — | 1 | 8.60 |
| CHEMBL112991 | — | — | 1 | 8.55 |
| CHEMBL324950 | — | — | 1 | 8.54 |
| CHEMBL113222 | — | — | 1 | 8.51 |
| CHEMBL333832 | — | — | 1 | 8.47 |
| CHEMBL324575 | — | — | 1 | 8.41 |
| CHEMBL325601 | — | — | 1 | 8.27 |
| CHEMBL113502 | — | — | 1 | 8.22 |
| CHEMBL114915 | — | — | 1 | 8.20 |
| CHEMBL114180 | — | — | 1 | 8.08 |
| CHEMBL325742 | — | — | 1 | 8.04 |
| CHEMBL112360 | — | — | 1 | 8.04 |
| CHEMBL113176 | — | — | 1 | 7.34 |
| CHEMBL325624 | — | — | 1 | 6.80 |
| CHEMBL113320 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113169 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL113963 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL325255 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL115163 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL112140 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL323693 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL114732 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL114401 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL113465 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL112991 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL324950 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL113222 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL333832 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL324575 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL325601 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL113502 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL114915 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL114180 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL325742 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL112360 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL113176 | — | Ki | = | 45.4 | nM | 7.34 |
| CHEMBL325624 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL113320 | — | Ki | = | 1300.0 | nM | 5.89 |