Assay Detail
Functional
CHEMBL691344
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Inhibitory concentration against IKs current was measured in isolated guinea pig myocytes during a 1 s voltage clamp step from 50 to +50 mV
15
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Novel 5-cyclopropyl-1,4-benzodiazepin-2-ones as potent and selective I(Ks)-blocking class III antiarrhythmic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.96 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277513 | — | — | 2 | 10.10 |
| CHEMBL430293 | — | — | 2 | 9.40 |
| CHEMBL16023 | — | — | 2 | 8.92 |
| CHEMBL428691 | — | — | 1 | 8.82 |
| CHEMBL279168 | — | — | 2 | 8.43 |
| CHEMBL275422 | — | — | 2 | 8.40 |
| CHEMBL277609 | — | — | 1 | 8.22 |
| CHEMBL16900 | L-768673 | — | 1 | 8.22 |
| CHEMBL279169 | — | — | 2 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277513 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL430293 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL16023 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL428691 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL279168 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL275422 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL277609 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL16900 | L-768673 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL279169 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL279168 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL277513 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL16023 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL430293 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL275422 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL279169 | — | IC50 | = | 280.0 | nM | 6.55 |