Assay Detail
Functional
CHEMBL970829
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Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension relative to control
29
Total Activities
21
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Cardiac atrium |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 6.18 | 7.16 |
| EC30 | 7 | - | - |
| IC50 | 1 | 5.58 | 5.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441691 | — | — | 1 | 7.16 |
| CHEMBL492270 | — | — | 2 | 6.60 |
| CHEMBL864 | CARBINOXAMINE | 4.0 | 2 | 6.60 |
| CHEMBL301711 | — | — | 1 | 6.52 |
| CHEMBL386435 | — | — | 2 | 6.51 |
| CHEMBL492268 | — | — | 1 | 6.47 |
| CHEMBL492668 | — | — | 1 | 6.46 |
| CHEMBL429298 | — | — | 1 | 6.37 |
| CHEMBL492271 | — | — | 1 | 6.35 |
| CHEMBL492269 | — | — | 2 | 6.28 |
| CHEMBL459734 | — | — | 2 | 6.14 |
| CHEMBL23 | DILTIAZEM | 4.0 | 3 | 6.10 |
| CHEMBL492669 | — | — | 1 | 6.08 |
| CHEMBL523664 | — | — | 1 | 6.08 |
| CHEMBL491663 | — | — | 2 | 6.01 |
| CHEMBL453747 | — | — | 1 | 5.98 |
| CHEMBL506219 | — | — | 1 | 5.96 |
| CHEMBL275742 | DEXPROPRANOLOL | 2.0 | 1 | 5.81 |
| CHEMBL516619 | — | — | 1 | 5.66 |
| CHEMBL447418 | — | — | 1 | 5.45 |
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441691 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL864 | CARBINOXAMINE | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL492270 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL301711 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL386435 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL492268 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL492668 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL429298 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL492271 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL492269 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL459734 | — | EC50 | = | 730.0 | nM | 6.14 |
| CHEMBL23 | DILTIAZEM | EC50 | = | 790.0 | nM | 6.10 |
| CHEMBL492669 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL523664 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL491663 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL453747 | — | EC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL506219 | — | EC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL275742 | DEXPROPRANOLOL | EC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL516619 | — | EC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL447418 | — | EC50 | = | 3590.0 | nM | 5.45 |
| CHEMBL511 | PYRILAMINE | EC50 | = | 6260.0 | nM | 5.20 |
| CHEMBL864 | CARBINOXAMINE | EC30 | = | 0.48 | uM | - |
| CHEMBL23 | DILTIAZEM | EC30 | = | 0.07 | uM | - |
| CHEMBL459734 | — | EC30 | = | 0.48 | uM | - |
| CHEMBL386435 | — | EC30 | = | 0.48 | uM | - |
| CHEMBL492270 | — | EC30 | = | 0.48 | uM | - |
| CHEMBL492269 | — | EC30 | = | 0.48 | uM | - |
| CHEMBL491663 | — | EC30 | = | 0.48 | uM | - |