Assay Detail
Functional
CHEMBL785237
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Tested in vitro on K+ -depolarized rat aorta strips to evaluate its ability to relax the initial contraction induced by K
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Aorta |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Synthesis and preliminary biological evaluation of 4,6-disubstituted 3-cyanopyridin-2(1H)-ones, a new class of calcium entry blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.14 | 9.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441913 | — | — | 1 | 9.02 |
| CHEMBL293997 | — | — | 1 | 8.96 |
| CHEMBL54555 | — | — | 1 | 7.92 |
| CHEMBL299069 | — | — | 1 | 7.52 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 7.32 |
| CHEMBL418109 | — | — | 1 | 6.42 |
| CHEMBL59577 | — | — | 1 | 6.30 |
| CHEMBL292441 | — | — | 1 | 6.00 |
| CHEMBL54354 | — | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441913 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL293997 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL54555 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL299069 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL418109 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL59577 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL292441 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL54354 | — | IC50 | = | 17000.0 | nM | 4.77 |