Assay Detail
Functional
CHEMBL2383752
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Relaxant activity in potassium depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.27 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 8.82 |
| CHEMBL2381470 | — | — | 1 | 8.64 |
| CHEMBL2381582 | — | — | 1 | 7.34 |
| CHEMBL2381468 | — | — | 1 | 6.96 |
| CHEMBL2381472 | — | — | 1 | 6.75 |
| CHEMBL2381466 | — | — | 1 | 6.02 |
| CHEMBL2381469 | — | — | 1 | 5.86 |
| CHEMBL2381462 | — | — | 1 | 5.59 |
| CHEMBL2381463 | — | — | 1 | 5.55 |
| CHEMBL2381473 | — | — | 1 | 5.49 |
| CHEMBL2381471 | — | — | 1 | 5.45 |
| CHEMBL2381464 | — | — | 1 | 5.45 |
| CHEMBL2381467 | — | — | 1 | 5.01 |
| CHEMBL2381465 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2381470 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2381582 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL2381468 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2381472 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2381466 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL2381469 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL2381462 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL2381463 | — | IC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL2381473 | — | IC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL2381471 | — | IC50 | = | 3520.0 | nM | 5.45 |
| CHEMBL2381464 | — | IC50 | = | 3550.0 | nM | 5.45 |
| CHEMBL2381467 | — | IC50 | = | 9690.0 | nM | 5.01 |
| CHEMBL2381465 | — | IC50 | = | 15960.0 | nM | 4.80 |