Assay Detail
ADMET
CHEMBL4411995
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Inhibition of calcium-induced contraction in K+-depolarized guinea pig ileum
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 5.93 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 8.82 |
| CHEMBL4590632 | — | — | 1 | 6.31 |
| CHEMBL4443178 | — | — | 1 | 6.11 |
| CHEMBL514508 | — | — | 1 | 5.93 |
| CHEMBL4574696 | — | — | 1 | 5.90 |
| CHEMBL4577064 | — | — | 1 | 5.60 |
| CHEMBL475745 | — | — | 1 | 5.48 |
| CHEMBL4449273 | — | — | 1 | 5.43 |
| CHEMBL4549511 | — | — | 1 | 4.92 |
| CHEMBL4573134 | — | — | 1 | 4.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193 | NIFEDIPINE | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4590632 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4443178 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL514508 | — | EC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL4574696 | — | EC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4577064 | — | EC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL475745 | — | EC50 | = | 3330.0 | nM | 5.48 |
| CHEMBL4449273 | — | EC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL4549511 | — | EC50 | = | 12060.0 | nM | 4.92 |
| CHEMBL4573134 | — | EC50 | = | 14660.0 | nM | 4.83 |