Assay Detail
Binding
CHEMBL2383744
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Displacement of [3H]-PN200-110 from voltage-gated calcium channel subunit alpha Cav1.2a (unknown origin) expressed in HEK293 cells after 90 mins by liquid scintillation counting analysis
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| Ki | 7 | 7.16 | 8.80 |
| IC50 | 7 | 6.70 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL412260 | — | — | 2 | 8.80 |
| CHEMBL271356 | — | — | 2 | 7.64 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 2 | 7.50 |
| CHEMBL2381470 | — | — | 2 | 6.82 |
| CHEMBL271355 | — | — | 2 | 6.72 |
| CHEMBL2381582 | — | — | 2 | 6.52 |
| CHEMBL2381468 | — | — | 2 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL412260 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL412260 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL271356 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL193 | NIFEDIPINE | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL271356 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL193 | NIFEDIPINE | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL2381470 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL271355 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL2381582 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL2381470 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL271355 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL2381468 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL2381582 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL2381468 | — | IC50 | = | 2150.0 | nM | 5.67 |