Assay Detail
Binding
CHEMBL4181722
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Cav1.2 (unknown origin) expressed in HEK293 cells assessed as decrease in calcium flux preincubated for 3 mins followed by KCl addition by Fluo-4-AM dye-based FLIPR assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-dependent L-type calcium channel subunit alpha-1C (CHEMBL1940) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.61 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4207291 | — | — | 1 | 5.96 |
| CHEMBL4212176 | — | — | 1 | 5.83 |
| CHEMBL4204573 | — | — | 1 | 5.68 |
| CHEMBL4218608 | — | — | 1 | 5.62 |
| CHEMBL4217292 | APINOCALTAMIDE | 2.0 | 1 | 5.62 |
| CHEMBL4211644 | — | — | 1 | 5.55 |
| CHEMBL4208907 | — | — | 1 | 5.48 |
| CHEMBL4205005 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4207291 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4212176 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL4204573 | — | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL4218608 | — | IC50 | = | 2420.0 | nM | 5.62 |
| CHEMBL4217292 | APINOCALTAMIDE | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL4211644 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4208907 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL4205005 | — | IC50 | = | 7100.0 | nM | 5.15 |