Assay Detail
Binding
CHEMBL3611366
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay
21
Total Activities
19
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 T-type calcium channel subunit alpha-1H (CHEMBL1859) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.64 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3608943 | — | — | 1 | 7.12 |
| CHEMBL3609819 | — | — | 1 | 7.08 |
| CHEMBL3608942 | — | — | 1 | 6.97 |
| CHEMBL3608316 | — | — | 1 | 6.95 |
| CHEMBL3608941 | — | — | 1 | 6.88 |
| CHEMBL3609822 | — | — | 1 | 6.83 |
| CHEMBL45816 | MIBEFRADIL | 4.0 | 1 | 6.74 |
| CHEMBL3609818 | — | — | 1 | 6.74 |
| CHEMBL3609824 | — | — | 1 | 6.71 |
| CHEMBL3608946 | — | — | 1 | 6.68 |
| CHEMBL3609823 | — | — | 1 | 6.68 |
| CHEMBL3608947 | — | — | 2 | 6.66 |
| CHEMBL3609820 | — | — | 1 | 6.65 |
| CHEMBL3608940 | — | — | 1 | 6.50 |
| CHEMBL3608945 | — | — | 2 | 6.46 |
| CHEMBL3608944 | — | — | 1 | 6.44 |
| CHEMBL3609817 | — | — | 1 | 6.40 |
| CHEMBL3609825 | — | — | 1 | 6.25 |
| CHEMBL3609821 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3608943 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3609819 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3608942 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3608316 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL3608941 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3609822 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL45816 | MIBEFRADIL | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL3609818 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL3609824 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL3608946 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3609823 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL3608947 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL3609820 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL3608947 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL3608940 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL3608945 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3608944 | — | IC50 | = | 361.0 | nM | 6.44 |
| CHEMBL3609817 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL3608945 | — | IC50 | = | 432.0 | nM | 6.37 |
| CHEMBL3609825 | — | IC50 | = | 557.0 | nM | 6.25 |
| CHEMBL3609821 | — | IC50 | = | 2065.0 | nM | 5.68 |