Assay Detail
Binding
CHEMBL3855324
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant T-type calcium channel Cav3.2 (unknown origin) expressed in HEK293 cells assessed as inhibition of CaCl2-induced calcium influx preincubated for 3 mins prior CaCl2 addition by Fluo-4-AM dye-based FLIPR assay
38
Total Activities
38
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
Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.80 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1684950 | SUVECALTAMIDE | 2.0 | 1 | 8.09 |
| CHEMBL3894794 | — | — | 1 | 7.80 |
| CHEMBL3962647 | — | — | 1 | 7.68 |
| CHEMBL3981633 | — | — | 1 | 7.60 |
| CHEMBL3928071 | — | — | 1 | 7.48 |
| CHEMBL3892579 | — | — | 1 | 7.48 |
| CHEMBL3964030 | — | — | 1 | 7.40 |
| CHEMBL3966141 | — | — | 1 | 7.34 |
| CHEMBL3966824 | — | — | 1 | 7.26 |
| CHEMBL3969496 | — | — | 1 | 7.22 |
| CHEMBL3901517 | — | — | 1 | 7.17 |
| CHEMBL3947301 | — | — | 1 | 7.16 |
| CHEMBL3934636 | ULIXACALTAMIDE | 1.0 | 1 | 7.14 |
| CHEMBL3893662 | — | — | 1 | 6.96 |
| CHEMBL3946972 | — | — | 1 | 6.92 |
| CHEMBL3898970 | — | — | 1 | 6.85 |
| CHEMBL3960151 | — | — | 1 | 6.70 |
| CHEMBL3930559 | — | — | 1 | 6.62 |
| CHEMBL3897833 | — | — | 1 | 6.55 |
| CHEMBL3942685 | — | — | 1 | 6.50 |
| CHEMBL3920575 | — | — | 1 | 6.50 |
| CHEMBL3910259 | — | — | 1 | 6.48 |
| CHEMBL3941425 | — | — | 1 | 6.46 |
| CHEMBL3923714 | — | — | 1 | 6.42 |
| CHEMBL3969020 | — | — | 1 | 6.41 |
| CHEMBL3919508 | — | — | 1 | 6.39 |
| CHEMBL3973610 | — | — | 1 | 6.39 |
| CHEMBL3937064 | — | — | 1 | 6.38 |
| CHEMBL3932660 | — | — | 1 | 6.38 |
| CHEMBL3902564 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1684950 | SUVECALTAMIDE | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3894794 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3962647 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3981633 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3928071 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3892579 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3964030 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3966141 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3966824 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3969496 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3901517 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3947301 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3934636 | ULIXACALTAMIDE | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3893662 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3946972 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3898970 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3960151 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3930559 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3897833 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL3942685 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL3920575 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3910259 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3941425 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3923714 | — | IC50 | = | 382.0 | nM | 6.42 |
| CHEMBL3969020 | — | IC50 | = | 393.0 | nM | 6.41 |
| CHEMBL3919508 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3973610 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3937064 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3932660 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3902564 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3933724 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL3914689 | — | IC50 | = | 613.0 | nM | 6.21 |
| CHEMBL3893591 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL3911637 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3951427 | — | IC50 | = | 5390.0 | nM | 5.27 |
| CHEMBL3938181 | — | IC50 | > | 5300.0 | nM | - |
| CHEMBL3983284 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3905702 | — | IC50 | > | 10000.0 | nM | - |