Assay Detail
Binding
CHEMBL4181720
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Cav3.2 (unknown origin) expressed in HEK293 cells assessed as decrease in calcium flux preincubated for 3 mins followed by CaCl2 addition by Fluo-4-AM dye-based FLIPR assay
76
Total Activities
75
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 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 | 76 | 7.41 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4205005 | — | — | 1 | 8.47 |
| CHEMBL4203101 | — | — | 1 | 8.42 |
| CHEMBL4204077 | — | — | 1 | 8.39 |
| CHEMBL4215974 | — | — | 1 | 8.37 |
| CHEMBL4204507 | — | — | 1 | 8.29 |
| CHEMBL4212039 | — | — | 1 | 8.28 |
| CHEMBL4205399 | — | — | 2 | 8.26 |
| CHEMBL4207031 | — | — | 1 | 8.22 |
| CHEMBL4206509 | — | — | 1 | 8.21 |
| CHEMBL4214862 | — | — | 1 | 8.17 |
| CHEMBL4208907 | — | — | 1 | 8.15 |
| CHEMBL4218608 | — | — | 1 | 8.12 |
| CHEMBL4207291 | — | — | 1 | 8.11 |
| CHEMBL4216687 | — | — | 1 | 8.11 |
| CHEMBL4203847 | — | — | 1 | 8.08 |
| CHEMBL4209481 | — | — | 1 | 8.07 |
| CHEMBL4203748 | — | — | 1 | 8.00 |
| CHEMBL4213335 | — | — | 1 | 8.00 |
| CHEMBL4209376 | — | — | 1 | 8.00 |
| CHEMBL4211105 | — | — | 1 | 7.96 |
| CHEMBL4208950 | — | — | 1 | 7.92 |
| CHEMBL4208626 | — | — | 1 | 7.89 |
| CHEMBL4218161 | — | — | 1 | 7.85 |
| CHEMBL4207159 | — | — | 1 | 7.85 |
| CHEMBL4207979 | — | — | 1 | 7.82 |
| CHEMBL4217292 | APINOCALTAMIDE | 2.0 | 1 | 7.75 |
| CHEMBL4204573 | — | — | 1 | 7.75 |
| CHEMBL4204611 | — | — | 1 | 7.70 |
| CHEMBL4209946 | — | — | 1 | 7.68 |
| CHEMBL4205068 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4205005 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4203101 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4204077 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4215974 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4204507 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4212039 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4205399 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4207031 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4206509 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4214862 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4208907 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4218608 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4216687 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4207291 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4203847 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4209481 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4213335 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4203748 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4209376 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4211105 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4208950 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4208626 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4218161 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4205399 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4207159 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4207979 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4204573 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4217292 | APINOCALTAMIDE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4204611 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4209946 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4205068 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4216756 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4218617 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4212176 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4218220 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4205975 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4205754 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4204873 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4206219 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4204295 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4208413 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4217227 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4209751 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4211393 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4216279 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4209075 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4210292 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4210341 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4203931 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4217691 | — | IC50 | = | 90.0 | nM | 7.05 |