Assay Detail
Binding
CHEMBL2399368
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rabbit voltage-dependent L-type calcium channel Cav1.2alpha-1C expressed in HEK293 cells by FLIPR assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-dependent L-type calcium channel subunit alpha-1C (CHEMBL2830) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Antagonism of L-type Ca2+ channels CaV1.3 and CaV1.2 by 1,4-dihydropyrimidines and 4H-pyrans as dihydropyridine mimics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 5.53 | 6.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1648 | ISRADIPINE | 4.0 | 1 | 6.97 |
| CHEMBL2381007 | — | — | 1 | 6.77 |
| CHEMBL2398415 | — | — | 1 | 6.46 |
| CHEMBL2398408 | — | — | 1 | 6.39 |
| CHEMBL2398396 | — | — | 1 | 6.38 |
| CHEMBL2398418 | — | — | 1 | 6.30 |
| CHEMBL2398404 | — | — | 1 | 6.30 |
| CHEMBL2398425 | — | — | 1 | 6.24 |
| CHEMBL2398421 | — | — | 1 | 6.19 |
| CHEMBL2398409 | — | — | 1 | 6.07 |
| CHEMBL2398401 | — | — | 1 | 5.99 |
| CHEMBL2398406 | — | — | 1 | 5.99 |
| CHEMBL2398399 | — | — | 1 | 5.74 |
| CHEMBL2398422 | — | — | 1 | 5.71 |
| CHEMBL2398402 | — | — | 1 | 5.63 |
| CHEMBL2398400 | — | — | 1 | 5.61 |
| CHEMBL2398419 | — | — | 1 | 5.61 |
| CHEMBL2398414 | — | — | 1 | 5.61 |
| CHEMBL2398407 | — | — | 1 | 5.51 |
| CHEMBL282279 | — | — | 1 | 5.48 |
| CHEMBL2398393 | — | — | 1 | 5.37 |
| CHEMBL2398394 | — | — | 1 | 5.32 |
| CHEMBL2398398 | — | — | 1 | 5.26 |
| CHEMBL2398395 | — | — | 1 | 5.21 |
| CHEMBL2398423 | — | — | 1 | 5.21 |
| CHEMBL2398405 | — | — | 1 | 5.01 |
| CHEMBL2398420 | — | — | 1 | 4.98 |
| CHEMBL2398413 | — | — | 1 | 4.97 |
| CHEMBL2398410 | — | — | 1 | 4.93 |
| CHEMBL2398424 | — | — | 1 | 4.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1648 | ISRADIPINE | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL2381007 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2398415 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2398408 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2398396 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2398418 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2398404 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2398425 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2398421 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2398409 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL2398401 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL2398406 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL2398399 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL2398422 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL2398402 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL2398400 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL2398414 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL2398419 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL2398407 | — | IC50 | = | 3070.0 | nM | 5.51 |
| CHEMBL282279 | — | IC50 | = | 3290.0 | nM | 5.48 |
| CHEMBL2398393 | — | IC50 | = | 4230.0 | nM | 5.37 |
| CHEMBL2398394 | — | IC50 | = | 4750.0 | nM | 5.32 |
| CHEMBL2398398 | — | IC50 | = | 5540.0 | nM | 5.26 |
| CHEMBL2398395 | — | IC50 | = | 6110.0 | nM | 5.21 |
| CHEMBL2398423 | — | IC50 | = | 6130.0 | nM | 5.21 |
| CHEMBL2398405 | — | IC50 | = | 9870.0 | nM | 5.01 |
| CHEMBL2398420 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL2398413 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL2398410 | — | IC50 | = | 11670.0 | nM | 4.93 |
| CHEMBL2398424 | — | IC50 | = | 13920.0 | nM | 4.86 |
| CHEMBL2398416 | — | IC50 | = | 14840.0 | nM | 4.83 |
| CHEMBL2398397 | — | IC50 | = | 16130.0 | nM | 4.79 |
| CHEMBL2398403 | — | IC50 | = | 21740.0 | nM | 4.66 |
| CHEMBL2398412 | — | IC50 | = | 54970.0 | nM | 4.26 |
| CHEMBL2398417 | — | IC50 | = | 56580.0 | nM | 4.25 |
| CHEMBL167975 | — | IC50 | = | 58100.0 | nM | 4.24 |
| CHEMBL2398411 | — | IC50 | > | 100000.0 | nM | - |