Assay Detail
Functional
CHEMBL1121085
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rabbit Cav1.2 expressed in HEK293 cells assessed as inhibition of voltage pulse-induced calcium current by FLIPR calcium 4 assay
69
Total Activities
69
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels Ca V 1.3 and Ca V 1.2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 69 | 7.24 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1098840 | — | — | 1 | 8.22 |
| CHEMBL1098864 | — | — | 1 | 8.15 |
| CHEMBL1096841 | — | — | 1 | 8.10 |
| CHEMBL1086836 | — | — | 1 | 8.10 |
| CHEMBL1098210 | — | — | 1 | 8.10 |
| CHEMBL1099222 | — | — | 1 | 8.10 |
| CHEMBL1098856 | — | — | 1 | 8.05 |
| CHEMBL1098871 | — | — | 1 | 8.05 |
| CHEMBL1096501 | — | — | 1 | 8.00 |
| CHEMBL1097880 | — | — | 1 | 8.00 |
| CHEMBL1095558 | — | — | 1 | 8.00 |
| CHEMBL1095231 | — | — | 1 | 8.00 |
| CHEMBL1094740 | — | — | 1 | 8.00 |
| CHEMBL1094406 | — | — | 1 | 8.00 |
| CHEMBL1098802 | — | — | 1 | 7.89 |
| CHEMBL1096378 | — | — | 1 | 7.85 |
| CHEMBL1099188 | — | — | 1 | 7.82 |
| CHEMBL1098209 | — | — | 1 | 7.82 |
| CHEMBL1097857 | — | — | 1 | 7.80 |
| CHEMBL1098474 | — | — | 1 | 7.80 |
| CHEMBL1098841 | — | — | 1 | 7.77 |
| CHEMBL1096376 | — | — | 1 | 7.75 |
| CHEMBL1096843 | — | — | 1 | 7.72 |
| CHEMBL1094989 | — | — | 1 | 7.70 |
| CHEMBL1098803 | — | — | 1 | 7.70 |
| CHEMBL1094352 | — | — | 1 | 7.70 |
| CHEMBL1098064 | — | — | 1 | 7.66 |
| CHEMBL1097157 | — | — | 1 | 7.66 |
| CHEMBL1094560 | — | — | 1 | 7.64 |
| CHEMBL1096518 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1098840 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1098864 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1086836 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1098210 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1099222 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1096841 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1098856 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1098871 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1094406 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1094740 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1095231 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1095558 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1097880 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1096501 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1098802 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1096378 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1099188 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1098209 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1097857 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1098474 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1098841 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1096376 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1096843 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1094352 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1094989 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1098803 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1098064 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1097157 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1094560 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1096518 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1095559 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1097657 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1098473 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1097858 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1098001 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1098804 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1096842 | PRANIDIPINE | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1097285 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1094405 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1095663 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1099071 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1098796 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1097464 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1095532 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL1094892 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL1097472 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1096160 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL1099070 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL1094404 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL1095557 | — | IC50 | = | 130.0 | nM | 6.89 |