Assay Detail
Binding
CHEMBL1821177
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay
31
Total Activities
31
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-1G (CHEMBL4641) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and pharmacological evaluation of 1-alkyl-N-[2-ethyl-2-(4-fluorophenyl)butyl]piperidine-4-carboxamide derivatives as novel antihypertensive agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.55 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1819515 | — | — | 1 | 7.44 |
| CHEMBL1819517 | — | — | 1 | 7.09 |
| CHEMBL1819509 | — | — | 1 | 7.07 |
| CHEMBL1819511 | — | — | 1 | 7.05 |
| CHEMBL1819521 | — | — | 1 | 7.05 |
| CHEMBL1819519 | — | — | 1 | 7.03 |
| CHEMBL1819518 | — | — | 1 | 6.92 |
| CHEMBL1819522 | — | — | 1 | 6.89 |
| CHEMBL1819508 | — | — | 1 | 6.89 |
| CHEMBL1819516 | — | — | 1 | 6.89 |
| CHEMBL1819525 | — | — | 1 | 6.85 |
| CHEMBL1819524 | — | — | 1 | 6.77 |
| CHEMBL1819523 | — | — | 1 | 6.75 |
| CHEMBL1819520 | — | — | 1 | 6.70 |
| CHEMBL45816 | MIBEFRADIL | 4.0 | 1 | 6.70 |
| CHEMBL1819501 | — | — | 1 | 6.66 |
| CHEMBL1819512 | — | — | 1 | 6.62 |
| CHEMBL1819513 | — | — | 1 | 6.60 |
| CHEMBL1819514 | — | — | 1 | 6.58 |
| CHEMBL1819500 | — | — | 1 | 6.50 |
| CHEMBL1819510 | — | — | 1 | 6.43 |
| CHEMBL1819502 | — | — | 1 | 6.41 |
| CHEMBL1819499 | — | — | 1 | 6.29 |
| CHEMBL1819506 | — | — | 1 | 6.12 |
| CHEMBL1819526 | — | — | 1 | 6.11 |
| CHEMBL1819507 | — | — | 1 | 6.07 |
| CHEMBL1819504 | — | — | 1 | 5.92 |
| CHEMBL1819498 | — | — | 1 | 5.92 |
| CHEMBL1819505 | — | — | 1 | 5.70 |
| CHEMBL1819503 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1819515 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1819517 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL1819509 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1819511 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL1819521 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1819519 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL1819518 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1819522 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1819508 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1819516 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1819525 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1819524 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1819523 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1819520 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL45816 | MIBEFRADIL | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1819501 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1819512 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1819513 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1819514 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1819500 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1819510 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL1819502 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1819499 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1819506 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1819526 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1819507 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL1819504 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1819498 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1819505 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1819503 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1819497 | — | IC50 | = | 3000.0 | nM | 5.52 |