Assay Detail
Functional
CHEMBL2076045
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | LLC-PK1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.79 | 5.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | 5.34 |
| CHEMBL1085699 | MANIDIPINE 6300 | 3.0 | 1 | 5.33 |
| CHEMBL2218858 | — | — | 1 | 5.30 |
| CHEMBL2103761 | BARNIDIPINE | 2.0 | 1 | 4.90 |
| CHEMBL2074922 | EFONIDIPINE | 2.0 | 1 | 4.89 |
| CHEMBL517427 | NILVADIPINE | 3.0 | 1 | 4.75 |
| CHEMBL1726 | NISOLDIPINE | 4.0 | 1 | 4.36 |
| CHEMBL475534 | NITRENDIPINE | 3.0 | 1 | 4.17 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 4.11 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1484 | NICARDIPINE | IC50 | = | 4540.0 | nM | 5.34 |
| CHEMBL1085699 | MANIDIPINE 6300 | IC50 | = | 4650.0 | nM | 5.33 |
| CHEMBL2218858 | — | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL2103761 | BARNIDIPINE | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL2074922 | EFONIDIPINE | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL517427 | NILVADIPINE | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1726 | NISOLDIPINE | IC50 | = | 44100.0 | nM | 4.36 |
| CHEMBL475534 | NITRENDIPINE | IC50 | = | 68200.0 | nM | 4.17 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 77700.0 | nM | 4.11 |
| CHEMBL193 | NIFEDIPINE | IC50 | = | 472000.0 | nM | - |