Assay Detail
Functional
CHEMBL754160
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Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.04 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64391 | ITRACONAZOLE | 4.0 | 1 | 7.52 |
| CHEMBL6067487 | IVERMECTIN | 4.0 | 1 | 6.70 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 6.52 |
| CHEMBL584 | NELFINAVIR | 4.0 | 1 | 6.46 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 6.40 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 6.30 |
| CHEMBL1423 | PIMOZIDE | 4.0 | 1 | 6.10 |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | 6.02 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 6.00 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 5.96 |
| CHEMBL104 | CLOTRIMAZOLE | 4.0 | 1 | 5.89 |
| CHEMBL45816 | MIBEFRADIL | 4.0 | 1 | 5.82 |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | 5.82 |
| CHEMBL114 | SAQUINAVIR | 4.0 | 1 | 5.80 |
| CHEMBL91 | MICONAZOLE | 4.0 | 1 | 5.70 |
| CHEMBL159 | VINBLASTINE | 4.0 | 1 | 5.70 |
| CHEMBL1294 | QUINIDINE | 4.0 | 1 | 5.66 |
| CHEMBL532 | ERYTHROMYCIN | 4.0 | 1 | 4.37 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | - |
| CHEMBL1751 | DIGOXIN | 4.0 | 1 | - |
| CHEMBL1790041 | RANITIDINE | 4.0 | 1 | - |
| CHEMBL70 | MORPHINE | 4.0 | 1 | - |
| CHEMBL655 | MIDAZOLAM | 4.0 | 1 | - |
| CHEMBL389621 | HYDROCORTISONE | 4.0 | 1 | - |
| CHEMBL30 | CIMETIDINE | 4.0 | 1 | - |
| CHEMBL31421 | — | — | 1 | - |
| CHEMBL44657 | ETOPOSIDE | 4.0 | 1 | - |
| CHEMBL107 | COLCHICINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64391 | ITRACONAZOLE | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL6067487 | IVERMECTIN | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL584 | NELFINAVIR | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1423 | PIMOZIDE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1484 | NICARDIPINE | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL104 | CLOTRIMAZOLE | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL45816 | MIBEFRADIL | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL163 | RITONAVIR | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL114 | SAQUINAVIR | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL91 | MICONAZOLE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL159 | VINBLASTINE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1294 | QUINIDINE | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL532 | ERYTHROMYCIN | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL384467 | DEXAMETHASONE | IC50 | > | 50000.0 | nM | - |
| CHEMBL1751 | DIGOXIN | IC50 | > | 50000.0 | nM | - |
| CHEMBL1790041 | RANITIDINE | IC50 | > | 50000.0 | nM | - |
| CHEMBL70 | MORPHINE | IC50 | > | 50000.0 | nM | - |
| CHEMBL655 | MIDAZOLAM | IC50 | > | 50000.0 | nM | - |
| CHEMBL389621 | HYDROCORTISONE | IC50 | > | 50000.0 | nM | - |
| CHEMBL30 | CIMETIDINE | IC50 | > | 50000.0 | nM | - |
| CHEMBL31421 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL44657 | ETOPOSIDE | IC50 | > | 50000.0 | nM | - |
| CHEMBL107 | COLCHICINE | IC50 | > | 50000.0 | nM | - |