Assay Detail
Functional
CHEMBL2076214
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | NIH-3T3-G185 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.04 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1294 | QUINIDINE | 4.0 | 1 | 6.00 |
| CHEMBL1292 | CLOFAZIMINE | 4.0 | 1 | 5.96 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 5.75 |
| CHEMBL772 | RESERPINE | 4.0 | 1 | 5.68 |
| CHEMBL64391 | ITRACONAZOLE | 4.0 | 1 | 5.62 |
| CHEMBL50588 | EMETINE | 4.0 | 1 | 5.62 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 5.60 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.33 |
| CHEMBL2074971 | N-Norgallopamil | — | 1 | 5.31 |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | 5.25 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 1 | 5.24 |
| CHEMBL723 | CARVEDILOL | 4.0 | 1 | 5.22 |
| CHEMBL422 | TRIFLUOPERAZINE | 4.0 | 1 | 5.20 |
| CHEMBL1741 | CLARITHROMYCIN | 4.0 | 1 | 5.14 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 4.92 |
| CHEMBL159 | VINBLASTINE | 4.0 | 1 | 4.70 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 4.63 |
| CHEMBL932 | DIPYRIDAMOLE | 4.0 | 1 | 4.62 |
| CHEMBL1064 | SIMVASTATIN | 4.0 | 1 | 4.58 |
| CHEMBL1480 | FELODIPINE | 4.0 | 1 | 4.49 |
| CHEMBL503 | LOVASTATIN | 4.0 | 1 | 4.49 |
| CHEMBL428647 | PACLITAXEL | 4.0 | 1 | 4.27 |
| CHEMBL170 | QUININE | 4.0 | 1 | 4.13 |
| CHEMBL564085 | TROLEANDOMYCIN | 4.0 | 1 | 4.11 |
| CHEMBL103 | PROGESTERONE | 4.0 | 1 | 4.05 |
| CHEMBL1182234 | TETRAPHENYLPHOSPHONIUM | — | 1 | - |
| CHEMBL52606 | COLFORSIN | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1294 | QUINIDINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1292 | CLOFAZIMINE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL772 | RESERPINE | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL64391 | ITRACONAZOLE | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL50588 | EMETINE | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL2074971 | N-Norgallopamil | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL1484 | NICARDIPINE | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL726 | FLUPHENAZINE | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL422 | TRIFLUOPERAZINE | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1741 | CLARITHROMYCIN | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL159 | VINBLASTINE | IC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 23400.0 | nM | 4.63 |
| CHEMBL932 | DIPYRIDAMOLE | IC50 | = | 23700.0 | nM | 4.62 |
| CHEMBL1064 | SIMVASTATIN | IC50 | = | 26100.0 | nM | 4.58 |
| CHEMBL1480 | FELODIPINE | IC50 | = | 32300.0 | nM | 4.49 |
| CHEMBL503 | LOVASTATIN | IC50 | = | 32700.0 | nM | 4.49 |
| CHEMBL428647 | PACLITAXEL | IC50 | = | 53900.0 | nM | 4.27 |
| CHEMBL170 | QUININE | IC50 | = | 74400.0 | nM | 4.13 |
| CHEMBL564085 | TROLEANDOMYCIN | IC50 | = | 78200.0 | nM | 4.11 |
| CHEMBL103 | PROGESTERONE | IC50 | = | 88100.0 | nM | 4.05 |
| CHEMBL1182234 | TETRAPHENYLPHOSPHONIUM | IC50 | = | 426600.0 | nM | - |
| CHEMBL52606 | COLFORSIN | IC50 | = | 188200.0 | nM | - |