Assay Detail
Functional
CHEMBL2076213
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells
27
Total Activities
27
Compounds Tested
2
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 | 24 | 4.84 | 6.00 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1292 | CLOFAZIMINE | 4.0 | 1 | 6.00 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 5.77 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 5.57 |
| CHEMBL772 | RESERPINE | 4.0 | 1 | 5.41 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.19 |
| CHEMBL723 | CARVEDILOL | 4.0 | 1 | 5.18 |
| CHEMBL2074971 | N-Norgallopamil | — | 1 | 5.07 |
| CHEMBL50588 | EMETINE | 4.0 | 1 | 5.02 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 1 | 4.98 |
| CHEMBL422 | TRIFLUOPERAZINE | 4.0 | 1 | 4.96 |
| CHEMBL1741 | CLARITHROMYCIN | 4.0 | 1 | 4.82 |
| CHEMBL159 | VINBLASTINE | 4.0 | 1 | 4.53 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 4.50 |
| CHEMBL1294 | QUINIDINE | 4.0 | 1 | 4.47 |
| CHEMBL932 | DIPYRIDAMOLE | 4.0 | 1 | 4.46 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 4.27 |
| CHEMBL1064 | SIMVASTATIN | 4.0 | 1 | 4.25 |
| CHEMBL428647 | PACLITAXEL | 4.0 | 1 | 4.15 |
| CHEMBL170 | QUININE | 4.0 | 1 | 4.06 |
| CHEMBL564085 | TROLEANDOMYCIN | 4.0 | 1 | 4.06 |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | - |
| CHEMBL1480 | FELODIPINE | 4.0 | 1 | - |
| CHEMBL52606 | COLFORSIN | 2.0 | 1 | - |
| CHEMBL64391 | ITRACONAZOLE | 4.0 | 1 | - |
| CHEMBL1182234 | TETRAPHENYLPHOSPHONIUM | — | 1 | - |
| CHEMBL103 | PROGESTERONE | 4.0 | 1 | - |
| CHEMBL503 | LOVASTATIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1292 | CLOFAZIMINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL772 | RESERPINE | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL2074971 | N-Norgallopamil | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL50588 | EMETINE | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL726 | FLUPHENAZINE | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL422 | TRIFLUOPERAZINE | IC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL1741 | CLARITHROMYCIN | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL159 | VINBLASTINE | IC50 | = | 29500.0 | nM | 4.53 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 31400.0 | nM | 4.50 |
| CHEMBL1294 | QUINIDINE | IC50 | = | 33900.0 | nM | 4.47 |
| CHEMBL932 | DIPYRIDAMOLE | IC50 | = | 34300.0 | nM | 4.46 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 53400.0 | nM | 4.27 |
| CHEMBL1064 | SIMVASTATIN | IC50 | = | 56800.0 | nM | 4.25 |
| CHEMBL428647 | PACLITAXEL | IC50 | = | 70200.0 | nM | 4.15 |
| CHEMBL170 | QUININE | IC50 | = | 87600.0 | nM | 4.06 |
| CHEMBL564085 | TROLEANDOMYCIN | IC50 | = | 86300.0 | nM | 4.06 |
| CHEMBL1484 | NICARDIPINE | IC50 | > | 25800.0 | nM | - |
| CHEMBL1480 | FELODIPINE | IC50 | > | 60000.0 | nM | - |
| CHEMBL52606 | COLFORSIN | Activity | - | — | - | |
| CHEMBL64391 | ITRACONAZOLE | Activity | - | — | - | |
| CHEMBL1182234 | TETRAPHENYLPHOSPHONIUM | Activity | - | — | - | |
| CHEMBL103 | PROGESTERONE | IC50 | = | 192200.0 | nM | - |
| CHEMBL503 | LOVASTATIN | IC50 | = | 114400.0 | nM | - |