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Assay Detail

CHEMBL2076218

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
24
Total Activities
24
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

Target

ATP-dependent translocase ABCB1 (CHEMBL4302)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.
Wang EJ, Casciano CN, Clement RP, Johnson WW.
Biochem Biophys Res Commun (2001) 289 : 580 -585
PubMed 11716514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.08 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL772 RESERPINE 4.0 1 6.30
CHEMBL1292 CLOFAZIMINE 4.0 1 6.22
CHEMBL160 CYCLOSPORINE 4.0 1 5.85
CHEMBL17157 TERFENADINE 4.0 1 5.75
CHEMBL1484 NICARDIPINE 4.0 1 5.50
CHEMBL2074971 N-Norgallopamil 1 5.44
CHEMBL1741 CLARITHROMYCIN 4.0 1 5.42
CHEMBL6966 VERAPAMIL 4.0 1 5.38
CHEMBL723 CARVEDILOL 4.0 1 5.34
CHEMBL157101 KETOCONAZOLE 4.0 1 5.25
CHEMBL83 TAMOXIFEN 4.0 1 5.19
CHEMBL726 FLUPHENAZINE 4.0 1 5.19
CHEMBL422 TRIFLUOPERAZINE 4.0 1 5.14
CHEMBL50588 EMETINE 4.0 1 5.04
CHEMBL159 VINBLASTINE 4.0 1 4.75
CHEMBL1294 QUINIDINE 4.0 1 4.73
CHEMBL170 QUININE 4.0 1 4.65
CHEMBL932 DIPYRIDAMOLE 4.0 1 4.64
CHEMBL1480 FELODIPINE 4.0 1 4.58
CHEMBL428647 PACLITAXEL 4.0 1 4.27
CHEMBL564085 TROLEANDOMYCIN 4.0 1 4.17
CHEMBL52606 COLFORSIN 2.0 1 4.10
CHEMBL103 PROGESTERONE 4.0 1 4.02
CHEMBL1182234 TETRAPHENYLPHOSPHONIUM 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL772 RESERPINE IC50 = 500.0 nM 6.30
CHEMBL1292 CLOFAZIMINE IC50 = 600.0 nM 6.22
CHEMBL160 CYCLOSPORINE IC50 = 1400.0 nM 5.85
CHEMBL17157 TERFENADINE IC50 = 1800.0 nM 5.75
CHEMBL1484 NICARDIPINE IC50 = 3200.0 nM 5.50
CHEMBL2074971 N-Norgallopamil IC50 = 3600.0 nM 5.44
CHEMBL1741 CLARITHROMYCIN IC50 = 3800.0 nM 5.42
CHEMBL6966 VERAPAMIL IC50 = 4200.0 nM 5.38
CHEMBL723 CARVEDILOL IC50 = 4600.0 nM 5.34
CHEMBL157101 KETOCONAZOLE IC50 = 5600.0 nM 5.25
CHEMBL83 TAMOXIFEN IC50 = 6400.0 nM 5.19
CHEMBL726 FLUPHENAZINE IC50 = 6500.0 nM 5.19
CHEMBL422 TRIFLUOPERAZINE IC50 = 7200.0 nM 5.14
CHEMBL50588 EMETINE IC50 = 9200.0 nM 5.04
CHEMBL159 VINBLASTINE IC50 = 17700.0 nM 4.75
CHEMBL1294 QUINIDINE IC50 = 18800.0 nM 4.73
CHEMBL170 QUININE IC50 = 22600.0 nM 4.65
CHEMBL932 DIPYRIDAMOLE IC50 = 22700.0 nM 4.64
CHEMBL1480 FELODIPINE IC50 = 26300.0 nM 4.58
CHEMBL428647 PACLITAXEL IC50 = 54000.0 nM 4.27
CHEMBL564085 TROLEANDOMYCIN IC50 = 68300.0 nM 4.17
CHEMBL52606 COLFORSIN IC50 = 80200.0 nM 4.10
CHEMBL103 PROGESTERONE IC50 = 96200.0 nM 4.02
CHEMBL1182234 TETRAPHENYLPHOSPHONIUM IC50 = 490000.0 nM -