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Assay Detail

CHEMBL2076240

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
14
Total Activities
14
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

Target

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

Publication

Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4.
Wang E, Lew K, Barecki M, Casciano CN, Clement RP, Johnson WW.
Chem Res Toxicol (2001) 14 : 1596 -1603
PubMed 11743742 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 8 - -
IC50 6 5.32 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1298 NORVERAPAMIL 1 6.05
CHEMBL223643 VALINOMYCIN 1 5.50
CHEMBL51149 GALLOPAMIL 2.0 1 5.50
CHEMBL76447 NOBILETIN 1 4.94
CHEMBL1393 SPIRONOLACTONE 4.0 1 4.63
CHEMBL193 NIFEDIPINE 4.0 1 -
CHEMBL14130 P-NITROPHENOL 1 -
CHEMBL79 LIDOCAINE 4.0 1 -
CHEMBL139 DICLOFENAC 4.0 1 -
CHEMBL52440 DEXTROMETHORPHAN 4.0 1 -
CHEMBL88 CYCLOPHOSPHAMIDE ANHYDROUS 4.0 1 -
CHEMBL8 CIPROFLOXACIN 4.0 1 -
CHEMBL529 AZITHROMYCIN 4.0 1 -
CHEMBL112 ACETAMINOPHEN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1298 NORVERAPAMIL IC50 = 900.0 nM 6.05
CHEMBL223643 VALINOMYCIN IC50 = 3200.0 nM 5.50
CHEMBL51149 GALLOPAMIL IC50 = 3200.0 nM 5.50
CHEMBL76447 NOBILETIN IC50 = 11500.0 nM 4.94
CHEMBL1393 SPIRONOLACTONE IC50 = 23600.0 nM 4.63
CHEMBL193 NIFEDIPINE IC50 = 113000.0 nM -
CHEMBL14130 P-NITROPHENOL Activity - -
CHEMBL79 LIDOCAINE Activity - -
CHEMBL139 DICLOFENAC Activity - -
CHEMBL52440 DEXTROMETHORPHAN Activity - -
CHEMBL88 CYCLOPHOSPHAMIDE ANHYDROUS Activity - -
CHEMBL8 CIPROFLOXACIN Activity - -
CHEMBL529 AZITHROMYCIN Activity - -
CHEMBL112 ACETAMINOPHEN Activity - -