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Assay Detail

CHEMBL939118

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

Binding
Inhibition of Pgp by daunorubicin accumulation assay
10
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.
Müller H, Pajeva IK, Globisch C, Wiese M.
Bioorg Med Chem (2008) 16 : 2448 -2462
PubMed 18083034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.54 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL348475 TARIQUIDAR 3.0 2 7.42
CHEMBL444075 2 7.06
CHEMBL346292 2 6.60
CHEMBL160 CYCLOSPORINE 4.0 2 6.36
CHEMBL6966 VERAPAMIL 4.0 2 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL348475 TARIQUIDAR IC50 = 38.0 nM 7.42
CHEMBL348475 TARIQUIDAR IC50 = 38.02 nM 7.42
CHEMBL444075 IC50 = 87.0 nM 7.06
CHEMBL444075 IC50 = 87.1 nM 7.06
CHEMBL346292 IC50 = 250.0 nM 6.60
CHEMBL346292 IC50 = 251.19 nM 6.60
CHEMBL160 CYCLOSPORINE IC50 = 440.0 nM 6.36
CHEMBL160 CYCLOSPORINE IC50 = 436.52 nM 6.36
CHEMBL6966 VERAPAMIL IC50 = 5800.0 nM 5.24
CHEMBL6966 VERAPAMIL IC50 = 5754.4 nM 5.24