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Assay Detail

CHEMBL939121

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

Binding
Inhibition of mouse Pgp in EMT6/AR1.0 cells after 1 hr by daunorubicin accumulation assay
10
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

ATP-dependent translocase ABCB1 (CHEMBL3467)
Type SINGLE PROTEIN
Organism Mus musculus

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 6.82 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL444075 2 7.30
CHEMBL348475 TARIQUIDAR 3.0 2 7.19
CHEMBL258896 2 6.59
CHEMBL346292 2 6.52
CHEMBL428402 2 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL444075 IC50 = 50.0 nM 7.30
CHEMBL444075 IC50 = 50.12 nM 7.30
CHEMBL348475 TARIQUIDAR IC50 = 64.0 nM 7.19
CHEMBL348475 TARIQUIDAR IC50 = 64.57 nM 7.19
CHEMBL258896 IC50 = 257.04 nM 6.59
CHEMBL258896 IC50 = 260.0 nM 6.58
CHEMBL346292 IC50 = 300.0 nM 6.52
CHEMBL346292 IC50 = 302.0 nM 6.52
CHEMBL428402 IC50 = 320.0 nM 6.50
CHEMBL428402 IC50 = 316.23 nM 6.50