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Assay Detail

CHEMBL4196465

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

Binding
Inhibition of ABCB1 in human A2780adr cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure activity relationships, multidrug resistance reversal and selectivity of heteroarylphenyl ABCG2 inhibitors.
Köhler SC, Vahdati S, Scholz MS, Wiese M.
Eur J Med Chem (2018) 146 : 483 -500
PubMed 29407974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.98 5.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4210844 1 5.23
CHEMBL4202709 1 5.07
CHEMBL4209777 1 4.96
CHEMBL4202725 1 4.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4210844 IC50 = 5910.0 nM 5.23
CHEMBL4202709 IC50 = 8550.0 nM 5.07
CHEMBL4209777 IC50 = 11000.0 nM 4.96
CHEMBL4202725 IC50 = 21200.0 nM 4.67