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Assay Detail

CHEMBL3096291

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

Binding
Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A2780 ADR
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Investigation of quinazolines as inhibitors of breast cancer resistance protein (ABCG2).
Juvale K, Gallus J, Wiese M.
Bioorg Med Chem (2013) 21 : 7858 -7873
PubMed 24184213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.19 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160 CYCLOSPORINE 4.0 1 6.04
CHEMBL3092483 1 5.46
CHEMBL2158554 1 5.23
CHEMBL3092485 1 5.02
CHEMBL3092482 1 4.93
CHEMBL2158551 1 4.91
CHEMBL3092490 1 4.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160 CYCLOSPORINE IC50 = 920.0 nM 6.04
CHEMBL3092483 IC50 = 3490.0 nM 5.46
CHEMBL2158554 IC50 = 5850.0 nM 5.23
CHEMBL3092485 IC50 = 9560.0 nM 5.02
CHEMBL3092482 IC50 = 11760.0 nM 4.93
CHEMBL2158551 IC50 = 12380.0 nM 4.91
CHEMBL3092490 IC50 = 18210.0 nM 4.74