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Assay Detail

CHEMBL3240733

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

Binding
Inhibition of human ABCG2 ATPase activity transfected in Sf9 insect cells using quercetin as substrate after 30 mins by colorimetry relative to control
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Symmetric bis-chalcones as a new type of breast cancer resistance protein inhibitors with a mechanism different from that of chromones.
Winter E, Devantier Neuenfeldt P, Chiaradia-Delatorre LD, Gauthier C, Yunes RA, Nunes RJ, Creczynski-Pasa TB, Di Pietro A.
J Med Chem (2014) 57 : 2930 -2941
PubMed 24611893 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.65 6.72
Imax 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3238330 1 6.72
CHEMBL3238340 2 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3238330 IC50 = 190.0 nM 6.72
CHEMBL3238340 IC50 = 270.0 nM 6.57
CHEMBL3238340 Imax = 72.0 % -