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Assay Detail

CHEMBL4132972

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

Binding
Inhibition of human GFP-fused ABCG2 expressed in MDCK2 cells assessed as potentiation of mitoxantrone-induced cell growth inhibition after 72 hrs by MTT assay
2
Total Activities
2
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

Publication

Synthesis and biological investigation of 2,4-substituted quinazolines as highly potent inhibitors of breast cancer resistance protein (ABCG2).
Krapf MK, Gallus J, Wiese M.
Eur J Med Chem (2017) 139 : 587 -611
PubMed 28841513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.07 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092486 1 8.13
CHEMBL4160529 1 8.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092486 EC50 = 7.4 nM 8.13
CHEMBL4160529 EC50 = 9.7 nM 8.01