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Assay Detail

CHEMBL4015699

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

Binding
Inhibition of ABCC1 in human H69AR 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
3
Total Activities
3
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

Multidrug resistance-associated protein 1 (CHEMBL3004)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Anilino-2-pyridylquinazolines and -pyrimidines as Highly Potent and Nontoxic Inhibitors of Breast Cancer Resistance Protein (ABCG2).
Krapf MK, Gallus J, Wiese M.
J Med Chem (2017) 60 : 4474 -4495
PubMed 28471656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.04 5.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160 CYCLOSPORINE 4.0 1 5.53
CHEMBL1499954 1 4.80
CHEMBL4088963 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160 CYCLOSPORINE IC50 = 2970.0 nM 5.53
CHEMBL1499954 IC50 = 15900.0 nM 4.80
CHEMBL4088963 IC50 = 15900.0 nM 4.80