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Assay Detail

CHEMBL1687517

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

Binding
Inhibition of MRP1 expressed in human 2008 cells assessed as calcein AM accumulation by cell based assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type 2008
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP).
Pick A, Müller H, Mayer R, Haenisch B, Pajeva IK, Weigt M, Bönisch H, Müller CE, Wiese M.
Bioorg Med Chem (2011) 19 : 2090 -2102
PubMed 21354800 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.50 4.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6 INDOMETHACIN 4.0 1 4.90
CHEMBL74898 AYANIN 1 4.30
CHEMBL77966 RETUSIN 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6 INDOMETHACIN IC50 = 12600.0 nM 4.90
CHEMBL74898 AYANIN IC50 = 50000.0 nM 4.30
CHEMBL77966 RETUSIN IC50 = 50000.0 nM 4.30