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Assay Detail

CHEMBL975398

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Binding
Inhibition of human MRP1 in human 2008 cells
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 2008
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins.
Leyers S, Häcker HG, Wiendlocha J, Gütschow M, Wiese M.
Bioorg Med Chem Lett (2008) 18 : 4761 -4763
PubMed 18707884 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.16 5.92
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510556 1 5.92
CHEMBL160 CYCLOSPORINE 4.0 1 5.32
CHEMBL89768 1 5.12
CHEMBL6966 VERAPAMIL 4.0 1 5.01
CHEMBL6 INDOMETHACIN 4.0 1 4.92
CHEMBL452312 1 4.69
CHEMBL452241 1 -
CHEMBL452313 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510556 IC50 = 1210.0 nM 5.92
CHEMBL160 CYCLOSPORINE IC50 = 4780.0 nM 5.32
CHEMBL89768 IC50 = 7570.0 nM 5.12
CHEMBL6966 VERAPAMIL IC50 = 9660.0 nM 5.01
CHEMBL6 INDOMETHACIN IC50 = 12000.0 nM 4.92
CHEMBL452312 IC50 = 20400.0 nM 4.69
CHEMBL452241 Activity - -
CHEMBL452313 Activity - -