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Assay Detail

CHEMBL3866569

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

Binding
Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

ATP-binding cassette sub-family C member 2 (CHEMBL5748)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Indolylmethylenebenzofuranones as first effective inhibitors of ABCC2.
Baiceanu E, Nguyen KA, Gonzalez-Lobato L, Nasr R, Baubichon-Cortay H, Loghin F, Le Borgne M, Chow L, Boumendjel A, Peuchmaur M, Falson P.
Eur J Med Chem (2016) 122 : 408 -418
PubMed 27393949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.00 5.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3974624 1 5.39
CHEMBL3921707 1 5.35
CHEMBL3263914 1 5.35
CHEMBL3263916 1 5.32
CHEMBL3263915 1 5.20
CHEMBL3964042 1 5.14
CHEMBL3945493 1 5.09
CHEMBL3263569 1 5.05
CHEMBL3263906 1 4.98
CHEMBL3263904 1 4.97
CHEMBL3263570 1 4.96
CHEMBL3263913 1 4.94
CHEMBL3263907 1 4.91
CHEMBL3259861 1 4.86
CHEMBL3263910 1 4.84
CHEMBL3948408 1 4.81
CHEMBL3928271 1 4.80
CHEMBL3263909 1 4.76
CHEMBL3914655 1 4.75
CHEMBL160 CYCLOSPORINE 4.0 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3974624 IC50 = 4100.0 nM 5.39
CHEMBL3921707 IC50 = 4500.0 nM 5.35
CHEMBL3263914 IC50 = 4500.0 nM 5.35
CHEMBL3263916 IC50 = 4800.0 nM 5.32
CHEMBL3263915 IC50 = 6300.0 nM 5.20
CHEMBL3964042 IC50 = 7300.0 nM 5.14
CHEMBL3945493 IC50 = 8200.0 nM 5.09
CHEMBL3263569 IC50 = 9000.0 nM 5.05
CHEMBL3263906 IC50 = 10500.0 nM 4.98
CHEMBL3263904 IC50 = 10600.0 nM 4.97
CHEMBL3263570 IC50 = 11100.0 nM 4.96
CHEMBL3263913 IC50 = 11400.0 nM 4.94
CHEMBL3263907 IC50 = 12200.0 nM 4.91
CHEMBL3259861 IC50 = 13900.0 nM 4.86
CHEMBL3263910 IC50 = 14400.0 nM 4.84
CHEMBL3948408 IC50 = 15400.0 nM 4.81
CHEMBL3928271 IC50 = 15800.0 nM 4.80
CHEMBL3263909 IC50 = 17500.0 nM 4.76
CHEMBL3914655 IC50 = 17800.0 nM 4.75
CHEMBL160 CYCLOSPORINE IC50 = 25600.0 nM 4.59