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Assay Detail

CHEMBL2077556

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

Functional
TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicles from MRP2-expressing LLC PK1 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type LLC-PK1
Subcellular Membrane vesicle
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Effect of multidrug resistance-reversing agents on transporting activity of human canalicular multispecific organic anion transporter.
Chen ZS, Kawabe T, Ono M, Aoki S, Sumizawa T, Furukawa T, Uchiumi T, Wada M, Kuwano M, Akiyama SI.
Mol Pharmacol (1999) 56 : 1219 -1228
PubMed 10570049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.05 5.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2074650 1 5.43
CHEMBL160 CYCLOSPORINE 4.0 1 5.33
CHEMBL15177 MK-571 1 4.88
CHEMBL1086218 VALSPODAR 3.0 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2074650 Ki = 3700.0 nM 5.43
CHEMBL160 CYCLOSPORINE Ki = 4700.0 nM 5.33
CHEMBL15177 MK-571 Ki = 13100.0 nM 4.88
CHEMBL1086218 VALSPODAR Ki = 28900.0 nM 4.54