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Assay Detail

CHEMBL2076525

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Functional
TP_TRANSPORTER: inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates.
Leier I, Jedlitschky G, Buchholz U, Cole SP, Deeley RG, Keppler D.
J Biol Chem (1994) 269 : 27807 -27810
PubMed 7961706 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 4.94 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160 CYCLOSPORINE 4.0 1 5.30
CHEMBL1086218 VALSPODAR 3.0 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160 CYCLOSPORINE Ki = 5000.0 nM 5.30
CHEMBL1086218 VALSPODAR Ki = 27000.0 nM 4.57