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Assay Detail

CHEMBL2077067

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Functional
TP_TRANSPORTER: inhibition of DHEAS in membrane vesicles from MRP4-expressing Sf9 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type Sf9
Subcellular Membrane vesicle
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

ATP-binding cassette sub-family C member 4 (CHEMBL1743128)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4).
Zelcer N, Reid G, Wielinga P, Kuil A, van der Heijden I, Schuetz JD, Borst P.
Biochem J (2003) 371 : 361 -367
PubMed 12523936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.60 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1162492 ESTRADIOL DISULFATE 1 6.70
CHEMBL1697724 ESTRADIOL 17B GLUCURONIDE 1 4.52
CHEMBL3349339 1 4.16
CHEMBL2074591 1 4.10
CHEMBL2074982 1 4.10
CHEMBL494753 ESTRONE SULFURIC ACID 4.0 1 4.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1162492 ESTRADIOL DISULFATE IC50 = 200.0 nM 6.70
CHEMBL1697724 ESTRADIOL 17B GLUCURONIDE IC50 = 30000.0 nM 4.52
CHEMBL3349339 IC50 = 70000.0 nM 4.16
CHEMBL2074591 IC50 = 80000.0 nM 4.10
CHEMBL2074982 IC50 = 80000.0 nM 4.10
CHEMBL494753 ESTRONE SULFURIC ACID IC50 = 95000.0 nM 4.02