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Assay Detail

CHEMBL4011671

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

ADMET
Inhibition of recombinant human BSEP expressed in baculovirus infected sf21 cell plasma membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake in to vesicles after 5 mins by microbeta filtration method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Subcellular Plasma Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bile salt export pump (CHEMBL6020)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
Aleo MD, Luo Y, Swiss R, Bonin PD, Potter DM, Will Y.
Hepatology (2014) 60 : 1015 -1022
PubMed 24799086 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.06 5.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1159650 CLOBETASOL PROPIONATE 4.0 1 5.07
CHEMBL54349 ALPIDEM 4.0 1 5.04
CHEMBL95889 BETAINE 4.0 1 -
CHEMBL372795 STREPTOMYCIN 4.0 1 -
CHEMBL35 FUROSEMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1159650 CLOBETASOL PROPIONATE IC50 = 8500.0 nM 5.07
CHEMBL54349 ALPIDEM IC50 = 9200.0 nM 5.04
CHEMBL95889 BETAINE IC50 > 1000000.0 nM -
CHEMBL372795 STREPTOMYCIN IC50 > 1000000.0 nM -
CHEMBL35 FUROSEMIDE IC50 > 1000000.0 nM -