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Assay Detail

CHEMBL5152411

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

Binding
Inhibition of human NTCP mediated TCA uptake in U2OS expresseing HA-tagged NTCP cells preincubated for 10 mins followed by substrate addition and measured after 2 mins using [3H]-taurocholate as substrate by liquid scintillation counter analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hepatic sodium/bile acid cotransporter (CHEMBL5287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
Chen S, Zhang L, Chen Y, Fu L.
J Med Chem (2022) 65 : 12546 -12561
PubMed 36111355 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.13 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603 ZAFIRLUKAST 4.0 1 5.19
CHEMBL41632 TIRATRICOL 3.0 1 5.16
CHEMBL311909 CHICAGO SKY BLUE 1 5.15
CHEMBL421 SULFASALAZINE 4.0 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603 ZAFIRLUKAST IC50 = 6500.0 nM 5.19
CHEMBL41632 TIRATRICOL IC50 = 6900.0 nM 5.16
CHEMBL311909 CHICAGO SKY BLUE IC50 = 7100.0 nM 5.15
CHEMBL421 SULFASALAZINE IC50 = 9600.0 nM 5.02