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Assay Detail

CHEMBL2078145

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

Functional
TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.
Kim RB, Leake B, Cvetkovic M, Roden MM, Nadeau J, Walubo A, Wilkinson GR.
J Pharmacol Exp Ther (1999) 291 : 1204 -1209
PubMed 10565843

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.31 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160 CYCLOSPORINE 4.0 1 6.00
CHEMBL1551 URSODIOL 4.0 1 5.44
CHEMBL224867 TAUROCHOLIC ACID 1 5.28
CHEMBL27 PROPRANOLOL 4.0 1 5.26
CHEMBL452861 LEVOPROPRANOLOL 2.0 1 5.21
CHEMBL453904 SULFOBROMOPHTHALEIN SODIUM -1.0 1 5.14
CHEMBL35 FUROSEMIDE 4.0 1 4.82
CHEMBL157101 KETOCONAZOLE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160 CYCLOSPORINE IC50 = 1000.0 nM 6.00
CHEMBL1551 URSODIOL IC50 = 3600.0 nM 5.44
CHEMBL224867 TAUROCHOLIC ACID IC50 = 5300.0 nM 5.28
CHEMBL27 PROPRANOLOL IC50 = 5500.0 nM 5.26
CHEMBL452861 LEVOPROPRANOLOL IC50 = 6100.0 nM 5.21
CHEMBL453904 SULFOBROMOPHTHALEIN SODIUM IC50 = 7300.0 nM 5.14
CHEMBL35 FUROSEMIDE IC50 = 15000.0 nM 4.82
CHEMBL157101 KETOCONAZOLE IC50 = 264000.0 nM -