Assay Detail

CHEMBL3389575

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ADMET

Inhibition of BSEP (unknown origin) expressed in HEK293 cells using [3H]taurocholic acid substrate

ChEMBL ↗

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Target

Bile salt export pump (CHEMBL6020) ↗

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Bile salt export pump (CHEMBL6020) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Bile salt export pump

CHEMBL6020

Anchored from Assay target.

Protein identity Bile salt export pump

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	ADMET
Organism	Homo sapiens
Cell Type	HEK293
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Bile salt export pump (CHEMBL6020) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.

Fu J, Tjandra M, Becker C, Bednarczyk D, Capparelli M, Elling R, Hanna I, Fujimoto R, Furegati M, Karur S, Kasprzyk T, Knapp M, Leung K, Li X, Lu P, Mergo W, Miault C, Ng S, Parker D, Peng Y, Roggo S, Rivkin A, Simmons RL, Wang M, Wiedmann B, Weiss AH, Xiao L, Xie L, Xu W, Yifru A, Yang S, Zhou B, Sweeney ZK.
J Med Chem (2014) 57 : 8503 -8516
PubMed 25310383 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	6.38	6.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1651956	ALISPORIVIR	3.0	1	6.96
CHEMBL3344501	—	—	1	5.80

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1651956	ALISPORIVIR	IC50	=	110.0	nM	6.96
CHEMBL3344501	—	IC50	=	1600.0	nM	5.80