Assay Detail

CHEMBL4015597

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ADMET

Transactivation of PXR (unknown origin)

ChEMBL ↗

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Target

Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401) ↗

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Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Nuclear receptor subfamily 1 group I member 2

CHEMBL3401

Anchored from Assay target.

Protein identity Nuclear receptor subfamily 1 group I member 2

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
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.

Yeung KS, Beno BR, Parcella K, Bender JA, Grant-Young KA, Nickel A, Gunaga P, Anjanappa P, Bora RO, Selvakumar K, Rigat K, Wang YK, Liu M, Lemm J, Mosure K, Sheriff S, Wan C, Witmer M, Kish K, Hanumegowda U, Zhuo X, Shu YZ, Parker D, Haskell R, Ng A, Gao Q, Colston E, Raybon J, Grasela DM, Santone K, Gao M, Meanwell NA, Sinz M, Soars MG, Knipe JO, Roberts SB, Kadow JF.
J Med Chem (2017) 60 : 4369 -4385
PubMed 28430437 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	3	5.80	5.80

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4078188	—	—	1	5.80
CHEMBL4093031	BMS-929075	1.0	1	-
CHEMBL4104000	—	—	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4078188	—	EC50	=	1600.0	nM	5.80
CHEMBL4093031	BMS-929075	EC50	>	50000.0	nM	-
CHEMBL4104000	—	EC50	>	50000.0	nM	-