Assay Detail

CHEMBL2187816

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Binding

Activation of human PXR

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	Binding
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 benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality.

Liu P, Lanza TJ, Chioda M, Jones C, Chobanian HR, Guo Y, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM, Marsh DJ, Metzger JM, Ramsay K, Wang SP, Strack AM, Miller R, Pang J, Lyons K, Dragovic J, Ning JG, Schafer WA, Welch CJ, Gong X, Gao YD, Hornak V, Ball RG, Tsou N, Reitman ML, Wyvratt MJ, Nargund RP, Lin LS.
ACS Med Chem Lett (2011) 2 : 933 -937
PubMed 24900283 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	1	6.17	6.17

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2164575	—	—	1	6.17

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2164575	—	EC50	=	678.0	nM	6.17