Assay Detail

CHEMBL5225992

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Binding

Inhibition of human alpha3beta4 nAChR

ChEMBL ↗

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Target

Neuronal acetylcholine receptor subunit alpha-3 (CHEMBL3068) ↗

Open DB target context

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Neuronal acetylcholine receptor subunit alpha-3 (CHEMBL3068) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Neuronal acetylcholine receptor subunit alpha-3

CHEMBL3068

Anchored from Assay target.

Protein identity Neuronal acetylcholine receptor subunit alpha-3

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

Neuronal acetylcholine receptor subunit alpha-3 (CHEMBL3068) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.

Roecker AJ, Schirripa KM, Loughran HM, Tong L, Liang T, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Drolet RE, Cosden M, Jinn S, Hatcher NG, Yao L, Kandebo M, Vardigan JD, Flick RB, Liu X, Minnick C, Price LA, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME.
ACS Med Chem Lett (2023) 14 : 146 -155
PubMed 36793422 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	5.66	5.66

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5272946	—	—	1	5.66
CHEMBL5275403	—	—	1	5.66

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5272946	—	IC50	=	2200.0	nM	5.66
CHEMBL5275403	—	IC50	=	2200.0	nM	5.66