Assay Detail

CHEMBL4017801

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Binding

Inhibition of human Nav1.7 expressed in HEK293 cells

ChEMBL ↗

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Target

Sodium channel protein type 9 subunit alpha (CHEMBL4296) ↗

Open DB target context

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Sodium channel protein type 9 subunit alpha (CHEMBL4296) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sodium channel protein type 9 subunit alpha

CHEMBL4296

Anchored from Assay target.

Protein identity Sodium channel protein type 9 subunit alpha

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
Cell Type	HEK293
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Sodium channel protein type 9 subunit alpha (CHEMBL4296) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice.

Roecker AJ, Egbertson M, Jones KLG, Gomez R, Kraus RL, Li Y, Koser AJ, Urban MO, Klein R, Clements M, Panigel J, Daley C, Wang J, Finger EN, Majercak J, Santarelli V, Gregan I, Cato M, Filzen T, Jovanovska A, Wang YH, Wang D, Joyce LA, Sherer EC, Peng X, Wang X, Sun H, Coleman PJ, Houghton AK, Layton ME.
Bioorg Med Chem Lett (2017) 27 : 2087 -2093
PubMed 28389149 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.96	7.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2325014	PF-05089771	2.0	1	7.96

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2325014	PF-05089771	IC50	=	11.0	nM	7.96