Assay Detail

CHEMBL4012363

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Binding

Inhibition of human Nav1.7 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay

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

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.

Graceffa RF, Boezio AA, Able J, Altmann S, Berry LM, Boezio C, Butler JR, Chu-Moyer M, Cooke M, DiMauro EF, Dineen TA, Feric Bojic E, Foti RS, Fremeau RT, Guzman-Perez A, Gao H, Gunaydin H, Huang H, Huang L, Ilch C, Jarosh M, Kornecook T, Kreiman CR, La DS, Ligutti J, Milgram BC, Lin MJ, Marx IE, Nguyen HN, Peterson EA, Rescourio G, Roberts J, Schenkel L, Shimanovich R, Sparling BA, Stellwagen J, Taborn K, Vaida KR, Wang J, Yeoman J, Yu V, Zhu D, Moyer BD, Weiss MM.
J Med Chem (2017) 60 : 5990 -6017
PubMed 28324649 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	8.22	8.22

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3979498	—	—	1	8.22

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3979498	—	IC50	=	6.0	nM	8.22