Assay Detail

CHEMBL4012362

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding

Inhibition of human Nav1.6 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay

ChEMBL ↗

Free Research Context This assay will appear in recent viewed items on this browser. Open the demo workspace to preview project-only review queues.

Research home Demo workspace

Target

Sodium channel protein type 8 subunit alpha (CHEMBL5202) ↗

Open DB target context

Use one target anchor to keep assay intent, target linkage, and tested compound review aligned.

Loading context

Sodium channel protein type 8 subunit alpha (CHEMBL5202) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sodium channel protein type 8 subunit alpha

CHEMBL5202

Anchored from Assay target.

Protein identity Sodium channel protein type 8 subunit alpha

Disease frame Disease evidence pending

Open the live target snapshot or evidence card before reviewing assay metadata so target fit and disease framing stay reusable.

Review focus Open DB context pending

Open the live target snapshot before relying on this target frame across surface handoff.

Open target snapshot Open evidence card Search with this context

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 8 subunit alpha (CHEMBL5202) ↗

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	6.19	6.19

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3979498	—	—	1	6.19

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3979498	—	IC50	=	650.0	nM	6.19