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Assay Detail

CHEMBL4012366

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

Binding
Inhibition of dog Nav1.7 measured after 3 to 5 mins by patchXpress electrophysiology assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 7.50 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3979498 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3979498 IC50 = 32.0 nM 7.50