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Assay Detail

CHEMBL5264213

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

Binding
Inhibition of rat Nav1.7 at -60 mV holding potential by PatchXpress automated voltage clamp electrophysiology technique
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 9 subunit alpha (CHEMBL3312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (Na<sub>V</sub>) 1.7 with Potent Analgesic Activity.
Sun S, Jia Q, Zenova AY, Wilson MS, Chowdhury S, Focken T, Li J, Decker S, Grimwood ME, Andrez JC, Hemeon I, Sheng T, Chen CA, White A, Hackos DH, Deng L, Bankar G, Khakh K, Chang E, Kwan R, Lin S, Nelkenbrecher K, Sellers BD, DiPasquale AG, Chang J, Pang J, Sojo L, Lindgren A, Waldbrook M, Xie Z, Young C, Johnson JP, Robinette CL, Cohen CJ, Safina BS, Sutherlin DP, Ortwine DF, Dehnhardt CM.
J Med Chem (2019) 62 : 908 -927
PubMed 30499663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.24 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3662190 1 8.43
CHEMBL3662077 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3662190 IC50 = 3.7 nM 8.43
CHEMBL3662077 IC50 = 9.0 nM 8.05