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Assay Detail

CHEMBL4714786

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

Binding
Inhibition of recombinant human KNa1.1 F346L mutant expressed in human HEK-TREX cells at -80 mV holding potential by automated patch clamp assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type T-REx-293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of the First Orally Available, Selective K1.1 Inhibitor: In Vitro and In Vivo Activity of an Oxadiazole Series.
Griffin AM,Kahlig KM,Hatch RJ,Hughes ZA,Chapman ML,Antonio B,Marron BE,Wittmann M,Martinez-Botella G
ACS Med Chem Lett (2021) 12 : 593 -602
PubMed 33859800 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.75 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4741793 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4741793 IC50 = 1768.0 nM 5.75