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Assay Detail

CHEMBL4714779

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

Binding
Inhibition of recombinant wild type mouse KNa1.1 expressed in human HEK-TREX cells at -80 mV holding potential by automated patch clamp assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type T-REx-293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Potassium channel subfamily T member 1 (CHEMBL4739694)
Type SINGLE PROTEIN
Organism Mus musculus

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 7 5.53 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4741793 1 6.21
CHEMBL4763955 1 5.94
CHEMBL4754084 1 5.90
CHEMBL4788669 1 5.52
CHEMBL4786255 1 4.84
CHEMBL4750925 1 4.77
CHEMBL4793279 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4741793 IC50 = 622.0 nM 6.21
CHEMBL4763955 IC50 = 1143.0 nM 5.94
CHEMBL4754084 IC50 = 1251.0 nM 5.90
CHEMBL4788669 IC50 = 3001.0 nM 5.52
CHEMBL4786255 IC50 = 14500.0 nM 4.84
CHEMBL4750925 IC50 = 17140.0 nM 4.77
CHEMBL4793279 IC50 > 30000.0 nM -