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Assay Detail

CHEMBL4257703

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Binding
Inhibition of human NaV1.5
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 5 subunit alpha (CHEMBL1980)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of a potent Na<sub>v</sub>1.3 inhibitor with good oral pharmacokinetics.
Pryde DC, Swain NA, Stupple PA, West CW, Marron B, Markworth CJ, Printzenhoff D, Lin Z, Cox PJ, Suzuki R, McMurray S, Waldron GJ, Payne CE, Warmus JS, Chapman ML.
Medchemcomm (2017) 8 : 1255 -1267
PubMed 30108836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.05 5.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4293085 1 5.31
CHEMBL3617053 1 5.04
CHEMBL4276884 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4293085 IC50 = 4870.0 nM 5.31
CHEMBL3617053 IC50 = 9200.0 nM 5.04
CHEMBL4276884 IC50 = 15800.0 nM 4.80