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Assay Detail

CHEMBL3590774

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

Binding
Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 3 subunit alpha (CHEMBL5163)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.
Bagal SK, Bungay PJ, Denton SM, Gibson KR, Glossop MS, Hay TL, Kemp MI, Lane CA, Lewis ML, Maw GN, Million WA, Payne CE, Poinsard C, Rawson DJ, Stammen BL, Stevens EB, Thompson LR.
ACS Med Chem Lett (2015) 6 : 650 -654
PubMed 26101568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.06 5.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3589893 1 5.46
CHEMBL3589892 1 5.16
CHEMBL3589894 1 4.85
CHEMBL741 LAMOTRIGINE 4.0 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3589893 IC50 = 3500.0 nM 5.46
CHEMBL3589892 IC50 = 6900.0 nM 5.16
CHEMBL3589894 IC50 = 14000.0 nM 4.85
CHEMBL741 LAMOTRIGINE IC50 = 17000.0 nM 4.77