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Assay Detail

CHEMBL5622376

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

Binding
Inhibition of human Nav1.3 expressed in CHO cells under resting state by automated patch clamp electrophysiology analysis
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
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

New aryl and acylsulfonamides as state-dependent inhibitors of Na<sub>v</sub>1.3 voltage-gated sodium channel.
Zidar N, Tomašič T, Kikelj D, Durcik M, Tytgat J, Peigneur S, Rogers M, Haworth A, Kirby RW.
Eur J Med Chem (2023) 258 : 115530 -115530
PubMed 37329714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 5.18 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL507974 TETRODOTOXIN 3.0 1 8.40
CHEMBL5630885 1 5.16
CHEMBL5624805 1 4.77
CHEMBL5630002 1 4.75
CHEMBL5630861 1 4.62
CHEMBL5630791 1 4.58
CHEMBL5624797 1 4.57
CHEMBL5630705 1 4.57
CHEMBL5629870 1 -
CHEMBL5630235 1 -
CHEMBL2137576 1 -
CHEMBL5630638 1 -
CHEMBL5630810 1 -
CHEMBL5624709 1 -
CHEMBL4943076 1 -
CHEMBL5630255 1 -
CHEMBL5630699 1 -
CHEMBL5630513 1 -
CHEMBL5630319 1 -
CHEMBL5630223 1 -
CHEMBL5624922 1 -
CHEMBL1543696 1 -
CHEMBL5630627 1 -
CHEMBL1426769 1 -
CHEMBL5630398 1 -
CHEMBL5631158 1 -
CHEMBL5630208 1 -
CHEMBL5630560 1 -
CHEMBL5630650 1 -
CHEMBL5629953 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL507974 TETRODOTOXIN IC50 = 4.0 nM 8.40
CHEMBL5630885 IC50 = 6900.0 nM 5.16
CHEMBL5624805 IC50 = 17000.0 nM 4.77
CHEMBL5630002 IC50 = 18000.0 nM 4.75
CHEMBL5630861 IC50 = 24000.0 nM 4.62
CHEMBL5630791 IC50 = 26000.0 nM 4.58
CHEMBL5624797 IC50 = 27000.0 nM 4.57
CHEMBL5630705 IC50 = 27000.0 nM 4.57
CHEMBL5624875 IC50 > 30000.0 nM -
CHEMBL5630235 IC50 > 30000.0 nM -
CHEMBL5625104 IC50 > 30000.0 nM -
CHEMBL5630548 IC50 > 30000.0 nM -
CHEMBL5625110 IC50 > 30000.0 nM -
CHEMBL5624791 IC50 > 30000.0 nM -
CHEMBL5625112 IC50 > 30000.0 nM -
CHEMBL5631122 IC50 > 30000.0 nM -
CHEMBL5624820 IC50 > 30000.0 nM -
CHEMBL5630077 IC50 > 30000.0 nM -
CHEMBL5630754 IC50 > 30000.0 nM -
CHEMBL5630779 IC50 > 30000.0 nM -
CHEMBL5624961 IC50 > 30000.0 nM -
CHEMBL629 AMITRIPTYLINE IC50 - -
CHEMBL5624724 IC50 > 30000.0 nM -
CHEMBL5630825 IC50 > 30000.0 nM -
CHEMBL5631186 IC50 > 30000.0 nM -
CHEMBL5630768 IC50 > 30000.0 nM -
CHEMBL5630639 IC50 > 30000.0 nM -
CHEMBL5629882 IC50 > 30000.0 nM -
CHEMBL5624631 IC50 > 30000.0 nM -
CHEMBL5630223 IC50 > 30000.0 nM -
CHEMBL5629953 IC50 > 30000.0 nM -
CHEMBL5630650 IC50 > 30000.0 nM -
CHEMBL5630560 IC50 > 30000.0 nM -
CHEMBL5630208 IC50 > 30000.0 nM -
CHEMBL5631158 IC50 > 30000.0 nM -
CHEMBL5630398 IC50 > 30000.0 nM -
CHEMBL1426769 IC50 > 30000.0 nM -
CHEMBL5630627 IC50 > 30000.0 nM -
CHEMBL1543696 IC50 > 30000.0 nM -
CHEMBL5624922 IC50 > 30000.0 nM -
CHEMBL5630319 IC50 > 30000.0 nM -
CHEMBL5629870 IC50 > 30000.0 nM -
CHEMBL2137576 IC50 > 30000.0 nM -
CHEMBL5630638 IC50 > 30000.0 nM -
CHEMBL5630810 IC50 > 30000.0 nM -
CHEMBL5624709 IC50 > 30000.0 nM -
CHEMBL4943076 IC50 > 30000.0 nM -
CHEMBL5630255 IC50 > 30000.0 nM -
CHEMBL5630699 IC50 > 30000.0 nM -
CHEMBL5630513 IC50 > 30000.0 nM -