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Assay Detail

CHEMBL4813111

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

Binding
Inhibition of human Nav1.5 by automated voltage clamp electrophysiology
29
Total Activities
26
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

Identification of aryl sulfonamides as novel and potent inhibitors of Na<sub>V</sub>1.5.
Sun S, Jia Q, Zenova AY, Lin S, Hussainkhel A, Mezeyova J, Chang E, Goodchild SJ, Xie Z, Lindgren A, de Boer G, Kwan R, Khakh K, Sojo L, Bichler P, Johnson JP, Empfield JR, Cohen CJ, Dehnhardt CM, Dean R.
Bioorg Med Chem Lett (2021) 45 : 128133 -128133
PubMed 34044121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.93 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4864812 1 7.51
CHEMBL4854735 3 7.41
CHEMBL4849813 2 6.62
CHEMBL4863095 1 6.58
CHEMBL4853170 1 6.34
CHEMBL4860097 1 6.33
CHEMBL4865860 1 6.21
CHEMBL4876448 1 6.17
CHEMBL4859414 1 6.16
CHEMBL4872374 1 6.12
CHEMBL4867480 1 5.96
CHEMBL4867340 1 5.93
CHEMBL4870820 1 5.89
CHEMBL4850129 1 5.81
CHEMBL4850942 1 5.37
CHEMBL4862429 1 5.34
CHEMBL4846327 1 5.33
CHEMBL4863596 1 5.30
CHEMBL4855375 1 5.20
CHEMBL4877705 1 5.15
CHEMBL4867251 1 5.11
CHEMBL4857167 1 4.88
CHEMBL4849208 1 4.60
CHEMBL4862578 1 4.59
CHEMBL4872687 1 -
CHEMBL4865549 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4864812 IC50 = 31.0 nM 7.51
CHEMBL4854735 IC50 = 39.0 nM 7.41
CHEMBL4854735 IC50 = 65.0 nM 7.19
CHEMBL4854735 IC50 = 170.0 nM 6.77
CHEMBL4849813 IC50 = 240.0 nM 6.62
CHEMBL4863095 IC50 = 260.0 nM 6.58
CHEMBL4849813 IC50 = 430.0 nM 6.37
CHEMBL4853170 IC50 = 460.0 nM 6.34
CHEMBL4860097 IC50 = 470.0 nM 6.33
CHEMBL4865860 IC50 = 610.0 nM 6.21
CHEMBL4876448 IC50 = 680.0 nM 6.17
CHEMBL4859414 IC50 = 700.0 nM 6.16
CHEMBL4872374 IC50 = 750.0 nM 6.12
CHEMBL4867480 IC50 = 1100.0 nM 5.96
CHEMBL4867340 IC50 = 1180.0 nM 5.93
CHEMBL4870820 IC50 = 1290.0 nM 5.89
CHEMBL4850129 IC50 = 1550.0 nM 5.81
CHEMBL4850942 IC50 = 4320.0 nM 5.37
CHEMBL4862429 IC50 = 4580.0 nM 5.34
CHEMBL4846327 IC50 = 4650.0 nM 5.33
CHEMBL4863596 IC50 = 5040.0 nM 5.30
CHEMBL4855375 IC50 = 6330.0 nM 5.20
CHEMBL4877705 IC50 = 7140.0 nM 5.15
CHEMBL4867251 IC50 = 7830.0 nM 5.11
CHEMBL4857167 IC50 = 13210.0 nM 4.88
CHEMBL4849208 IC50 = 25050.0 nM 4.60
CHEMBL4862578 IC50 = 25490.0 nM 4.59
CHEMBL4872687 IC50 > 30000.0 nM -
CHEMBL4865549 IC50 > 30000.0 nM -