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Assay Detail

CHEMBL4158631

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

Binding
Inhibition of human Nav1.4 expressed in HEK293 cells at holding potential of -125 mV after 10 mins by patchxpress-based electrophysiology assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 4 subunit alpha (CHEMBL2072)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.
Wu B, Murray JK, Andrews KL, Sham K, Long J, Aral J, Ligutti J, Amagasu S, Liu D, Zou A, Min X, Wang Z, Ilch CP, Kornecook TJ, Lin MJ, Be X, Miranda LP, Moyer BD, Biswas K.
J Med Chem (2018) 61 : 9500 -9512
PubMed 30346167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.07 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170712 1 7.64
CHEMBL4159473 1 7.64
CHEMBL4167379 1 7.43
CHEMBL4160074 1 7.41
CHEMBL4160943 1 7.28
CHEMBL4169884 1 7.28
CHEMBL4174312 1 7.14
CHEMBL4163637 1 7.05
CHEMBL4162835 1 7.04
CHEMBL4167720 1 6.99
CHEMBL4159169 1 6.98
CHEMBL4174592 1 6.93
CHEMBL4164272 1 6.84
CHEMBL4163942 1 6.79
CHEMBL4175995 1 6.75
CHEMBL4167083 1 6.74
CHEMBL4175589 1 6.71
CHEMBL4168880 1 6.59
CHEMBL4171314 1 -
CHEMBL4175832 1 -
CHEMBL4167979 1 -
CHEMBL4172428 1 -
CHEMBL4164545 1 -
CHEMBL4159239 1 -
CHEMBL4160718 1 -
CHEMBL4174769 1 -
CHEMBL4170776 1 -
CHEMBL4171687 1 -
CHEMBL4175203 1 -
CHEMBL4165596 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170712 IC50 = 23.0 nM 7.64
CHEMBL4159473 IC50 = 23.0 nM 7.64
CHEMBL4167379 IC50 = 37.0 nM 7.43
CHEMBL4160074 IC50 = 39.0 nM 7.41
CHEMBL4160943 IC50 = 52.0 nM 7.28
CHEMBL4169884 IC50 = 53.0 nM 7.28
CHEMBL4174312 IC50 = 72.0 nM 7.14
CHEMBL4163637 IC50 = 89.0 nM 7.05
CHEMBL4162835 IC50 = 92.0 nM 7.04
CHEMBL4167720 IC50 = 102.0 nM 6.99
CHEMBL4159169 IC50 = 104.0 nM 6.98
CHEMBL4174592 IC50 = 117.0 nM 6.93
CHEMBL4164272 IC50 = 145.0 nM 6.84
CHEMBL4163942 IC50 = 162.0 nM 6.79
CHEMBL4175995 IC50 = 177.0 nM 6.75
CHEMBL4167083 IC50 = 182.0 nM 6.74
CHEMBL4175589 IC50 = 193.0 nM 6.71
CHEMBL4168880 IC50 = 258.0 nM 6.59
CHEMBL4171314 IC50 - -
CHEMBL4175832 IC50 - -
CHEMBL4167979 IC50 - -
CHEMBL4172428 IC50 - -
CHEMBL4164545 IC50 - -
CHEMBL4159239 IC50 - -
CHEMBL4160718 IC50 - -
CHEMBL4174769 IC50 - -
CHEMBL4170776 IC50 - -
CHEMBL4171687 IC50 - -
CHEMBL4175203 IC50 - -
CHEMBL4165596 IC50 - -
CHEMBL4174202 IC50 - -
CHEMBL4164121 IC50 - -
CHEMBL4165380 IC50 - -