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Assay Detail

CHEMBL4158634

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

Binding
Inhibition of human Nav1.8 expressed in HEK293 cells after 10 mins by patchxpress-based electrophysiology
3
Total Activities
3
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 10 subunit alpha (CHEMBL5451)
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 3 6.29 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4169884 1 6.29
CHEMBL4164272 1 -
CHEMBL4159169 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4169884 IC50 = 509.0 nM 6.29
CHEMBL4164272 IC50 > 1000.0 nM -
CHEMBL4159169 IC50 > 1000.0 nM -