AM-6120   Click here for help

GtoPdb Ligand ID: 10119

Synonyms: AM6120 | peptide 41 [PMID: 30346167]
Immunopharmacology Ligand
Compound class: Peptide
Comment: AM-6120 is a peptidic voltage-gated sodium channel blocker with the sequence Glu-[Pra1;Nle6;Ala12;5-BrW24;Glu28]JzTx-V(1-29), where JzTx-V is a sodium channel inhibitor isolated from tarantula venom [2]. JzTx-V inhibits NaV1.7 activity by interacting with the second voltage sensor domain of the NaV1.7 pore forming α-subunit and thereby holding the ion channel in a closed conformation, but its action is non-selective [1].
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
References
1. Moyer BD, Murray JK, Ligutti J, Andrews K, Favreau P, Jordan JB, Lee JH, Liu D, Long J, Sham K et al.. (2018)
Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V.
PLoS ONE, 13 (5): e0196791. DOI: 10.1371/journal.pone.0196791 [PMID:29723257]
2. Wu B, Murray JK, Andrews KL, Sham K, Long J, Aral J, Ligutti J, Amagasu S, Liu D, Zou A et al.. (2018)
Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.
J Med Chem, 61 (21): 9500-9512. [PMID:30346167]