AM-6120   Click here for help

GtoPdb Ligand ID: 10119

Synonyms: AM6120 | peptide 41 [PMID: 30346167]
Immunopharmacology Ligand
Compound class: Peptide or derivative
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
Bioactivity Comments
AM-6120 is >750-fold selective for NaV1.7 compared to NaV1.5, 1.6, and 1.8 in patch clamp electrophysiology experiments using human NaVs stably expressed in HEK293 cells [2]. The native receptor in cultured mouse dorsal root ganglia neurons is inhibited with an IC50 of 5.1 nM using manual whole cell patch clamp. electrophysiology
Selectivity at ion channels
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
Nav1.7 Primary target of this compound Hs Inhibitor Inhibition 9.1 pIC50 - 2
⤷ pIC50 9.1 (IC50 8x10-10 M) [2]
Description: Determined in a PatchXpress electrophysiology experiment using HEK293 cells stably expressing hNaV1.7.
Nav1.7 Mm Inhibitor Inhibition 8.3 pIC50 - 2
⤷ pIC50 8.3 (IC50 5.4x10-9 M) [2]
Description: Determined in a PatchXpress electrophysiology experiment using HEK293 cells stably expressing mNaV1.7.
Nav1.4 Hs Inhibitor Inhibition 7.0 pIC50 - 2
⤷ pIC50 7.0 (IC50 1.04x10-7 M) [2]
Description: Determined in a PatchXpress electrophysiology experiment using HEK293 cells stably expressing hNaV1.4.
Nav1.6 Hs Inhibitor Inhibition 6.2 pIC50 - 2
⤷ pIC50 6.2 (IC50 6.04x10-7 M) [2]
Description: Determined in a PatchXpress electrophysiology experiment using HEK293 cells stably expressing hNaV1.6.
Nav1.8 Hs Inhibitor Inhibition <6.0 pIC50 - 2
⤷ pIC50 <6.0 (IC50 >1x10-6 M) [2]
Description: Determined in a PatchXpress electrophysiology experiment using HEK293 cells stably expressing hNaV1.8.
Nav1.5 Hs Inhibitor Inhibition 5.2 pIC50 - 2
⤷ pIC50 5.2 (IC50 6.64x10-6 M) [2]
Description: Determined in a PatchXpress electrophysiology experiment using HEK293 cells stably expressing hNaV1.5.