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Synonyms: AM6120 | peptide 41 [PMID: 30346167]
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].
Ligand Activity Visualisation ChartsThese 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. ✖ |
Peptide Sequence  |
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| EXCQKWXWTCDSARACCECLRCKLXCRKEI | |
| Glu-Pra-Cys-Gln-Lys-Trp-Nle-Trp-Thr-Cys-Asp-Ser-Ala-Arg-Ala-Cys-Cys-Glu-Cys-Leu-Arg-Cys-Lys-Leu-Trp-Cys-Arg-Lys-Glu-Ile-NH2 | |
| Chemical Modification | |
| Substitution details: X2= Pra (propargylglycine), X7= Nle (norleucine), X25 (W)= 5-Br-Trp (5-bromotryptophan) | |
