mambalgin-1   Click here for help

GtoPdb Ligand ID: 10308

Compound class: Peptide or derivative
Comment: Mambalgin-1 is a polypeptide component of the venom from the black mamba (Dendroaspis polylepis polylepis) [2]. Mambalgin-2 has also been identified and this differs from Mambalgin-1 by only one amino acid at residue 4 of the mature peptide (Tyr replaced by Phe in Mambaglin-2) [2]. These Mambalgin peptides have been shown to block acid-sensing ion channels, principally ASIC1a- and ASIC1b-containing channels [1-2].
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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
In mice, central and peripheral administration of Mambalgin-1 produces a potent analgesic effect that is naloxone-resistant and is devoid of the tolerance-producing and respiratory depressing actions of morphine. Mambalgin-1 has no effect on rat ASIC2a, rat ASIC3, rat ASIC1a-ASIC3 and rat ASIC1b-ASIC3 channels, or on human TRPV1, P2RX2 (P2X2), HTR3A (5-HT3A), Nav1.8 (SCN10A), Cav3.2 (CACNA1H) and Kv1.2 (KCNA2) channels [2].
Selectivity at ion channels
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
ASIC1 Hs Channel blocker - ~7.0 – 7.3 pIC50 - 1-2
⤷ pIC50 ~7.3 ASIC1a [2]
pIC50 ~7.0 ASIC1b [1]