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Compound class:
Peptide or derivative
Comment: RgIA4 is an α-conotoxin RgIA derivative, designed for potential pain therapy. Functionally it is a potent and selective α9α10 nicotinic acetylcholine receptor (nAChR) antagonist [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. ✖ |
| Bioactivity Comments |
| RgIA4 is 1,000- to 10,000-fold selective for the α9α10 nAChR compared with all other tested receptors (including opioid receptors and GABAB receptors) and ion channels, and exhibits no hERG liability [1]. In a rodent chemotherapy-induced model of pain, RgIA4-induced inhibition of α9α10 nAChRs prevented chemotherapy(oxaliplatin)-induced neuropathic pain. |
| Selectivity at ion channels | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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