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Compound class:
Peptide
Comment: C4Pen is a μ-conotoxin KIIIA analogue [1-2]. It is a potent NaV1.4 ion channel blocker.
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. ✖ |
| References |
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1. Khoo KK, Feng ZP, Smith BJ, Zhang MM, Yoshikami D, Olivera BM, Bulaj G, Norton RS. (2009)
Structure of the analgesic mu-conotoxin KIIIA and effects on the structure and function of disulfide deletion. Biochemistry, 48 (6): 1210-9. [PMID:19170536] |
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2. Pan T, Li X, Zhou Y, Wang N, Song X, Zhang Z, Jiang T, Huang Z, Wang W, Wu G et al.. (2026)
Design, Synthesis, and Structure–Activity Relationship Study of μ-Conotoxin KIIIA toward NaV1.4. J Med Chem, Epub ahead of print. DOI: 10.1021/acs.jmedchem.5c03142 |
