C21   Click here for help

GtoPdb Ligand ID: 7037

Compound class: Peptide
Comment: C21 is a synthetic analogue of a histone H4 tail peptide sequence bearing a chloroacetamidine side group. This compound was developed as a protein arginine methyltransferase (PRMT) inhibitor. Full information describing the design and synthesis of C21 is available in Obianyo et al (2011) [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
C21 is an irreversible PRMT1 inhibitor, with lower affinity (IC50) for PRMT6 than for PRMT1 (8800nM vs.1800nM respectively) [1].
Selectivity at enzymes
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
protein arginine methyltransferase 1 Hs Inhibitor Inhibition 5.7 pIC50 - 1
⤷ pIC50 5.7 (IC50 1.8x10-6 M) [1]
protein arginine methyltransferase 6 Hs Inhibitor Inhibition 5.1 pIC50 - 1
⤷ pIC50 5.1 (IC50 8.8x10-6 M) [1]