C21   Click here for help

GtoPdb Ligand ID: 7037

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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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]