Table of Contents

GSK343 3μM R03 exp124

Mechanism of Action

Inhibits EZH1 catalytic subunit of PRC2 histone methyltransferase (H3K27me3)

Technical Notes

Protein References

  • PubChem Name: N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide
  • Synonyms: N/A
  • CAS #: 1346704-33-3
  • PubChem CID: 71268957
  • IUPAC: N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide
  • INCHI Name: InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)
  • INCHI Key: ULNXAWLQFZMIHX-UHFFFAOYSA-N
  • Molecular Weight: 541.7
  • Canonical SMILES: CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C
  • Isomeric SMILES: N/A
  • Molecular Formula: C31H39N7O2

Protein Supplier

  • Supplier Name: Structural Genomics Consortium
  • Catalog #: N/A
  • Lot #: N/A

Protein Characterization

  • HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C31H39N7O2 542.3238; found 542.3251

Dose Response Curve

  • Platform ID: GSK343
  • Min: -1.8961; Max: 98.3550





IC Concentration (µM)
IC10 N/A
IC20 1.9378
IC30 2.9381
IC40 4.1327
IC50 5.6521
IC60 N/A
IC70 N/A
IC80 N/A
IC90 N/A


Screen Summary

Screen Results

Sensitive/Resistant hits (FDR<0.05)CRANKSScore PlotTop 30 GenesScreen SimilarityTop 30 Sensitive GO termsTop 30 Resistant GO terms
4/0ScoresViewViewViewViewView