GSK461364A 0.005μM R03 exp125

Mechanism of Action

Inhibits PLK1

  • Class / Subclass 1: Signal Transduction / Kinase Inhibitor
  • Class / Subclass 2: Cell Cycle / Mitotic Inhibitor

Technical Notes

Compound References

  • PubChem Name: Gsk-461364
  • Synonyms: GSK461364A
  • CAS #: 929095-18-1
  • PubChem CID: 15983966
  • IUPAC: 5-[6-[(4-methylpiperazin-1-yl)methyl]benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
  • INCHI Name: InChI=1S/C27H28F3N5O2S/c1-17(19-5-3-4-6-20(19)27(28,29)30)37-23-14-24(38-25(23)26(31)36)35-16-32-21-8-7-18(13-22(21)35)15-34-11-9-33(2)10-12-34/h3-8,13-14,16-17H,9-12,15H2,1-2H3,(H2,31,36)/t17-/m1/s1
  • INCHI Key: ZHJGWYRLJUCMRT-QGZVFWFLSA-N
  • Molecular Weight: 543.6
  • Canonical SMILES: CC(C1=CC=CC=C1C(F)(F)F)OC2=C(SC(=C2)N3C=NC4=C3C=C(C=C4)CN5CCN(CC5)C)C(=O)N
  • Isomeric SMILES: C[C@H](C1=CC=CC=C1C(F)(F)F)OC2=C(SC(=C2)N3C=NC4=C3C=C(C=C4)CN5CCN(CC5)C)C(=O)N
  • Molecular Formula: C27H28F3N5O2S

Compound Supplier

  • Supplier Name: Med Chem Express
  • Catalog #: HY-50877
  • Lot #: CS-0069-03047

Compound Characterization

  • HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C27H28F3N5O2S 544.19886; found 544.20114

Dose Response Curve

  • Platform ID: GSK461364A
  • Min: 0.3593; Max: 95.3469





IC Concentration (µM)
IC10 N/A
IC20 N/A
IC30 0.0022
IC40 0.0102
IC50 0.0421
IC60 N/A
IC70 N/A
IC80 N/A
IC90 N/A


Screen Summary

  • Round: 03
  • Dose: 5nM
  • Days of incubation: 8
  • Doublings: 6.5
  • Numbers of reads: 13142837

Screen Results

Sensitive/Resistant hits (FDR<0.05)CRANKSScore PlotTop 30 GenesScreen SimilarityTop 30 Sensitive GO termsTop 30 Resistant GO terms
23/0ScoresViewViewViewViewView

  • Last modified: 2026/01/15 21:36
  • by 127.0.0.1