BI-2536 0.0042μM R03 exp95

Mechanism of Action

Inhibits PLK1 kinase, causes G2/M arrest

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

Technical Notes

Compound References

  • PubChem Name: BI-2536
  • Synonyms: N/A
  • CAS #: 755038-02-9
  • PubChem CID: 11364421
  • IUPAC: 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
  • INCHI Name: InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1
  • INCHI Key: XQVVPGYIWAGRNI-JOCHJYFZSA-N
  • Molecular Weight: 521.7
  • Canonical SMILES: CCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C
  • Isomeric SMILES: CC[C@@H]1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C
  • Molecular Formula: C28H39N7O3

Compound Supplier

  • Supplier Name: Med Chem Express
  • Catalog #: HY-50698
  • Lot #: N/A

Compound Characterization

  • HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C28H39N7O3 522.31871; found 522.32029

Dose Response Curve

  • Platform ID: BI2536
  • Min: -5.0598; Max: 98.9203





IC Concentration (µM)
IC10 N/A
IC20 0.0014
IC30 0.0041
IC40 0.0097
IC50 0.0214
IC60 N/A
IC70 N/A
IC80 N/A
IC90 N/A


Screen Summary

  • Round: 03
  • Dose: 4.2nM
  • Days of incubation: 8
  • Doublings: 4.4
  • Numbers of reads: 12660576

Screen Results

Sensitive/Resistant hits (FDR<0.05)CRANKSScore PlotTop 30 GenesScreen SimilarityTop 30 Sensitive GO termsTop 30 Resistant GO terms
36/37ScoresViewViewViewViewView

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