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HIT105088172
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HIT105088172
  • HIT ID:HIT105088172
  • Cas No:438481-33-5
  • 常用名:Syntelin
  • IUPAC:2-({5-[({3-amino-8-thia-4,6-diazatricyclo[7.4.0.0^{2,7}]trideca-1(9),2,4,6-tetraen-5-yl}sulfanyl)methyl]-4-phenyl-4H-1,2,4-triazol-3-yl}sulfanyl)acetic acid
    IUPAC:2-({5-[({3-amino-8-thia-4,6-diazatricyclo[7.4.0.0^{2,7}]trideca-1(9),2,4,6-tetraen-5-yl}sulfanyl)methyl]-4-phenyl-4H-1,2,4-triazol-3-yl}sulfanyl)acetic acid
  • InChI key:SPRISILOMIVCIR-UHFFFAOYSA-N
  • 分子式:C21H20N6O2S3
  • 分子量:484.61
  • 氢键供体数 (HBD):2
  • 氢键受体数 (HBA):7
  • LogP:4.11
  • SMILES:Nc1nc(SCc2nnc(SCC(O)=O)n2-c2ccccc2)nc2sc3CCCCc3c12
    SMILES:Nc1nc(SCc2nnc(SCC(O)=O)n2-c2ccccc2)nc2sc3CCCCc3c12
  • Syntelin is a selectively CENP-E inhibitor. Syntelin inhibited CENP-E motility in a dose-dependent manner with an IC50 value of 160 nM. Among an extensive list of mitotic kinesins examined, syntelin was found to be highly selective for CENP-E. Syntelin binds to different sites from those of GSK923295, a recently identified CENP-E ATPase inhibitor, as syntelin inhibits CENP-E mutants resistant to GSK923295 in a manner indistinguishable from that of wild type motor. Syntelin represents a novel class of CENP-E motor inhibitor.
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