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VER-246608 | VER-246608 : ATP competitive of inhibitor of PDK1, PDK2, PDK3, PDK4
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PDK1
  • Kd:150 nM
  • IC50:79 nM
  • IC50:35 nM
  • IC50:266 nM
PDK2
  • IC50:84 nM
    PDK3
    • IC50:40 nM
      PDK4
      • IC50:91 nM
        up to 2 uM

        Selectivity

        In Vitro Selectivity Assessment
        Potency Assay Off-Target:
        ScanEDGE screen was performed by DiscoverRx with 10 µM VER-246608 against a panel of 96 kinases enco ...
        Selectivity Assessment Description:
        At 10 μM VER-246608 inhibits 8 out of 96 kinases by more than 65%. Ligand binding to the respective ...

        Potency
        Cellular
        In Vitro

        PDK1

        Mode of Action: ATP competitive

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.18632/oncotarget.2656

        PDK2

        Mode of Action: ATP competitive

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.18632/oncotarget.2656

        PDK3

        Mode of Action: ATP competitive

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.18632/oncotarget.2656

        PDK4

        Mode of Action: ATP competitive

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.18632/oncotarget.2656

        Chemical Information

        Molecular Formula C28H23ClF2N4O4
        SMILEs Cc1cnc(Cl)nc1-c1ccc(N(Cc2ccc(C/N=C(\O)C(F)F)cc2)C(=O)c2ccc(O)cc2O)cc1
        InChI InChI=1S/C28H23ClF2N4O4/c1-16-13-33-28(29)34-24(16)19-6-8-20(9-7-19)35(27(39)22-11-10-21(36)12-23(22)37)15-18-4-2-17(3-5-18)14-32-26(38)25(30)31/h2-13,25,36-37H,14-15H2,1H3,(H,32,38)
        Molecular weight 552.14 Da
        AlogP 6.085220000000006
        HBond acceptors 8
        HBond donors 3
        Atoms 62

        References

        Publications

        Cross References

        canSAR: CANSAR3450497

        Expert Reviews

        No SERP comments found for VER-246608

        Probe VER-246608 is in the process of SERP review.

        Please continue to check back for new reviews and commentary.

        If you would like to explore AI-generated evaluations, you may wish to visit the page for this compound on our collaborator website