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T3-CLK | Inhibitor of CLK1, CLK2, CLK3, CLK4
RATINGS:
Cellular Use: (1 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
CLK1
  • IC50:0.67 nM
  • IC50:3.49 nM
CLK2
  • IC50:15 nM
  • IC50:16.6 nM
CLK3
  • IC50:110 nM
    CLK4
      • IC50:1.98 nM
      Inhibitor
      < 100 nM

      Selectivity

      In Vitro Selectivity Assessment
      Selectivity Assessment Description:
      200 to 300 times selective against dual specificity kinases such as DYRK1A (IC50 = 260 nM) and DYRK1 ...

      Potency
      Cellular
      In Vitro

      CLK1

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1038/s41467-016-0008-7

      CLK2

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1038/s41467-016-0008-7

      CLK3

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1038/s41467-016-0008-7

      CLK4

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1038/s41467-016-0008-7

      Negative Control Compounds

      T3-CLK-N
      Notes: Control clean and not active Closest off-targets in the GPCR scan are TMEM97 (Ki = 411.9 nM), SIGMAR1 (Ki = 798.34 nM), OPRK1 (Ki =990.27 nM) and HTR2C (Ki = 1066.46 nM).

      Orthogonal Probes def

      SGC-CLK-1
      KH-CB19

      Chemical Information

      Molecular Formula C28H30N6O2
      SMILEs CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5ccncc5)ccc4n3)cc2)CC1
      InChI InChI=1S/C28H30N6O2/c1-28(2,27(36)33-16-14-32(3)15-17-33)23-7-4-21(5-8-23)26(35)31-24-19-34-18-22(6-9-25(34)30-24)20-10-12-29-13-11-20/h4-13,18-19H,14-17H2,1-3H3,(H,31,35)
      Molecular weight 482.24 Da
      AlogP 3.7002000000000024
      HBond acceptors 8
      HBond donors 1
      Atoms 66

      Vendors

      Note: This is not an exhaustive list and does not indicate endorsement by the portal.

      Expert Reviews

      by SERP+
      (on 17 Jun 2024 )
      Cellular Use Rating
      T3-CLK is a pan-CLK inhibitor with high in vitro and cellular potency and with a proven on-target engagement and good negative control compound. There is only little activity on off-targets. The compound...
      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria