CDK11-In-37 | CDK11-In-37 : Inhibitor of CDK11A, CDK11B
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Control Compounds
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK11A
    • IC50:4 nM
    • GI50:400 nM
    • GI50:3700 nM
    CDK11B
      • IC50:4 nM
      up to 1 uM

      Selectivity

      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      KinomeSCAN
      Selectivity Assessment Description:
      Highly selective CDK11 inhibitor against other kinases in an extended kinase panel profiling (>100 k ...
      In Cell Selectivity Assessment
      Potency Assay Off-Target:
      NanoBRET
      Selectivity Assessment Description:
      Selective against CDK7 (50x) and CDK9 (IC50 >10 uM)

      Potency
      Cellular
      In Vitro

      CDK11A

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1002/cmdc.202500882

      CDK11B

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1002/cmdc.202500882

      In Vivo Validations

      Mouse
      Dose: 15 mg/Kg
      Route of delivery: Oral
      Plasma half life: 1.09 h
      Cmax: 489 ng/mL
      Tmax: 0.5 h
      Area Under the Curve:: 833 h*ng/mL

      DOI Reference: 10.1002/cmdc.202500882

      Chemical Information

      Molecular Formula C19H21ClFN5
      SMILEs Cl.F[C@@H]1CNC[C@@H](Nc2nccc(-c3ccn(-c4ccccc4)c3)n2)C1
      InChI InChI=1S/C19H20FN5.ClH/c20-15-10-16(12-21-11-15)23-19-22-8-6-18(24-19)14-7-9-25(13-14)17-4-2-1-3-5-17;/h1-9,13,15-16,21H,10-12H2,(H,22,23,24);1H/t15-,16-;/m0./s1
      Molecular weight 373.15 Da
      AlogP 3.4680000000000017
      HBond acceptors 5
      HBond donors 2
      Atoms 47

      References

      Cross References

      canSAR: 7719208 canSAR: 10

      Expert Reviews


      No SERP comments found for CDK11-In-37

      Probe CDK11-In-37 is in the process of SERP review.

      Please continue to check back for new reviews and commentary.

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