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WNK463 | WNK463 : Inhibitor of WNK1, WNK2, WNK3, WNK4
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
WNK1
  • IC50:5 nM
  • Kd:~ 4 nM
  • Kd:3.7 nM
  • Kd:5.3 nM
  • IC50:41 nM
  • IC50:106 nM
WNK2
  • IC50:1 nM
    WNK3
    • IC50:6 nM
      WNK4
      • IC50:9 nM
      • Kd:~ 4 nM
      • Kd:3.8 nM
        Inhibitor
        up to 1 uM

        Selectivity

        In Vitro Selectivity Assessment
        Potency Assay Off-Target:
        At 10 μM, 2,500-fold above the binding KD for human WNK1 (∼4 nM) and WNK4 (∼4 nM), WNK463 showed >50 ...

        Potency
        Cellular
        In Vitro

        WNK1

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1038/nchembio.2168

        WNK2

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1038/nchembio.2168

        WNK3

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1038/nchembio.2168

        WNK4

        Mode of Action: Inhibitor

        Structure-Activity-Relationship data available? No

        DOI Reference: 10.1038/nchembio.2168

        In Vivo Validations

        Mouse
        Dose: 0.5 mg/Kg
        Route of delivery: Intravenous
        Plasma half life: 3.6 h
        Systemic clearance: 3.3 mL/min/Kg
        Volume of Distribution at Steady-State: 0.9 L/Kg

        DOI Reference: 10.1038/nchembio.2168

        Dose: 1.5 mg/Kg
        Route of delivery: Oral
        Cmax: 1856 nM
        Tmax: 2 h
        Area Under the Curve:: 9926 nM*h
        Bioavailability: 108%

        DOI Reference: 10.1038/nchembio.2168

        Rat
        Dose: 0.5 mg/Kg
        Route of delivery: Intravenous
        Plasma half life: 2.1 h
        Systemic clearance: 6.6 mL/min/Kg
        Volume of Distribution at Steady-State: 1.2 L/Kg

        DOI Reference: 10.1038/nchembio.2168

        Dose: 1.5 mg/Kg
        Route of delivery: Oral
        Cmax: 1203 nM
        Tmax: 2.3 h
        Area Under the Curve:: 5418 nM*h
        Bioavailability: 74%

        DOI Reference: 10.1038/nchembio.2168

        Chemical Information

        Molecular Formula C21H24F3N7O2
        SMILEs CC(C)(C)NC(=O)c1cncn1C1CCN(c2ccc(-c3nnc(C(F)(F)F)o3)cn2)CC1
        InChI InChI=1S/C21H24F3N7O2/c1-20(2,3)27-17(32)15-11-25-12-31(15)14-6-8-30(9-7-14)16-5-4-13(10-26-16)18-28-29-19(33-18)21(22,23)24/h4-5,10-12,14H,6-9H2,1-3H3,(H,27,32)
        Molecular weight 463.19 Da
        AlogP 3.716700000000003
        HBond acceptors 9
        HBond donors 1
        Atoms 57

        References

        Publications

        Cross References

        Expert Reviews

        No SERP comments found for WNK463

        Probe WNK463 is in the process of SERP review.

        Please continue to check back for new reviews and commentary.