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JNJ-6204 | JNJ-6204 : Inhibitor of CSNK1D, CSNK1E
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CSNK1D
  • Kd:2.3 nM
  • IC50:72 nM
  • IC50:542 nM
CSNK1E
  • Kd:137 nM
    up to 10µM
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Closely related kinases: CSNK1A1 (IC50 = 419 nM) Panel of 370 kinases at 1 μM: clean; Closest hit: T ...

    Potency
    Cellular
    In Vitro

    CSNK1D

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acsmedchemlett.3c00523

    CSNK1E

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acsmedchemlett.3c00523

    In Vivo Validations

    Mouse
    Dose: 1 mg/Kg IV, 5 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Systemic clearance: 33 mL/min/Kg
    Cmax: 1250 ng/mL
    Area Under the Curve:: 113 h*ng/mL
    Bioavailability: 43%

    DOI Reference: 10.1021/acsmedchemlett.3c00523

    Negative Control Compounds

    CANSAR3893768
    Notes: JNJ-0293: Purified Enzyme, ADP-GLO: IC50 = 6.9 μM; BRET whole cell binding assay: IC50 > 10 μM

    Chemical Information

    Molecular Formula C19H17FN6O
    SMILEs CC1(C)Cn2nc(-c3ccc(F)cn3)c(-c3ccnc4[nH]ncc34)c2CO1
    InChI InChI=1S/C19H17FN6O/c1-19(2)10-26-15(9-27-19)16(12-5-6-21-18-13(12)8-23-24-18)17(25-26)14-4-3-11(20)7-22-14/h3-8H,9-10H2,1-2H3,(H,21,23,24)
    Molecular weight 364.14 Da
    AlogP 3.3313000000000015
    HBond acceptors 7
    HBond donors 1
    Atoms 44

    Expert Reviews

    by SERP
    (on 30 May 2023)
    Cellular Use Rating
    In Model Organisms
    Selective CK1 delta inhibitor with a 542 nM IC50 for PER2 functional activity in cells. Good bioavailability in mice, but the dosing regimen should be carefully designed to achieve desired coverage over...
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