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ULIXERTINIB | ULIXERTINIB : Inhibitor of MAPK1, MAPK3
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
MAPK1
  • IC50:140 nM (pRSK)
  • EC50:180 nM
MAPK3
    Inhibitor
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    BVD-523 demonstrated ERK1/2 kinase selectivity based on biochemical counter-screens against 75 kinas ...

    Potency
    Cellular
    In Vitro

    MAPK1

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5b00466

    MAPK3

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5b00466

    In Vivo Validations

    Mouse
    Dose: 1 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 1.16 h
    Systemic clearance: 7.90 mL/min/kg
    Area Under the Curve:: 2109 ng*h/mL
    Volume of Distribution at Steady-State: 0.79 L/kg

    DOI Reference: 10.1016/j.jpba.2016.03.036

    Dose: 10 mg/Kg
    Route of delivery: Oral
    Plasma half life: 2.74 h
    Cmax: 8104 ng/mL
    Tmax: 0.5 h
    Area Under the Curve:: 23425 ng*h/mL
    Bioavailability: 100%

    DOI Reference: 10.1016/j.jpba.2016.03.036

    Orthogonal Probes def

    SCH772984
    ERKi

    Chemical Information

    Molecular Formula C21H22Cl2N4O2
    SMILEs CC(C)Nc1cc(-c2c[nH]c(C(=O)N[C@H](CO)c3cccc(Cl)c3)c2)c(Cl)cn1
    InChI InChI=1S/C21H22Cl2N4O2/c1-12(2)26-20-8-16(17(23)10-25-20)14-7-18(24-9-14)21(29)27-19(11-28)13-4-3-5-15(22)6-13/h3-10,12,19,24,28H,11H2,1-2H3,(H,25,26)(H,27,29)/t19-/m1/s1
    Molecular weight 432.11 Da
    AlogP 4.667200000000003
    HBond acceptors 6
    HBond donors 4
    Atoms 51

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    Expert Reviews

    No SERP comments found for ULIXERTINIB

    Probe ULIXERTINIB is in the process of SERP review.

    Please continue to check back for new reviews and commentary.