IMARADENANT | IMARADENANT : Antagonist of ADORA2A
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ADORA2A
    • IC50:0.79 nM @ 0.1 uM Adenosine
    • EC50:53 nM
    • Ki:1.7 nM
    Antagonist
    100 nM up to 1 µM
    100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Selectivity within the target family: In radioligand binding competition assays AZD4635 is selectiv ...

    Potency
    Cellular
    In Vitro

    ADORA2A

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1136/jitc-2019-000417

    In Vivo Validations

    Mouse
    Dose: 50 mg/Kg BID
    Route of delivery: Oral

    DOI Reference: 10.1136/jitc-2019-000417

    Chemical Information

    Molecular Formula C15H11ClFN5
    SMILEs Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(Cl)n1
    InChI InChI=1S/C15H11ClFN5/c1-8-6-10(7-12(16)19-8)14-13(20-15(18)22-21-14)9-2-4-11(17)5-3-9/h2-7H,1H3,(H2,18,20,22)
    Molecular weight 315.07 Da
    AlogP 3.2837200000000006
    HBond acceptors 5
    HBond donors 2
    Atoms 33

    References

    Cross References

    canSARChEMBLBindingDBPDB

    Vendors

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    Expert Reviews


    (on 31 Oct 2022 )
    Cellular Use Rating
    In Model Organisms
    Imaradenant (AZD 4635) appears to be a very good compound to probe the effects of A2A receptor signalling in vitro and in vivo. Publication of preclinical pharmacokinetic data and physical properties such...
    (on 14 Oct 2025 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    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