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

In Model Organisms: (2 reviews)
Control Compounds

Probe Summary

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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 public 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