Chemical Probes logo
Ogerin | Positive allosteric of GPR68
RATINGS:
Cellular Use: (1 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GPR68
    • EC50:150 nM
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    Screened for radioligand binding modulation of CNS GPCRs and toxic pharmacological off-targets. M ...

    Potency
    Cellular
    In Vitro

    GPR68

    Mode of Action: Positive allosteric

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/nature15699

    In Vivo Validations

    Mouse
    Dose: 10 mg/Kg
    Route of delivery: Intraperitoneal
    Organ of interest (O): Brain

    DOI Reference: 10.1038/nature15699

    Negative Control Compounds

    ZINC32547799
    Notes: ZINC32547799: no measurable effect on learning and memory in wild-type mice; Clean GPCR scan with one exception: HTR1A Ki = 849.86 nM

    Chemical Information

    Molecular Formula C17H17N5O
    SMILEs Nc1nc(NCc2ccccc2)nc(-c2ccccc2CO)n1
    InChI InChI=1S/C17H17N5O/c18-16-20-15(14-9-5-4-8-13(14)11-23)21-17(22-16)19-10-12-6-2-1-3-7-12/h1-9,23H,10-11H2,(H3,18,19,20,21,22)
    Molecular weight 307.14 Da
    AlogP 2.2252000000000005
    HBond acceptors 6
    HBond donors 4
    Atoms 40

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the Portal.

    Expert Reviews

    by SERP
    (on 18 Oct 2020)
    Cellular Use Rating
    In Model Organisms
    Ogerin has moderate affinity at two GPCRs, 5-HT2B and the A2A receptor.
    If you would like to explore AI-generated evaluations, you may wish to visit the page for this compound on our collaborator website
    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