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TC-G-1008 | TC-G-1008 : Agonist of GPR39
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GPR39
    • EC50:60 nM
    • EC50:20 nM
    • EC50:60 nM
    • EC50:0.8 nM
    Agonist
    up to 100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Tested against a broad panel of enzymes (kinases and proteases), transporters, nuclear hormone recep ...

    Potency
    Cellular
    In Vitro

    GPR39

    Mode of Action: Agonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/ml500240d

    In Vivo Validations

    Mouse
    Dose: 10, 30. 100 mg/Kg
    Route of delivery: Oral
    Plasma half life: 7 h (10 mg/Kg)
    Cmax: 1.4, 6.1, and 25.3 μM
    Tmax: 1-1.5 h

    DOI Reference: 10.1021/ml500240d

    Chemical Information

    Molecular Formula C18H19ClN6O2S
    SMILEs CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1
    InChI InChI=1S/C18H19ClN6O2S/c1-20-18-23-16(15-5-3-4-8-21-15)10-17(24-18)22-11-12-6-7-13(9-14(12)19)25-28(2,26)27/h3-10,25H,11H2,1-2H3,(H2,20,22,23,24)
    Molecular weight 418.10 Da
    AlogP 3.2173000000000016
    HBond acceptors 8
    HBond donors 3
    Atoms 47

    References

    Publications

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    Vendors

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    Expert Reviews

    by SERP
    (on 15 Aug 2023 )
    Cellular Use Rating
    In Model Organisms
    TC-G 1008 is a recommended GPR39 tool compound with a favorable profile, confirmed independently by multiple research groups. S. Peukert et al (Med. Chem. Lett. 2014, 5, 1114−1118) is providing initial...
    by SERP
    (on 31 Aug 2023 )
    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