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TP-024 | Agonist of GPR52
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
GPR52
    • IC50:93 nM in human; 141 nM in Mouse; 134 nM in Rat
    Agonist
    1 uM

    Selectivity

    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    No significant activity at 10 μM.

    Potency
    Cellular
    In Vitro

    GPR52

    Mode of Action: Agonist

    Structure-Activity-Relationship data available? No

    In Vivo Validations

    Rat, Mouse, Human
    Dose: 10 to 30 mg/Kg in Rat
    Route of delivery: Oral

    Reference: --

    Negative Control Compounds

    TP-024n

    Chemical Information

    Molecular Formula C19H16F4N4O
    SMILEs Cc1cc(-n2nc(Cc3cc(F)cc(C(F)(F)F)c3)nc2C)ccc1C(N)=O
    InChI InChI=1S/C19H16F4N4O/c1-10-5-15(3-4-16(10)18(24)28)27-11(2)25-17(26-27)8-12-6-13(19(21,22)23)9-14(20)7-12/h3-7,9H,8H2,1-2H3,(H2,24,28)
    Molecular weight 392.13 Da
    AlogP 3.731740000000002
    HBond acceptors 5
    HBond donors 2
    Atoms 44

    References

    Publications

      Cross References

      SGC additional analysis

      Vendors

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      Expert Reviews

      by SERP
      (on 7 Apr 2025 )
      Cellular Use Rating
      In Model Organisms
      TP-024 (also called FTBMT) is a well-characterized potent GPR52 agonist (orphan receptor). It show good selectivity in several selectivity panels (including receptors, ion channels & enzymes). TP-024 has...
      by SERP+
      (on 14 Oct 2025 )
      Cellular Use Rating
      In Model Organisms
      GPR52 agonists PW0787 and HTL0041178 both have comparable potency, selectivity and more in vivo PK characterisation.
      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