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GD433 | GD433 : peptide substrate-competitive, Inhibitor of NTMT1, NTMT2
RATINGS:
Cellular Use: (1 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
NTMT1
  • Kd:8.28 ± 2.58 nM
  • Kd:36.9 ± 8.18 nM
  • IC50:27 nM
  • IC50:<30 nM
NTMT2
  • INH:~ 90 %
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Inhibitory activity of GD433 was assessed against five different in-house methyltransferases (G9a, P ...
    Selectivity Assessment Description:
    At 10 and 30 μM, GD433 displayed no significant inhibition against these six enzymes. Even at 100 μM ...
    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    GD433 was evaluated for its inhibition against a panel of 40 SAM-dependent methyltransferases at a s ...
    Selectivity Assessment Description:
    GD433 potently inhibited NTMT1 and its close homologue NTMT2, which shares the same X-P-K/R recognit ...

    Potency
    Cellular
    In Vitro

    NTMT1

    Mode of Action: peptide substrate-competitive

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.2c01854

    NTMT2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.2c01854

    In Vivo Validations

    Mouse
    Dose: 25 mg/kg
    Route of delivery: Oral
    Plasma half life: 2.63 h
    Cmax: 81.9 ng/mL
    Tmax: 0.25 h
    Area Under the Curve:: 157 h*ng/mL

    DOI Reference: 10.1021/acs.jmedchem.2c01854

    Negative Control Compounds

    YD2160
    Notes: The inactive analogue YD2160 (cpd 26) did not induce any change in either me3-RCC1 or me3-SET up to 30 μM.

    Chemical Information

    Molecular Formula C20H24FN3O3S
    SMILEs CC(C)(NC(=O)O[C@@H]1CN2CCC1CC2)c1csc(-c2ccc(F)c(O)c2)n1
    InChI InChI=1S/C20H24FN3O3S/c1-20(2,23-19(26)27-16-10-24-7-5-12(16)6-8-24)17-11-28-18(22-17)13-3-4-14(21)15(25)9-13/h3-4,9,11-12,16,25H,5-8,10H2,1-2H3,(H,23,26)/t16-/m1/s1
    Molecular weight 405.15 Da
    AlogP 3.710300000000003
    HBond acceptors 6
    HBond donors 2
    Atoms 52

    References

    Publications

    Cross References

    ChEMBL BindingDB PDB PubChem canSAR

    Expert Reviews

    by SERP
    (on 26 Jun 2026)
    Cellular Use Rating
    In Model Organisms
    While a concentration of up to 1 uM is the right recommendation but it is worth saying that GD433 inhibits GCS at 300 nM.
    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