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PNU-120596 | PNU-120596 : Type II Positive allosteric modulator of CHRNA7
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
CHRNA7
    • EC50:216 nM
    • Ratio:7-fold at 1 μM
    Type II Positive allosteric modulator
    1 -5 μM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Whole-cell voltage clamp of cDNA injected Xenopus Oocytes.
    Selectivity Assessment Description:
    No detectable modulation of human α4β2, α3β4, or α9α10 nicotinic acetylcholine receptors, at 50 μM, ...

    Potency
    Cellular
    In Vitro

    CHRNA7

    Mode of Action: Type II Positive allosteric modulator

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1523/JNEUROSCI.5269-04.2005

    In Vivo Validations

    Rat
    Dose: 1 mg/kg
    Route of delivery: Intravenous
    Organ of interest (O): Brain

    DOI Reference: 10.1523/JNEUROSCI.5269-04.2005

    Orthogonal Probes def

    TQS
    Notes: EC50 6.2 μM at 100 μM ACh, whole cell voltage clamp, cDNA injected Xenopus oocytes. DOI: 10.1073/pnas.1017975108
    METHYLLYCACONITINE
    Notes: General nicotinic antagonist - additional treatment with methyllycaconitine recommended as a negative control.

    Chemical Information

    Molecular Formula C13H14ClN3O4
    SMILEs COc1cc(OC)c(NC(=O)Nc2cc(C)on2)cc1Cl
    InChI InChI=1S/C13H14ClN3O4/c1-7-4-12(17-21-7)16-13(18)15-9-5-8(14)10(19-2)6-11(9)20-3/h4-6H,1-3H3,(H2,15,16,17,18)
    Molecular weight 311.07 Da
    AlogP 3.297620000000001
    HBond acceptors 7
    HBond donors 2
    Atoms 35

    Expert Reviews

    by SERP
    (on 11 Mar 2026)
    Cellular Use Rating
    In Model Organisms
    PNU-120596 is a potent positive allosteric modulator (PAM) of the α7 homomeric nicotinic acetylcholine receptor (α7 nAChR) that enhances receptor responses to endogenous agonists without directly activating...
    by SERP
    (on 15 Apr 2026)
    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