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PNU-120596 | PNU-120596 : Type II Positive allosteric modulator of CHRNA7
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
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

    canSAR1809441
    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...
    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