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Emraclidine | Emraclidine : Positive Allosteric of CHRM4
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CHRM4
    • EC50:12.2 nM
    Positive Allosteric
    up to 1 uM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    PF-06852231 was evaluated across the five mAChRs in the PAM mode where it was tested in the presence ...
    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Additionally, PF-06852231 was evaluated against a broad safety screening panel at 10 uM, and demons ...

    Potency
    Cellular
    In Vitro

    CHRM4

    Mode of Action: Positive Allosteric

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.4c00293

    Chemical Information

    Molecular Formula C20H21F3N4O
    SMILEs Cc1cc(C)c2c(n1)CN(C(=O)CC1CN(c3ccnc(C(F)(F)F)c3)C1)C2
    InChI InChI=1S/C20H21F3N4O/c1-12-5-13(2)25-17-11-27(10-16(12)17)19(28)6-14-8-26(9-14)15-3-4-24-18(7-15)20(21,22)23/h3-5,7,14H,6,8-11H2,1-2H3
    Molecular weight 390.17 Da
    AlogP 0.0
    HBond acceptors 5
    HBond donors --
    Atoms 49

    Expert Reviews

    by SERP
    (on 11 Aug 2024 )
    Cellular Use Rating
    Emraclidine (PF-06852231; CVL-231) is a positive allosteric modulator (PAM) that selectively targets the muscarinic acetylcholine receptor M4 subtype. The selectivity against the related M2 subtype is...
    by SERP+
    (on 14 Oct 2025 )
    Cellular Use Rating
    Emraclidine is a potent M4 PAM probe, selective over M2 and other family members. It is more potent than VU0152100, and more selective than LY2119620. No structurally related negative control compound...

    Portal Comments

    A recent publication by Luo et al. (2025; Eur. J. Med. Chem.) reports new pharmacokinetic data in mice, suggesting that this probe may be suitable for in vivo studies.

    (last updated: 21 Oct 2025)

    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