Emraclidine

Emraclidine : Positive Allosteric of CHRM4

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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.

Probe Emraclidine is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

CHRM4

Positive Allosteric

up to 1 uM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): PF-06852231 was evaluated across the five mAChRs in the PAM mode where it was tested in the presence of an EC20 of acetylcholine

Potency assay (off target): Additionally, PF-06852231 was evaluated against a broad safety screening panel at 10 uM, and demonstrated minimal response (<25%) at any of these targets.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

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 good (more than 100-fold in HEK293 cells). Activity against human and rat M4 orthologs seems to align, despite some structural differences in the receptors.

(last updated: 11 Aug 2024 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

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 is available.

(last updated: 14 Oct 2025 )

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)