Emraclidine

Emraclidine : Positive Allosteric of CHRM4

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe Emraclidine is in the process of SERP review.

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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.

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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 )