PF470

Negative Allosteric Modulator of GRM5

Structure

Information

  • GRM5
  • Negative Allosteric Modulator
  • up to 1 uM

In Vitro Validations

Uniprot ID: P41594
Target Class: GPCR
Target SubClass: Metabatropic Glutamate Receptor
Potency: Ki
Potency Value: 0.9 nM
Potency Assay: Human mGluR5 Radioligand Binding Assay
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: yes
Target aliases:
Metabotropic glutamate receptor 5, MGLUR5, GPRC1E, ...

DOI Reference: 10.1021/jm401622k

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
Selective vs mGLU1 (IC50 = 30.5 uM), PF470 showed no apparent functional agonism (orthosteric or allosteric) or antagonism activities at any other mGluR up to 50 μM. Outside Target Family: Broader selectivity screening with PF470 revealed no significant activities in kinase panels (<50% inhibition at 10 uM), a proprietary phosphodiesterase (PDE) panel (IC50 > 10 μM), and a broad spectrum BioPrint panel in which the adenosine A2A receptor had the highest affinity (Ki = 6.1 μM).
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SERP ratings and comments


No SERP comments found for PF470