HTL-0041178

HTL-0041178 : Agonist of GPR52

Structure

SERP Rating

Probe HTL-0041178 is in the process of SERP review.

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Information

GPR52

Agonist

up to 5 uM

In Vitro Validations

Uniprot ID: Q9Y2T5

Target Class: GPCR

Target SubClass: --

Potency Assay: Recombinant functional cAMP assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

G-protein coupled receptor 52, GPR52, GPR52_HUMAN

DOI Reference: 10.1021/acsmedchemlett.3c00052

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): HTL0041178 shows low cardiovascular toxicity risk (hERG and hNaV1.5 IC50 > 10 μM), no significant off-target activity in the Eurofins Safety 47 panel (IC50 > 3 μM against all targets), no significant inhibition of any major cytochrome P450 isoform (all IC50 > 25 μM), no reactive metabolite formation in a glutathione trapping assay, and no detectable genotoxicity in Ames and in vitro micronucleus tests.

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SERP ratings and comments

No SERP comments found for HTL-0041178