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COMPOUND 43

Development stage: Preclinical
Modality: Small Molecules

Overview

COMPOUND 43 is a novel small molecule identified through docking-based virtual screening as a selective antagonist of the adenosine A2A receptor (AR). It exhibits substantial activity against the A2A AR with a Ki of 0.42 μM and demonstrates good selectivity over the A1 adenosine receptor. In functional assays, COMPOUND 43 showed antagonistic activity with a cAMP IC50 of 1.67 μM. Preclinical studies in the haloperidol-induced catalepsy (HIC) rat model, a model for Parkinson's disease, indicated good efficacy at doses up to 30 mg/kg, suggesting its potential as a therapeutic agent for Parkinson's disease.

Targets

ADORA2A (Adenosine A₂A Receptor)

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