In vitro activity: VU 0364439 is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with EC50 value of 19.8 nM. VU 0364439 possessed less favorable pharmacokinetic properties. The properties of VU 0364439 prevents VU 0364439 itself from being used as an in vivo tool, but VU 0364439 might inform the mGlu4 community with more in vitro tool compounds. The activation of the mGlu4 receptor, either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinson's disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons.

Kinase Assay: VU 0364439 is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with EC50 value of 19.8 nM.

Cell Assay: VU 0364439 exhibited excellent in vitro maximal response and potency relative to another PAM, (–)-PHCCC (a partially selective mGlu4 potentiator, its chemical structure could be found in reference 4). Starting at 30μM, using a 1:3 serial dilutions, VU 0364439 was tested in triplicate. The entire test was performed on one day. Finally, the % (–)-PHCCC value of VU 0364439 was 102.3. The value of % (–)-PHCCC was computed through dividing the maximal response elicited by VU 0364439 by the response of the control PAM, (–)-PHCCC, on the same day. It was also found that the EC50 value of VU 0364439 was 19.8 nM at human mGlu4