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up to 1 uM
1H NMR (400 MHz, DMSO-d6) δ 9.00 (s, 1H), 8.60 (br d, J = 4.8 Hz, 1H), 8.49 (d, J = 5.0 Hz, 1H), 8.43 (s, 1H), 7.86 (dd, J = 7.6, 7.6 Hz, 1H), 7.63 (d, J = 7.8 Hz, 1H), 7.35–7.43 (m, 2H), 5.61 (s, 2H), 4.04 (s, 3H), 2.53 (s, 3H).
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).