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Structure and pharmacological profile of HTS hit 7 (VU0480131). A) Structure and pharmacology of 7 as an HTS stock solution (hM5 IC50 = 9.3 μM) and as resynthesized, fresh powder (hM5 IC50 = 1.12 μM). B) Concentration-response curves (CRCs) of 7 for human and rat M5, as well as human M1-M4 (IC50s >30 μM, n=3). C) [3H]NMS competition binding [n = 3] in membranes prepped from human M5 cells, showing competitive displacement (Ki = 1.3 μM).
