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. 2019 Sep 30;62(20):9217–9235. doi: 10.1021/acs.jmedchem.9b01099

Table 3. In Vitro Evaluation of Compound 31 Effect against Other Enzymes, Ion Channels, and Receptors.

protein activity (μM)
human monoamine oxidase A (MAOA) inhibitor IC50 > 100
β2 adrenoreceptor human agonist EC50 > 100
β2 adrenoreceptor human antagonist IC50 > 100
human PXR (NR1I2) agonist EC50 > 50
human KCNQ1/KCNE1 (Kv7.1/MinK) blocker IC50 > 25
human aryl hydrocarbon receptor (AhR) agonist EC50 > 50
organic anion transport polypeptide OATP1B1 inhibitor IC50 > 30
acetylcholinesterase (AChE) inhibitor IC50 = 0.40
phosphodiesterase 3A (PDE3A) inhibitor IC50 > 100
human CaV1.2 (L-type) calcium channel blocker IC50 > 30