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. Author manuscript; available in PMC: 2018 Jun 8.
Published in final edited form as: J Med Chem. 2017 May 19;60(11):4594–4610. doi: 10.1021/acs.jmedchem.6b01885

Table 3.

Effects of the Substituent at the 5-Position of the Isoxazole on Activity in the SMN-luc Reporter Gene Assaya

graphic file with name nihms951984u4.jpg
Compd # R EC50 (µM) % Activation Compd # R EC50 (µM) % Activation
4 graphic file with name nihms951984t24.jpg 1.8 242 8a H IA IA
8b graphic file with name nihms951984t25.jpg IA IA 8c graphic file with name nihms951984t26.jpg 8.8 ± 1.1 165 ± 8.4
8d graphic file with name nihms951984t27.jpg 1.5 ± 0.6 180 ± 16 8e graphic file with name nihms951984t28.jpg 1.93 ± 0.7 140 ± 21
8f graphic file with name nihms951984t29.jpg IA IA 8g graphic file with name nihms951984t30.jpg IA IA
8h graphic file with name nihms951984t31.jpg IA IA 8i graphic file with name nihms951984t32.jpg 3.56 ± 1.1 116 ± 15
a

Data are expressed as SEM. Compounds were analyzed in duplicate on two separate occasions, and compounds with >150% induction and EC50 < 1 µM were repeated (n = 3).

IA, inactive.