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. Author manuscript; available in PMC: 2014 Jan 6.
Published in final edited form as: J Med Chem. 2013 Nov 1;56(21):10.1021/jm401002r. doi: 10.1021/jm401002r

Table 4.

The effect of different substituents at the N-atom on LSD1 inhibition.

graphic file with name nihms-539339-t0029.jpg

Comp. R1 R2 IC50(μM) Comp. R1 R2 IC50(μM)
53 CH3 o-F >125 68 graphic file with name nihms-539339-t0030.jpg o-F 39.8±1.1
54 CH3 p-CH3 >125 69 graphic file with name nihms-539339-t0031.jpg p-F 43.9±2.5
55 CH3 p-F >125 70 graphic file with name nihms-539339-t0032.jpg p-CH3 35.7±2.0
56 CH3 o-Cl >125 71 graphic file with name nihms-539339-t0033.jpg o-F 45.7±1.9
57 graphic file with name nihms-539339-t0034.jpg p-CH3 >125 72 graphic file with name nihms-539339-t0035.jpg p-F 55.1±3.3
58 graphic file with name nihms-539339-t0036.jpg o-F >125 73 H o-F 17.3±1.7
59 graphic file with name nihms-539339-t0037.jpg p-CH3 >125 74 H p-F 69.3±1.8
60 graphic file with name nihms-539339-t0038.jpg o-F >125 75 H o-Cl >125
61 graphic file with name nihms-539339-t0039.jpg p-CH3 83.4±2.1 76 H p-Cl >125
62 graphic file with name nihms-539339-t0040.jpg o-F 100.1±9.3 77 H p-CH3 28.9±2.0
63 graphic file with name nihms-539339-t0041.jpg p-F >125 78 H p-OCH3 19.5±1.9
64 graphic file with name nihms-539339-t0042.jpg p-CH3 40.3±2.1 79 H p-CF3 87.4±2.3
65 graphic file with name nihms-539339-t0043.jpg o-F >125 80 H o, o-diF >125
66 graphic file with name nihms-539339-t0044.jpg p-F >125 81 H m, p-diCl >125
67 graphic file with name nihms-539339-t0045.jpg p-CH3 27.6±1.2 82 H m,p,m-triOCH3 >125