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. Author manuscript; available in PMC: 2016 May 1.
Published in final edited form as: Chem Biol Drug Des. 2014 Nov 18;85(5):549–564. doi: 10.1111/cbdd.12443

Table 3. a Biochemical data for analogs exploring Region B.

graphic file with name nihms-633066-t0034.jpg
Compound R2 TbrPDEB1
(% inh)		 TbrPDEB1
(IC50 μM)
17a graphic file with name nihms-633066-t0035.jpg 94 ± 3.5 6.4 ± 1.7
21a graphic file with name nihms-633066-t0036.jpg 41 ± 5.8 -
21b graphic file with name nihms-633066-t0037.jpg 0 -
22a graphic file with name nihms-633066-t0038.jpg 19 ± 6.6 -
22b graphic file with name nihms-633066-t0039.jpg 19 ± 4.2 -
22c graphic file with name nihms-633066-t0040.jpg 22 ± 20 28 ± 3.4
22d graphic file with name nihms-633066-t0041.jpg 80 ± 4.8 ndb
22e graphic file with name nihms-633066-t0042.jpg 59 ± 3.6 -
22f graphic file with name nihms-633066-t0043.jpg 72 ± 14 26 ± 1.3
19a graphic file with name nihms-633066-t0044.jpg 83.7 ± 9.1 3.8 ± 0.4
24a graphic file with name nihms-633066-t0045.jpg 34 ± 0.3 -
24b graphic file with name nihms-633066-t0046.jpg 60 ±16 7 ± 0.9
24c graphic file with name nihms-633066-t0047.jpg 82 ±12 4.2 ± 0.6
24d graphic file with name nihms-633066-t0048.jpg 67 ± 7.5 3.5 ± 0.5
24e graphic file with name nihms-633066-t0049.jpg 85 ± 11 3.5 ± 0.6
24f graphic file with name nihms-633066-t0050.jpg 69 ±16 3.7 ± 0.2
24g graphic file with name nihms-633066-t0051.jpg 21 ± 6.5 -
28 graphic file with name nihms-633066-t0052.jpg 76 ± 2.2 5.9 ± 0.67
a

All values are the mean of three or more replicates ± SEM.

b

No IC50 obtained due to limited solubility at higher concentrations.