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. Author manuscript; available in PMC: 2018 Jan 9.
Published in final edited form as: ChemMedChem. 2016 Aug 25;11(19):2127–2131. doi: 10.1002/cmdc.201600384

Table 1.

IC50s of dipeptidomimetics against β5i and β5c. Data were average of at least three independent experiments.

ID graphic file with name nihms929271u2.jpg IC50 (μM)* SIapp
β5i (ANW) β5c (LLVY)
P1: β-AA (m=0, n=1)
PKS2249 graphic file with name nihms929271t1.jpg 0.190 ± 0.018 88.38 ± 5.81 465
PKS2251 graphic file with name nihms929271t2.jpg 0.057 ± 0.012 76.02 ± 25.61 1333
PKS2252 graphic file with name nihms929271t3.jpg 0.0055 ± 0.0010 74.87 ± 10.52 13600
PKS2260 graphic file with name nihms929271t4.jpg 0.012 ± 0.001 13.85 ± 3.79 1154
PKS2272 graphic file with name nihms929271t5.jpg 0.135 ± 0.022 >100 >600
PKS2295 graphic file with name nihms929271t6.jpg 0.148 ± 0.016 22.18 ± 5.77 150
PKS3054 graphic file with name nihms929271t7.jpg 0.0053 ± 0.0003 0.30 ± 0.08 57
P2: β-AA (m=1, n=0)
PKS2278 graphic file with name nihms929271t8.jpg 3.35 ± 0.64 >100 >44
PKS2279 graphic file with name nihms929271t9.jpg 0.014 ± 0.002 35.3 2521
P1, P2: β-AAs (m = 1, n = 1)
PKS2291 graphic file with name nihms929271t10.jpg 9.60 ± 0.66 >100 >11
PKS2292 graphic file with name nihms929271t11.jpg >100 >100 -

AA: amino acid.

ANW: ac-ANW-AMC.

LLVY: suc-LLVY-AMC.

SIapp: apparent selectivity index = IC50β5c / IC50β5i.

*

Data were given as mean ± SEM.