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. 2014 Aug 4;5(10):1167–1172. doi: 10.1021/ml500239m

Table 2. Examples of Discrete Amino Acid Modifications and Impact on EPSA and Permeability.

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ID EPSA RRCK Papp (10–6 cm/s) AA1 AA2 AA3 AA4 AA5 AA6
11 75 8.9 Leu N-Me-d-Leu N-Me-Ile Leu d-Pro N-Me-Tyr
12 76 5.5 Leu N-Me-d-Leu N-Me-Ala Leu d-Pro N-Me-Tyr
5 78 13.0 Leu N-Me-d-Leu N-Me-Leu Leu d-Pro N-Me-Tyr
13 83 1.6 Leu N-Me-d-Leu N-Me-Ser Leu d-Pro N-Me-Tyr
14 83 4.7 Leu N-Me-d-Leu N-Me-Thr Leu d-Pro N-Me-Tyr
15 100 1.3 Leu N-Me-d-Leu N-Me-Tyr Leu d-Pro N-Me-Tyr
16 103 0.3 Leu N-Me-d-Leu N-Me-Lys Leu d-Pro N-Me-Tyr
17 125 0.6 Leu N-Me-d-Leu N-Me-Asp Leu d-Pro N-Me-Tyr
6 84 0.5 d-Leu Leu Leu Leu d-Pro Tyr
7 76 4.1 N-Me-d-Leu N-Me-Leu Leu N-Me-Leu d-Pro N-Me-Tyr
8 79 6.1 N-Me-d-Leu N-Me-Leu N-Me-Leu N-Me-Leu d-Pro N-Me-Tyr
6 84 0.5 d-Leu Leu Leu Leu d-Pro Tyr
9 85 1.8 Leu d-Leu Leu Leu d-Pro Tyr
16 103 0.3 Leu N-Me-d-Leu N-Me-Lys Leu d-Pro N-Me-Tyr
18 98 0.2 Leu N-Me-d-Leu N-Me-Lys(N-Me) Leu d-Pro N-Me-Tyr