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Both enantiomers of RAB1 possess favorable inhibition profiles
| TMP enantiomer | IC50 (Ki)a |
||
|---|---|---|---|
| wt (Phe 98) | TMPr (Tyr98) | Activity ratio (Y98/F98) | |
| TMP | 14.4 ± 3.6 (4.4 ± 1.1) | 539.7 ± 101.1 (53.6 ± 10.0) | 37.5 (12.3) |
| (S,R)-RAB1 | 9.4 ± 3.9 (2.8 ± 1.2) | 8.8 ± 0.9 (0.9 ± 0.03) | 0.9 (0.3) |
| S-RAB1 | 2.9 ± 0.1 (0.9 ± 0.03) | 1.8 ± 0.3 (0.2 ± 0.03) | 0.6 (0.2) |
| R-RAB1 | 11.5 ± 2.3 (3.5 ± 0.7) | 65.4 ± 3.3 (6.5 ± 0.3) | 5.7 (1.9) |
Values expressed in nM.
