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. 2015 Sep 29;58(19):7695–7706. doi: 10.1021/acs.jmedchem.5b00596

Table 2. Stereochemical Investigation around the Original Hit.

graphic file with name jm-2015-00596k_0009.jpg

  T. b. brucei EC50 (μM)a MRC-5 EC50 (μM)a mouse microsomal intrinsic clearance (mL min–1 g–1)
1 0.027 >50 4.4
(S)-26 41 >50 4.0
(R)-27 0.029 >50 3.6
a

EC50 values are shown as mean values of two or more determinations. Standard deviation is typically within 2–3-fold from the EC50.