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. 2015 Nov 4;7(1):23–27. doi: 10.1021/acsmedchemlett.5b00253

Table 2. SAR of R1 Portion and R3 Portion.

graphic file with name ml-2015-002533_0005.jpg

      RORγ-LUC EC50a (μM)
     MS in liver S9 (remaining %)
compd R1 R3 human mouse LE Fsp3 10 min 60 min
3l c-Hex(CH2)2 Et 0.90 0.60 0.30 0.61 36 0
3n c-Pr 0.98 0.45 0.28 0.63 55 23
3o c-Bu 9.5 1.8 0.23 0.64 49 27
3p 2,2-di-F-c-Pr 0.92 0.50 0.27 0.63 75 59
3qb 2-Bu(CH2)2 c-Pr 3.9 1.4 0.27 0.59 63 27
3r i-Pr(CH2)3 1.7 0.61 0.29 0.59 67 27
3s t-Bu(CH2)3 2.8 1.3 0.27 0.61 71 51
a

The EC50s are mean values of at least two replicates.

b

Racemic.