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. Author manuscript; available in PMC: 2012 Feb 23.
Published in final edited form as: J Med Chem. 2010 Oct 14;53(19):7067–7075. doi: 10.1021/jm100691c

Table 1.

Alkyl, carbocycle and unsubstituted aryl analogues

graphic file with name nihms233914u1.jpg
IC50(nM)a
Compd R Human Murine logP (±0.5)b
2 graphic file with name nihms233914t1.jpg 2.8 1.2 3.1
3 graphic file with name nihms233914t2.jpg 3.9 0.9 2.3
4 graphic file with name nihms233914t3.jpg 12 3.5 1.8
5 graphic file with name nihms233914t4.jpg 3.2 0.4 3.5
6 graphic file with name nihms233914t5.jpg 2.7 7.4 1.8
7 graphic file with name nihms233914t6.jpg 130 49 1.3
8 graphic file with name nihms233914t7.jpg 3.0 4.2 2.4
9 graphic file with name nihms233914t8.jpg 3,800 >5,000 ndc
a

IC50 values were determined with a fluorescent assay using homogenous recombinant murine and human enzymes (see methods).

b

Confidence refers to logP value. See supplementary material for full explaination.

c

The HPLC method used is limited to logP values greater than zero.