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. Author manuscript; available in PMC: 2017 May 4.
Published in final edited form as: Eur J Med Chem. 2016 Feb 4;113:273–292. doi: 10.1016/j.ejmech.2016.02.006

Table 3.

Investigation into the significance of the inhibitor’s carboxylic acid and hydroxyl group towards the inhibition of Mcl-1. Experimental data determined by a fluorescence polarization competition assay.

graphic file with name nihms758150u2.jpg

Compound X Y Mcl-1
Ki (μM)a 		Mcl-1
LGFE (kcal mol-1)
3ca CO2H OH 0.566 ± 0.031 -42
10 CO2Me OH >500 -34
11 CO2Me OMe >500 -35
12 CO2H OMe 23.4 ± 2.6 -42
a

Ki values determined by Nikolovska-Coleska equation from IC50 values.50 Data represent the average of at least two independent assays; errors are standard deviations.