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. Author manuscript; available in PMC: 2021 Dec 10.
Published in final edited form as: J Med Chem. 2020 Nov 20;63(23):14626–14646. doi: 10.1021/acs.jmedchem.0c01174

Table 7.

Microsomal stability and physiochemical properties

graphic file with name nihms-1655834-t0047.jpg
Entry Compound Ar Microsomal
stability (%) b
Aq. solubility
(μg/mL) b
cLogD
c
1 4 graphic file with name nihms-1655834-t0048.jpg 0 42 1.27
2 11u graphic file with name nihms-1655834-t0049.jpg 0 59 0.90
3 11y graphic file with name nihms-1655834-t0050.jpg 18 52 1.28
4 11c graphic file with name nihms-1655834-t0051.jpg 24 69 0.33
5 11g graphic file with name nihms-1655834-t0052.jpg 35 23 1.95
6 11f graphic file with name nihms-1655834-t0053.jpg 38 74 1.41
7 11w graphic file with name nihms-1655834-t0054.jpg 45 51 0.77
8 11r graphic file with name nihms-1655834-t0055.jpg 47 56 0.33
9 11p graphic file with name nihms-1655834-t0056.jpg 63 61 0.61
10 11s graphic file with name nihms-1655834-t0057.jpg 63 5 1.65
11 11h graphic file with name nihms-1655834-t0058.jpg 66 55 1.49
12 11o graphic file with name nihms-1655834-t0059.jpg 73 54 0.60
13 11z graphic file with name nihms-1655834-t0060.jpg 88 49 0.47
14 11aa graphic file with name nihms-1655834-t0061.jpg 88 57 1.49
15 11x graphic file with name nihms-1655834-t0062.jpg 95 65 0.72
a

% compound remaining in mouse liver microsomes at 30 min.

b

Kinetic solubility at pH 7.4.

c

Calculated LogD at pH 7.0.