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. Author manuscript; available in PMC: 2020 Aug 24.
Published in final edited form as: J Med Chem. 2019 Apr 23;62(10):4884–4901. doi: 10.1021/acs.jmedchem.9b00193

Table 2:

Inhibitory activity of cyclopentylpyridine Ar1 substitutiona

graphic file with name nihms-1617532-t0011.jpg
Compound R PDE4D7-
S129D
IC50 (nM)
PDE4B1-
S133D
IC50 (nM)
PDE4D7-
S129(wt)
IC50 (nM)
Ratio
B/D
Ratio
Basal/Activated
12 4-CH2CH2OH 9 562 2111 60 226
13 4-(CH2)2CONH2 35 166 1283 5 37
14 4-CH2CO-NMe2 51 356 914 7 18
15 4-CH2CO-N(H)Me 133 98 1991 1 15
16 3- CH2CH2OH 226 1419 6325 6 28
17 4-CH2CO2H 1165 1642 NTb 1 -
a

See table 1 for assay definitions. See experimental section for methods and detailed synthetic procedures.

b

NT: Not tested