Skip to main content
. 2019 Jul 15;10(8):1228–1233. doi: 10.1021/acsmedchemlett.9b00274

Table 2. N-Aryl Potency SAR on the 5 Desmethylcyclohexane Core.

graphic file with name ml-2019-00274b_0006.jpg

cmpd R hTRPV4 IC50 ± SEM (nM)a ChromLogD
5 p-F (±) 1,900 ± 610 4.5
6 H 820 ± 200 4.6
7 p-OEt 140 ± 7.9 4.8
8 m-OEt 74 ± 11 5.0
9 m-Cl 240 ± 51 5.3
10 o-Cl 63 ± 2.9 4.3
11 o-F 540 ± 150 4.2
12 o-Me 310 ± 29 4.6
13 o-OMe 340 ± 85 4.2
a

TRPV4 IC50 is an average of at least two measurements.