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. 2018 Apr 9;9(5):422–427. doi: 10.1021/acsmedchemlett.7b00510

Table 1. Potency of 2-Substituted 2-(1H-Tetrazol-5-yl)aniline Derivatives in DMR Assays.

graphic file with name ml-2017-00510p_0007.jpg

compd R1 R2 R3 EC50a (μM) desensitization IC50b (μM) antagonist IC50c (μM)
7a       29.99 ± 2.80 35.56 ± 2.54 0.67 ± 0.19
7b       44.06 ± 4.06 75.34 ± 9.31 0.67 ± 0.25
14 Br H ethyl 0.62 ± 0.06 0.70 ± 0.07 0.47 ± 0.11
15 Br H isopropyl 0.38 ± 0.02 0.28 ± 0.02 0.58 ± 0.06
16 Br H cyclohexyl 0.44 ± 0.03 0.20 ± 0.01 0.43 ± 0.08
17 Br H furyl 1.06 ± 0.13 0.44 ± 0.03 0.29 ± 0.08
18 Br H thienyl 0.51 ± 0.02 0.26 ± 0.03 0.50 ± 0.05
a

EC50 to trigger DMR.

b

IC50 to desensitize upon cells repeated stimulation with 1 μM zaprinast.

c

IC50 of known GPR35 antagonist 5 to block the agonism. The data respresent mean ± sd from two independent measurements, each with four replicates (n = 8).