Table 2. Potency of N-(2-(1H-Tetrazol-5-yl)phenyl)benzamide Derivatives in the DMR Assay.

			R3
compd	R1	R2	ortho	meta	para	EC50a (μM)	desensitization IC50b (μM)	antagonist IC50c (μM)
37						inactive
42	Br	H	H	H	H	0.87 ± 0.09	0.30 ± 0.03	0.47 ± 0.06
43	Br	H	CH3	H	H	2.05 ± 0.11	0.81 ± 0.05	0.19 ± 0.02
44	Br	H	H	CH3	H	0.86 ± 0.04	0.36 ± 0.02	0.12 ± 0.03
45	Br	H	H	H	CH3	1.33 ± 0.13	0.51 ± 0.03	0.13 ± 0.04
46	Br	H	Cl	H	H	0.87 ± 0.10	0.41 ± 0.03	0.77 ± 0.08
47	Br	H	H	Cl	H	2.18 ± 0.37	0.48 ± 0.03	0.42 ± 0.11
48	Br	H	H	H	Cl	0.52 ± 0.03	0.21 ± 0.01	0.52 ± 0.05
49	Br	H	Cl	H	Cl	0.31 ± 0.03	0.11 ± 0.01	1.11 ± 0.42
50	Br	H	F	H	H	0.35 ± 0.02	0.17 ± 0.01	0.52 ± 0.07
51	Br	H	H	F	H	0.61 ± 0.07	0.21 ± 0.02	0.57 ± 0.07
52	Br	H	H	H	F	0.45 ± 0.02	0.16 ± 0.01	0.18 ± 0.06
53	Br	H	F	H	F	0.13 ± 0.01	0.06 ± 0.01	0.22 ± 0.03
54	Br	H	OCH3	H	H	0.86 ± 0.06	0.40 ± 0.03	0.28 ± 0.05
55	Br	H	H	OCH3	H	1.94 ± 0.08	0.81 ± 0.07	0.56 ± 0.08
56	Br	H	H	H	OCH3	0.059 ± 0.007	0.026 ± 0.003	0.20 ± 0.09
57	Br	H	H	OCH3	OCH3	0.83 ± 0.07	0.26 ± 0.02	1.00 ± 0.16
58	H	Br	H	H	OCH3	0.30 ± 0.03	0.11 ± 0.01	1.38 ± 0.15
59	F	H	H	H	OCH3	0.20 ± 0.01	0.082 ± 0.005	0.34 ± 0.08
60	H	H	H	H	OCH3	0.65 ± 0.05	0.28 ± 0.02	1.00 ± 0.22
61	Br	H	H	CF3	H	4.60 ± 0.46	1.28 ± 0.08	0.84 ± 0.06
62	Br	H	H	H	CF3	3.65 ± 0.19	1.36 ± 0.16	0.25 ± 0.05
63	Br	H	F	H	OCH3	0.041 ± 0.005	0.014 ± 0.002	1.69 ± 0.16
64					OCH3	17.58 ± 3.30	8.36 ± 0.99	0.63 ± 0.19

^aEC₅₀ to trigger DMR.

^bIC₅₀ to desensitize cells upon cells repeated stimulation with 1 μM zaprinast.

^cIC₅₀ of known GPR35 antagonist 5 to block the agonist-induced DMR. The data represents mean ± sd from two independent measurements, each with four replicates (n = 8).