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. 2013 Mar;344(3):568–578. doi: 10.1124/jpet.112.201798

TABLE 1.

Characterization of novel GPR35 agonists

The chemical structures of compounds 1–5 are shown as are pEC50 and Emax values obtained in the various assays employed.

Zaprinast Compound 1 Compound 2 Compound 3 Compound 4 Compound 5
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PathHunter β-arrestin Hu GPR35 pEC50 5.1 ± 0.01 7.6 ± 0.05 6.3 ± 0.05 5.4 ± 0.11 5.6 ± 0.01 4.9 ± 0.07
Max 100.0 ± 0.00 95.3 ± 2.24 98.3 ± 5.22 105.0 ± 9.95 101.8 ± 8.75 72.0 ± 5.58
PathHunter (Gqi5) Hu GPR35 pEC50 6.0 ± 0.34 8.5 ± 0.05 6.0 ± 0.04 5.5 ± 0.10 4.9 ± 0.03 6.2 ± 0.09
Max 1.7 ± 0.05 1.6 ± 0.05 1.7 ± 0.02 1.8 ± 0.06 1.5 ± 0.03 1.6 ± 0.01
BRET β-arrestin Hu GPR35 pEC50 5.6 ± 0,03 7.6 ± 0.03 5.5 ± 0.04 5.5 ± 0.03 4.9 ± 0.06 4.7 ± 0.04
Max 100 ± 1.35 100.2 ± 1.32 96.1 ± 1.81 123.0 ± 1.98 104.3 ± 4.25 134.4 ± 4.10
Mu GPR35 pEC50 6.6 ± 0.04 4.78 ± 0.05 <4 <4 4.7 ± 0.16 4.0 ± 0.24
Max 101.1 ± 1.53 61.7 ± 2.52 — — 68.1 ± 7.97 109.4 ± 32.7
Rat GPR35 pEC50 7.1 ± 0.04 5.1 ± 0.08 <4 <4 4.3 ± 0.09 4.9 ± 0.05
Max 100.0 ± 1.67 36.0 ± 1.53 — — 88.4 ± 8.00 116.9 ± 3.8
Inositol phosphate (Gαqα13) Hu GPR35 pEC50 6.9 ± 0.06 8.1 ± 0.09 6.5 ± 0.06 6.8 ± 0.07 5.6 ± 0.10 6.0 ± 0.10
Max 99.0 ± 2.87 86.0 ± 3.53 100.9 ± 3.1 84.1 ± 4.63 96.8 ± 5.60 92.5 ± 5.18
Mu GPR35 pEC50 7.9 ± 0.60 5.6 ± 0.09 4.5 ± 0.14 <4 6.0 ± 0.08 5.0 ± 0.16
Max 99.3 ± 5.49 133.7 ± 6.08 197.0 ± 20.7 — 107.3 ± 3.80 101.4 ± 11.02
Rat GPR35 pEC50 8.3 ± 0.42 5.6 ± 0.10 4.5 ± 0.14 <4 5.8 ± 0.11 5. ± 0.93
Max 97.9 ± 6.36 110.6 ± 6.29 197.2 ± 21.3 — 92.9 ± 5.81 105.5 ± 4.96

Hu, human; Mu, mouse.