Table 2 In vitro pharmacology of agonist AZ2429 compared with known PAR2 agonists GB110 and SLIGKV-NH2.

From: Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Compounds

Competition binding

Ca2+ flux

IP1

β-arrestin

pERK1/2

AZ2429

7.2 ± 0.2 (n = 4)

6.78 ± 0.04 (n = 3)

6.70 ± 0.03 (n = 6)

6.6 ± 0.1 (n = 4)

7.4 ± 0.1 (n = 4)

GB110

8.2 ± 0.3 (n = 2)

7.5 ± 0.1 (n = 3)

6.5 ± 0.1 (n = 8)

7.3 ± 0.1 (n = 4)

8.2 ± 0.1 (n = 4)

SLIGKV-NH2

6.33 ± 0.04 (n = 5)

5.9 ± 0.1 (n = 3)

4.6 ± 0.1 (n = 6)

4.9 ± 0.1 (n = 4)

5.0 ± 0.1 (n = 3)

  1. IP1 and Ca2+ were assessed in 1321N1-hPAR2 cells, β-arrestin-2 and pERK1/2 in U2OS-hPAR2, binding was measured in membranes from HEKexpi293F cells. Data are presented as mean pKi (binding only) or pEC50 ± s.e.m. based on n independent experiments.
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