Table 2

Ki values for kinase inhibitors determined from displacement curves of radioligand binding from various GPRs

ReceptorInhibitor
H-89H-85H-7KT5720STBisIX
beta-2AR0.182-a 1.5>500>>10>>102.2
beta-2AR0.35 1.7>500>>10>>102.3
beta-2AR (BEAS-2B)0.17 1.8>500>>10>>102.3
m1 mAchR>102-b >>102-c 200>>10>>102.0
m2 mAchR>10 >10 200>>10>>101.0
alpha-2 ARC10 6 >>10 >>500>>10>>105
TXA2αR>10 >>10 >>500>>10>>10>10

  • ↵2-a Values reported are micromolar concentrations calculated as the mean of two to five experiments.

  • ↵2-b >20 to 40% inhibition observed at this concentration.

  • ↵2-c >>,<20% inhibition observed at this concentration.