Table 1.

Enzyme inhibition data of imidazopyridines (IC50, μm)

Compound no.E/CDK2 IC50m)D1/CDK4 IC50m)B/CDK1 IC50m)PKA-a IC50m)PKC-bII IC50m)CAMKII IC50m)GSK3-b IC50m)
1a0.3245.2210.326>2019.53.39
1b0.1220.9470.0579.571.420.48
1c0.0260.7860.1055.542.29798>205.9
1d0.0280.4640.1436.343.262013.89>20
  • Note: Compound 1d, potent inhibitor of CDK2 (IC50 = 28 nm) and a weaker inhibitor of CDK4 and CDK1 (IC50 = 464 and 143 nm), was tested against a panel of representative kinases and found to be highly selective: GSK3β (>500-fold), CAMKII, PKA, PKC-α,β,ε,γ (>100-fold).