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UFP-502 bound with high affinity (pKi 9.43) to recombinant DOP receptors displaying moderate selectivity over MOP and KOP.
Four of them (G1, G2, G4, and G5) inhibit PDE4 with the IC50 values < 20 μM and G1 is the most potent ingredient with an IC50 of 245 nM and moderate selectivity over other PDE families.
Kinase assays were conducted and showed that compound 11 inhibited CDK5 with an inhibitory concentration of 160 nM with a moderate selectivity over GSK3 compared to the reference C which exhibited a slightly lower activity on CDK5 (1.5 μM).
These compounds have excellent selectivity over MMP-1 and MMP-9, but only moderate selectivity over MMP-2.
Compound 4 showed inhibitory activity of 25%% at 6.5 μ m against MMP‐13 and moderate selectivity over the antitargets MMP‐2, MMP‐12 and MMP‐14, which supported our molecular modeling results (Table 1).
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16 The structurally similar Lewis acid BEt3 was also tried and moderate selectivity for 5 a over 4 a was seen with low yields of products (Table 1, entry 13).
Several compounds are determined to have a high or moderate selectivity for mutant over wild-type kinase.
The synthesized DDR membrane exhibits a very high selectivity for CO2 and a moderate selectivity for N2 over CH4 with good permeances.
This moderate selectivity towards μ- over κ-opioid receptors was also confirmed in vitro using opioid receptor preparations from guinea pig brains [ 22].
B16 preferentially inhibited Btk (IC50 = 21.70 ± 0.82 nM) over closely related kinases with moderate selectivity.
Over 10-membered ring zeolite ZSM-5, the catalyst shows moderate selectivity to 4,4′-DMBP.
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