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The most potent selective hMAO-B inhibitor D7 has a selectivity ratio of 20.93, with an IC50 value of 2.78 μM, similar or better than selegiline (IC50 = 2.89 μM), a selective hMAO-B inhibitor currently in the market for the treatment of Parkinson's disease.
However 2e, 3b, 3c and 3i compounds were the most potent selective COX-2 inhibitors of this study with 3b showing the best COX-2 profile.
Thirty-three analogs were prepared and tested, among which hecogenin 12- 3′-methylphenyl thiosemicarbazone) (30) displayed the most potent selective anticancer effects.
Citalopram (CIT) is an antidepressant drug from the group ofselective serotonin reuptake inhibitors in which it is the most potent selective inhibitor ofserotonin uptake currently available.
These represent the most potent selective plant-type A. fumigatus chitinase inhibitors to date.
The most potent, selective compounds from the indazole and pyrrolopyrimidine classes were cocrystallized with GRK2 and GRK1, respectively, in order to elucidate molecular determinants underlying their binding and selectivity.
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We report that 16α-LE2, PPT and 3β,5α-GSD have a high ERα-selective agonist potency while 8β-VE2, DPN, genistein and biochanin A show ERβ selectivity with 8β-VE2 being the most potent and selective ERβ agonist.
Among this class of compounds, 2- 4-methylpiperidin-1-yl -N- naphth-1-ylmethyl pyrimidin-4-amine (9e) was identified as the most potent and selective BuChE inhibitor (IC50 = 2- 4-methylpiperidin-1-yl -N- naphth-1-ylmethyl pyrimidin-4-amineent compared to the commercial, approved reference drug galanthamine (BuChE IC50 = 12- 4-methylpiperidin-1-yl -N- naphth-1-ylmethyl pyrimidin-4-amine
Compound -16b, which displayed an EC50 of 4.2 nM at 5-HT2C, no activity at 5-HT2B, and an 89-fold selectivity against 5-HT2A, is one of the most potent and selective 5-HT2C agonists reported to date.
Among these derivatives, compound (5c) was the most potent and selective COX-2 inhibitor (IC50 = 1.33 μM), with a significant selectivity index (SI >60).
We selected PD173074 for in vivo assessment as it was the most potent and selective compound, with the lowest IC50 values and the most pronounced cell cycle and apoptotic effects in vitro.
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