Table 3.
Acronymd | Enzyme | CMNPC | t-DPPO | ||||
---|---|---|---|---|---|---|---|
Humana | Mousea | Rata | Humanb | Dogc | |||
Structure | IC50 | ||||||
1 | AUDA | 3 | 10 | 11 | 10 | 3 | |
3 | AEPU | 14 | 3 | 5 | 45 | 86 | |
14 | APAU | 15 | 9 | 6 | 300 | 500 | |
24 | TPAU | 12 | 97 | 79 | 160 | 9300 | |
27 | TUPS | 3 | 5 | 9 | 26 | 3200 | |
31 | CPAU | 28 | 12 | 7 | 300 | 930 | |
39 | t-AUCB | 2 | 8 | 8 | 2 | 1 | |
40 | c-AUCB | 1 | 4 | 7 | 1 | 1 | |
45 | c-TUCB | 1 | 4 | 6 | 1 | 4 | |
62 | AUSM | 3 | 10 | 8 | 6 | 31 |
measured with purified recombinant enzyme at protein concentration of 0.012 μg/ml.
measured with purified recombinant enzyme at protein concentration of 0.12 μg/ml.
measured with liver cytosolic preparation at protein concentration of 0.2 mg/ml.
acronym commonly used in the literature. AUDA, 12-(3-adamantane-1-yl-ureido)- dodecanoic acid; AEPU, 1-adamantan-1-yl-3-{5-[2-(2- ethoxyethoxy)ethoxy]pentyl}urea; APAU, N-(1-acetylpiperidin-4-yl)-N’-(adamant-1-yl) urea; TPAU, 1-trifluoromethoxyphenyl-3-(1-acetylpiperidin-4-yl) urea; TUPS, 1-(1-methylsulfonyl-piperidin-4-yl)-3-(4-trifluoromethoxy-phenyl)-urea; CPAU, 1-cycloheptyl-3-(1-acetylpiperidin-4-yl) urea; t-AUCB, trans-4-[4-(3-adamantan-1-yl-ureido)-cyclohexyloxy]-benzoic acid; c-AUCB, cis-4-[4-(3-adamantan-1-yl-ureido)-cyclohexyloxy]-benzoic acid; c-TUCB, cis-4-[4-(3-trifluoromethoxyphenyl-l-ureido)-cyclohexyloxy]-benzoic acid ; AUSM, 4-(3-adamantane-1-yl-ureido)-2-hydroxyl-benzoic acid methyl ester.