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A quinolone antibiotic that inhibits HIV-1 integrase (IC50 = 7.2 nM); has antiviral activity against laboratory strains and clinical isolates of HIV-1 in MAGI cells (EC50s = 0.1-1.26 nM) and HIV-2 in PBMCs (EC50s = 0.3-0.9)
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A serine proteases inhibitor that is capable of inhibiting trypsin (a digestive system protease; Ki = 15 nM), tryptase (a mast cell protease; Ki = 95.3 pM), and additional proteases in the coagulation cascade including thrombin (Ki = 0.84 μM); 300 mg/kg decreases the total number of eosinophils and lymphocytes in bronchoalveolar lavage fluid in a mouse model of allergic asthma
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An O-methylated anthocyanidin that imparts blue-red pigments to flowers, fruits, and red wine; suppresses the activity of focal adhesion kinase and the proliferation of HCT116 colon cancer cells
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12(S)-hydroxy-16-Heptadecynoic acid is a mechanism-based inhibitor of CYP450 ω-hydroxylase.{1051} It inhibits prostaglandin ω-hydroxylase with a Ki value of 1.8 µM.{1051}
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A β-lactamase inhibitor that is effective against Ambler class A β-lactamases (IC50 values range from 12 to 60 nM); commonly used with other antibiotics that would be inactivated by β-lactamases
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A GABAA receptor agonist whose potency varies depending on the receptor subunit composition (partial agonist at α1β2γ2 (ED50 = 143 µM), full agonist at α5 (ED50 = 28-129 µM), and super agonist at α4β3δ (ED50 = 6 µM)); acts as an antagonist at ρ1 GABAC receptors (IC50 = 25 µM).
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An agonist of FP receptors (EC50 = 4.12 µM), an active metabolite of unoprostone isopropyl ester. and a derivative of PGF2α; increases inositol phosphate production in HEK293 cells expressing the human receptor; prevents constant light-induced degradation of photoreceptors in rats at 1.2, 3.6, or 6 UG/µl
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Furegrelate is a potent inhibitor of thromboxane synthase with little effect on other enzymes essential for arachidonate metabolism. The IC50 value is 15 nM for human platelet microsomal thromboxane synthase.{1227,1228}
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An endocannabinoid containing dihomo-γ-linoleate in place of the arachidonate moiety of AEA; binds to recombinant human CB1 and CB2 receptors with Ki values of 857 and 598 nM, respectively
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6-MNA is a competitive, non-selective COX inhibitor.{1286,1364,1791} The Ki values for ovine COX-1 and -2 are 21 and 19 µM, respectively.{1364} The IC50 values are 70 and 20 µM for human recombinant COX-1 and -2, respectively.{1286}
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The second most potent CB1 receptor agonist in the methanandamide series (Ki = 26 nM for the CB1 receptor); less prone to FAAH inactivation and inhibits the murine vas deferens twitch response (IC50 = 47 nM)
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