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Nepafenac is a potent NSAID that rapidly penetrates the eye following topical ocular administration. In the eye, nepafenac is converted to amfenac, which has unique time-dependent inhibitory properties for COX-1 and COX-2.
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Artemisinin, a potent antimalarial, can be used to cure multidrug-resistant Plasmodium falciparum infections.
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Asenapine inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
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Masitinib, a novel phenylaminothiazole-type derivative, is an inhibitor of the class III receptor tyrosine kinase stem-cell growth factor receptor (c-Kit) with IC50 of 200 nM, platelet-derived growth factor receptor α and β and the non-receptor tyrosine kinase Lyn(PDGFRα/β with IC50 of 540 nM/800 nM).
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Quisinostat (JNJ-26481585) is a novel second-generation HDACi inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. , in NSCLC cells. In vitro, quisinostat has shown anti-proliferative activity against NSCLC cell lines. quisinostat extremely changed protein acetylation patterns of A549 cells and inhibited epithelial-mesenchymal transition (EMT) process.
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