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Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

The system optimised the molecules that were most likely to succeed in terms of potency, metabolic stability, synthetic accessibility, and more. Prior to founding Insilico, Alex worked in senior roles at ATI Technologies (a GPU company acquired by AMD in 2006), NeuroGNeuroinformatics, and the Biogerontology Research Foundation.

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Metabolism of macrocyclic drugs

Metabolite Tales Blog

Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolic stability and low propensity for P-gp efflux compared to the acyclic analog [13]. Nagasaka et al.,

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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. The resulting macrocyclic structure was found to be associated with improved metabolic stability and low propensity for P-gp efflux compared to the acyclic analog [13]. Nagasaka et al.,

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Metabolism of five membered nitrogen containing heterocycles

Metabolite Tales Blog

2006 , 34, 145-51 [link] 3 Drug Metab. 1990, 1034, 233-237 [link] 13 Metabolism of pyrazole in the Rat [link] 14 Drug Metab. 2006, 34,748-755 [link] 15 Drug Metab. Instead, be on the lookout for N -glucuronides. References 1 Chem. 2002, 15, 3, 269–299 [link] 2 Chem. 2017, 30, 1, 13–37 [link] 2a Drug Metab. Food Drug Anal.