Drug Target Review

JUNE 12, 2023

The system optimised the molecules that were most likely to succeed in terms of potency, metabolic stability, synthetic accessibility, and more. The novel molecules were further ranked based on their ADME and selectivity profiles.

Metabolic Stability 92

Metabolic Stability Clinical Trials Small Molecule Pharmacokinetics 92

Metabolite Tales Blog

JULY 5, 2023

Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Although in vitro studies showed low metabolic activity, more than 20 metabolites could be identified, resulting from two main routes.

Drugs 52

Drugs Metabolic Stability FDA Approval Treatment 52

Metabolite Tales Blog

JULY 5, 2023

Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Although in vitro studies showed low metabolic activity, more than 20 metabolites could be identified, resulting from two main routes.

Metabolic Stability 52

Metabolic Stability Drugs FDA Approval Treatment 52

Metabolite Tales Blog

DECEMBER 13, 2023

To curb glucuronidation at that position a gem-dimethyl group was incorporated which not only boosted metabolic stability, but also resulted in increased potency of the final lead compound. Figure 4: Optimisation of an IDO1 inhibitor incorporating installation of a gem-dimethyl group to control glucuronidation of a key hydroxyl group.

Small Molecule 59

Small Molecule Metabolic Stability Treatment Drugs 59

Metabolite Tales Blog

MARCH 1, 2023

2013, 41, 508-517 [link] 21 J. 44, 797–814 [link] Take a look at our other blogs The post Metabolism of five membered nitrogen containing heterocycles appeared first on Hypha Discovery. 1994, 22, 659-662 [link] 18a Xenobiotica , 1986, 16, 11-20 [link] 18b Wood and Fibre Science. 2009, 41, 157-167 [link] 19 Molecules.

Metabolic Stability 52

Metabolic Stability Drugs Pharmacokinetics Science 52

Drug Target Review

JANUARY 16, 2025

Drug Discovery Today , 18(13-14):659666, 2013. Cyclic Peptide Design, Chapter 2: Strategies to Enhance Metabolic Stabilities. Journal of Medicinal Chemistry , 59(6):23122327, 2016. Yusof I, Segall MD. Considering the impact drug-like properties have on the chance of success. Bhardwaj G, OConnor J, Rettie S, et al.

Drug Development 52

Drug Development Small Molecule Drugs FDA Approval 52