New chemotype of selective and potent inhibitors of human delta 24-dehydrocholesterol reductase.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.08.011
Abstract: The enzyme Δ24-dehydrocholesterol reductase (DHCR24) catalyzes the reduction of the Δ24-double bond in the side chain of cholesterol precursors. Recent biochemical investigations fuel the hope that inhibition of DHCR24, resulting in an accumulation of desmosterol,… read more here.
Keywords: new chemotype; selective potent; dehydrocholesterol reductase; dhcr24 ... See more keywords
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01099
Abstract: Kinase fusions involving tropomyosin receptor kinases (TRKs) have been proven to act as strong oncogenic drivers and are therefore recognized as attractive therapeutic targets. We screened an in-house kinase-focused library and identified a promising hit… read more here.
Keywords: selective potent; orally bioavailable; bioavailable selective; trk inhibitor ... See more keywords
Highly Selective and Potent α4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01250
Abstract: The α4β2 nAChR is the most predominant subtype in the brain and is a well-known culprit for nicotine addiction. Previously we presented a series of α4β2 nAChR selective compounds that were discovered from a mixture-based… read more here.
Keywords: self administration; selective potent; administration; highly selective ... See more keywords
Discovery of a highly selective and potent kappa opioid receptor agonist from N-cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydro- northebaines with reduced central nervous system (CNS) side effects navigated by the message-address concept.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00857
Abstract: Effective and safe analgesics represent an unmet medical need for the treatment of acute and chronic pain. A series of N-cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaines were designed, synthesized and assayed, leading to the discovery of a benzylamine derivative (compound… read more here.
Keywords: selective potent; opioid receptor; highly selective; cyclopropylmethyl phenyl ... See more keywords
First‐in‐human study of deucravacitinib: A selective, potent, allosteric small‐molecule inhibitor of tyrosine kinase 2
Sign Up to like & getrecommendations! Published in 2022 at "Clinical and Translational Science"
DOI: 10.1111/cts.13435
Abstract: This randomized, double‐blind, single‐ and multiple‐ascending dose study assessed the pharmacokinetics (PKs), pharmacodynamics, and safety of deucravacitinib (Sotyktu™), a selective and potent small‐molecule inhibitor of tyrosine kinase 2, in 100 (75 active, 25 placebo) healthy… read more here.
Keywords: small molecule; selective potent; inhibitor tyrosine; molecule inhibitor ... See more keywords
S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth.
Sign Up to like & getrecommendations! Published in 2018 at "Oncotarget"
DOI: 10.2210/pdb6gl8/pdb
Abstract: Escape from apoptosis is one of the major hallmarks of cancer cells. The B-cell Lymphoma 2 (BCL-2) gene family encodes pro-apoptotic and anti-apoptotic proteins that are key regulators of the apoptotic process. Overexpression of the… read more here.
Keywords: selective potent; potent inhibitor; s55746; novel orally ... See more keywords