Results 101 to 110 of about 35,679 (167)

Direct‐to‐Biology: Streamlining the Path From Chemistry to Biology in Drug Discovery

ChemMedChem, Volume 21, Issue 4, 25 February 2026.
Crude yet clever: Direct‐to‐biology workflows exploit nanoscale synthesis and plate‐based assays to accelerate hit discovery, save precious intermediates, and rethink early drug discovery. Direct‐to‐biology (D2B) has emerged as a transformative concept in early drug discovery, defined by the direct on‐target screening of crude reaction mixtures without
Ariane F. Hübner, Fabian Barthels
wiley   +1 more source

Humanization of Drug Metabolism in the <i>Plasmodium berghei</i> Mouse Model for Antimalarial Drug Discovery. [PDF]

ACS Infect Dis
MacLeod AK, Merino C, Viera-Morilla S, Frame L, Tavendale A, Duncan C, Ferguson L, Pinto EG, Simeons FRC, Gomez-Jimenez V, García AB, Riley J, Shishikura Y, Martínez-Martínez MS, Wolf CR, Read KD.   +15 more
europepmc   +1 more source

An Imidazo[2,1‐b][1,3,4]thiadiazole Derivative Inhibits the Virulence Factor α‐Hemolysin by Blocking the Pullout of Its Stem Domain

ChemMedChem, Volume 21, Issue 4, 25 February 2026.
A high‐throughput cellular screen based on Ca2+ influx in U937 monocytic cells identified thiadiazoles as small‐molecule inhibitors of α‐hemolysin, a key virulence factor of Staphylococcus aureus. The thiadiazole 1 prevents pore formation by a dual mechanism that prevents stem loop unfolding as well as membrane attachment.
Vadim S. Korotkov, Peer Lukat, Raffaella Di Lucrezia, Aditya Shekhar, Carsten Degenhart, Randi Diestel, Ursula Bilitewski, Klaus Dinkel, Wulf Blankenfeldt, Mark Brönstrup   +9 more
wiley   +1 more source

Cyp3a4-Mediated in vitro Metabolism and in vivo Disposition of Lorlatinib in Rats. [PDF]

Drug Des Devel Ther
Xie C, Guan T, Huang J, Chen J, Li Y, Zheng P.   +5 more
europepmc   +1 more source

The Effect of <i>N</i>-Alkyl Azole Difluorination on Molecular Properties Relevant for Compound Optimization: A Comparative Study. [PDF]

ACS Med Chem Lett
Herrick RM, Green SA, Rich S, Grandner JM, Huard K, Altman RA.   +5 more
europepmc   +1 more source

Triethylamine N-oxygenation mediated by liver and kidney microsomes and recombinant flavin-containing monooxygenase 3 (FMO3) and FMO1 proteins from humans, monkeys, pigs, and dogs. [PDF]

Drug Metab Dispos
Shimizu M, Nii A, Uno Y, Yamazaki H.
europepmc   +1 more source

Study on Phase I Metabolic Processes and Metabolite Biomarker Identification of Synthetic Cannabinoids 5F-ADB-PINACA and 5F-ADBICA in Human Liver Microsomes and Zebrafish Model. [PDF]

Molecules
Li H, Zheng H, Zhong S, Zhao Y, Lin J, Su H, Qian Z, Wang Y.   +7 more
europepmc   +1 more source

Characterization of trazodone metabolic pathways and species-specific profiles. [PDF]

Front Pharmacol
Petrucci V, Dragone P, Laurenti MC, Oggianu L, Zabela V, Cattaneo A.   +5 more
europepmc   +1 more source

Rough microsomes isolated from snap-frozen canine pancreatic tissue retain their co-translational translocation functionality. [PDF]

Biol Methods Protoc
Croonenborghs M, Verhaegen M, Pauwels E, Provinciael B, Vermeire K.   +4 more
europepmc   +1 more source

UGT2B7-mediated drug-drug interaction between cannabinoids and hydromorphone. [PDF]

Drug Metab Dispos
Coates S, Bardhi K, Zhao M, Lazarus P.
europepmc   +1 more source