Journal: Journal of Medicinal Chemistry

Article Title: Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor

doi: 10.1021/acs.jmedchem.0c00208

Figure Lengend Snippet: Profiling of 1 and 13 a

Article Snippet: The following assays were performed according to the standard protocols of Cyprotex: Caco-2 permeability, dog microsomal stability, hepatocyte stability (human, mouse, dog, rat, and cynomolgus), CYP3A4 inhibition, mouse plasma stability, mouse plasma protein binding, and Ames test.

Techniques: Solubility, Inhibition, Ames Test

Journal: Journal of controlled release : official journal of the Controlled Release Society

Article Title: Application of activated nucleoside analogs for the treatment of drug-resistant tumors by oral delivery of nanogel-drug conjugates

doi: 10.1016/j.jconrel.2013.01.020

Figure Lengend Snippet: (A) Gastrointestinal (GI) transfer efficacy of nanogel-drug conjugates, empty nanogels and free drugs in Caco-2 cell monolayers. (A) Percentage of drug transfer across the Caco-2 cell monolayer: (a) empty nanogel without drug, (b–d) nanogel-drug conjugates, and (e–f) free nucleoside analogs, Floxuridine and Gemcitabine (60–240 min incubation at 37°C). Data represents means ± SEM (n=3). (B) Permeability coefficients of nanogel-drug conjugates and free drugs calculated from the transfer data. Papp were compared for each formulation to determine their GI transport efficacy.

Article Snippet: CacoReady kit for an in vitro evaluation of drug permeability in Caco-2 monolayers was purchased from ADMEcell (Emeryville, CA) and used according to the manufacturer’s protocol.

Techniques: Incubation, Permeability

Journal: Chemistryselect

Article Title: In Silico Identification of Potential Inhibitors of ADP‐Ribose Phosphatase of SARS‐CoV‐2 nsP3 by Combining E‐Pharmacophore‐ and Receptor‐Based Virtual Screening of Database

doi: 10.1002/slct.202001419

Figure Lengend Snippet: QikProp properties and descriptors of six selected inhibitors.

Article Snippet: Only few properties like Caco‐2 cell permeability in nm/sec (QPPCaco) and apparent MDCK cell permeability in nm/sec (QPPMDCK) for molecules MolPort‐000‐735‐951 and MolPort‐021‐745‐738 defy the acceptable range.

Techniques: