Zobrazeno 1 - 10
of 112
pro vyhledávání: '"John J. Herbst"'
Autor:
Harold N. Weller, Ying Li, Xianmei Cai, Wilson Z. Shou, Anthony A. Paiva, Shilpa Madari, Aaron Walker, John J. Herbst
Publikováno v:
SLAS Discovery. 24:738-744
The Caco-2 permeability assay is a well-accepted in vitro model to evaluate compounds' potential for oral absorption at early discovery. However, for many lipophilic compounds, no meaningful Caco-2 data could be generated due to their low solubility
Autor:
Sokhom S. Pin, Deborah A. Cook, John E. Macor, Laura J. Signor, Carl Davis, Valerie J. Whiterock, Gene M. Dubowchik, Richard Schartman, Ping Chen, Chaturvedula Prasad, Kimberly A. Widmann, George Thalody, Walter Kostich, Robert Macci, John J. Herbst, Stephen E. Mercer, Charles M. Conway, Cen Xu
Publikováno v:
Bioorganicmedicinal chemistry letters. 31
Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown clinically to be effective treatments for migraine. Zavegepant (BHV-3500, BMS-742413) is a high affinity antagonist of the CGRP receptor (hCGRP Ki = 0.023 nM) that has demons
Publikováno v:
SLAS Discovery. 19:1409-1414
Plastic labware is used in all processes of modern pharmaceutical research, including compound storage and biological assays. The use of these plastics has created vast increases in productivity and cost savings as experiments moved from glass test t
Autor:
Kan He, Donglu Zhang, Wilson Z. Shou, John J. Herbst, Yong-Hae Han, Praveen Balimane, Jinping Gan, W. Griffith Humphreys, Charles Frost, Janet Kolb, Lifei Wang
Publikováno v:
Drug Metabolism and Disposition. 41:827-835
The studies reported here were conducted to investigate the transport characteristics of apixaban (1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide) and to understand the impact o
Autor:
Cen Xu, Xiaojun Han, Brett R. Beno, John E. Macor, Rita L. Civiello, John J. Herbst, Gene M. Dubowchik, Chaturvedula Prasad, Charles M. Conway
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(4)
Calcitonin gene-related peptide (CGRP) is a potent neuropeptide implicated in the pathophysiology of migraine. In the course of seeking CGRP antagonists with improved oral bioavailability, metabolic stability, and pharmacokinetic properties, lower mo
Autor:
Timothy V Olah, Tatyana Zvyaga, Janet Kolb, Harold N. Weller, John J. Herbst, Andrew Dennis Wagner, Can C. Özbal, Wilson Z. Shou
Publikováno v:
Rapid Communications in Mass Spectrometry. 25:1231-1240
The evaluation of interactions between drug candidates and transporters such as P-glycoprotein (P-gp) has gained considerable interest in drug discovery and development. Inhibition of P-gp can be assessed by performing bi-directional permeability stu
Autor:
Jeremy Stewart, John J. Herbst, Jun Zhang, Wilson Z. Shou, Marianne Vath, Harold N. Weller, Larry Elvebak, Kasia Kieltyka, Jennifer W. Maloney
Publikováno v:
Rapid Communications in Mass Spectrometry. 24:3593-3601
Quantification of small molecules using liquid chromatography/tandem mass spectrometry (LC/MS/MS) on a triple quadrupole mass spectrometer has become a common practice in bioanalytical support of in vitro adsorption, distribution, metabolism and excr
Autor:
John J. Herbst, Meredith Ferrante, Annapurna Pendri, Kristin L. Rockwell, Jonathan O’Connell, Susan Jenkins, James Loy, Chi Shing Sum, Adam Hendricson, Martyn Banks, Robert G. Gentles, Yulia Benitex, Robert L. Bertekap, Neil T. Burford, Mary Ellen Cvijic, John E. Macor, Andrew Alt, Litao Zhang, Ryan Westphal, Jing Chen, Michelle Nophsker, Guo Li
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 356(2)
The muscarinic acetylcholine receptor subtype 1 (M1) receptors play an important role in cognition and memory, and are considered to be attractive targets for the development of novel medications to treat cognitive impairments seen in schizophrenia a
Autor:
Jonathan O’Connell, Molly R. Ryan, Marta Filizola, Tom S. Wehrman, Daniel Bassoni, Neil T. Burford, Martyn Banks, Yi Shang, Andrew Alt, Samuel Gerritz, Kathryn E. Livingston, Lauren Budenholzer, John R. Traynor, John J. Herbst, Litao Zhang, Arthur Christopoulos, Ying Han, Meritxell Canals
Allosteric modulators of G protein-coupled receptors (GPCRs) have a number of potential advantages compared to agonists or antagonists that bind to the orthosteric site of the receptor. These include the potential for receptor selectivity, maintenanc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c185e7de02206a5d1a7ec518591e52aa
https://europepmc.org/articles/PMC4703104/
https://europepmc.org/articles/PMC4703104/
Autor:
Henry Wong, John J. Herbst, Kin Sing Lam, Kim Esposito, Shuhao Shi, Samuel Gerritz, Yue Zhong Shu, Michael J. Sofia, Wenying Li, Ramesh Padmanabha, Shirong Zhu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4151-4154
The solid-phase synthesis of a library based on the natural product anisomycin is described. The resulting library was tested against a panel of bacterial and fungal targets, and active compounds were identified in a Staphylococcus aureus whole-cell