Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Judith Skaptason"'
Autor:
Kia Sepassi, Xiahou Deng, Brad M. Savall, Wall Jessica L, Nicholas I. Carruthers, Hong Ao, Anindya Bhattacharya, Brian Lord, Michael A. Letavic, Tatiana Koudriakova, Kevin J. Coe, Anita Everson, Freddy Schoetens, Devin M. Swanson, Meri De Angelis, Brian Scott, Timothy W. Lovenberg, Jason C. Rech, Judith Skaptason, Qi Wang
Publikováno v:
Journal of Medicinal Chemistry. 59:8535-8548
The synthesis and SAR of a series of 4,5,6,7-tetrahydro-imidazo[4,5-c]pyridine P2X7 antagonists are described. Addressing P2X7 affinity and liver microsomal stability issues encountered with this template afforded methyl substituted 4,5,6,7-tetrahydr
Autor:
Jennifer A. Digits, Jeff Elleraas, Gang Zhang, Ketan S. Gajiwala, Pei-Pei Kung, Michael J. Hickey, Min-Jean Yin, Michael Zientek, Buwen Huang, Caroline Rodgers, Shinji Yamazaki, Michael R. Gehring, Joe Zhongxiang Zhou, Jay F. Davies, Judith Skaptason, Jeff Wang, David Neul, Pramod P. Mehta
Publikováno v:
Journal of Medicinal Chemistry. 53:499-503
The discovery and optimization of potency and metabolic stability of a novel class of dihyroxyphenylisoindoline amides as Hsp90 inhibitors are presented. Optimization of a screening hit using structure-based design and modification of log D and chemi
Autor:
Judith Skaptason, Janice Bower, Emi Kimoto, Timothy G. Heath, David Romero, Lisa N. Toth, Shinji Yamazaki
Publikováno v:
Drug Metabolism and Disposition. 37:937-945
The primary objective of this study was to demonstrate the use of stable isotope (SI)-labeled compound as an approach for pharmacokinetic analysis such as fraction absorbed, hepatic extraction ratio, and fraction metabolized from the parent drug to a
Autor:
Karen Lundgren, Maria E. Arango, Cathy Zhang, Zhengming Yan, Joseph Higgins, Michelle Yang, Jim Nonomiya, Patrick M. O'Connor, Andrea Huber, Cristina Lewis, Sharon Price, Gabriel Troche, Judith Skaptason, Tatiana Koudriakova, Bart Jessen, Steve Bender, Gerrit Los
Publikováno v:
Molecular Cancer Therapeutics. 7:818-828
AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. Here, we report the potent antitumor efficacies of AG-012986 against mul
Publikováno v:
Methods in Pharmacology and Toxicology ISBN: 9781627037419
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d6460e0253b099673cdf668d85474267
https://doi.org/10.1007/978-1-62703-742-6_18
https://doi.org/10.1007/978-1-62703-742-6_18
Autor:
Jeffrey R. Koup, Helen Y. Zou, Shinji Yamazaki, James G. Christensen, Judith Skaptason, Tatiana Koudriakova, David Romero, Joseph H. Lee, Bill J. Smith
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 36(7)
(R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine (PF02341066) was identified as an orally available, ATP-competitive small molecule inhibitor of cMet receptor tyrosine kinase. The objectives of th