Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Heather Grbic"'
Autor:
Monica Patel, Mita Patel, Thomas Wai-Ho Lee, John Lord, Brian Christopher Raudenbush, Heather Grbic, Hossein Razavi, Darren Disalvo, David Joseph, Maryanne L. Brown, Alan David Swinamer, Della White, Siqi Lin, Karen Berg, Alison Kukulka, David S. Thomson, Christopher Ronald Sarko, Kim Fletcher, Pingrong Liu, Can Mao, Laura Amodeo, Christian Harcken
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(3)
A HTS screen for CCR1 antagonists afforded a novel sub-micromolar hit 5 containing a pyrazole core. In this report the design, optimization, and SAR of novel CCR1 antagonists based on a pyrazole core motif is presented. Optimization led to the advanc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e864650ab9ef4500685ce7b687049a7
https://pubmed.ncbi.nlm.nih.gov/30455146
https://pubmed.ncbi.nlm.nih.gov/30455146
Autor:
Heather Grbic, Monica Patel, Micheal B. Fisher, Lifen Wu, Edward Walker, Doris Riether, Sabine Löbbe, Patricia Amouzegh, David S. Thomson, Claudia Albrecht, Brian Linehan, Daw-Tsun Shih, Monika Ermann, Mita Patel, John D. Scott, Renee Zindell, Mark J. Gemkow, Paul Kaplita, Svenja Block, Cody L. Fullenwider
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4276-4280
A high throughput screening campaign identified aryl 1,4-diazepane compounds as potent and selective cannabinoid receptor 2 agonists as compared to cannabinoid receptor 1. This class of compounds suffered from poor drug-like parameters as well as low
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a944fcd194fddad63c17f449e5277bf3
https://doi.org/10.1016/j.bmcl.2011.05.068
https://doi.org/10.1016/j.bmcl.2011.05.068
Autor:
Edward Walker, Doris Riether, Sabine Löbbe, Jenkins James Edward, Clemens Möller, Mark J. Gemkow, Dan Albaugh, Lifen Wu, Michael B. Fisher, Daw-Tsun Shih, Angela Berry, Achim Sauer, Beatriz Noya-Marino, Heather Grbic, Monika Ermann, David S. Thomson, Claudia Albrecht, Pier F. Cirillo, Kathy O’Shea
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2011-2016
A high-throughput screening campaign has identified 1,4-diazepane compounds which are potent Cannabinoid receptor 2 agonists with excellent selectivity against the Cannabinoid receptor 1. This class of compounds suffered from low metabolic stability.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8d7df6ea42df00b701d6e848440cefc
https://doi.org/10.1016/j.bmcl.2011.02.017
https://doi.org/10.1016/j.bmcl.2011.02.017
Autor:
Kathy O’Shea, Denice M. Spero, Ronald L. Magolda, Mario G. Cardozo, Lisa H. Liu, Hanbo Hu, Derek Cogan, Heather Grbic, Thomas M. Farrell, John P. Wolak, John D. Ginn, Della White, Deborah D. Jeanfavre, Mohammed A. Kashem, Maryanne L. Brown, Anthony S. Prokopowicz, Carol Ann Homon, Erick R. R. Young, Joseph R. Woska, Paul Kaplita, Darren Disalvo, Georg Dahmann, Charles L. Cywin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:225-230
An uHTS campaign was performed to identify selective inhibitors of PKC-theta. Initial triaging of the hit set based on selectivity and historical analysis led to the identification of 2,4-diamino-5-nitropyrimidines as potent and selective PKC-theta i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a34c352960493e0ce0044cbad949680
https://doi.org/10.1016/j.bmcl.2006.09.056
https://doi.org/10.1016/j.bmcl.2006.09.056
Publikováno v:
Journal of the Association for Laboratory Automation. 10:140-148
An evolving union of high throughput screening (HTS) and absorption, distribution, metabolism, excretion, and toxicology (ADMET) technologies have transformed drug discovery. Human tissue-based, in vitro ADMET assays can efficiently generate reliable
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d95071c927e805061228209b87964ecc
https://doi.org/10.1016/j.jala.2005.03.004
https://doi.org/10.1016/j.jala.2005.03.004