JUMP Cell Painting dataset: morphological impact of 136,000 chemical and genetic perturbations

Autor: Srinivas Niranj Chandrasekaran, Jeanelle Ackerman, Eric Alix, D. Michael Ando, John Arevalo, Melissa Bennion, Nicolas Boisseau, Adriana Borowa, Justin D. Boyd, Laurent Brino, Patrick J. Byrne, Hugo Ceulemans, Carolyn Ch’ng, Beth A. Cimini, Djork-Arne Clevert, Nicole Deflaux, John G Doench, Thierry Dorval, Regis Doyonnas, Vincenza Dragone, Ola Engkvist, Patrick W. Faloon, Briana Fritchman, Florian Fuchs, Sakshi Garg, Tamara J. Gilbert, David Glazer, David Gnutt, Amy Goodale, Jeremy Grignard, Judith Guenther, Yu Han, Zahra Hanifehlou, Santosh Hariharan, Desiree Hernandez, Shane R Horman, Gisela Hormel, Michael Huntley, Ilknur Icke, Makiyo Iida, Christina B. Jacob, Steffen Jaensch, Jawahar Khetan, Maria Kost-Alimova, Tomasz Krawiec, Daniel Kuhn, Charles-Hugues Lardeau, Amanda Lembke, Francis Lin, Kevin D. Little, Kenneth R. Lofstrom, Sofia Lotfi, David J. Logan, Yi Luo, Franck Madoux, Paula A. Marin Zapata, Brittany A. Marion, Glynn Martin, Nicola Jane McCarthy, Lewis Mervin, Lisa Miller, Haseeb Mohamed, Tiziana Monteverde, Elizabeth Mouchet, Barbara Nicke, Arnaud Ogier, Anne-Laure Ong, Marc Osterland, Magdalena Otrocka, Pieter J. Peeters, James Pilling, Stefan Prechtl, Chen Qian, Krzysztof Rataj, David E Root, Sylvie K. Sakata, Simon Scrace, Hajime Shimizu, David Simon, Peter Sommer, Craig Spruiell, Iffat Sumia, Susanne E Swalley, Hiroki Terauchi, Amandine Thibaudeau, Amy Unruh, Jelle Van de Waeter, Michiel Van Dyck, Carlo van Staden, Michał Warchoł, Erin Weisbart, Amélie Weiss, Nicolas Wiest-Daessle, Guy Williams, Shan Yu, Bolek Zapiec, Marek Żyła, Shantanu Singh, Anne E. Carpenter

Image-based profiling has emerged as a powerful technology for various steps in basic biological and pharmaceutical discovery, but the community has lacked a large, public reference set of data from chemical and genetic perturbations. Here we present

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0ad294298f87b0d35776a491fba28d7f
https://doi.org/10.1101/2023.03.23.534023

Rhodium(III)-Catalyzed C–H Activation: Annulation of Petrochemical Feedstocks for the Construction of Isoquinolone Scaffolds

Autor: Dehuan Kong, Wei Li, Ryan L. Patman, Sylvie K. Sakata, Indrawan James Mcalpine, Joyann S. Barber, Nicole Sun, Sajiv Krishnan Nair

Publikováno v: Synlett. 32:202-206

We describe a simple and robust procedure for the Rh(III)-catalyzed [4+2] cycloaddition of feedstock gases enabled through C–H activation. A diverse set of 3,4-dihydroisoquinolones and 3-methylisoquinolones have been prepared in good to excellent y

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7fccd9ec827855aa5f064a5ba6a79577
https://doi.org/10.1055/s-0040-1706548

Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis

Autor: Bruce Allen Lefker, Melissa Holmstrom, Christopher John Helal, Oleg Zakaryants, Chakrapani Subramanyam, Mark W. Bundesmann, Jacquelyn Klug-McLeod, Dale Gordon Mcleod, Susan Hammond, Sylvie K. Sakata

Publikováno v: ACS Med Chem Lett

[Image: see text] Many pharmaceutical companies have invested millions of dollars in establishing internal chemical stores to provide reliable access to large numbers of building blocks (BB) for the synthesis of new molecules, especially for the time

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1dd9241dc1d1559fa5091e91784140d
https://pubmed.ncbi.nlm.nih.gov/31413793

Introduction of a Crystalline, Shelf-Stable Reagent for the Synthesis of Sulfur(VI) Fluorides

Autor: Hua Zhou, Sylvie K. Sakata, Dianpeng Wang, Butler Todd W, Liu Rongqiang, John M. Humphrey, Christopher John Helal, Edelweiss Evrard, Lise R. Hoth, Paramita Mukherjee, Jeffrey B. Sperry, Christopher W. am Ende

Publikováno v: Organic letters. 20(3)

The design, synthesis, and application of [4-(acetylamino)phenyl]imidodisulfuryl difluoride (AISF), a shelf-stable, crystalline reagent for the synthesis of sulfur(VI) fluorides, is described. The utility of AISF is demonstrated in the synthesis of a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d1a519e0126c90b4e17f915aaeba3da
https://pubmed.ncbi.nlm.nih.gov/29327935

Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. 6. Structure−Activity Studies of Orally Bioavailable, 2-Pyridone-Containing Peptidomimetics

Autor: and Rose Ann Ferre, Minerva R. Batugo, Thomas J. Prins, Peter S. Dragovich, Maha B. Kosa, Tove Tuntland, Stephen T. Worland, Fausto Maldonado, Thomas F. Hendrickson, Leora S. Zalman, Lijian Chen, David A. Matthews, Jean-Paul R. Gleeson, Edward L. Brown, Amy K. Patick, Shella A. Fuhrman, James W. Meador, Ru Zhou, Bo Liu, Mark Christopher Guzman, Caroline A. Lee, Sylvie K. Sakata

Publikováno v: Journal of Medicinal Chemistry. 45:1607-1623

The structure-based design, chemical synthesis, and biological evaluation of various 2-pyridone-containing human rhinovirus (HRV) 3C protease (3CP) inhibitors are described. These compounds are comprised of a peptidomimetic binding determinant and a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3571102e02d05c8a04310cc97968a7bd
https://doi.org/10.1021/jm010469k