Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2.
Han Wee Ong, Xuan Yang, Jeffery L Smith, Sharon Taft-Benz, Stefanie Howell, Rebekah J Dickmander, Tammy M Havener, Marcia K Sanders, Jason W Brown, Rafael M Couñago and 7 more
Article in Molecules (Basel, Switzerland), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
2 · The registry
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
5 · Who and what money
Authors and funding
17 authors.
Han Wee OngRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.ORCID 0000-0003-3232-2373
Xuan YangRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.
Jeffery L SmithStructural Genomics Consortium (SGC) and Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.ORCID 0000-0003-2189-0420
Sharon Taft-BenzRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.
Stefanie HowellStructural Genomics Consortium (SGC) and Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Rebekah J DickmanderRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.
Tammy M HavenerStructural Genomics Consortium (SGC) and Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Marcia K SandersRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.
Jason W BrownTakeda Development Center Americas, Inc., San Diego, CA 92121, USA.
Rafael M CouñagoStructural Genomics Consortium (SGC) and Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.ORCID 0000-0003-1847-5090
Edcon ChangTakeda Development Center Americas, Inc., San Diego, CA 92121, USA.ORCID 0000-0001-9534-0291
Andreas KrämerStructural Genomics Consortium (SGC), Institute of Pharmaceutical Chemistry, Goethe University Frankfurt am Main, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.ORCID 0000-0003-3294-2660
Nathaniel J MoormanRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.
Mark HeiseRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.
Alison D AxtmanRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.ORCID 0000-0003-4779-9932
David H DrewryRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.ORCID 0000-0001-5973-5798
Timothy M WillsonRapidly Emerging Antiviral Drug Development Initiative (READDI), Chapel Hill, NC 27599, USA.ORCID 0000-0003-4181-8223
Funding
Illuminating Function of the Understudied Druggable KinomeU24DK116204 · NIDDK · UNIV OF NORTH CAROLINA CHAPEL HILL · PI JOHNSON, GARY L. · 2017 to 2022
$13.6M
Request for a 500 MHz NMR console and nitrogen-cooled cryoprobeS10OD032476 · OD · UNIV OF NORTH CAROLINA CHAPEL HILL · PI LEE, ANDREW L · 2022 to 2022
$599k
Department of Defense ALSRP award AL190107Millennium Pharmaceuticals (Takeda) N/ANC Biotech Center Institutional support grant 2018-IDG-1030NIDDK NIH HHS U24 DK116204NIH HHS S10 OD032476NIH HHS S10OD032476NIH Illuminating the Druggable Genome 1U24DK116204-01Rapidly Emerging Antiviral Drug Development Initiative (READDI) N/AStructural Genomics Consortium (SGC) N/A
6 · The paper itself
Abstract
The host kinase casein kinase 2 (CSNK2) has been proposed to be an antiviral target against β-coronaviral infection. To pharmacologically validate CSNK2 as a drug target in vivo, potent and selective CSNK2 inhibitors with good pharmacokinetic properties are required. Inhibitors based on the pyrazolo[1,5-
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.
Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2. · full record | OpenQuestion