Matches in SemOpenAlex for { <https://semopenalex.org/work/W3035584768> ?p ?o ?g. }
Showing items 1 to 84 of
84
with 100 items per page.
- W3035584768 abstract "Abstract The Published Kinase Inhibitor Set (PKIS) is a publicly-available chemogenomic library distributed to more than 300 laboratories by GlaxoSmithKline (GSK) between 2011–2015 and by SGC-UNC from 2015–2017. Screening this library of well-annotated, published kinase inhibitors has yielded a plethora of data in diverse therapeutic and scientific areas, funded applications, publications, and provided impactful pre-clinical results. Based on kinome-wide screening results, we report a thorough investigation of one PKIS compound, GW296115, as an inhibitor of several members of the Illuminating the Druggable Genome (IDG) list of understudied dark kinases. Specifically, GW296115 validates as a potent lead chemical tool that inhibits six IDG kinases with IC 50 values less than 100nM. Focused studies establish that GW296115 is cell active, and directly engages BRSK2. Further evaluation showed that GW296115 downregulates BRSK2-driven phosphorylation and downstream signaling. Summary Statement GW296115 inhibits understudied kinases, including BRSK2, with IC 50 values less than 100nM." @default.
- W3035584768 created "2020-06-19" @default.
- W3035584768 creator A5007350449 @default.
- W3035584768 creator A5022973468 @default.
- W3035584768 creator A5032297873 @default.
- W3035584768 creator A5075720582 @default.
- W3035584768 creator A5078651083 @default.
- W3035584768 date "2020-06-16" @default.
- W3035584768 modified "2023-10-16" @default.
- W3035584768 title "PKIS Deep Dive Yields a Chemical Starting Point for Dark Kinases and a Cell Active BRSK2 Inhibitor" @default.
- W3035584768 cites W1918079945 @default.
- W3035584768 cites W1969704231 @default.
- W3035584768 cites W1970637701 @default.
- W3035584768 cites W2023724309 @default.
- W3035584768 cites W2030205108 @default.
- W3035584768 cites W2047985610 @default.
- W3035584768 cites W2080693065 @default.
- W3035584768 cites W2086286404 @default.
- W3035584768 cites W2115286566 @default.
- W3035584768 cites W2138319716 @default.
- W3035584768 cites W2152265294 @default.
- W3035584768 cites W2160411684 @default.
- W3035584768 cites W2569825304 @default.
- W3035584768 cites W2767051972 @default.
- W3035584768 cites W2769161116 @default.
- W3035584768 cites W2804509374 @default.
- W3035584768 cites W2888326900 @default.
- W3035584768 cites W2888510964 @default.
- W3035584768 cites W2981620099 @default.
- W3035584768 cites W2996359815 @default.
- W3035584768 cites W3034250721 @default.
- W3035584768 doi "https://doi.org/10.1101/2020.06.15.153072" @default.
- W3035584768 hasPublicationYear "2020" @default.
- W3035584768 type Work @default.
- W3035584768 sameAs 3035584768 @default.
- W3035584768 citedByCount "0" @default.
- W3035584768 crossrefType "posted-content" @default.
- W3035584768 hasAuthorship W3035584768A5007350449 @default.
- W3035584768 hasAuthorship W3035584768A5022973468 @default.
- W3035584768 hasAuthorship W3035584768A5032297873 @default.
- W3035584768 hasAuthorship W3035584768A5075720582 @default.
- W3035584768 hasAuthorship W3035584768A5078651083 @default.
- W3035584768 hasBestOaLocation W30355847681 @default.
- W3035584768 hasConcept C104317684 @default.
- W3035584768 hasConcept C10679952 @default.
- W3035584768 hasConcept C11960822 @default.
- W3035584768 hasConcept C184235292 @default.
- W3035584768 hasConcept C185592680 @default.
- W3035584768 hasConcept C41008148 @default.
- W3035584768 hasConcept C54174078 @default.
- W3035584768 hasConcept C55493867 @default.
- W3035584768 hasConcept C70721500 @default.
- W3035584768 hasConcept C74187038 @default.
- W3035584768 hasConcept C86803240 @default.
- W3035584768 hasConceptScore W3035584768C104317684 @default.
- W3035584768 hasConceptScore W3035584768C10679952 @default.
- W3035584768 hasConceptScore W3035584768C11960822 @default.
- W3035584768 hasConceptScore W3035584768C184235292 @default.
- W3035584768 hasConceptScore W3035584768C185592680 @default.
- W3035584768 hasConceptScore W3035584768C41008148 @default.
- W3035584768 hasConceptScore W3035584768C54174078 @default.
- W3035584768 hasConceptScore W3035584768C55493867 @default.
- W3035584768 hasConceptScore W3035584768C70721500 @default.
- W3035584768 hasConceptScore W3035584768C74187038 @default.
- W3035584768 hasConceptScore W3035584768C86803240 @default.
- W3035584768 hasLocation W30355847681 @default.
- W3035584768 hasLocation W30355847682 @default.
- W3035584768 hasLocation W30355847683 @default.
- W3035584768 hasOpenAccess W3035584768 @default.
- W3035584768 hasPrimaryLocation W30355847681 @default.
- W3035584768 hasRelatedWork W10562162 @default.
- W3035584768 hasRelatedWork W3698395 @default.
- W3035584768 hasRelatedWork W4001122 @default.
- W3035584768 hasRelatedWork W447235 @default.
- W3035584768 hasRelatedWork W4700414 @default.
- W3035584768 hasRelatedWork W611565 @default.
- W3035584768 hasRelatedWork W6298287 @default.
- W3035584768 hasRelatedWork W790358 @default.
- W3035584768 hasRelatedWork W8074829 @default.
- W3035584768 hasRelatedWork W8735992 @default.
- W3035584768 isParatext "false" @default.
- W3035584768 isRetracted "false" @default.
- W3035584768 magId "3035584768" @default.
- W3035584768 workType "article" @default.