Matches in SemOpenAlex for { <https://semopenalex.org/work/W2807030217> ?p ?o ?g. }
- W2807030217 endingPage "5244" @default.
- W2807030217 startingPage "5235" @default.
- W2807030217 abstract "Janus kinases (JAKs) have been demonstrated to be critical in cytokine signaling and have thus been implicated in both cancer and inflammatory diseases. The JAK family consists of four highly homologous members: JAK1–3 and TYK2. The development of small-molecule inhibitors that are selective for a specific family member would represent highly desirable tools for deconvoluting the intricacies of JAK family biology. Herein, we report the discovery of a potent JAK1 inhibitor, 24, which displays ∼1000-fold selectivity over the other highly homologous JAK family members (determined by biochemical assays), while also possessing good selectivity over other kinases (determined by panel screening). Moreover, this compound was demonstrated to be orally bioavailable and possesses acceptable pharmacokinetic parameters. In an in vivo study, the compound was observed to dose dependently modulate the phosphorylation of STAT3 (a downstream marker of JAK1 inhibition)." @default.
- W2807030217 created "2018-06-13" @default.
- W2807030217 creator A5001064231 @default.
- W2807030217 creator A5010293166 @default.
- W2807030217 creator A5013946717 @default.
- W2807030217 creator A5016791761 @default.
- W2807030217 creator A5024143296 @default.
- W2807030217 creator A5026616665 @default.
- W2807030217 creator A5030065450 @default.
- W2807030217 creator A5033169967 @default.
- W2807030217 creator A5033356973 @default.
- W2807030217 creator A5038935034 @default.
- W2807030217 creator A5040552786 @default.
- W2807030217 creator A5042406680 @default.
- W2807030217 creator A5043152088 @default.
- W2807030217 creator A5044437841 @default.
- W2807030217 creator A5047822719 @default.
- W2807030217 creator A5047829223 @default.
- W2807030217 creator A5048516275 @default.
- W2807030217 creator A5048914331 @default.
- W2807030217 creator A5054565788 @default.
- W2807030217 creator A5057480173 @default.
- W2807030217 creator A5059472140 @default.
- W2807030217 creator A5065356202 @default.
- W2807030217 creator A5066313823 @default.
- W2807030217 creator A5067040049 @default.
- W2807030217 creator A5070023163 @default.
- W2807030217 creator A5075510757 @default.
- W2807030217 creator A5078391610 @default.
- W2807030217 creator A5078687678 @default.
- W2807030217 creator A5091003796 @default.
- W2807030217 date "2018-06-01" @default.
- W2807030217 modified "2023-10-09" @default.
- W2807030217 title "Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors" @default.
- W2807030217 cites W1484324193 @default.
- W2807030217 cites W1489601464 @default.
- W2807030217 cites W1952507411 @default.
- W2807030217 cites W1975947882 @default.
- W2807030217 cites W1992197271 @default.
- W2807030217 cites W1995629248 @default.
- W2807030217 cites W1996112634 @default.
- W2807030217 cites W2007501395 @default.
- W2807030217 cites W2014737409 @default.
- W2807030217 cites W2016116775 @default.
- W2807030217 cites W2021277288 @default.
- W2807030217 cites W2034881138 @default.
- W2807030217 cites W2041762667 @default.
- W2807030217 cites W2042386826 @default.
- W2807030217 cites W2049726262 @default.
- W2807030217 cites W2054417387 @default.
- W2807030217 cites W2056961869 @default.
- W2807030217 cites W2064540997 @default.
- W2807030217 cites W2067637255 @default.
- W2807030217 cites W2075490622 @default.
- W2807030217 cites W2076841538 @default.
- W2807030217 cites W2079787008 @default.
- W2807030217 cites W2087687370 @default.
- W2807030217 cites W2099805317 @default.
- W2807030217 cites W2107345670 @default.
- W2807030217 cites W2119146437 @default.
- W2807030217 cites W2123633897 @default.
- W2807030217 cites W2132416790 @default.
- W2807030217 cites W2132631303 @default.
- W2807030217 cites W2160371778 @default.
- W2807030217 cites W2444392663 @default.
- W2807030217 cites W2532500892 @default.
- W2807030217 cites W2781491897 @default.
- W2807030217 cites W2915389437 @default.
- W2807030217 doi "https://doi.org/10.1021/acs.jmedchem.8b00076" @default.
- W2807030217 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29856615" @default.
- W2807030217 hasPublicationYear "2018" @default.
- W2807030217 type Work @default.
- W2807030217 sameAs 2807030217 @default.
- W2807030217 citedByCount "15" @default.
- W2807030217 countsByYear W28070302172018 @default.
- W2807030217 countsByYear W28070302172019 @default.
- W2807030217 countsByYear W28070302172020 @default.
- W2807030217 countsByYear W28070302172022 @default.
- W2807030217 countsByYear W28070302172023 @default.
- W2807030217 crossrefType "journal-article" @default.
- W2807030217 hasAuthorship W2807030217A5001064231 @default.
- W2807030217 hasAuthorship W2807030217A5010293166 @default.
- W2807030217 hasAuthorship W2807030217A5013946717 @default.
- W2807030217 hasAuthorship W2807030217A5016791761 @default.
- W2807030217 hasAuthorship W2807030217A5024143296 @default.
- W2807030217 hasAuthorship W2807030217A5026616665 @default.
- W2807030217 hasAuthorship W2807030217A5030065450 @default.
- W2807030217 hasAuthorship W2807030217A5033169967 @default.
- W2807030217 hasAuthorship W2807030217A5033356973 @default.
- W2807030217 hasAuthorship W2807030217A5038935034 @default.
- W2807030217 hasAuthorship W2807030217A5040552786 @default.
- W2807030217 hasAuthorship W2807030217A5042406680 @default.
- W2807030217 hasAuthorship W2807030217A5043152088 @default.
- W2807030217 hasAuthorship W2807030217A5044437841 @default.
- W2807030217 hasAuthorship W2807030217A5047822719 @default.
- W2807030217 hasAuthorship W2807030217A5047829223 @default.
- W2807030217 hasAuthorship W2807030217A5048516275 @default.
- W2807030217 hasAuthorship W2807030217A5048914331 @default.