Matches in SemOpenAlex for { <https://semopenalex.org/work/W3014882016> ?p ?o ?g. }
- W3014882016 endingPage "6693" @default.
- W3014882016 startingPage "6679" @default.
- W3014882016 abstract "Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new technologies and strategies are aiding in the target's resurgence. As previously reported, the tetrahydropyridopyrimidines were identified as irreversible covalent inhibitors of KRASG12C that bind in the switch-II pocket of KRAS and make a covalent bond to cysteine 12. Using structure-based drug design in conjunction with a focused in vitro absorption, distribution, metabolism and excretion screening approach, analogues were synthesized to increase the potency and reduce metabolic liabilities of this series. The discovery of the clinical development candidate MRTX849 as a potent, selective covalent inhibitor of KRASG12C is described." @default.
- W3014882016 created "2020-04-10" @default.
- W3014882016 creator A5008501938 @default.
- W3014882016 creator A5009869639 @default.
- W3014882016 creator A5010395017 @default.
- W3014882016 creator A5011083469 @default.
- W3014882016 creator A5013889220 @default.
- W3014882016 creator A5016544434 @default.
- W3014882016 creator A5017750917 @default.
- W3014882016 creator A5020361767 @default.
- W3014882016 creator A5027555707 @default.
- W3014882016 creator A5029014694 @default.
- W3014882016 creator A5034410111 @default.
- W3014882016 creator A5036014338 @default.
- W3014882016 creator A5041504457 @default.
- W3014882016 creator A5042557251 @default.
- W3014882016 creator A5046487180 @default.
- W3014882016 creator A5051720564 @default.
- W3014882016 creator A5052279694 @default.
- W3014882016 creator A5057285781 @default.
- W3014882016 creator A5057797392 @default.
- W3014882016 creator A5059989618 @default.
- W3014882016 creator A5061390774 @default.
- W3014882016 creator A5062077509 @default.
- W3014882016 creator A5064251187 @default.
- W3014882016 creator A5068350117 @default.
- W3014882016 creator A5069948075 @default.
- W3014882016 creator A5071835934 @default.
- W3014882016 creator A5074923974 @default.
- W3014882016 creator A5080771669 @default.
- W3014882016 creator A5081491244 @default.
- W3014882016 creator A5083558388 @default.
- W3014882016 creator A5084006763 @default.
- W3014882016 creator A5085606910 @default.
- W3014882016 creator A5086754835 @default.
- W3014882016 creator A5089383748 @default.
- W3014882016 date "2020-04-06" @default.
- W3014882016 modified "2023-10-10" @default.
- W3014882016 title "Identification of the Clinical Development Candidate <b>MRTX849</b>, a Covalent KRAS<sup>G12C</sup> Inhibitor for the Treatment of Cancer" @default.
- W3014882016 cites W152943885 @default.
- W3014882016 cites W1977059612 @default.
- W3014882016 cites W1998948060 @default.
- W3014882016 cites W2004132523 @default.
- W3014882016 cites W2026128118 @default.
- W3014882016 cites W2052490505 @default.
- W3014882016 cites W2068332174 @default.
- W3014882016 cites W2116482041 @default.
- W3014882016 cites W2128339707 @default.
- W3014882016 cites W2134917212 @default.
- W3014882016 cites W2161434860 @default.
- W3014882016 cites W2233032895 @default.
- W3014882016 cites W2300615341 @default.
- W3014882016 cites W2501247313 @default.
- W3014882016 cites W2540525654 @default.
- W3014882016 cites W2560367892 @default.
- W3014882016 cites W2597182072 @default.
- W3014882016 cites W2732767128 @default.
- W3014882016 cites W2785187242 @default.
- W3014882016 cites W2796153225 @default.
- W3014882016 cites W2800484366 @default.
- W3014882016 cites W2804697234 @default.
- W3014882016 cites W2900061002 @default.
- W3014882016 cites W2902268901 @default.
- W3014882016 cites W2951887320 @default.
- W3014882016 cites W2982321167 @default.
- W3014882016 cites W2982602983 @default.
- W3014882016 cites W307680137 @default.
- W3014882016 doi "https://doi.org/10.1021/acs.jmedchem.9b02052" @default.
- W3014882016 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32250617" @default.
- W3014882016 hasPublicationYear "2020" @default.
- W3014882016 type Work @default.
- W3014882016 sameAs 3014882016 @default.
- W3014882016 citedByCount "248" @default.
- W3014882016 countsByYear W30148820162020 @default.
- W3014882016 countsByYear W30148820162021 @default.
- W3014882016 countsByYear W30148820162022 @default.
- W3014882016 countsByYear W30148820162023 @default.
- W3014882016 crossrefType "journal-article" @default.
- W3014882016 hasAuthorship W3014882016A5008501938 @default.
- W3014882016 hasAuthorship W3014882016A5009869639 @default.
- W3014882016 hasAuthorship W3014882016A5010395017 @default.
- W3014882016 hasAuthorship W3014882016A5011083469 @default.
- W3014882016 hasAuthorship W3014882016A5013889220 @default.
- W3014882016 hasAuthorship W3014882016A5016544434 @default.
- W3014882016 hasAuthorship W3014882016A5017750917 @default.
- W3014882016 hasAuthorship W3014882016A5020361767 @default.
- W3014882016 hasAuthorship W3014882016A5027555707 @default.
- W3014882016 hasAuthorship W3014882016A5029014694 @default.
- W3014882016 hasAuthorship W3014882016A5034410111 @default.
- W3014882016 hasAuthorship W3014882016A5036014338 @default.
- W3014882016 hasAuthorship W3014882016A5041504457 @default.
- W3014882016 hasAuthorship W3014882016A5042557251 @default.
- W3014882016 hasAuthorship W3014882016A5046487180 @default.
- W3014882016 hasAuthorship W3014882016A5051720564 @default.
- W3014882016 hasAuthorship W3014882016A5052279694 @default.
- W3014882016 hasAuthorship W3014882016A5057285781 @default.
- W3014882016 hasAuthorship W3014882016A5057797392 @default.
- W3014882016 hasAuthorship W3014882016A5059989618 @default.