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Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.

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Title: Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
Authors: Szychowski J; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Papp R; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Dietrich E; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Liu B; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Vallée F; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Leclaire ME; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Fourtounis J; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Martino G; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Perryman AL; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Pau V; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada., Yin SY; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Mader P; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada., Roulston A; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Truchon JF; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Marshall CG; Repare Therapeutics, 1 Broadway, 15th Floor, Cambridge, Massachusetts 02142, United States., Diallo M; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Duffy NM; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Stocco R; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Godbout C; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Bonneau-Fortin A; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Kryczka R; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Bhaskaran V; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Mao D; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada., Orlicky S; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada., Beaulieu P; OmegaChem Inc., 480 Rue Perreault, Saint-Romuald, QC G6W 7V6, Canada., Turcotte P; AdMare BioInnovations, 7171 Frederick-Banting, Montréal, QC H4S 1Z9, Canada., Kurinov I; Department of Chemistry and Chemical Biology, Cornell University, NE-CAT, Argonne, Illinois 60439, United States., Sicheri F; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.; Departments of Biochemistry and Molecular Genetics, University of Toronto, Ontario M5S 1A8, Canada., Mamane Y; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Gallant M; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada., Black WC; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Source: Journal of medicinal chemistry [J Med Chem] 2022 Aug 11; Vol. 65 (15), pp. 10251-10284. Date of Electronic Publication: 2022 Jul 26.
Publication Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
FullText Text:
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PubType: Academic Journal
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  Data: Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
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  Data: <searchLink fieldCode="AU" term="%22Szychowski+J%22">Szychowski J</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Papp+R%22">Papp R</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Dietrich+E%22">Dietrich E</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Liu+B%22">Liu B</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Vallée+F%22">Vallée F</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Leclaire+ME%22">Leclaire ME</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Fourtounis+J%22">Fourtounis J</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Martino+G%22">Martino G</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Perryman+AL%22">Perryman AL</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Pau+V%22">Pau V</searchLink>; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.<br /><searchLink fieldCode="AU" term="%22Yin+SY%22">Yin SY</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Mader+P%22">Mader P</searchLink>; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.<br /><searchLink fieldCode="AU" term="%22Roulston+A%22">Roulston A</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Truchon+JF%22">Truchon JF</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Marshall+CG%22">Marshall CG</searchLink>; Repare Therapeutics, 1 Broadway, 15th Floor, Cambridge, Massachusetts 02142, United States.<br /><searchLink fieldCode="AU" term="%22Diallo+M%22">Diallo M</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Duffy+NM%22">Duffy NM</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Stocco+R%22">Stocco R</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Godbout+C%22">Godbout C</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Bonneau-Fortin+A%22">Bonneau-Fortin A</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Kryczka+R%22">Kryczka R</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Bhaskaran+V%22">Bhaskaran V</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Mao+D%22">Mao D</searchLink>; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.<br /><searchLink fieldCode="AU" term="%22Orlicky+S%22">Orlicky S</searchLink>; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.<br /><searchLink fieldCode="AU" term="%22Beaulieu+P%22">Beaulieu P</searchLink>; OmegaChem Inc., 480 Rue Perreault, Saint-Romuald, QC G6W 7V6, Canada.<br /><searchLink fieldCode="AU" term="%22Turcotte+P%22">Turcotte P</searchLink>; AdMare BioInnovations, 7171 Frederick-Banting, Montréal, QC H4S 1Z9, Canada.<br /><searchLink fieldCode="AU" term="%22Kurinov+I%22">Kurinov I</searchLink>; Department of Chemistry and Chemical Biology, Cornell University, NE-CAT, Argonne, Illinois 60439, United States.<br /><searchLink fieldCode="AU" term="%22Sicheri+F%22">Sicheri F</searchLink>; Lunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.; Departments of Biochemistry and Molecular Genetics, University of Toronto, Ontario M5S 1A8, Canada.<br /><searchLink fieldCode="AU" term="%22Mamane+Y%22">Mamane Y</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Gallant+M%22">Gallant M</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.<br /><searchLink fieldCode="AU" term="%22Black+WC%22">Black WC</searchLink>; Repare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2022 Aug 11; Vol. 65 (15), pp. 10251-10284. <i>Date of Electronic Publication: </i>2022 Jul 26.
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