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Optimization of α-Fluoro, β-Heteroaryl Acrylamide Warheads for KRASG12C Active-State Inhibition.

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Title: Optimization of α-Fluoro, β-Heteroaryl Acrylamide Warheads for KRASG12C Active-State Inhibition.
Authors: Condakes ML; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Civiello RL; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Venables BL; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Danahy DB; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Moore RR; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Balachander SB; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Chourb LS; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Downes DP; Bristol Myers Squibb, Route 206 and Province Line Rd., Princeton, New Jersey 08540, United States., Drexler DM; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Dzhekieva L; Bristol Myers Squibb, Route 206 and Province Line Rd., Princeton, New Jersey 08540, United States., El-Samin M; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Lakkaraju SK; Bristol Myers Squibb, Route 206 and Province Line Rd., Princeton, New Jersey 08540, United States., Levins C; Bristol Myers Squibb, Route 206 and Province Line Rd., Princeton, New Jersey 08540, United States., Meyer MJ; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Mosure K; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Parker MF; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Qi J; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Sloane JL; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Soars M; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Stedman J; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Szapiel N; Bristol Myers Squibb, Route 206 and Province Line Rd., Princeton, New Jersey 08540, United States., Thompson RL; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Wu YJ; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Zhang Z; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Zhuo X; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Stewart ML; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States., Bronson JJ; Bristol Myers Squibb, 250 Water St., Cambridge, Massachusetts 02446, United States.
Source: Journal of medicinal chemistry [J Med Chem] 2026 Mar 12; Vol. 69 (5), pp. 5935-5943. Date of Electronic Publication: 2026 Mar 02.
Publication Type: Journal Article
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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IllustrationInfo
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  Data: Optimization of α-Fluoro, β-Heteroaryl Acrylamide Warheads for KRAS<superscript>G12C</superscript> Active-State Inhibition.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2026 Mar 12; Vol. 69 (5), pp. 5935-5943. <i>Date of Electronic Publication: </i>2026 Mar 02.
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  Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22American+Chemical+Society%22">American Chemical Society </searchLink><i>Country of Publication: </i>United States <i>NLM ID: </i>9716531 <i>Publication Model: </i>Print-Electronic <i>Cited Medium: </i>Internet <i>ISSN: </i>1520-4804 (Electronic) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%2200222623%22">00222623 </searchLink><i>NLM ISO Abbreviation: </i>J Med Chem <i>Subsets: </i>MEDLINE
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        Value: 10.1021/acs.jmedchem.5c03307
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