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. 2024 Feb 9;67(4):2369–2378. doi: 10.1021/acs.jmedchem.3c01938

Figure 1.

Figure 1

Representative known protease inhibitors. A) Initial ReFRAME library hits identified as moderate (low μM) potency inhibitors of SARS-CoV-2. B) Peptidomimetic SARS-CoV-2 CLpro inhibitors PF-00835231 (Pfizer), PF-07321332 (Pfizer), and GC376 (Anivive). Generally, up to four distinct structural regions are found in all peptidomimetic CLpro inhibitors: warhead (WH), P1 (amino acid 1, recognition element with a lactam side chain), P2 (AA 2), and P3 (a N-Cap, or a third AA). Common warheads include hydroxymethyl ketones (e.g., PF-00835231), nitriles (e.g., nirmatrelvir), aldehydes, or bisulfite adducts thereof (e.g., GC376), and aryloxymethyl ketones (e.g., emricasan).