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Literature summary for 3.4.24.B4 extracted from

  • Nara, H.; Sato, K.; Naito, T.; Mototani, H.; Oki, H.; Yamamoto, Y.; Kuno, H.; Santou, T.; Kanzaki, N.; Terauchi, J.; Uchikawa, O.; Kori, M.
    Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach (2014), J. Med. Chem., 57, 8886-8902.
    View publication on PubMed
Search for more literature for 3.4.24.B4

Inhibitors

Inhibitors Comment Organism Structure
4-[2-([6-fluoro-2-[([[3-(methyloxy)phenyl]methyl]amino)-carbonyl]-4-oxo-3,4-dihydroquinazolin-5-yl]oxy)ethyl]-benzoic acid inhibitor exhibits excellent potency and selectivity for MMP-13 over other MMPs. No overt toxicity is observed in a preliminary repeat dose oral toxicity study of compound in rats. A single oral dose of the monosodium salt significantly reduces degradation products released from articular cartilage into the joint cavity in a rat MIA model in vivo Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P45452
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000000039
-
 pH 7.5, 37°C Homo sapiens 4-[2-([6-fluoro-2-[([[3-(methyloxy)phenyl]methyl]amino)-carbonyl]-4-oxo-3,4-dihydroquinazolin-5-yl]oxy)ethyl]-benzoic acid