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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.
    Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: Highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1'' binding site (2014), Bioorg. Med. Chem., 22, 5487-5505.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
4-([(2-([(3-methoxyphenyl)methyl]carbamoyl)-4-oxo-3H,4H-thieno[2,3-d]pyrimidin-5-yl)methoxy]methyl)benzoic acid highly potent and selective MMP-13 inhibitor. Compound shows shows more than 2600fold selectivity over the other related metalloenzymes. The disodium salt formulation is well absorbed in all species tested at the oral dose of 10-20 mg/kg. Compound is active in in bovine nasal cartilage explants assay Homo sapiens
N-(3-methoxybenzyl)-4-oxo-3,4-dihydroquinazoline-2-carboxamide lead compound for the development of thieno[2,3-d]pyrimidine-2-carboxamide inhibitors Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P45452
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000000069
-
 pH 7.5, 37°C Homo sapiens 4-([(2-([(3-methoxyphenyl)methyl]carbamoyl)-4-oxo-3H,4H-thieno[2,3-d]pyrimidin-5-yl)methoxy]methyl)benzoic acid
0.000012
-
 pH 7.5, 37°C Homo sapiens N-(3-methoxybenzyl)-4-oxo-3,4-dihydroquinazoline-2-carboxamide