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Literature summary for 1.14.11.29 extracted from

  • Hamada, M.; Takayama, T.; Shibata, T.; Hiratate, A.; Takahashi, M.; Yashiro, M.; Takayama, N.; Okumura-Kitajima, L.; Koretsune, H.; Kajiyama, H.; Naruse, T.; Kato, S.; Takano, H.; Kakinuma, H.
    Discovery of novel 2-[(4-hydroxy-6-oxo-2,3-dihydro-1H-pyridine-5-carbonyl)amino]acetic acid derivatives as HIF prolyl hydroxylase inhibitors for treatment of renal anemia (2018), Bioorg. Med. Chem. Lett., 28, 1725-1730 .
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
N-(1-[[6-(4-chlorophenoxy)pyridin-3-yl]methyl]-4-hydroxy-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonyl)glycine clinical candidate as PHD2 inhibitor, promotes the production of erythropoietin following oral administration in mice and rats. The predicted half-life in humans is 1.3-5.6 h Homo sapiens
N-(4-hydroxy-1-[[4-(4-methylphenoxy)phenyl]methyl]-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonyl)glycine
-
 Homo sapiens
N-(4-hydroxy-1-[[5-(4-methylphenoxy)pyridin-2-yl]methyl]-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonyl)glycine
-
 Homo sapiens
N-(4-hydroxy-1-[[6-(4-methylphenoxy)pyridin-3-yl]methyl]-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonyl)glycine
-
 Homo sapiens
N-[1-[([1,1'-biphenyl]-4-yl)methyl]-4-hydroxy-2-oxo-1-azaspiro[5.5]undec-3-ene-3-carbonyl]glycine lead compound for synthesis of orally administered agents for the treatment of renal anemia Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9GZT9
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000013
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(1-[[6-(4-chlorophenoxy)pyridin-3-yl]methyl]-4-hydroxy-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonyl)glycine
0.000039
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(4-hydroxy-1-[[6-(4-methylphenoxy)pyridin-3-yl]methyl]-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonyl)glycine
0.000049
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(4-hydroxy-1-[[4-(4-methylphenoxy)phenyl]methyl]-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonyl)glycine
0.000069
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-(4-hydroxy-1-[[5-(4-methylphenoxy)pyridin-2-yl]methyl]-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonyl)glycine