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Literature summary extracted from

  • Hong, Y.R.; Kim, H.T.; Ro, S.; Cho, J.M.; Lee, S.H.; Kim, I.S.; Jung, Y.H.
    Discovery of novel 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide derivatives as HIF prolyl 4-hydroxylase inhibitors; SAR, synthesis and modeling evaluation (2014), Bioorg. Med. Chem. Lett., 24, 3142-3145 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.11.29 (2R)-[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido](phenyl)acetic acid
-
 Homo sapiens
1.14.11.29 (2S)-[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido](phenyl)acetic acid
-
 Homo sapiens
1.14.11.29 2-(2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-methylthiazol-4-yl)-N-(2-(diethylamino)ethyl)acetamide
-
 Homo sapiens
1.14.11.29 2-(2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-phenylthiazol-4-yl)-N-(2-(pyridin-2-yl)ethyl)acetamide
-
 Homo sapiens
1.14.11.29 2-(2-(5-cyano-3-hydroxypyridin-2-yl)-5-phenylthiazol-4-yl)-N-(2-(pyridin-2-yl)ethyl)acetamide
-
 Homo sapiens
1.14.11.29 2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-1,3-thiazol-4-yl]-N-[2-(diethylamino)ethyl]acetamide
-
 Homo sapiens
1.14.11.29 2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
-
 Homo sapiens
1.14.11.29 2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-methyl-1,3-thiazol-4-yl]-N-propylacetamide
-
 Homo sapiens
1.14.11.29 2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-methyl-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
-
 Homo sapiens
1.14.11.29 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-(2-phenylethyl)acetamide
-
 Homo sapiens
1.14.11.29 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-[(1R)-2-hydroxy-1-phenylethyl]acetamide
-
 Homo sapiens
1.14.11.29 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-[(1S)-2-hydroxy-1-phenylethyl]acetamide
-
 Homo sapiens
1.14.11.29 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
-
 Homo sapiens
1.14.11.29 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-5-methyl-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
-
 Homo sapiens
1.14.11.29 2-[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido]-2-methylpropanoic acid
-
 Homo sapiens
1.14.11.29 5-hydroxy-6-[4-[2-oxo-2-(pyrrolidin-1-yl)ethyl]-1,3-thiazol-2-yl]pyridine-3-carbonitrile
-
 Homo sapiens
1.14.11.29 AKB-6548
-
 Homo sapiens
1.14.11.29 BAY85-3934
-
 Homo sapiens
1.14.11.29 deferoxamine
-
 Homo sapiens
1.14.11.29 FG-0041
-
 Homo sapiens
1.14.11.29 FG-2216
-
 Homo sapiens
1.14.11.29 FG-4592
-
 Homo sapiens
1.14.11.29 GSK1278863
-
 Homo sapiens
1.14.11.29 GSK360A
-
 Homo sapiens
1.14.11.29 N-benzyl-2-[2-(3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamide
-
 Homo sapiens
1.14.11.29 N-benzyl-2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamide
-
 Homo sapiens
1.14.11.29 N-oxalylglycine
-
 Homo sapiens
1.14.11.29 PN-3602
-
 Homo sapiens
1.14.11.29 [2-(3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetic acid
-
 Homo sapiens
1.14.11.29 [2-(3-hydroxypyridin-2-yl)-6-oxo-1,6-dihydropyrimidin-5-yl]acetic acid
-
 Homo sapiens
1.14.11.29 [2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetic acid
-
 Homo sapiens
1.14.11.29 [2-(5-cyano-3-hydroxypyridin-2-yl)-6-oxo-1,6-dihydropyrimidin-5-yl]acetic acid
-
 Homo sapiens
1.14.11.29 [2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido]acetic acid
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.11.29 hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2 Homo sapiens
-
 hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.14.11.29 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.11.29 HEP-3B cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.11.29 hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2
-
 Homo sapiens hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.14.11.29 HIF prolyl 4-hydroxylase
-
 Homo sapiens
1.14.11.29 PHD
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.14.11.29 0.0004
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-methylthiazol-4-yl)-N-(2-(diethylamino)ethyl)acetamide
1.14.11.29 0.0007
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
1.14.11.29 0.0008
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-methyl-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
1.14.11.29 0.0012
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-5-methyl-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
1.14.11.29 0.0014
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-methyl-1,3-thiazol-4-yl]-N-propylacetamide
1.14.11.29 0.002
-
 pH and temperature not specified in the publication Homo sapiens 5-hydroxy-6-[4-[2-oxo-2-(pyrrolidin-1-yl)ethyl]-1,3-thiazol-2-yl]pyridine-3-carbonitrile
1.14.11.29 0.0021
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-[(1R)-2-hydroxy-1-phenylethyl]acetamide
1.14.11.29 0.0022
-
 pH and temperature not specified in the publication Homo sapiens [2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido]acetic acid
1.14.11.29 0.0024
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-[(1S)-2-hydroxy-1-phenylethyl]acetamide
1.14.11.29 0.0026
-
 pH and temperature not specified in the publication Homo sapiens (2R)-[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido](phenyl)acetic acid
1.14.11.29 0.0028
-
 pH and temperature not specified in the publication Homo sapiens (2S)-[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido](phenyl)acetic acid
1.14.11.29 0.003
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
1.14.11.29 0.0034
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-(2-phenylethyl)acetamide
1.14.11.29 0.0038
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-1,3-thiazol-4-yl]-N-[2-(diethylamino)ethyl]acetamide
1.14.11.29 0.0039
-
 pH and temperature not specified in the publication Homo sapiens FG-2216
1.14.11.29 0.0054
-
 pH and temperature not specified in the publication Homo sapiens N-benzyl-2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamide
1.14.11.29 0.0057
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-phenylthiazol-4-yl)-N-(2-(pyridin-2-yl)ethyl)acetamide
1.14.11.29 0.006
-
 pH and temperature not specified in the publication Homo sapiens [2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetic acid
1.14.11.29 0.0073
-
 pH and temperature not specified in the publication Homo sapiens 2-[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido]-2-methylpropanoic acid
1.14.11.29 0.0135
-
 pH and temperature not specified in the publication Homo sapiens [2-(5-cyano-3-hydroxypyridin-2-yl)-6-oxo-1,6-dihydropyrimidin-5-yl]acetic acid
1.14.11.29 0.024
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-(5-cyano-3-hydroxypyridin-2-yl)-5-phenylthiazol-4-yl)-N-(2-(pyridin-2-yl)ethyl)acetamide
1.14.11.29 0.0275
-
 pH and temperature not specified in the publication Homo sapiens [2-(3-hydroxypyridin-2-yl)-6-oxo-1,6-dihydropyrimidin-5-yl]acetic acid
1.14.11.29 0.081
-
 pH and temperature not specified in the publication Homo sapiens N-benzyl-2-[2-(3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamide
1.14.11.29 0.195
-
 pH and temperature not specified in the publication Homo sapiens [2-(3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetic acid