1.14.11.29: hypoxia-inducible factor-proline dioxygenase

This is an abbreviated version, for detailed information about hypoxia-inducible factor-proline dioxygenase, go to the full flat file.

Reaction

hypoxia-inducible factor-L-proline
+
2-oxoglutarate
+
O2
=
hypoxia-inducible factor-trans-4-hydroxy-L-proline
+
succinate
+
CO2

Synonyms

EGLN, EGLN1, Egln2, EGLN3, factor inhibiting HIF, FIH, HIF hydroxylase, HIF prolyl, HIF prolyl 4-hydroxylase, HIF prolyl hydroxylase, HIF-1alpha PHD3, HIF-1alpha prolyl hydroxylase 3, HIF-alpha prolyl-hydroxylase, HIF-P4H-1, HIF-P4H-2, HIF-P4H-3, HIF-PH, Hif-prolyl hydroxylase, HIF-prolyl hydroxylase domain 2, HIF-prolyl hydroxylase-2, HPH-1, HPH-2, HPH-3, hydroxylase domain enzyme, hypoxia-inducible factor prolyl hydroxylase 2, hypoxia-inducible factor prolyl hydroxylase domain 2, PHD, PHD1, PHD2, PHD3, proline hydroxylase domain 2, prolyl 4-hydroxylase, prolyl hydroxylase, prolyl hydroxylase domain, prolyl hydroxylase domain protein, prolyl hydroxylase domain protein 2, prolyl hydroxylase-2, prolyl-4-hydroxylase 2, prolyl-4-hydroxylase domain 2

ECTree

     1 Oxidoreductases
         1.14 Acting on paired donors, with incorporation or reduction of molecular oxygen
             1.14.11 With 2-oxoglutarate as one donor, and incorporation of one atom of oxygen into each donor
                1.14.11.29 hypoxia-inducible factor-proline dioxygenase

IC50 Value

IC50 Value on EC 1.14.11.29 - hypoxia-inducible factor-proline dioxygenase

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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0026
(2R)-[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido](phenyl)acetic acid
Homo sapiens;
-
pH and temperature not specified in the publication
-
0.0028
(2S)-[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido](phenyl)acetic acid
Homo sapiens;
-
pH and temperature not specified in the publication
-
0.0295 - 0.0397
1,1',1'',1'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetrapropan-2-ol
0.0309
2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetamide
Homo sapiens;
-
recombinant enzyme, pH 7.0, 37°C
0.005
2,3-dihydroxypyridine
Homo sapiens;
-
pH 7.0, 37°C
0.0004
2-(2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-methylthiazol-4-yl)-N-(2-(diethylamino)ethyl)acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0057
2-(2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-phenylthiazol-4-yl)-N-(2-(pyridin-2-yl)ethyl)acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.024
2-(2-(5-cyano-3-hydroxypyridin-2-yl)-5-phenylthiazol-4-yl)-N-(2-(pyridin-2-yl)ethyl)acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.003
2-hydroxypyridine 1-oxide
Homo sapiens;
-
pH 7.0, 37°C
0.0038
2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-1,3-thiazol-4-yl]-N-[2-(diethylamino)ethyl]acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0007
2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0014
2-[2-(5-cyano-3-hydroxy-4-methylpyridin-2-yl)-5-methyl-1,3-thiazol-4-yl]-N-propylacetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0008
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;
-
pH and temperature not specified in the publication
0.0034
2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-(2-phenylethyl)acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0021
2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-[(1R)-2-hydroxy-1-phenylethyl]acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0024
2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-[(1S)-2-hydroxy-1-phenylethyl]acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.003
2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0012
2-[2-(5-cyano-3-hydroxypyridin-2-yl)-5-methyl-1,3-thiazol-4-yl]-N-[2-(pyridin-2-yl)ethyl]acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0073
2-[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido]-2-methylpropanoic acid
Homo sapiens;
-
pH and temperature not specified in the publication
-
0.0604
3,3'-[(pyridin-2-ylmethyl)imino]dipropanenitrile
Homo sapiens;
-
recombinant enzyme, pH 7.0, 37°C
0.0128
3,3'-[(pyridin-4-ylimino)bis(propane-3,1-diyliminomethanediyl)]diphenol
Homo sapiens;
-
recombinant enzyme, pH 7.0, 37°C
0.016
3,3'-[(pyridin-4-ylimino)bis[propane-3,1-diylnitrilo(Z)methylylidene]]diphenol
Homo sapiens;
-
recombinant enzyme, pH 7.0, 37°C
0.0103
3,6,9-tris(naphthalen-1-ylmethyl)-3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene
Homo sapiens;
-
recombinant enzyme, pH 7.0, 37°C
1
3-cyano-6-methyl-2(H)-pyridinone
Homo sapiens;
-
above, pH 7.0, 37°C
0.04
3-hydroxy-1,2-dimethyl-4(1H)-pyridinone
Homo sapiens;
-
pH 7.0, 37°C
1
3-hydroxy-2-methyl-4-pyrone
Homo sapiens;
-
above, pH 7.0, 37°C
0.004
4-methylcatechol
Homo sapiens;
-
pH 7.0, 37°C
0.006
4-nitrocatechol
Homo sapiens;
-
pH 7.0, 37°C
0.03
4-tert-butylcatechol
Homo sapiens;
-
pH 7.0, 37°C
0.4
5-hydroxy-2-hydroxymethyl-4-pyrone
Homo sapiens;
-
pH 7.0, 37°C
0.03
5-hydroxy-4-oxo-4H-pyran-2-carboxylic acid
Homo sapiens;
-
pH 7.0, 37°C
0.002
5-hydroxy-6-[4-[2-oxo-2-(pyrrolidin-1-yl)ethyl]-1,3-thiazol-2-yl]pyridine-3-carbonitrile
Homo sapiens;
-
pH and temperature not specified in the publication
-
0.0000048
6-[5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl]pyridine-3-carboxylic acid
Homo sapiens;
-
isoform PHD2, pH and temperature not specified in the publication
0.0039
FG-2216
Homo sapiens;
-
pH and temperature not specified in the publication
-
0.0207
N,N-dimethyl-5-[3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-trien-6-ylsulfonyl]naphthalen-1-amine
Homo sapiens;
-
recombinant enzyme, pH 7.0, 37°C
0.081
N-benzyl-2-[2-(3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0054
N-benzyl-2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamide
Homo sapiens;
-
pH and temperature not specified in the publication
0.0000022
N-oxalylglycine
0.0000016
tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate
-
0.000022
[(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbonyl)amino]acetic acid
Homo sapiens;
-
isoform PHD2, pH and temperature not specified in the publication
0.195
[2-(3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetic acid
Homo sapiens;
-
pH and temperature not specified in the publication
0.0275
[2-(3-hydroxypyridin-2-yl)-6-oxo-1,6-dihydropyrimidin-5-yl]acetic acid
Homo sapiens;
-
pH and temperature not specified in the publication
0.006
[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetic acid
Homo sapiens;
-
pH and temperature not specified in the publication
0.0135
[2-(5-cyano-3-hydroxypyridin-2-yl)-6-oxo-1,6-dihydropyrimidin-5-yl]acetic acid
Homo sapiens;
-
pH and temperature not specified in the publication
0.0022
[2-[2-(5-cyano-3-hydroxypyridin-2-yl)-1,3-thiazol-4-yl]acetamido]acetic acid
Homo sapiens;
-
pH and temperature not specified in the publication
-