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Literature summary for 1.14.11.29 extracted from

  • Chan, M.C.; Atasoylu, O.; Hodson, E.; Tumber, A.; Leung, I.K.; Chowdhury, R.; Gomez-Perez, V.; Demetriades, M.; Rydzik, A.M.; Holt-Martyn, J.; Tian, Y.M.; Bishop, T.; Claridge, T.D.; Kawamura, A.; Pugh, C.W.; Ratcliffe, P.J.; Schofield, C.J.
    Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain (2015), PLoS ONE, 10, e0132004 .
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
isoform PHD2 in complex with Mn2+, sitting drop vapor diffusion method, using 1.6 M sodium citrate/citric acid pH 6.5 Homo sapiens
isoform PHD2 in complex with Mn2+, sitting drop vapor diffusion method, using 1.6 M sodium citrate/citric acid pH 6.5 Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
6-[5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl]pyridine-3-carboxylic acid
-
Homo sapiens
6-[5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl]pyridine-3-carboxylic acid
-
Mus musculus
dimethyloxalylglycine
-
Homo sapiens
dimethyloxalylglycine
-
Mus musculus
N-oxalylglycine
-
Homo sapiens
N-oxalylglycine
-
Mus musculus
tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate potent and selective inhibitor of isoform PHD2 Homo sapiens
tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate potent and selective inhibitor of isoform PHD2 Mus musculus
[(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbonyl)amino]acetic acid
-
Homo sapiens
[(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbonyl)amino]acetic acid
-
Mus musculus
[(1-chloro-4-hydroxyisoquinoline-3-carbonyl)amino]acetic acid
-
Homo sapiens
[(1-chloro-4-hydroxyisoquinoline-3-carbonyl)amino]acetic acid
-
Mus musculus
[(2E)-3-hydroxy-2-({[(naphthalen-2-yl)methanesulfonyl]acetyl}imino)-2,3-dihydro-1,3-thiazol-4-yl]acetic acid
-
Homo sapiens
[(2E)-3-hydroxy-2-({[(naphthalen-2-yl)methanesulfonyl]acetyl}imino)-2,3-dihydro-1,3-thiazol-4-yl]acetic acid
-
Mus musculus
[(4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonyl)amino]acetic acid
-
Homo sapiens
[(4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbonyl)amino]acetic acid
-
Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens Q96KS0
-
-
Homo sapiens Q9GZT9
-
-
Homo sapiens Q9H6Z9
-
-
Mus musculus Q91UZ4
-
-
Mus musculus Q91YE2
-
-
Mus musculus Q91YE3
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Mus musculus
-
HeLa cell
-
Homo sapiens
-
HEP-3B cell
-
Homo sapiens
-
liver
-
Mus musculus
-
MCF-7 cell
-
Homo sapiens
-
RCC-4 cell
-
Homo sapiens
-
U2OS cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DLDLEMLAPYIPMDDDFQL + 2-oxoglutarate + O2
-
Homo sapiens ?
-
?
DLDLEMLAPYIPMDDDFQL + 2-oxoglutarate + O2
-
Mus musculus ?
-
?

Synonyms

Synonyms Comment Organism
Hif-prolyl hydroxylase
-
Homo sapiens
Hif-prolyl hydroxylase
-
Mus musculus
PHD1 isoform Homo sapiens
PHD1 isoform Mus musculus
PHD2 isoform Homo sapiens
PHD2 isoform Mus musculus
PHD3 isoform Homo sapiens
PHD3 isoform Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000016
-
isoform PHD2, pH and temperature not specified in the publication Homo sapiens tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate
0.0000016
-
isoform PHD2, pH and temperature not specified in the publication Mus musculus tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate
0.0000022
-
isoform PHD2, pH and temperature not specified in the publication Homo sapiens N-oxalylglycine
0.0000022
-
isoform PHD2, pH and temperature not specified in the publication Mus musculus N-oxalylglycine
0.0000048
-
isoform PHD2, pH and temperature not specified in the publication Homo sapiens 6-[5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl]pyridine-3-carboxylic acid
0.000022
-
isoform PHD2, pH and temperature not specified in the publication Homo sapiens [(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbonyl)amino]acetic acid