Literature summary for 1.14.11.29 extracted from

Holt-Martyn, J.P.; Chowdhury, R.; Tumber, A.; Yeh, T.L.; Abboud, M.I.; Lippl, K.; Lohans, C.T.; Langley, G.W.; Figg, W.; McDonough, M.A.; Pugh, C.W.; Ratcliffe, P.J.; Schofield, C.J.
Structure-activity relationship and crystallographic studies on 4-hydroxypyrimidine HIF prolyl hydroxylase domain inhibitors (2020), ChemMedChem, 15, 270-273 .

Search for more literature for 1.14.11.29

Crystallization (Commentary)

Crystallization (Comment)	Organism
structure of a truncated domain of PHD2 with MnII substituting for FeII and complexed with inhibitor 4-hydroxy-N-[(4-phenoxyphenyl)methyl]-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide reveals a binding mode involving chelation of the active site metal via nitrogen atoms of the pyrazolo and a pyrimidyl rings which adopt a coplanar conformation. The pyrazole ring of the inhibitor occupies the entrance of the active site pocket that is occupied by the CH2CO2H group of 2-oxoglutarate during catalysis	Homo sapiens

Crystallization (Comment)

Organism

structure of a truncated domain of PHD2 with MnII substituting for FeII and complexed with inhibitor 4-hydroxy-N-[(4-phenoxyphenyl)methyl]-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide reveals a binding mode involving chelation of the active site metal via nitrogen atoms of the pyrazolo and a pyrimidyl rings which adopt a coplanar conformation. The pyrazole ring of the inhibitor occupies the entrance of the active site pocket that is occupied by the CH2CO2H group of 2-oxoglutarate during catalysis

Homo sapiens

Inhibitors

Inhibitors	Comment	Organism
3-([1,1'-biphenyl]-4-yl)-8-[(3-methylpyridin-2-yl)methyl]-1-(pyrimidin-2-yl)-1,3,8-triazaspiro[4.5]decane-2,4-dione	compound stabilizes HIF-1alpha levels and is also active against lysine-specific demethylase KDM4A	Homo sapiens
4-hydroxy-2-(1H-pyrazol-1-yl)-N-[[4-(trifluoromethyl)phenyl]methyl]pyrimidine-5-carboxamide	-	Homo sapiens
4-hydroxy-N-[(1R)-2-hydroxy-1-phenylethyl]-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide	-	Homo sapiens
4-hydroxy-N-[(4-phenoxyphenyl)methyl]-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide	-	Homo sapiens
N-([1,1'-biphenyl]-4-yl)-4-hydroxy-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide	compound stabilizes HIF-1alpha levels	Homo sapiens
N-[(1,3-dihydro-2-benzofuran-5-yl)methyl]-4-hydroxy-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide	-	Homo sapiens
N-[([1,1'-biphenyl]-4-yl)methyl]-4-hydroxy-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	Q9GZT9	-	-

Synonyms

Synonyms	Comment	Organism
PHD2	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.000093	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	4-hydroxy-N-[(1R)-2-hydroxy-1-phenylethyl]-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide
0.000153	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	4-hydroxy-2-(1H-pyrazol-1-yl)-N-[[4-(trifluoromethyl)phenyl]methyl]pyrimidine-5-carboxamide
0.00021	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	N-[([1,1'-biphenyl]-4-yl)methyl]-4-hydroxy-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide
0.000213	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	N-([1,1'-biphenyl]-4-yl)-4-hydroxy-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide
0.000253	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	3-([1,1'-biphenyl]-4-yl)-8-[(3-methylpyridin-2-yl)methyl]-1-(pyrimidin-2-yl)-1,3,8-triazaspiro[4.5]decane-2,4-dione
0.000256	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	4-hydroxy-N-[(4-phenoxyphenyl)methyl]-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide
0.000261	-	pH not specified in the publication, temperature not specified in the publication	Homo sapiens	N-[(1,3-dihydro-2-benzofuran-5-yl)methyl]-4-hydroxy-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide