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Literature summary for 1.1.1.141 extracted from

  • Niesen, F.; Schultz, L.; Jadhav, A.; Bhatia, C.; Guo, K.; Maloney, D.; Pilka, E.; Wang, M.; Oppermann, U.; Heightman, T.; Simeonov, A.
    High-affinity inhibitors of human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase: mechanisms of inhibition and structure-activity relationships (2010), PLoS ONE, 5, e13719.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.1.1.141

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli as a His-tagged fusion protein Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4-([(4-chlorophenyl)sulfanyl]methyl)phenyl)(4-methylpiperidin-1-yl)methanone
-
 Homo sapiens
(4-[(2-bromophenoxy)methyl]phenyl)(piperidin-1-yl)methanone
-
 Homo sapiens
2-([(6-bromo-4H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]methyl)benzonitrile
-
 Homo sapiens
3-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
 Homo sapiens
[1-(3-methylphenyl)-1H-benzimidazol-5-yl](piperidin-1-yl)methanone
-
 Homo sapiens
[4-(4-methoxyphenyl)piperazin-1-yl](4-[(phenylsulfanyl)methyl]phenyl)methanone
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0028
-
 prostaglandin E2 pH 8.0, 25°C, 20 nM [1-(3-methylphenyl)-1H-benzimidazol-5-yl](piperidin-1-yl)methanone Homo sapiens
0.0037
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM [1-(3-methylphenyl)-1H-benzimidazol-5-yl](piperidin-1-yl)methanone Homo sapiens
0.0055
-
 prostaglandin E2 pH 8.0, 25°C Homo sapiens
0.0056
-
 prostaglandin E2 pH 8.0, 25°C, 4 nM 3-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine Homo sapiens
0.0064
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM 3-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine Homo sapiens
0.0075
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM 2-([(6-bromo-4H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]methyl)benzonitrile Homo sapiens
0.0135
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM 2-([(6-bromo-4H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]methyl)benzonitrile Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
prostaglandin E2 + NAD+
-
 Homo sapiens 15-oxoprostaglandin E2 + NADH + H+
-
 ?

Synonyms

Synonyms Comment Organism
15-hydroxyprostaglandin dehydrogenase
-
 Homo sapiens
15-PGDH
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 assay at Homo sapiens

Temperature Stability [°C]

Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
41.2
-
 melting point at pH 8.0, ligand free Homo sapiens
45.9
-
 melting point at pH 8.0, in the presence of NAD+ Homo sapiens
52.5
-
 melting point at pH 8.0, in the presence of NADH Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
6.1
-
 prostaglandin E2 pH 8.0, 25°C, 20 nM [1-(3-methylphenyl)-1H-benzimidazol-5-yl](piperidin-1-yl)methanone Homo sapiens
7.5
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM 3-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine Homo sapiens
10.3
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM [1-(3-methylphenyl)-1H-benzimidazol-5-yl](piperidin-1-yl)methanone Homo sapiens
11.1
-
 prostaglandin E2 pH 8.0, 25°C, 4 nM 3-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine Homo sapiens
12.4
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM 2-([(6-bromo-4H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]methyl)benzonitrile Homo sapiens
13.6
-
 prostaglandin E2 pH 8.0, 25°C Homo sapiens
14.1
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM 2-([(6-bromo-4H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]methyl)benzonitrile Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000056
-
 pH 8, 25°C Homo sapiens [1-(3-methylphenyl)-1H-benzimidazol-5-yl](piperidin-1-yl)methanone
0.000089
-
 pH 8, 25°C Homo sapiens (4-[(2-bromophenoxy)methyl]phenyl)(piperidin-1-yl)methanone
0.000141
-
 pH 8, 25°C Homo sapiens 2-([(6-bromo-4H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]methyl)benzonitrile
0.000631
-
 pH 8, 25°C Homo sapiens (4-([(4-chlorophenyl)sulfanyl]methyl)phenyl)(4-methylpiperidin-1-yl)methanone
0.00089
-
 pH 8, 25°C Homo sapiens 3-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
0.01
-
 value above, pH 8, 25°C Homo sapiens [4-(4-methoxyphenyl)piperazin-1-yl](4-[(phenylsulfanyl)methyl]phenyl)methanone

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
900
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM 2-([(6-bromo-4H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]methyl)benzonitrile Homo sapiens
1200
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM 3-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine Homo sapiens
1800
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM 2-([(6-bromo-4H-imidazo[4,5-b]pyridin-2-yl)sulfanyl]methyl)benzonitrile Homo sapiens
2000
-
 prostaglandin E2 pH 8.0, 25°C, 4 nM 3-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine Homo sapiens
2100
-
 prostaglandin E2 pH 8.0, 25°C, 20 nM [1-(3-methylphenyl)-1H-benzimidazol-5-yl](piperidin-1-yl)methanone Homo sapiens
2500
-
 prostaglandin E2 pH 8.0, 25°C Homo sapiens
2800
-
 prostaglandin E2 pH 8.0, 25°C, 10 nM [1-(3-methylphenyl)-1H-benzimidazol-5-yl](piperidin-1-yl)methanone Homo sapiens