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Literature summary extracted from

  • Weber, J.E.; Oakley, A.J.; Christ, A.N.; Clark, A.G.; Hayes, J.D.; Hall, R.; Hume, D.A.; Board, P.G.; Smythe, M.L.; Flanagan, J.U.
    Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D2 synthase (2010), Eur. J. Med. Chem., 45, 447-454.
    View publication on PubMed

Application

EC Number Application Comment Organism
5.3.99.2 medicine prostaglandin D2 synthesized by the hematopoietic prostaglandin D2 synthase has a pro-inflammatory effect in allergic asthma, regulating many hallmark characteristics of the disease Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.3.99.2 into the vector pET17b for expression in Escherichia coli BL21DE3 cells Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
5.3.99.2 the structure of H-PGDS in complex with GSH and nocodazole is solved to a resolution of 1.9 A Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.2 1-benzoyl piperazine
-
 Homo sapiens
5.3.99.2 1-benzoyl piperidine
-
 Homo sapiens
5.3.99.2 1-benzoyl-4-(methylsulfonyl)piperazine
-
 Homo sapiens
5.3.99.2 1-phenyl-1-(2-thienyl)methanamine
-
 Homo sapiens
5.3.99.2 3-benzoylpyrrole
-
 Homo sapiens
5.3.99.2 AB179670
-
 Homo sapiens
5.3.99.2 benzophenone
-
 Homo sapiens
5.3.99.2 Cibacron blue 3GA
-
 Homo sapiens
5.3.99.2 CMB5190724
-
 Homo sapiens
5.3.99.2 CMB5256165
-
 Homo sapiens
5.3.99.2 cyclohexyl-phenylketone
-
 Homo sapiens
5.3.99.2 cyclopentyl-phenylketone
-
 Homo sapiens
5.3.99.2 Ethacrynic acid
-
 Homo sapiens
5.3.99.2 HQL-79
-
 Homo sapiens
5.3.99.2 N-phenyl-2-thiophene-carboxamide
-
 Homo sapiens
5.3.99.2 nocodazole
-
 Homo sapiens
5.3.99.2 NSC151248
-
 Homo sapiens
5.3.99.2 NSC4502
-
 Homo sapiens
5.3.99.2 oxfendazole
-
 Homo sapiens
5.3.99.2 phenyl-(2-thienyl)-methanol
-
 Homo sapiens
5.3.99.2 phenyl-(3-thienyl)-methanone
-
 Homo sapiens
5.3.99.2 Sulfobromophthalein
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.3.99.2 Prostaglandin H2 Homo sapiens
-
 Prostaglandin D2
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.2 Homo sapiens O60760
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
5.3.99.2 on a GSTPrep FF 16/10 column Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.2 Prostaglandin H2
-
 Homo sapiens Prostaglandin D2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.3.99.2 H-PGDS
-
 Homo sapiens
5.3.99.2 hematopoietic prostaglandin D2 synthase
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
5.3.99.2 25
-
 enzyme assay Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
5.3.99.2 8
-
 enzyme assay Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
5.3.99.2 glutathione GSH Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.2 0.0002
-
-
 Homo sapiens Cibacron blue 3GA
5.3.99.2 0.0018
-
-
 Homo sapiens HQL-79
5.3.99.2 0.0092
-
-
 Homo sapiens NSC4502
5.3.99.2 0.0114
-
-
 Homo sapiens phenyl-(3-thienyl)-methanone
5.3.99.2 0.016
-
-
 Homo sapiens cyclopentyl-phenylketone
5.3.99.2 0.027
-
-
 Homo sapiens Sulfobromophthalein
5.3.99.2 0.0622
-
-
 Homo sapiens benzophenone
5.3.99.2 0.065
-
-
 Homo sapiens nocodazole
5.3.99.2 0.0875
-
-
 Homo sapiens 3-benzoylpyrrole
5.3.99.2 0.1
-
 larger than 0.100 mM Homo sapiens cyclohexyl-phenylketone
5.3.99.2 0.1
-
 larger than 0.100 mM Homo sapiens 1-benzoyl piperidine
5.3.99.2 0.1
-
 larger than 0.100 mM Homo sapiens 1-benzoyl piperazine
5.3.99.2 0.1
-
 larger than 0.100 mM Homo sapiens 1-benzoyl-4-(methylsulfonyl)piperazine
5.3.99.2 0.1
-
 larger than 0.100 mM Homo sapiens CMB5256165
5.3.99.2 0.1
-
 larger than 0.100 mM Homo sapiens phenyl-(2-thienyl)-methanol
5.3.99.2 0.1
-
 larger than 0.100 mM Homo sapiens 1-phenyl-1-(2-thienyl)methanamine
5.3.99.2 0.1
-
 larger than 0.100 mM Homo sapiens N-phenyl-2-thiophene-carboxamide
5.3.99.2 0.1
-
 larger than 0.100 mM Homo sapiens AB179670
5.3.99.2 0.105
-
-
 Homo sapiens NSC151248
5.3.99.2 0.117
-
-
 Homo sapiens CMB5190724
5.3.99.2 0.1223
-
-
 Homo sapiens Ethacrynic acid
5.3.99.2 0.3
-
 larger than 0.300 mM Homo sapiens oxfendazole