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Literature summary extracted from

  • Edfeldt, F.; Evenaes, J.; Lepistoe, M.; Ward, A.; Petersen, J.; Wissler, L.; Rohman, M.; Sivars, U.; Svensson, K.; Perry, M.; Feierberg, I.; Zhou, X.H.; Hansson, T.; Narjes, F.
    Identification of indole inhibitors of human hematopoietic prostaglandin D2 synthase (hH-PGDS) (2015), Bioorg. Med. Chem. Lett., 25, 2496-2500 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.3.99.2 expressed in Escherichia coli Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
5.3.99.2
-
 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.2 2'-methoxy-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl][2,4'-bipyridine]-5-carboxamide
-
 Homo sapiens
5.3.99.2 2'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',2'-dihydro[2,4'-bipyridine]-5-carboxamide
-
 Homo sapiens
5.3.99.2 2-phenyl-5-(1H-pyrazol-3-yl)-1,3-thiazole
-
 Homo sapiens
5.3.99.2 3-(1H-indol-4-yl)-N-(3-methoxypropyl)-1,2,4-oxadiazole-5-carboxamide
-
 Homo sapiens
5.3.99.2 3-acetamido-N-[5-(1H-indol-4-yl)pyridin-3-yl]propanamide
-
 Homo sapiens
5.3.99.2 4-(dimethylamino)-N-[5-(1H-indol-4-yl)pyridin-3-yl]butanamide
-
 Homo sapiens
5.3.99.2 4-methyl-2-phenyl-N-(4-sulfamoylphenyl)-1,3-thiazole-5-carboxamide
-
 Homo sapiens
5.3.99.2 6'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',6'-dihydro[2,2'-bipyridine]-5-carboxamide
-
 Homo sapiens
5.3.99.2 6'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',6'-dihydro[2,3'-bipyridine]-5-carboxamide
-
 Homo sapiens
5.3.99.2 6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.2 6-(3-methoxyphenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.2 6-(3-oxopiperazin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.2 6-(dimethylamino)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.2 6-(morpholin-4-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.2 6-(piperazin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.2 6-(piperidin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.2 6-(pyrrolidin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.2 6-phenoxy-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.2 N-([4-[5-(2-hydroxypropan-2-yl)-1,2,4-oxadiazol-3-yl]phenyl]methyl)-2-phenylpyrimidine-5-carboxamide
-
 Homo sapiens
5.3.99.2 N-[4-(morpholin-4-yl)phenyl]-2-phenoxypyrimidine-5-carboxamide
-
 Homo sapiens
5.3.99.2 N-[5-(1H-indol-4-yl)pyridin-3-yl]-2-(1-methyl-1H-imidazol-5-yl)acetamide
-
 Homo sapiens
5.3.99.2 N-[5-(1H-indol-4-yl)pyridin-3-yl]-2-(1H-tetrazol-1-yl)acetamide
-
 Homo sapiens
5.3.99.2 N-[5-(1H-indol-4-yl)pyridin-3-yl]-3-(piperidin-1-yl)propanamide
-
 Homo sapiens
5.3.99.2 N-[5-(1H-indol-4-yl)pyridin-3-yl]-3-(pyridin-3-yl)propanamide
-
 Homo sapiens
5.3.99.2 N-[5-(1H-indol-4-yl)pyridin-3-yl]-5-oxopyrrolidine-2-carboxamide (incorrect configuration definition!)
-
 Homo sapiens
5.3.99.2 N-[5-(1H-indol-4-yl)pyridin-3-yl]propanamide
-
 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 (5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate Homo sapiens
-
 (5Z,13E,15S)-9alpha,15-dihydroxy-11-oxoprosta-5,13-dienoate
-
 ?
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 cation exchange column chromatography and gel filtration Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.2 (5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
 Homo sapiens (5Z,13E,15S)-9alpha,15-dihydroxy-11-oxoprosta-5,13-dienoate
-
 ?
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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.2 0.000026
-
 at 37°C, pH not specified in the publication Homo sapiens N-[5-(1H-indol-4-yl)pyridin-3-yl]-3-(pyridin-3-yl)propanamide
5.3.99.2 0.000031
-
 at 37°C, pH not specified in the publication Homo sapiens 6-phenoxy-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
5.3.99.2 0.000032
-
 at 37°C, pH not specified in the publication Homo sapiens N-[5-(1H-indol-4-yl)pyridin-3-yl]propanamide
5.3.99.2 0.000035
-
 at 37°C, pH not specified in the publication Homo sapiens N-[5-(1H-indol-4-yl)pyridin-3-yl]-5-oxopyrrolidine-2-carboxamide (incorrect configuration definition!)
5.3.99.2 0.000043
-
 at 37°C, pH not specified in the publication Homo sapiens N-[5-(1H-indol-4-yl)pyridin-3-yl]-2-(1H-tetrazol-1-yl)acetamide
5.3.99.2 0.000048
-
 at 37°C, pH not specified in the publication Homo sapiens 6-(piperidin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
5.3.99.2 0.00006
-
 at 37°C, pH not specified in the publication Homo sapiens 6-(3-methoxyphenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
5.3.99.2 0.000071
-
 at 37°C, pH not specified in the publication Homo sapiens 6'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',6'-dihydro[2,2'-bipyridine]-5-carboxamide
5.3.99.2 0.00013
-
 at 37°C, pH not specified in the publication Homo sapiens N-[5-(1H-indol-4-yl)pyridin-3-yl]-3-(piperidin-1-yl)propanamide
5.3.99.2 0.00018
-
 at 37°C, pH not specified in the publication Homo sapiens 4-(dimethylamino)-N-[5-(1H-indol-4-yl)pyridin-3-yl]butanamide
5.3.99.2 0.00023
-
 at 37°C, pH not specified in the publication Homo sapiens 6-(pyrrolidin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
5.3.99.2 0.0003
-
 at 37°C, pH not specified in the publication Homo sapiens 3-acetamido-N-[5-(1H-indol-4-yl)pyridin-3-yl]propanamide
5.3.99.2 0.00032
-
 at 37°C, pH not specified in the publication Homo sapiens 6-(morpholin-4-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
5.3.99.2 0.00059
-
 at 37°C, pH not specified in the publication Homo sapiens 6-(3-oxopiperazin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
5.3.99.2 0.0012
-
 at 37°C, pH not specified in the publication Homo sapiens N-[5-(1H-indol-4-yl)pyridin-3-yl]-2-(1-methyl-1H-imidazol-5-yl)acetamide
5.3.99.2 7
-
 at 37°C, pH not specified in the publication Homo sapiens 2'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',2'-dihydro[2,4'-bipyridine]-5-carboxamide