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Literature summary for 5.3.99.2 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
Search for more literature for 5.3.99.2

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2'-methoxy-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl][2,4'-bipyridine]-5-carboxamide
-
 Homo sapiens
2'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',2'-dihydro[2,4'-bipyridine]-5-carboxamide
-
 Homo sapiens
2-phenyl-5-(1H-pyrazol-3-yl)-1,3-thiazole
-
 Homo sapiens
3-(1H-indol-4-yl)-N-(3-methoxypropyl)-1,2,4-oxadiazole-5-carboxamide
-
 Homo sapiens
3-acetamido-N-[5-(1H-indol-4-yl)pyridin-3-yl]propanamide
-
 Homo sapiens
4-(dimethylamino)-N-[5-(1H-indol-4-yl)pyridin-3-yl]butanamide
-
 Homo sapiens
4-methyl-2-phenyl-N-(4-sulfamoylphenyl)-1,3-thiazole-5-carboxamide
-
 Homo sapiens
6'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',6'-dihydro[2,2'-bipyridine]-5-carboxamide
-
 Homo sapiens
6'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',6'-dihydro[2,3'-bipyridine]-5-carboxamide
-
 Homo sapiens
6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
6-(3-methoxyphenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
6-(3-oxopiperazin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
6-(dimethylamino)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
6-(morpholin-4-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
6-(piperazin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
6-(piperidin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
6-(pyrrolidin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
6-phenoxy-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
 Homo sapiens
N-([4-[5-(2-hydroxypropan-2-yl)-1,2,4-oxadiazol-3-yl]phenyl]methyl)-2-phenylpyrimidine-5-carboxamide
-
 Homo sapiens
N-[4-(morpholin-4-yl)phenyl]-2-phenoxypyrimidine-5-carboxamide
-
 Homo sapiens
N-[5-(1H-indol-4-yl)pyridin-3-yl]-2-(1-methyl-1H-imidazol-5-yl)acetamide
-
 Homo sapiens
N-[5-(1H-indol-4-yl)pyridin-3-yl]-2-(1H-tetrazol-1-yl)acetamide
-
 Homo sapiens
N-[5-(1H-indol-4-yl)pyridin-3-yl]-3-(piperidin-1-yl)propanamide
-
 Homo sapiens
N-[5-(1H-indol-4-yl)pyridin-3-yl]-3-(pyridin-3-yl)propanamide
-
 Homo sapiens
N-[5-(1H-indol-4-yl)pyridin-3-yl]-5-oxopyrrolidine-2-carboxamide (incorrect configuration definition!)
-
 Homo sapiens
N-[5-(1H-indol-4-yl)pyridin-3-yl]propanamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate Homo sapiens
-
 (5Z,13E,15S)-9alpha,15-dihydroxy-11-oxoprosta-5,13-dienoate
-
 ?
Prostaglandin H2 Homo sapiens
-
 Prostaglandin D2
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens O60760
-
-

Purification (Commentary)

Purification (Comment) Organism
cation exchange column chromatography and gel filtration Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
 Homo sapiens (5Z,13E,15S)-9alpha,15-dihydroxy-11-oxoprosta-5,13-dienoate
-
 ?
Prostaglandin H2
-
 Homo sapiens Prostaglandin D2
-
 ?

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
0.000032
-
 at 37°C, pH not specified in the publication Homo sapiens N-[5-(1H-indol-4-yl)pyridin-3-yl]propanamide
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!)
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
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
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
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
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
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
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
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
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
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
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
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