Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Christ, A.N.; Labzin, L.; Bourne, G.T.; Fukunishi, H.; Weber, J.E.; Sweet, M.J.; Smythe, M.L.; Flanagan, J.U.
    Development and characterization of new inhibitors of the human and mouse hematopoietic prostaglandin D2 synthases (2010), J. Med. Chem., 53, 5536-5548.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.3.99.2 expressed in Escherichia coli BL21(DE3) cells Mus musculus
5.3.99.2 expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.2 2-phenyl-5-(1H-pyrazol-3-yl)thiazole
-
 Homo sapiens
5.3.99.2 2-phenyl-5-(1H-pyrazol-3-yl)thiazole
-
 Mus musculus
5.3.99.2 4-[[4-(4-fluoro-3-methylphenyl)-1,3-thiazol-2-yl]amino]-2-hydroxybenzoic acid
-
 Homo sapiens
5.3.99.2 4-[[4-(4-fluoro-3-methylphenyl)-1,3-thiazol-2-yl]amino]-2-hydroxybenzoic acid
-
 Mus musculus
5.3.99.2 5-(3-aminophenyl)-N-benzhydrylthiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 5-(3-cyanophenyl)-N-(diphenylmethyl)thiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 5-(3-cyanophenyl)-N-(diphenylmethyl)thiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 5-(3-hydroxyphenyl)thiophene-2-carboxylic acid
-
 Homo sapiens
5.3.99.2 5-(3-hydroxyphenyl)thiophene-2-carboxylic acid
-
 Mus musculus
5.3.99.2 5-amino-4-[[(3'-hydroxybiphenyl-4-yl)carbonyl]amino]-5-oxopentanoic acid
-
 Homo sapiens
5.3.99.2 5-amino-4-[[(3'-hydroxybiphenyl-4-yl)carbonyl]amino]-5-oxopentanoic acid
-
 Mus musculus
5.3.99.2 HQL-79
-
 Homo sapiens
5.3.99.2 HQL-79
-
 Mus musculus
5.3.99.2 N-(1,6-diamino-1-oxohexan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1,6-diamino-1-oxohexan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-2,3'-dihydroxybiphenyl-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-2,3'-dihydroxybiphenyl-4-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-3-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-3-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3,3'-dihydroxybiphenyl-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3,3'-dihydroxybiphenyl-4-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(1H-indol-4-yl)benzamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(1H-indol-4-yl)benzamide
-
 Mus musculus
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(thiophen-2-yl)benzamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(thiophen-2-yl)benzamide
-
 Mus musculus
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-6-(thiophen-2-yl)nicotinamide selective H-PGDS inhibitor with low micromolar potency in the inhibition of the purified enzyme Homo sapiens
5.3.99.2 N-(1-amino-1-oxo-3-phenylpropan-2-yl)-6-(thiophen-2-yl)nicotinamide selective H-PGDS inhibitor with low micromolar potency in the inhibition of the purified enzyme Mus musculus
5.3.99.2 N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-3-cyclohexyl-1-oxopropan-2-yl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-3-cyclohexyl-1-oxopropan-2-yl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-3-methyl-1-oxobutan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-3-methyl-1-oxobutan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-4-methyl-1-oxopentan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-4-methyl-1-oxopentan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
 Mus musculus
5.3.99.2 N-(1-amino-4-methyl-1-oxopentan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 N-(1-amino-4-methyl-1-oxopentan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 N-(2-amino-2-oxoethyl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 N-(2-amino-2-oxoethyl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 N-(diphenylmethyl)-2-(3-hydroxyphenyl)-1,3-thiazole-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(diphenylmethyl)-2-(3-hydroxyphenyl)-1,3-thiazole-4-carboxamide
-
 Mus musculus
5.3.99.2 N-(diphenylmethyl)-2-phenyl-1,3-thiazole-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(diphenylmethyl)-2-phenyl-1,3-thiazole-4-carboxamide
-
 Mus musculus
5.3.99.2 N-(diphenylmethyl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 N-(diphenylmethyl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 N-(diphenylmethyl)-5-phenylthiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 N-(diphenylmethyl)-5-phenylthiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 N-(diphenylmethyl)-5-[3-(hydroxymethyl)phenyl]thiophene-2-carboxamide
-
 Homo sapiens
5.3.99.2 N-(diphenylmethyl)-5-[3-(hydroxymethyl)phenyl]thiophene-2-carboxamide
-
 Mus musculus
5.3.99.2 N-(diphenylmethyl)biphenyl-4-carboxamide
-
 Homo sapiens
5.3.99.2 N-(diphenylmethyl)biphenyl-4-carboxamide
-
 Mus musculus
5.3.99.2 N-benzhydryl-5-(3-hydroxyphenyl)thiophene-2-carboxamide low micromolar potency in the inhibition of the purified enzyme Homo sapiens
5.3.99.2 N-[4-methyl-3-({3-[(4-methylpiperazin-1-yl)methyl]benzoyl}amino)phenyl]-3-phenyl-1,2-thiazole-5-carboxamide
-
 Homo sapiens
5.3.99.2 N-[4-methyl-3-({3-[(4-methylpiperazin-1-yl)methyl]benzoyl}amino)phenyl]-3-phenyl-1,2-thiazole-5-carboxamide
-
 Mus musculus
5.3.99.2 phenyl(thiophen-2-yl)methanone
-
 Homo sapiens
5.3.99.2 phenyl(thiophen-2-yl)methanone
-
 Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.2 Homo sapiens
-
-
-
5.3.99.2 Mus musculus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
5.3.99.2 GST-Prep column chromatography Mus musculus
5.3.99.2 GST-Prep column chromatography Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.3.99.2 bone marrow-derived macrophage primary cell Mus musculus
-
5.3.99.2 MEG-01S cell
-
 Homo sapiens
-
5.3.99.2 primary bone marrow-derived macrophage
-
 Mus musculus
-

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

EC Number Cofactor Comment Organism Structure
5.3.99.2 glutathione required Mus musculus
5.3.99.2 glutathione required Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.2 0.0007
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens 2-phenyl-5-(1H-pyrazol-3-yl)thiazole
5.3.99.2 0.0007
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-benzhydryl-5-(3-hydroxyphenyl)thiophene-2-carboxamide
5.3.99.2 0.001
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
5.3.99.2 0.0012
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(1-amino-1-oxo-3-phenylpropan-2-yl)-6-(thiophen-2-yl)nicotinamide
5.3.99.2 0.0013
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
5.3.99.2 0.0014
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens 4-[[4-(4-fluoro-3-methylphenyl)-1,3-thiazol-2-yl]amino]-2-hydroxybenzoic acid
5.3.99.2 0.0019
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens 5-(3-aminophenyl)-N-benzhydrylthiophene-2-carboxamide
5.3.99.2 0.0021
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
5.3.99.2 0.0037
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(1-amino-1-oxo-3-phenylpropan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
5.3.99.2 0.0038
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens HQL-79
5.3.99.2 0.0046
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
5.3.99.2 0.0071
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(1-amino-4-methyl-1-oxopentan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
5.3.99.2 0.008
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(2-amino-2-oxoethyl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
5.3.99.2 0.0108
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(diphenylmethyl)-2-(3-hydroxyphenyl)-1,3-thiazole-4-carboxamide
5.3.99.2 0.0128
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens phenyl(thiophen-2-yl)methanone
5.3.99.2 0.023
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens 5-amino-4-[[(3'-hydroxybiphenyl-4-yl)carbonyl]amino]-5-oxopentanoic acid
5.3.99.2 0.0248
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3,3'-dihydroxybiphenyl-4-carboxamide