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Literature summary for 5.3.99.2 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
Search for more literature for 5.3.99.2

Cloned(Commentary)

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

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Purification (Commentary)

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
glutathione required Mus musculus
glutathione required Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0007
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens 2-phenyl-5-(1H-pyrazol-3-yl)thiazole
0.0007
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens N-benzhydryl-5-(3-hydroxyphenyl)thiophene-2-carboxamide
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
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
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
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
0.0019
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens 5-(3-aminophenyl)-N-benzhydrylthiophene-2-carboxamide
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
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
0.0038
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens HQL-79
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
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
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
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
0.0128
-
 in 0.1 M Tris-HCl, pH 8.0, at 25°C Homo sapiens phenyl(thiophen-2-yl)methanone
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
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