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1-benzoyl-4-(methylsulfonyl)piperazine
-
1-phenyl-1-(2-thienyl)methanamine
-
11-hydroxy-DELTA9-tetrahydrocannabinol
-
-
11-nor-9-carboxy-DELTA9-tetrahydrocannabinol
-
-
15-Hydroperoxyarachidonic acid
-
-
2'-methoxy-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl][2,4'-bipyridine]-5-carboxamide
-
2'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',2'-dihydro[2,4'-bipyridine]-5-carboxamide
-
2-(2'-benzothiazolyl)-5-styryl-3-(4'-phthalhydrazyl) tetrazolium chloride
-
IC50: 0.0362 mM in presence of EDTA, 0.0981 in presence of Mg2+
2-phenyl-5-(1H-pyrazol-3-yl)-1,3-thiazole
2-phenyl-5-(1H-pyrazol-3-yl)thiazole
3,3',5'-triiodo-L-thyronine
-
0.0093 mM, 50% inhibition
3,3',5-triiodo-L-thyronine
-
0.011 mM, 50% inhibition
3-(1H-indol-4-yl)-N-(3-methoxypropyl)-1,2,4-oxadiazole-5-carboxamide
-
3-(1H-pyrazol-4-yl)pyridine
-
58% inhibition at 0.1 mM
3-(3-cyclopropyl-1H-pyrazol-4-yl)-N-ethyl-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide
-
-
3-(3-cyclopropyl-1H-pyrazol-4-yl)pyridine
-
-
3-acetamido-N-[5-(1H-indol-4-yl)pyridin-3-yl]propanamide
-
3-phenyl-5-(1H-pyrazol-3-yl)-1,2-oxazole
-
4-(3-methyl-1H-pyrazol-4-yl)benzonitrile
-
52% inhibition at 0.03 mM
4-(dimethylamino)-N-[5-(1H-indol-4-yl)pyridin-3-yl]butanamide
-
4-(diphenylmethoxy)-1-[3-(1H-tetrazol-5-yl)propyl]piperidine
-
-
4-benzhydryloxy-1-[3-(1H-tetrazol-5-yl)-propyl]piperidine
-
HQL-79
4-dibenzo [a,d]cyclohepten-5-ylidene-1-[4-(2H-tetrazol-5-yl)-butyl]-piperidine
4-methyl-2-phenyl-N-(4-sulfamoylphenyl)-1,3-thiazole-5-carboxamide
-
4-[[4-(4-fluoro-3-methylphenyl)-1,3-thiazol-2-yl]amino]-2-hydroxybenzoic acid
5-(3-aminophenyl)-N-benzhydrylthiophene-2-carboxamide
-
-
5-(3-cyanophenyl)-N-(diphenylmethyl)thiophene-2-carboxamide
5-(3-hydroxyphenyl)thiophene-2-carboxylic acid
5-amino-4-[[(3'-hydroxybiphenyl-4-yl)carbonyl]amino]-5-oxopentanoic acid
6'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',6'-dihydro[2,2'-bipyridine]-5-carboxamide
-
6'-oxo-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-1',6'-dihydro[2,3'-bipyridine]-5-carboxamide
-
6-(3-fluorophenyl)-N-[1-(1-methyl-1H-tetrazol-5-yl)piperidin-4-yl]pyridine-3-carboxamide
-
-
6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
6-(3-methoxyphenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
6-(3-oxopiperazin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
6-(dimethylamino)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
6-(morpholin-4-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
6-(piperazin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
6-(piperidin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
6-(pyrrolidin-1-yl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
6-phenoxy-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
all-trans-retinoic acid
-
-
anthralin
i.e. 1,8-dihydroxyanthracen-9(10H)-one
AT-56
-
inhibition of prostaglandin-D synthase, resulting in suppression of prostaglandin D2 production under serum-starved conditions
bilirubin
-
0.0068 mM, 50% inhibition
Biliverdin
-
0.0053 mM, 50% inhibition
chlorophyllide copper complex sodium salt
linear competitive inhibitor
Cibacron blue
0.00003 mM, 50% inhibition
cyclohexyl-phenylketone
-
cyclopentyl-phenylketone
-
DELTA9-tetrahydrocannabinol
-
-
deoxycorticosterone acetate
-
epirubicin hydrochloride
-
erythrosine sodium
i.e. disodium 2-(2,4,5,7-tetraiodo-6-oxido-3-oxo-3H-xanthen-9-yl)benzoate
haematin
0.00008 mM, 50% inhibition
iopanic acid
linear competitive inhibitor, i.e. 2-[(3-amino-2,4,6-triiodophenyl)methyl]butanoic acid
Ketoprofen
i.e. [3-(3-hydroxybut-3-en-2-yl)phenyl](phenyl)methanone
L-thyroxine
-
0.0039 mM, 50% inhibition, noncompetitve inhibition
N-(1,6-diamino-1-oxohexan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-2,3'-dihydroxybiphenyl-4-carboxamide
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-3-carboxamide
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3,3'-dihydroxybiphenyl-4-carboxamide
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(1H-indol-4-yl)benzamide
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(thiophen-2-yl)benzamide
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-6-(thiophen-2-yl)nicotinamide
N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
N-(1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
N-(1-amino-3-cyclohexyl-1-oxopropan-2-yl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
N-(1-amino-3-methyl-1-oxobutan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
N-(1-amino-4-methyl-1-oxopentan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
N-(1-amino-4-methyl-1-oxopentan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
N-(2-amino-2-oxoethyl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
N-(5-fluoro-3-methyl-1H-indol-1-yl)-2-(pyridin-2-yl)pyrimidine-5-carboxamide
-
-
N-(diphenylmethyl)-2-(3-hydroxyphenyl)-1,3-thiazole-4-carboxamide
N-(diphenylmethyl)-2-phenyl-1,3-thiazole-4-carboxamide
N-(diphenylmethyl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
N-(diphenylmethyl)-5-phenylthiophene-2-carboxamide
N-(diphenylmethyl)-5-[3-(hydroxymethyl)phenyl]thiophene-2-carboxamide
N-(diphenylmethyl)biphenyl-4-carboxamide
N-([4-[5-(2-hydroxypropan-2-yl)-1,2,4-oxadiazol-3-yl]phenyl]methyl)-2-phenylpyrimidine-5-carboxamide
-
N-benzhydryl-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
low micromolar potency in the inhibition of the purified enzyme
N-cyclopentyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine
-
-
N-cyclopentyl-3-(3-cyclopropyl-1H-pyrazol-4-yl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide
-
66% inhibition at 10 nM
N-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
-
-
N-methoxy-N-methyl-4-(5-benzoylbenzimidazole-2-yl)-3,5-dimethylpyrrole-2-carboxamide
-
TAS-204, specific H-PGDS inhibitor
N-phenyl-2-thiophene-carboxamide
-
N-[4-(morpholin-4-yl)phenyl]-2-phenoxypyrimidine-5-carboxamide
-
N-[4-methyl-3-({3-[(4-methylpiperazin-1-yl)methyl]benzoyl}amino)phenyl]-3-phenyl-1,2-thiazole-5-carboxamide
N-[4-methyl-3-[([3-[(4-methylpiperazin-1-yl)methyl]phenyl]carbonyl)amino]phenyl]-3-phenylisothiazole-5-carboxamide
-
N-[5-(1H-indol-4-yl)pyridin-3-yl]-2-(1-methyl-1H-imidazol-5-yl)acetamide
-
N-[5-(1H-indol-4-yl)pyridin-3-yl]-2-(1H-tetrazol-1-yl)acetamide
-
N-[5-(1H-indol-4-yl)pyridin-3-yl]-3-(piperidin-1-yl)propanamide
-
N-[5-(1H-indol-4-yl)pyridin-3-yl]-3-(pyridin-3-yl)propanamide
-
N-[5-(1H-indol-4-yl)pyridin-3-yl]-5-oxopyrrolidine-2-carboxamide (incorrect configuration definition!)
-
N-[5-(1H-indol-4-yl)pyridin-3-yl]propanamide
-
Na2SeO3
-
systemic administration of the inhibitor has sleep-reducing potency
p-hydroxymercuribenzoate
-
-
phenyl(thiophen-2-yl)methanone
phenyl-(2-thienyl)-methanol
-
phenyl-(3-thienyl)-methanone
-
prostaglandin E2-glyceryl ester
-
-
prostaglandin F2alpha
-
-
retinoic acid
non-competitive
sanguinarine sulfate
linear competitive inhibitor
Se2+
-
organic selenocompounds have no effect, hexavalent selenium compound is ineffective. The inhibition requires the preincubation of the metal with sulfhydryl compounds such as dithiothreitol, reversal of inhibition by excess amount of dithiothreitol. The rat spleen enzyme is much less inhibited than the rat brain enzyme
Tannic acid
nonlinear competitive inhibitor
tranilast
i.e. 2-{[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino}benzoic acid
Tributyltin acetate
0.00009 mM, 50% inhibition
tributyltin bromide
0.00003 mM, 50% inhibition
Tributyltin chloride
0.00001 mM, 50% inhibition
2-phenyl-5-(1H-pyrazol-3-yl)-1,3-thiazole
inhibitor generated by fragment-based drug design, crystallographic data
2-phenyl-5-(1H-pyrazol-3-yl)-1,3-thiazole
-
2-phenyl-5-(1H-pyrazol-3-yl)thiazole
-
-
2-phenyl-5-(1H-pyrazol-3-yl)thiazole
-
-
4-dibenzo [a,d]cyclohepten-5-ylidene-1-[4-(2H-tetrazol-5-yl)-butyl]-piperidine
-
i.e. AT-56, inhibits the activity of lipocalin-type prostaglandin-D synthase in a concentration-dependent manner, but does not affect the activities of hematopoietic prostaglandin-D synthase, cyclooxygenase-1 and -2, and microsomal PGE synthase-1. AT-56 inhibits the lipocalin-type prostaglandin-D synthase activity in a competitive manner against the substrate prostaglandin H2 but does not inhibit the binding of 13-cis-retinoic acid. AT-56 occupies the catalytic pocket, but not the retinoid-binding pocket, of lipocalin-type prostaglandin-D synthase
4-dibenzo [a,d]cyclohepten-5-ylidene-1-[4-(2H-tetrazol-5-yl)-butyl]-piperidine
i.e. AT-56. Orally administered AT-56 below 30 mg/kg body weight decreases the prostaglandin D2 production to 40% in the brain of H-PGDS-deficient mice after a stab-wound injury in a dose-dependent manner without affecting the production of prostaglandin E2 and prostaglandin F2alpha, and also suppresses the accumulation of eosinophils and monocytes in the bronco-alveolar lavage fluid from the antigen-induced lung inflammation model of human L-PGDS-transgenic mice
4-[[4-(4-fluoro-3-methylphenyl)-1,3-thiazol-2-yl]amino]-2-hydroxybenzoic acid
-
4-[[4-(4-fluoro-3-methylphenyl)-1,3-thiazol-2-yl]amino]-2-hydroxybenzoic acid
-
-
4-[[4-(4-fluoro-3-methylphenyl)-1,3-thiazol-2-yl]amino]-2-hydroxybenzoic acid
-
-
5-(3-cyanophenyl)-N-(diphenylmethyl)thiophene-2-carboxamide
-
-
5-(3-cyanophenyl)-N-(diphenylmethyl)thiophene-2-carboxamide
-
-
5-(3-hydroxyphenyl)thiophene-2-carboxylic acid
-
-
5-(3-hydroxyphenyl)thiophene-2-carboxylic acid
-
-
5-amino-4-[[(3'-hydroxybiphenyl-4-yl)carbonyl]amino]-5-oxopentanoic acid
-
-
5-amino-4-[[(3'-hydroxybiphenyl-4-yl)carbonyl]amino]-5-oxopentanoic acid
-
-
6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
-
-
Ethacrynic acid
-
Ethacrynic acid
i.e. [2,3-dichloro-4-(2-methylidenebutanoyl)phenoxy]acetic acid
HQL-79
-
HQL-79
-
i.e. 4-benzhydryloxy-1-[3-(1H-tetrazol-5-yl)-propyl]-piperidine, H-PGDS-specific inhibitor
N-(1,6-diamino-1-oxohexan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1,6-diamino-1-oxohexan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-2,3'-dihydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-2,3'-dihydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-3-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-3-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3,3'-dihydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-3,3'-dihydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(1H-indol-4-yl)benzamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(1H-indol-4-yl)benzamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(thiophen-2-yl)benzamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-4-(thiophen-2-yl)benzamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
-
-
N-(1-amino-1-oxo-3-phenylpropan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
-
-
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
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
N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
-
N-(1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
-
N-(1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
-
N-(1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
-
N-(1-amino-3-cyclohexyl-1-oxopropan-2-yl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
-
-
N-(1-amino-3-cyclohexyl-1-oxopropan-2-yl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
-
-
N-(1-amino-3-methyl-1-oxobutan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-3-methyl-1-oxobutan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-4-methyl-1-oxopentan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-4-methyl-1-oxopentan-2-yl)-3'-hydroxybiphenyl-4-carboxamide
-
-
N-(1-amino-4-methyl-1-oxopentan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
-
-
N-(1-amino-4-methyl-1-oxopentan-2-yl)-5-(3-hydroxyphenyl)-thiophene-2-carboxamide
-
-
N-(2-amino-2-oxoethyl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
-
N-(2-amino-2-oxoethyl)-5-(3-hydroxyphenyl)thiophene-2-carboxamide
-
-
N-(diphenylmethyl)-2-(3-hydroxyphenyl)-1,3-thiazole-4-carboxamide
-
-
N-(diphenylmethyl)-2-(3-hydroxyphenyl)-1,3-thiazole-4-carboxamide
-
-
N-(diphenylmethyl)-2-phenyl-1,3-thiazole-4-carboxamide
-
-
N-(diphenylmethyl)-2-phenyl-1,3-thiazole-4-carboxamide
-
-
N-(diphenylmethyl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
-
-
N-(diphenylmethyl)-5-(1H-indol-4-yl)thiophene-2-carboxamide
-
-
N-(diphenylmethyl)-5-phenylthiophene-2-carboxamide
-
-
N-(diphenylmethyl)-5-phenylthiophene-2-carboxamide
-
-
N-(diphenylmethyl)-5-[3-(hydroxymethyl)phenyl]thiophene-2-carboxamide
-
-
N-(diphenylmethyl)-5-[3-(hydroxymethyl)phenyl]thiophene-2-carboxamide
-
-
N-(diphenylmethyl)biphenyl-4-carboxamide
-
-
N-(diphenylmethyl)biphenyl-4-carboxamide
-
-
N-[4-methyl-3-({3-[(4-methylpiperazin-1-yl)methyl]benzoyl}amino)phenyl]-3-phenyl-1,2-thiazole-5-carboxamide
-
-
N-[4-methyl-3-({3-[(4-methylpiperazin-1-yl)methyl]benzoyl}amino)phenyl]-3-phenyl-1,2-thiazole-5-carboxamide
-
-
PCMB
-
-
phenyl(thiophen-2-yl)methanone
-
-
phenyl(thiophen-2-yl)methanone
-
-
Se4+
-
-
Se4+
-
organic selenocompounds have no effect, hexavalent selenium compound is ineffective. The inhibition requires the preincubation of the metal with sulfhydryl compounds such as dithiothreitol, reversal of inhibition by excess amount of dithiothreitol. The rat spleen enzyme is much less inhibited than the rat brain enzyme
Se4+
-
SeCl4; systemic administration of the inhibitor has sleep-reducing potency
SeCl4
-
-
SeCl4
-
selective inhibition of enzyme. Intraperitoneal injection of SeCl4 decreases the prostaglandin D2 content in the brain without affecting the amounts of prostaglandins E2 and F2alpha. It inhibits sleep dose-dependently and immediately after the administration
additional information
the lipid transporter activity of the enzyme is competitively inhibited by pamitate, stearate and arachnoate
-
additional information
-
the lipid transporter activity of the enzyme is competitively inhibited by pamitate, stearate and arachnoate
-
additional information
-
not inhibited by oleamide, palmitoylethanolamide, oleoylethanolamide, prostamide F2alpha, N-arachidonoylethanolamine/anandamide, and 2-arachidonoylglycerol
-