Information on EC 3.5.1.99 - fatty acid amide hydrolase and Organism(s) Homo sapiens and UniProt Accession O00519

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anandamide + H2O

ethanolamine + arachidonic acid

5 entries

arachidonyl-7-amino-4-methylcoumarin amide + H2O

arachidonic acid + 7-amino-4-methylcoumarin

fluorogenic substrate

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?

myristic amide + H2O

myristic acid + NH3

65% of the activity with anandamide

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?

N-arachidonoylethanolamine + H2O

arachidonic acid + ethanolamine

N-oleoylethanolamine + H2O

oleic acid + ethanolamine

N-oleoyltaurine + H2O

taurine + oleic acid

4% of the activity with anandamide

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?

N-palmitoylethanolamine + H2O

palmitic acid + ethanolamine

oleamide + H2O

oleic acid + NH3

oleoylethanolamide + H2O

oleic acid + ethanolamine

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-

?

palmitic amide + H2O

palmitic acid + NH3

33% of the activity with anandamide

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?

stearic amide + H2O

stearic acid + NH3

5.8% of the activity with anandamide

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?

(9Z)-N-ethyloctadec-9-enamide + H2O

oleic acid + ethanolamine

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-

?

anandamide + H2O

arachidonic acid + ethanolamine

5 entries

anandamide + H2O

ethanolamine + arachidonic acid

arachidonoyl 7-amido-4-methylcoumarin + H2O

arachidonic acid + 7-amino-4-methylcoumarin

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?

arachidonoyl ethanolamide + H2O

arachidonic acid + ethanolamine

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?

decanoyl 7-amido-4-methylcoumarin + H2O

?

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-

?

N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide + H2O

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752965, 754281

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?

N-(4-nitrophenyl)decanamide + H2O

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?

N-(4-nitrophenyl)octanamide + H2O

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N-(6-methoxypyridin-3-yl)decanamide + H2O

?

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?

N-(6-methoxypyridin-3-yl)octanamide + H2O

?

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?

N-oleoylethanolamine + H2O

oleic acid + ethanolamine

23% of the activity with oleamide

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?

N-palmitoyl ethanolamine + H2O

palmitic acid + ethanolamine

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-

?

N-palmitoylethanolamine + H2O

palmitic acid + ethanolamine

2.3% of the activity with oleamide

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?

oleamide + H2O

oleic acid + NH3

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?

oleoyl ethanolamide + H2O

oleic acid + ethanolamine

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?

oleoylethanolamide + H2O

oleic acid + ethanolamine

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?

palmitoylethanolamide + H2O

palmitic acid + ethanolamine

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substrate of FAAH and FAAH-2, the latter shows lower activity than FAAH

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?

additional information

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6 entries

anandamide + H2O

arachidonic acid + ethanolamine

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-

?

anandamide + H2O

ethanolamine + arachidonic acid

N-arachidonoylethanolamine + H2O

arachidonic acid + ethanolamine

N-oleoylethanolamine + H2O

oleic acid + ethanolamine

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-

?

N-palmitoylethanolamine + H2O

palmitic acid + ethanolamine

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-

?

oleamide + H2O

oleic acid + NH3

(9Z)-N-ethyloctadec-9-enamide + H2O

oleic acid + ethanolamine

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-

?

anandamide + H2O

arachidonic acid + ethanolamine

N-palmitoyl ethanolamine + H2O

palmitic acid + ethanolamine

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?

palmitoylethanolamide + H2O

palmitic acid + ethanolamine

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substrate of FAAH and FAAH-2, the latter shows lower activity than FAAH

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?

additional information

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(1-benzhydryltriazol-4-yl)methyl N-cyclohexylcarbamate

73% inhibition at 0.1 mM

(1-benzyltriazol-4-yl)methyl N-cyclohexylcarbamate

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(1-phenethyltriazol-4-yl)methyl N-cyclohexylcarbamate

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(1-phenyltriazol-4-yl)methyl N-cyclohexylcarbamate

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(1H-benzo[d][1,2,3]triazol-1-yl)(4-(3-phenoxybenzyl)-piperazin-1-yl)-methanone

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(1H-benzo[d][1,2,3]triazol-1-yl)(4-(4-phenoxybenzyl)-piperazin-1-yl)-methanone hydrochloride

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(1H-imidazol-1-yl)(4-(3-phenoxybenzyl)piperazin-1-yl)methanone

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(1H-imidazol-1-yl)(4-(4-phenoxy-benzyl)-piperazin-1-yl)-methanone hydrochloride

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(3-phenylphenyl)methyl N-cyclohexylcarbamate

65% inhibition at 0.1 mM

(3H-[1,2,3]triazol[4,5-b]pyridin-3-yl)(4-(3-phenoxybenzyl)-piperazin-1-yl)-methanone

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(3R,4R)-4-acetoxy-3-((10R)-(t-butyldimethylsilyloxy)-ethyl)-azetidin-2-one

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(4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)-piperidin-1-yl)(1H-1,2,4-triazol-1-yl)methanone

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(4-benzhydrylpiperazin-1-yl)(4-phenyl-1H-imidazol-1-yl)methanone

62% activity remaining at 0.01 mM

(4-phenylpiperazin-1-yl)(1H-1,2,4-triazol-1-yl)methanone

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(benzyl-1,2,4-triazol-3-yl)methyl N-cyclohexylcarbamate

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(S)-(4-oxo-1-pent-4-enoylazetidin-2-yl)methyl 2-(biphenyl-4-yl)acetate

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(S)-(4-oxo-1-pent-4-enoylazetidin-2-yl)methyl 3-(1H-indol-3-yl)propanoate

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(S)-(4-oxo-1-pent-4-enoylazetidin-2-yl)methyl biphenyl-4-carboxylate

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(S)-(4-oxo-1-pent-4-enoylazetidin-2-yl)methyl-4-phenylbutanoate

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1,1,1,3,3,3-hexafluoropropan-2-yl 4-(3-phenoxybenzyl)piperazine-1-carboxylate

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1-(1-phenyl-1,2,4-triazol-3-yl)methyl N-cyclohexylcarbamate

70% inhibition at 0.1 mM

1-[(3S)-1-[4-(1-benzofuran-2-yl)pyrimidin-2-yl]piperidin-3-yl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one

the compound belongs to the ketobenzimidazoles, though containing a carbonyl moiety, that do not covalently modify Ser241. These inhibitors achieve potent inhibition of FAAH activity primarily from shape complementarity to the active site and through numerous hydrophobic interactions exhibiting excellent selectivity and good pharmacokinetic properties, nonmechanism-based inhibition

1-[(3S)-2-oxo-1-(pent-4-enoyl)azetidin-3-yl]ethyl (benzyloxy)acetate

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1-[(3S)-2-oxo-1-(pent-4-enoyl)azetidin-3-yl]ethyl 3-(1H-indol-3-yl)propanoate

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1-[(3S)-2-oxo-1-(pent-4-enoyl)azetidin-3-yl]ethyl 4-(pyridin-2-yl)butanoate

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1-[(3S)-2-oxo-1-(pent-4-enoyl)azetidin-3-yl]ethyl 4-(pyridin-4-yl)butanoate

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1-[(3S)-2-oxo-1-(pent-4-enoyl)azetidin-3-yl]ethyl biphenyl-4-carboxylate

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1-[(3S)-2-oxo-1-(pent-4-enoyl)azetidin-3-yl]ethyl biphenyl-4-ylacetate

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1-[4-[bis(1,3-benzodioxol-5-yl)(hydroxy)methyl]piperidin-1-yl]-3,3,3-trifluoro-2-(trifluoromethyl)propan-1-one

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1H-benzotriazol-1-yl[4-(diphenylmethyl)piperazin-1-yl]methanone

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2,2,2-trichloroethyl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate

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2-(1-benzyltriazol-4-yl)ethyl N-cyclohexylcarbamate

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2-(1-phenyltriazol-4-yl)ethyl N-cyclohexylcarbamate

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2-(methylamino)-2-oxoethyl [2-[1-(6-methylpyridin-2-yl)piperidin-4-yl]ethyl]carbamate

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2H-benzotriazol-2-yl(4-phenylpiperazin-1-yl)methanone

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2H-benzotriazol-2-yl[4-(diphenylmethyl)piperazin-1-yl]methanone

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3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate

3'-carbamoylbiphenyl-3-yl undec-10-yn-1-ylcarbamate

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3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate

i.e. ASP8477

4-(3-phenoxybenzyl)-N-(4-methoxyphenyl)piperazine-1-carboxamide

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4-(3-phenoxybenzyl)-N-(4-nitrophenyl)piperazine-1-carboxamide

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4-(3-phenoxybenzyl)-N-phenylpiperazine-1-carboxamide

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4-(3-phenyl-1,2,4-thiadiazol-5-yl)-N-(pyridazin-3-yl)piperazine-1-carboxamide

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4-(benzyloxy)phenyl butylcarbamate

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4-benzhydryl-N-(4-(trifluoromethyl)phenyl)piperazine-1-carboxamide

86% activity remaining at 0.01 mM

4-benzhydryl-N-(4-butylphenyl)piperazine-1-carboxamide

84% activity remaining at 0.01 mM

4-benzhydryl-N-(4-methoxyphenyl)piperazine-1-carboxamide

89% activity remaining at 0.01 mM

4-benzhydryl-N-(4-nitrophenyl)piperazine-1-carboxamide

84% activity remaining at 0.01 mM

4-benzhydryl-N-(pyridin-2-yl)piperazine-1-carboxamide

87% activity remaining at 0.01 mM

4-benzhydryl-N-(pyridin-3-yl)piperazine-1-carboxamide

87% activity remaining at 0.01 mM

4-benzhydryl-N-phenylpiperazine-1-carboxamide

88% activity remaining at 0.01 mM

4-nitrophenyl 4-(3-phenoxybenzyl)piperazine-1-carboxylate

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4-nitrophenyl 4-(diphenylmethyl)piperazine-1-carboxylate

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4-nitrophenyl 4-[bis(1,3-benzodioxol-5-yl)(hydroxy)methyl]piperidine-1-carboxylate

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4-nitrophenyl 4-[bis(4-fluorophenyl)methyl]piperazine-1-carboxylate

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4-nitrophenyl-4-(4-phenoxy-benzyl)-piperazine-1-carboxylate

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4-nitrophenyl-4-(bis(benzo[d][1,3]dioxol-5-yl)methyl)piperidine-1-carboxylate

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4-[2-(2,4-difluorophenyl)pyridin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

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4-[2-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

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4-[3-(4-chlorophenoxy)benzyl]-N-(pyridin-3-yl)piperazine-1-carboxamide

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4-[4-(2,3-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

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4-[4-(2,4-difluorophenyl)-1,3-thiazol-2-yl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)piperazine-1-carboxamide

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733500, 733508

4-[4-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

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4-[4-(2,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

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4-[4-(2,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

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4-[4-(3,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

analgesic effect of 21d in rat inflammatory pain model, overview

4-[4-(3,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

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4-[6-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

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4-[6-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

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5-(4-hydroxyphenyl)pentanesulfonyl fluoride

i.e. AM3506, irreversible inhibitor for both the rat and the human enzyme, that covalently modifies the enzyme

6-bromo-N-(2-fluorophenyl)-1'H,4H-spiro[1,3-benzodioxine-2,4'-piperidine]-1'-carboxamide

an irreversible covalent inhibitor, binding structure, overview

6-hydroxybiphenyl-3-yl cyclohexylcarbamate

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7-phenyl-1-(5-pyridin-2-yl-1,3-oxazol-2-yl)heptan-1-one

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7-phenyl-1-[5-(pyridin-2-yl)-1,3-oxazol-2-yl]heptan-1-one

benzyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)-piperidine-1-carboxylate

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biphenyl-3-yl cyclohexylcarbamate

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CF3-OH

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ethyl 4-(1H-1,2,4-triazol-1-ylcarbonyl)piperazine-1-carboxylate

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ethyl 4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-ylcarbonyl)piperazine-1-carboxylate

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hexadecyl sulfonylfluoride

i.e. AM374, is a potent irreversible in vitro and in vivo inhibitor of fatty acid amide hydrolase

methyl arachidonoyl fluorophosphonate

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N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide

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N-(pyridazin-3-yl)-4-(3-[[5-(trifluoromethyl)pyridin-2-yl]oxy]benzylidene)piperidine-1-carboxamide

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N-(pyridin-3-yl)-4-(3-[[5-(trifluoromethyl)pyridin-2-yl]oxy]benzyl)piperidine-1-carboxamide

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N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide

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N-phenyl-4-(3-phenyl-4,5-dihydro-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide

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OL-135

7-phenyl-1-[5-(pyridin-2-yl)-1,3-oxazol-2-yl]heptan-1-one

phenylmethane sulfonyl fluoride

irreversible inhibition

pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate

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URB597

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[(2S)-4-oxo-1-(pent-4-enoyl)azetidin-2-yl]methyl (benzyloxy)acetate

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[(2S)-4-oxo-1-(pent-4-enoyl)azetidin-2-yl]methyl 4-(pyridin-2-yl)butanoate

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[(2S)-4-oxo-1-(pent-4-enoyl)azetidin-2-yl]methyl 4-(pyridin-4-yl)butanoate

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[1-(2-naphthylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-(m-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-(o-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-(p-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(2,6-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(2-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(2-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(2-fluoro-3-methoxy-phenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(2-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

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[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

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[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

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[1-[(3,5-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(3,5-dimethoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(3-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(3-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(3-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

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[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

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[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

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[1-[(4-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(4-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(4-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

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[4-(3-phenoxybenzyl)piperazin-1-yl](1H-1,2,4-triazol-1-yl)methanone

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[4-(diphenylmethyl)piperazin-1-yl](1H-1,2,4-triazol-1-yl)methanone

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[4-(diphenylmethyl)piperazin-1-yl](1H-imidazol-1-yl)methanone

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[4-[bis(1,3-benzodioxol-5-yl)methyl]piperidin-1-yl](1H-1,2,4-triazol-1-yl)methanone

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[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl](1H-1,2,4-triazol-1-yl)methanone

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(1-benzothiophen-6-ylamino)([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)methanone

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(1-benzylpiperidin-4-yl)[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl]methanone

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(10Z)-1,1,1-trifluorononadec-10-en-2-one

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(10Z)-1-bromononadec-10-en-2-one

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(10Z)-2-oxononadec-10-enamide

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(4-benzylpiperazin-1-yl)[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl]methanone

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(5Z,8Z,11Z,14Z)-1-pyridazin-3-ylicosa-5,8,11,14-tetraen-1-one

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(5Z,8Z,11Z,14Z)-1-[1,3]oxazolo[4,5-b]pyridin-2-ylicosa-5,8,11,14-tetraen-1-one

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(5Z,8Z,11Z,14Z)-1-[1,3]oxazolo[4,5-c]pyridin-2-ylicosa-5,8,11,14-tetraen-1-one

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(5Z,8Z,11Z,14Z)-1-[1,3]oxazolo[5,4-c]pyridin-2-ylicosa-5,8,11,14-tetraen-1-one

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(9E)-1-pyridazin-3-yloctadec-9-en-1-one

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(9E)-1-[1,3]oxazolo[4,5-b]pyridin-2-yloctadec-9-en-1-one

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(9Z)-1-(1,3-benzothiazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(1,3-benzoxazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(1,3-oxazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(1,3-thiazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(1-methyl-1H-benzimidazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(1-methyl-1H-imidazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(1-methyl-1H-tetrazol-5-yl)octadec-9-en-1-one

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(9Z)-1-(1H-benzimidazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(1H-tetrazol-5-yl)octadec-9-en-1-one

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(9Z)-1-(2-methyl-2H-tetrazol-5-yl)octadec-9-en-1-one

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(9Z)-1-(4,5-dihydro-1,3-oxazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(4-methyl-1,3-benzoxazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(5-methyl-1,3-benzoxazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(6-methyl-1,3-benzoxazol-2-yl)octadec-9-en-1-one

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(9Z)-1-(7-methyl-1,3-benzoxazol-2-yl)octadec-9-en-1-one

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(9Z)-1-phenyloctadec-9-en-1-one

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(9Z)-1-pyrazin-2-yloctadec-9-en-1-one

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(9Z)-1-pyridazin-3-yloctadec-9-en-1-one

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(9Z)-1-pyridin-2-yloctadec-9-en-1-one

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(9Z)-1-pyrimidin-2-yloctadec-9-en-1-one

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(9Z)-1-pyrimidin-4-yloctadec-9-en-1-one

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(9Z)-1-[1,3]oxazolo[4,5-b]pyridin-2-yloctadec-9-en-1-one

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(9Z)-1-[1,3]oxazolo[4,5-c]pyridin-2-yloctadec-9-en-1-one

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(9Z)-1-[1,3]oxazolo[5,4-b]pyridin-2-yloctadec-9-en-1-one

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(9Z)-1-[1,3]oxazolo[5,4-c]pyridin-2-yloctadec-9-en-1-one

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(9Z)-octadec-9-enal

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(dodecylamino)[[(E)-[1-[3-(thiophen-2-yl)phenyl]ethylidene]amino]oxy]methanone

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(phenylamino)[[(4-phenylcyclohexylidene)amino]oxy]methanone

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(phenylamino)[[(E)-[1-[3-(thiophen-2-yl)phenyl]ethylidene]amino]oxy]methanone

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(phenylamino)[[(E)-[1-[4-(thiophen-2-yl)phenyl]ethylidene]amino]oxy]methanone

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([(E)-[1-(2,2'-bithiophen-5-yl)ethylidene]amino]oxy)(naphthalen-1-ylamino)methanone

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([(E)-[1-(4-cyclohexylphenyl)ethylidene]amino]oxy)(naphthalen-1-ylamino)methanone

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([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)(diphenylamino)methanone

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([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)(naphthalen-1-ylamino)methanone

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([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)(phenylamino)methanone

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([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)(piperidin-1-yl)methanone

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([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)[(4-fluorophenyl)amino]methanone

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([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)[(4-methoxyphenyl)amino]methanone

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([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)[(5-phenylpentyl)amino]methanone

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([(E)-[1-(biphenyl-4-yl)ethylidene]amino]oxy)(dimethylamino)methanone

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([(E)-[1-(biphenyl-4-yl)ethylidene]amino]oxy)(naphthalen-1-ylamino)methanone

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([(E)-[1-(biphenyl-4-yl)ethylidene]amino]oxy)(phenylamino)methanone

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1,1,1-trifluoro-N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)methanesulfonamide

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1,2,3,4-tetrahydronaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

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59.6% inhibition at 0.01 mM

1-(1,3-benzoxazol-2-yl)octadecan-1-one

-

1-(1H-benzimidazol-1-yl)-3-(4-octylphenoxy)propan-2-one

-

1-(1H-benzotriazol-1-yl)-3-(4-octylphenoxy)propan-2-one

-

1-(1H-benzotriazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one

-

1-(1H-benzotriazol-1-yl)-3-[(3'-chloro[1,1'-biphenyl]-4-yl)oxy]propan-2-one

-

1-(1H-benzotriazol-1-yl)-3-[(3'-fluoro[1,1'-biphenyl]-4-yl)oxy]propan-2-one

-

1-(1H-benzotriazol-1-yl)-3-[(4'-chloro[1,1'-biphenyl]-4-yl)oxy]propan-2-one

-

1-(1H-benzotriazol-1-yl)-3-[(4'-fluoro[1,1'-biphenyl]-4-yl)oxy]butan-2-one

-

1-(1H-benzotriazol-1-yl)-3-[(4'-fluoro[1,1'-biphenyl]-4-yl)oxy]propan-2-one

-

1-(1H-benzotriazol-1-yl)-3-[([1,1'-biphenyl]-4-yl)oxy]butan-2-one

-

1-(1H-benzotriazol-1-yl)-3-[([1,1'-biphenyl]-4-yl)oxy]pentan-2-one

-

1-(1H-benzotriazol-1-yl)-3-[([1,1'-biphenyl]-4-yl)oxy]propan-2-one

-

1-(1H-imidazol-1-yl)-3-(4-octylphenoxy)propan-2-one

-

1-(1H-imidazo[4,5-b]pyridin-1-yl)-3-(4-octylphenoxy)propan-2-one

-

1-(1H-indazol-1-yl)-3-(4-octylphenoxy)propan-2-one

-

1-(1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one

-

1-(3H-imidazo[4,5-b]pyridin-3-yl)-3-(4-octylphenoxy)propan-2-one

-

1-(4-octylphenoxy)-3-(1H-1,2,4-triazol-1-yl)propan-2-one

-

1-(4-octylphenoxy)-3-(1H-pyrazol-1-yl)propan-2-one

-

1-(4-octylphenoxy)-3-(1H-pyrazolo[3,4-b]pyridin-1-yl)propan-2-one

-

1-(4-octylphenoxy)-3-(1H-pyrazolo[4,3-b]pyridin-1-yl)propan-2-one

-

1-(4-octylphenoxy)-3-(1H-tetrazol-1-yl)propan-2-one

-

1-(4-octylphenoxy)-3-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)propan-2-one

-

1-(4-octylphenoxy)-3-(2H-1,2,3-triazol-2-yl)propan-2-one

-

1-(4-octylphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one

-

1-(4-octylphenoxy)-3-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)propan-2-one

-

1-(4-phenoxyphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one

-

1-(5-nitro-1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one

-

1-([1,3]oxazolo[4,5-b]pyridin-2-yl)-6-phenylhexan-1-one

-

1-benzothiophen-4-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

1-pyridazin-3-yloctadecan-1-one

-

1-[(3R)-1-[4-(1-benzofuran-2-yl)pyrimidin-2-yl]piperidin-3-yl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one

-

1-[([1,1'-biphenyl]-4-yl)oxy]-3-(1H-tetrazol-1-yl)propan-2-one

-

1-[([1,1'-biphenyl]-4-yl)oxy]-3-(2H-tetrazol-2-yl)butan-2-one

-

1-[([1,1'-biphenyl]-4-yl)oxy]-3-(2H-tetrazol-2-yl)propan-2-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-4-phenylbutan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-5-phenylpentan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-6-phenylhexan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-7-phenylheptan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-8-phenyloctan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-9-phenylnonan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yldec-9-en-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yldec-9-yn-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yldecan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yldodecan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-ylethanone

-

1-[1,3]oxazolo[4,5-b]pyridin-2-ylheptan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-ylhexadecan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-ylhexan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yloctadec-9-yn-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yloctadecan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yloctan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-ylpentan-1-one

-

1-[1,3]oxazolo[4,5-b]pyridin-2-yltetradecan-1-one

-

1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazole-5-carboxylic acid

-

1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid

-

719302

1-[3-[(4'-chlorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid

-

1H-benzimidazol-4-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

1H-indol-4-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

2,3-dihydro-1,4-benzodioxin-5-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

2-(1H-benzotriazol-1-yl)-1-(5-phenoxy-1,3-benzoxazol-2-yl)ethan-1-one

-

2-hydroxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide

-

2-methoxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide

-

3'-carbamoyl[1,1'-biphenyl]-3-yl cyclohexylcarbamate

-

752472, 752965

3'-[(1E)-N-[(phenylcarbamoyl)oxy]ethanimidoyl]biphenyl-3-carboxamide

-

3-(1H-benzotriazol-1-yl)-1-[([1,1'-biphenyl]-4-yl)oxy]butan-2-one

-

3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate

i.e. ASP8477

3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N,N-diethylazetidine-1-carboxamide

-

3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-ethyl-N-(2-hydroxyethyl)azetidine-1-carboxamide

-

3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methyl-N-(2-phenylethyl)azetidine-1-carboxamide

-

3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methyl-N-phenylazetidine-1-carboxamide

-

3-[([1,1'-biphenyl]-4-yl)oxy]-1-(1H-tetrazol-1-yl)butan-2-one

-

3-[([1,1'-biphenyl]-4-yl)oxy]-1-(2H-tetrazol-2-yl)butan-2-one

-

4-(3-phenyl-[1,2,4]thiadiazol-5-yl)piperazine-1-carboxylic acid phenylamide

-

4-carbamoylnaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

4-fluoronaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

4-hydroxynaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

4-methoxynaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

4-[([4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamoyl)oxy]naphthalene-1-carboxylic acid

-

5,6,7,8-tetrahydronaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

7-phenyl-1-[5-(pyridin-2-yl)-1,3-oxazol-2-yl]heptan-1-one

azepan-1-yl[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl]methanone

-

azetidin-1-yl[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl]methanone

-

ethyl (10Z)-2-oxononadec-10-enoate

-

JP104

-

methyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate

-

N,N-dibenzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidine-1-carboxamide

-

N-(phenylcarbamoyl)-3'-[(1E)-N-[(phenylcarbamoyl)oxy]ethanimidoyl]biphenyl-3-carboxamide

-

N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)benzenesulfonamide

-

N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)methanesulfonamide

-

N-benzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-(2-hydroxyethyl)azetidine-1-carboxamide

-

N-benzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methylazetidine-1-carboxamide

-

N-benzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-[2-(dimethylamino)ethyl]azetidine-1-carboxamide

-

N-benzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidine-1-carboxamide

-

N-benzyl-3-[(R)-(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methylazetidine-1-carboxamide

-

N-benzyl-3-[(S)-(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methylazetidine-1-carboxamide

-

N-cyclohexyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea

-

N-ethyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea

-

N-tert-butyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidine-1-carboxamide

-

N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]-N'-phenylurea

-

N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide

-

N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide

-

a reversible, albeit slowly dissociating inhibitor of FAAH, reversibly and noncovalently inhibiting, molecular docking and computational modeling of interactions of the benzothiazole analogue 1 with humanized rat FAAH by induced fit docking, overview. Failure to observe the formation of covalent enzyme-inhibitor adduct or putative cleavage product using electrospray mass spectrometric techniques

naphthalen-1-yl (3-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]propyl)carbamate

-

naphthalen-1-yl (4-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]butyl)carbamate

-

naphthalen-1-yl [3-[4-(2,3-dichlorophenyl)piperazin-1-yl]propyl]carbamate

-

naphthalen-1-yl [3-[4-(3-methoxyphenyl)piperazin-1-yl]propyl]carbamate

-

naphthalen-1-yl [3-[4-(3-methylphenyl)piperazin-1-yl]propyl]carbamate

-

naphthalen-1-yl [4-[4-(3-methoxyphenyl)piperazin-1-yl]butyl]carbamate

-

naphthalen-1-yl [4-[4-(3-methylphenyl)piperazin-1-yl]butyl]carbamate

-

OL-135

-

oleoyl ethylamide

-

FAAH inhibitor

oleoyl oxazolopyridine

-

, i.e. oloxa, a potent noncompetitive inhibitor, almost complete inhibition at 50 nM

palmitoyl ethanolamide

-

a non-CB1 non-CB2 cannabinoid-like compound

phenyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate

-

phenyl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

-

piperidin-1-yl[[(E)-[1-[3-(thiophen-2-yl)phenyl]ethylidene]amino]oxy]methanone

-

pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate

-

URB532

-

URB597

VER-156084

-

a tetrasubstituted azetidine urea FAAH inhibitor

[1-(4-phenoxyphenoxy)-3-(2H-tetrazol-2-yl)propan-2-yl]cyanamide

-

-

[3-[(2-chlorophenyl)(4-chlorophenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[(2-chloropyridin-3-yl)(2-methylphenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[(2-chloropyridin-3-yl)(3,4-dichlorophenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[(2-chloropyridin-3-yl)(3-methoxyphenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[(2-chloropyridin-3-yl)(phenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[(3-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](1,3-dihydro-2H-isoindol-2-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](2-hydroxypiperidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](2-methylpiperidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](3,4-dihydroisoquinolin-2(1H)-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](3-hydroxypiperidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](3-hydroxypyrrolidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](3-methylpiperidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4,4-difluoropiperidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4-fluoropiperidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4-hydroxypiperidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4-methylpiperazin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4-methylpiperidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](morpholin-4-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](pyrrolidin-1-yl)methanone

-

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl][4-(hydroxymethyl)piperidin-1-yl]methanone

-

[3-[(4-chlorophenyl)(2-methylphenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[(6-chloropyridin-3-yl)(2-methylphenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[(S)-(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[1,3-benzodioxol-5-yl(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[3-[phenyl(pyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

-

[[(E)-[1-[4-(2,5-dimethyl-1H-pyrrol-1-yl)phenyl]ethylidene]amino]oxy](naphthalen-1-ylamino)methanone

-

additional information

16 entries

-

0.0024 - 0.0123

anandamide

0.00843

N-(6-methoxypyridin-3-yl)decanamide

-

pH 8.0, 30°C

0.16

N-(6-methoxypyridin-3-yl)octanamide

-

pH 8.0, 30°C

additional information

-

Michaelis-Menten kinetics, overview

-

0.00000165 - 0.00000399

pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate

0.000082

(10Z)-1,1,1-trifluorononadec-10-en-2-one

-

0.001

(10Z)-1-bromononadec-10-en-2-one

-

0.0009

(10Z)-2-oxononadec-10-enamide

-

0.000047

(5Z,8Z,11Z,14Z)-1-pyridazin-3-ylicosa-5,8,11,14-tetraen-1-one

-

0.000001

(5Z,8Z,11Z,14Z)-1-[1,3]oxazolo[4,5-b]pyridin-2-ylicosa-5,8,11,14-tetraen-1-one

-

0.000002

(5Z,8Z,11Z,14Z)-1-[1,3]oxazolo[4,5-c]pyridin-2-ylicosa-5,8,11,14-tetraen-1-one

-

0.000018

(5Z,8Z,11Z,14Z)-1-[1,3]oxazolo[5,4-c]pyridin-2-ylicosa-5,8,11,14-tetraen-1-one

-

0.00015

(9E)-1-pyridazin-3-yloctadec-9-en-1-one

-

0.0000032

(9E)-1-[1,3]oxazolo[4,5-b]pyridin-2-yloctadec-9-en-1-one

-

0.00037

(9Z)-1-(1,3-benzoxazol-2-yl)octadec-9-en-1-one

-

0.000017

(9Z)-1-(1,3-oxazol-2-yl)octadec-9-en-1-one

-

0.0037

(9Z)-1-(1-methyl-1H-tetrazol-5-yl)octadec-9-en-1-one

-

0.0098

(9Z)-1-(1H-tetrazol-5-yl)octadec-9-en-1-one

-

0.000065

(9Z)-1-(2-methyl-2H-tetrazol-5-yl)octadec-9-en-1-one

-

0.0045

(9Z)-1-(4,5-dihydro-1,3-oxazol-2-yl)octadec-9-en-1-one

-

0.013

(9Z)-1-(7-methyl-1,3-benzoxazol-2-yl)octadec-9-en-1-one

-

0.00054

(9Z)-1-pyrazin-2-yloctadec-9-en-1-one

-

0.00013

(9Z)-1-pyridazin-3-yloctadec-9-en-1-one

-

0.0025

(9Z)-1-pyrimidin-2-yloctadec-9-en-1-one

-

0.00011

(9Z)-1-pyrimidin-4-yloctadec-9-en-1-one

-

0.0000023

(9Z)-1-[1,3]oxazolo[4,5-b]pyridin-2-yloctadec-9-en-1-one

-

0.0000072

(9Z)-1-[1,3]oxazolo[4,5-c]pyridin-2-yloctadec-9-en-1-one

-

0.000011

(9Z)-1-[1,3]oxazolo[5,4-b]pyridin-2-yloctadec-9-en-1-one

-

0.0000037

(9Z)-1-[1,3]oxazolo[5,4-c]pyridin-2-yloctadec-9-en-1-one

-

0.0085

(9Z)-octadec-9-enal

-

0.000038

(phenylamino)[[(E)-[1-[3-(thiophen-2-yl)phenyl]ethylidene]amino]oxy]methanone

-

pH 8.4, 37°C

0.0024

1-(1,3-benzoxazol-2-yl)octadecan-1-one

-

0.0007

1-pyridazin-3-yloctadecan-1-one

-

0.0000069

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-4-phenylbutan-1-one

-

0.0000003

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-5-phenylpentan-1-one

-

0.0000002

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-6-phenylhexan-1-one

-

0.00000028

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-7-phenylheptan-1-one

-

0.00000039

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-8-phenyloctan-1-one

-

0.00000052

1-[1,3]oxazolo[4,5-b]pyridin-2-yl-9-phenylnonan-1-one

-

0.00000015

1-[1,3]oxazolo[4,5-b]pyridin-2-yldec-9-en-1-one

-

0.00000018

1-[1,3]oxazolo[4,5-b]pyridin-2-yldec-9-yn-1-one

-

0.00000075

1-[1,3]oxazolo[4,5-b]pyridin-2-yldecan-1-one

-

0.00000057

1-[1,3]oxazolo[4,5-b]pyridin-2-yldodecan-1-one

-

0.0000021

1-[1,3]oxazolo[4,5-b]pyridin-2-ylheptan-1-one

-

0.0000019

1-[1,3]oxazolo[4,5-b]pyridin-2-ylhexadecan-1-one

-

0.000015

1-[1,3]oxazolo[4,5-b]pyridin-2-ylhexan-1-one

-

0.00000014

1-[1,3]oxazolo[4,5-b]pyridin-2-yloctadec-9-yn-1-one

-

0.000011

1-[1,3]oxazolo[4,5-b]pyridin-2-yloctadecan-1-one

-

0.00000069

1-[1,3]oxazolo[4,5-b]pyridin-2-yloctan-1-one

-

0.00005

1-[1,3]oxazolo[4,5-b]pyridin-2-ylpentan-1-one

-

0.0000017

1-[1,3]oxazolo[4,5-b]pyridin-2-yltetradecan-1-one

-

0.0005

ethyl (10Z)-2-oxononadec-10-enoate

-

additional information

-

time-dependent inhibition kinetics with N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide, recombinant enzyme not purified, detailed overview

-

0.000089

(1H-benzo[d][1,2,3]triazol-1-yl)(4-(3-phenoxybenzyl)-piperazin-1-yl)-methanone

Homo sapiens

pH and temperature not specified in the publication

0.000708

(1H-benzo[d][1,2,3]triazol-1-yl)(4-(4-phenoxybenzyl)-piperazin-1-yl)-methanone hydrochloride

Homo sapiens

pH and temperature not specified in the publication

0.000015

(1H-imidazol-1-yl)(4-(3-phenoxybenzyl)piperazin-1-yl)methanone

Homo sapiens

pH and temperature not specified in the publication

0.0000034

(1H-imidazol-1-yl)(4-(4-phenoxy-benzyl)-piperazin-1-yl)-methanone hydrochloride

Homo sapiens

pH and temperature not specified in the publication

0.000023

(3H-[1,2,3]triazol[4,5-b]pyridin-3-yl)(4-(3-phenoxybenzyl)-piperazin-1-yl)-methanone

Homo sapiens

pH and temperature not specified in the publication

0.000005

(3R,4R)-4-acetoxy-3-((10R)-(t-butyldimethylsilyloxy)-ethyl)-azetidin-2-one

Homo sapiens

pH 7.4, 37°C

0.00162

(4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)-piperidin-1-yl)(1H-1,2,4-triazol-1-yl)methanone

Homo sapiens

pH and temperature not specified in the publication

0.00782

(S)-(4-oxo-1-pent-4-enoylazetidin-2-yl)methyl 2-(biphenyl-4-yl)acetate

Homo sapiens

pH 7.4, 37°C

0.00805

(S)-(4-oxo-1-pent-4-enoylazetidin-2-yl)methyl 3-(1H-indol-3-yl)propanoate

Homo sapiens

pH 7.4, 37°C

0.00091

(S)-(4-oxo-1-pent-4-enoylazetidin-2-yl)methyl biphenyl-4-carboxylate

Homo sapiens

pH 7.4, 37°C

0.00503

(S)-(4-oxo-1-pent-4-enoylazetidin-2-yl)methyl-4-phenylbutanoate

Homo sapiens

pH 7.4, 37°C

0.00000188

1,1,1,3,3,3-hexafluoropropan-2-yl 4-(3-phenoxybenzyl)piperazine-1-carboxylate

Homo sapiens

pH and temperature not specified in the publication

0.000028

1-[(3S)-1-[4-(1-benzofuran-2-yl)pyrimidin-2-yl]piperidin-3-yl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one

Homo sapiens

pH and temperature not specified in the publication

0.000031

1-[(3S)-2-oxo-1-(pent-4-enoyl)azetidin-3-yl]ethyl (benzyloxy)acetate

Homo sapiens

pH 7.4, 37°C

0.00031

1-[(3S)-2-oxo-1-(pent-4-enoyl)azetidin-3-yl]ethyl 4-(pyridin-4-yl)butanoate

Homo sapiens

pH 7.4, 37°C

0.000012

1-[(3S)-2-oxo-1-(pent-4-enoyl)azetidin-3-yl]ethyl biphenyl-4-ylacetate

Homo sapiens

pH 7.4, 37°C

0.00196

2,2,2-trichloroethyl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate

Homo sapiens

pH and temperature not specified in the publication

0.00000038

3'-carbamoylbiphenyl-3-yl undec-10-yn-1-ylcarbamate

Homo sapiens

pH 9.0, 37°C

0.00000165 - 0.00000399

3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate

0.00000175

4-(3-phenoxybenzyl)-N-(4-methoxyphenyl)piperazine-1-carboxamide

Homo sapiens

pH and temperature not specified in the publication

0.00000199

4-(3-phenoxybenzyl)-N-(4-nitrophenyl)piperazine-1-carboxamide

Homo sapiens

pH and temperature not specified in the publication

0.00302

4-(3-phenoxybenzyl)-N-phenylpiperazine-1-carboxamide

Homo sapiens

pH and temperature not specified in the publication

0.0000029

4-(3-phenyl-1,2,4-thiadiazol-5-yl)-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.000283

4-(benzyloxy)phenyl butylcarbamate

Homo sapiens

pH 9.0, 37°C

0.00000163

4-nitrophenyl-4-(4-phenoxy-benzyl)-piperazine-1-carboxylate

Homo sapiens

pH and temperature not specified in the publication

0.00194

4-nitrophenyl-4-(bis(benzo[d][1,3]dioxol-5-yl)methyl)piperidine-1-carboxylate

Homo sapiens

pH and temperature not specified in the publication

0.000028

4-[2-(2,4-difluorophenyl)pyridin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.000023

4-[2-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.000000072

4-[4-(2,3-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.00000043

4-[4-(2,4-difluorophenyl)-1,3-thiazol-2-yl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.0000022 - 0.00014

4-[4-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

0.0000011

4-[4-(2,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.000000025

4-[4-(2,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.00000072

4-[4-(3,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.0000008

4-[4-(3,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.000036

4-[6-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.0000015

4-[6-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.0000051

5-(4-hydroxyphenyl)pentanesulfonyl fluoride

Homo sapiens

pH 7.4, 25°C

0.000005

6-bromo-N-(2-fluorophenyl)-1'H,4H-spiro[1,3-benzodioxine-2,4'-piperidine]-1'-carboxamide

Homo sapiens

pH and temperature not specified in the publication

0.000206

7-phenyl-1-(5-pyridin-2-yl-1,3-oxazol-2-yl)heptan-1-one

Homo sapiens

pH 9.0, 37°C

0.00195

benzyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)-piperidine-1-carboxylate

Homo sapiens

pH and temperature not specified in the publication

0.0000017

N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.000011

N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide

Homo sapiens

pH 9.0, 37°C

0.000016

OL-135

Homo sapiens

pH and temperature not specified in the publication

0.000004

URB597

Homo sapiens

pH and temperature not specified in the publication

0.04252

[(2S)-4-oxo-1-(pent-4-enoyl)azetidin-2-yl]methyl (benzyloxy)acetate

Homo sapiens

pH 7.4, 37°C

0.08706

[(2S)-4-oxo-1-(pent-4-enoyl)azetidin-2-yl]methyl 4-(pyridin-2-yl)butanoate

Homo sapiens

pH 7.4, 37°C

0.173

[(2S)-4-oxo-1-(pent-4-enoyl)azetidin-2-yl]methyl 4-(pyridin-4-yl)butanoate

Homo sapiens

pH 7.4, 37°C

0.002

[1-(2-naphthylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000245

[1-(m-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000215

[1-(o-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0005

[1-(p-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000119

[1-[(2,6-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000062

[1-[(2-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000195

[1-[(2-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000446

[1-[(2-fluoro-3-methoxy-phenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000099

[1-[(2-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000014

[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.000154

[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

Homo sapiens

pH 7.4, 37°C

0.0000032

[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

Homo sapiens

pH 7.4, 37°C

0.0000076

[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

Homo sapiens

pH 7.4, 37°C

0.0000104

[1-[(3,5-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000036

[1-[(3,5-dimethoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000132

[1-[(3-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000215

[1-[(3-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000121

[1-[(3-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000118

[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000098

[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

Homo sapiens

pH 7.4, 37°C

0.0000039

[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

Homo sapiens

pH 7.4, 37°C

0.0000058

[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate

Homo sapiens

pH 7.4, 37°C

0.000215

[1-[(4-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.002282

[1-[(4-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.0000955

[1-[(4-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.000627

[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate

Homo sapiens

pH 7.4, 37°C

0.000232

(1-benzothiophen-6-ylamino)([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)methanone

Homo sapiens

-

pH 8.4, 37°C

0.000537

(1-benzylpiperidin-4-yl)[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl]methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.00109

(4-benzylpiperazin-1-yl)[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl]methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.000116

(dodecylamino)[[(E)-[1-[3-(thiophen-2-yl)phenyl]ethylidene]amino]oxy]methanone

Homo sapiens

-

pH 8.4, 37°C

0.05

(phenylamino)[[(4-phenylcyclohexylidene)amino]oxy]methanone

Homo sapiens

-

pH 8.4, 37°C

0.000008

(phenylamino)[[(E)-[1-[3-(thiophen-2-yl)phenyl]ethylidene]amino]oxy]methanone

Homo sapiens

-

pH 8.4, 37°C

0.0002

(phenylamino)[[(E)-[1-[4-(thiophen-2-yl)phenyl]ethylidene]amino]oxy]methanone

Homo sapiens

-

pH 8.4, 37°C

0.001

([(E)-[1-(2,2'-bithiophen-5-yl)ethylidene]amino]oxy)(naphthalen-1-ylamino)methanone

Homo sapiens

-

pH 8.4, 37°C

0.001

([(E)-[1-(4-cyclohexylphenyl)ethylidene]amino]oxy)(naphthalen-1-ylamino)methanone

Homo sapiens

-

pH 8.4, 37°C

0.05

([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)(diphenylamino)methanone

Homo sapiens

-

pH 8.4, 37°C

0.00001

([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)(naphthalen-1-ylamino)methanone

Homo sapiens

-

pH 8.4, 37°C

0.000069

([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)(phenylamino)methanone

Homo sapiens

-

pH 8.4, 37°C

0.00022

([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)(piperidin-1-yl)methanone

Homo sapiens

-

pH 8.4, 37°C

0.000017

([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)[(4-fluorophenyl)amino]methanone

Homo sapiens

-

pH 8.4, 37°C

0.000028

([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)[(4-methoxyphenyl)amino]methanone

Homo sapiens

-

pH 8.4, 37°C

0.0001

([(E)-[1-(biphenyl-3-yl)ethylidene]amino]oxy)[(5-phenylpentyl)amino]methanone

Homo sapiens

-

pH 8.4, 37°C

0.05

([(E)-[1-(biphenyl-4-yl)ethylidene]amino]oxy)(dimethylamino)methanone

Homo sapiens

-

pH 8.4, 37°C

0.000401

([(E)-[1-(biphenyl-4-yl)ethylidene]amino]oxy)(naphthalen-1-ylamino)methanone

Homo sapiens

-

pH 8.4, 37°C

0.00076

([(E)-[1-(biphenyl-4-yl)ethylidene]amino]oxy)(phenylamino)methanone

Homo sapiens

-

pH 8.4, 37°C

0.00051

1,1,1-trifluoro-N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)methanesulfonamide

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.00048

1-(1H-benzimidazol-1-yl)-3-(4-octylphenoxy)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000015

1-(1H-benzotriazol-1-yl)-3-(4-octylphenoxy)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000024

1-(1H-benzotriazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one

Homo sapiens

-

pH and temperature not specified in the publication

0.000011

1-(1H-benzotriazol-1-yl)-3-[(3'-chloro[1,1'-biphenyl]-4-yl)oxy]propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000014

1-(1H-benzotriazol-1-yl)-3-[(3'-fluoro[1,1'-biphenyl]-4-yl)oxy]propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000021

1-(1H-benzotriazol-1-yl)-3-[(4'-chloro[1,1'-biphenyl]-4-yl)oxy]propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000012

1-(1H-benzotriazol-1-yl)-3-[(4'-fluoro[1,1'-biphenyl]-4-yl)oxy]butan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000012

1-(1H-benzotriazol-1-yl)-3-[(4'-fluoro[1,1'-biphenyl]-4-yl)oxy]propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000013

1-(1H-benzotriazol-1-yl)-3-[([1,1'-biphenyl]-4-yl)oxy]butan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0018

1-(1H-benzotriazol-1-yl)-3-[([1,1'-biphenyl]-4-yl)oxy]pentan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000012

1-(1H-benzotriazol-1-yl)-3-[([1,1'-biphenyl]-4-yl)oxy]propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.00041

1-(1H-imidazol-1-yl)-3-(4-octylphenoxy)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.00062

1-(1H-imidazo[4,5-b]pyridin-1-yl)-3-(4-octylphenoxy)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0023

1-(1H-indazol-1-yl)-3-(4-octylphenoxy)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0026

1-(1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.00041

1-(3H-imidazo[4,5-b]pyridin-3-yl)-3-(4-octylphenoxy)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000053

1-(4-octylphenoxy)-3-(1H-1,2,4-triazol-1-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.00084

1-(4-octylphenoxy)-3-(1H-pyrazol-1-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0016

1-(4-octylphenoxy)-3-(1H-pyrazolo[3,4-b]pyridin-1-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000093

1-(4-octylphenoxy)-3-(1H-pyrazolo[4,3-b]pyridin-1-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000039

1-(4-octylphenoxy)-3-(1H-tetrazol-1-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000049

1-(4-octylphenoxy)-3-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000112

1-(4-octylphenoxy)-3-(2H-1,2,3-triazol-2-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000013

1-(4-octylphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000013

1-(4-octylphenoxy)-3-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000008

1-(4-phenoxyphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one

Homo sapiens

-

pH and temperature not specified in the publication

0.00055

1-(5-nitro-1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0000029

1-([1,3]oxazolo[4,5-b]pyridin-2-yl)-6-phenylhexan-1-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0000114

1-benzothiophen-4-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.00211 - 0.99146

1-[(3R)-1-[4-(1-benzofuran-2-yl)pyrimidin-2-yl]piperidin-3-yl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one

0.000043

1-[([1,1'-biphenyl]-4-yl)oxy]-3-(1H-tetrazol-1-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0063

1-[([1,1'-biphenyl]-4-yl)oxy]-3-(2H-tetrazol-2-yl)butan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000011

1-[([1,1'-biphenyl]-4-yl)oxy]-3-(2H-tetrazol-2-yl)propan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000055

1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazole-5-carboxylic acid

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.00503

1-[3-[(4'-chlorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid

Homo sapiens

-

pH and temperature not specified in the publication

0.0000075

1H-benzimidazol-4-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000069

1H-indol-4-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000306

2,3-dihydro-1,4-benzodioxin-5-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.01

2-(1H-benzotriazol-1-yl)-1-(5-phenoxy-1,3-benzoxazol-2-yl)ethan-1-one

Homo sapiens

-

pH and temperature not specified in the publication

0.0054

2-hydroxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0063

2-methoxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.00006 - 0.000112

3'-carbamoyl[1,1'-biphenyl]-3-yl cyclohexylcarbamate

0.000084

3'-[(1E)-N-[(phenylcarbamoyl)oxy]ethanimidoyl]biphenyl-3-carboxamide

Homo sapiens

-

pH 8.4, 37°C

0.00063

3-(1H-benzotriazol-1-yl)-1-[([1,1'-biphenyl]-4-yl)oxy]butan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0000573

3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate

Homo sapiens

pH 8.0, 37°C, wild-type enzyme

0.0624

3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N,N-diethylazetidine-1-carboxamide

Homo sapiens

-

pH and temperature not specified in the publication

0.5

3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-ethyl-N-(2-hydroxyethyl)azetidine-1-carboxamide

Homo sapiens

-

above, pH and temperature not specified in the publication

0.00654

3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methyl-N-(2-phenylethyl)azetidine-1-carboxamide

Homo sapiens

-

pH and temperature not specified in the publication

0.193

3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methyl-N-phenylazetidine-1-carboxamide

Homo sapiens

-

pH and temperature not specified in the publication

0.000019

3-[([1,1'-biphenyl]-4-yl)oxy]-1-(1H-tetrazol-1-yl)butan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000009

3-[([1,1'-biphenyl]-4-yl)oxy]-1-(2H-tetrazol-2-yl)butan-2-one

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000012

4-(3-phenyl-[1,2,4]thiadiazol-5-yl)piperazine-1-carboxylic acid phenylamide

Homo sapiens

JNJ-1661010, without preincubation

0.0000033

4-carbamoylnaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000045

4-fluoronaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000062

4-hydroxynaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.000229

4-methoxynaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000034

4-[([4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamoyl)oxy]naphthalene-1-carboxylic acid

Homo sapiens

-

pH and temperature not specified in the publication

0.000244

5,6,7,8-tetrahydronaphthalen-1-yl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0111

azepan-1-yl[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl]methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.0988

azetidin-1-yl[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl]methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.000001

JP104

Homo sapiens

pH 9.0, 37°C

0.004

methyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.5

N,N-dibenzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidine-1-carboxamide

Homo sapiens

-

above, pH and temperature not specified in the publication

0.025

N-(phenylcarbamoyl)-3'-[(1E)-N-[(phenylcarbamoyl)oxy]ethanimidoyl]biphenyl-3-carboxamide

Homo sapiens

-

pH 8.4, 37°C

0.0047

N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)benzenesulfonamide

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.00077

N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)methanesulfonamide

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.5

N-benzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-(2-hydroxyethyl)azetidine-1-carboxamide

Homo sapiens

-

above, pH and temperature not specified in the publication

0.00209

N-benzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methylazetidine-1-carboxamide

Homo sapiens

-

pH and temperature not specified in the publication

0.5

N-benzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-[2-(dimethylamino)ethyl]azetidine-1-carboxamide

Homo sapiens

-

above, pH and temperature not specified in the publication

0.5

N-benzyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidine-1-carboxamide

Homo sapiens

-

above, pH and temperature not specified in the publication

0.887

N-benzyl-3-[(R)-(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methylazetidine-1-carboxamide

Homo sapiens

-

pH and temperature not specified in the publication

0.0408

N-benzyl-3-[(S)-(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]-N-methylazetidine-1-carboxamide

Homo sapiens

-

pH and temperature not specified in the publication

0.00084

N-cyclohexyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0016

N-ethyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.5

N-tert-butyl-3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidine-1-carboxamide

Homo sapiens

-

above, pH and temperature not specified in the publication

0.006

N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]-N'-phenylurea

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.0039

N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.000002 - 0.0000051

N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide

0.0000069

naphthalen-1-yl (3-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]propyl)carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000215

naphthalen-1-yl (4-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]butyl)carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000062

naphthalen-1-yl [3-[4-(2,3-dichlorophenyl)piperazin-1-yl]propyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000064

naphthalen-1-yl [3-[4-(3-methoxyphenyl)piperazin-1-yl]propyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000053

naphthalen-1-yl [3-[4-(3-methylphenyl)piperazin-1-yl]propyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000486

naphthalen-1-yl [4-[4-(3-methoxyphenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.000013

naphthalen-1-yl [4-[4-(3-methylphenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.0000134

OL-135

Homo sapiens

pH 9.0, 37°C

0.0000243

oleoyl oxazolopyridine

Homo sapiens

-

recombinant enzyme, pH 7.3, 37°C

0.0021

phenyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate

Homo sapiens

-

37°C, pH 7.4, assay in brain microsomes, substrate N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide

0.00000063

phenyl [4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]carbamate

Homo sapiens

-

pH and temperature not specified in the publication

0.000112

piperidin-1-yl[[(E)-[1-[3-(thiophen-2-yl)phenyl]ethylidene]amino]oxy]methanone

Homo sapiens

-

pH 8.4, 37°C

0.0000573

pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate

Homo sapiens

37°C, pH 8.0

0.00136

URB532

Homo sapiens

pH 9.0, 37°C

0.0053

[1-(4-phenoxyphenoxy)-3-(2H-tetrazol-2-yl)propan-2-yl]cyanamide

Homo sapiens

-

pH and temperature not specified in the publication

-

0.132

[3-[(2-chlorophenyl)(4-chlorophenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

above, pH and temperature not specified in the publication

0.206

[3-[(2-chloropyridin-3-yl)(2-methylphenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.00669

[3-[(2-chloropyridin-3-yl)(3,4-dichlorophenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.00717

[3-[(2-chloropyridin-3-yl)(3-methoxyphenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.00739

[3-[(2-chloropyridin-3-yl)(phenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.0366

[3-[(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.00501

[3-[(3-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.0247

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](1,3-dihydro-2H-isoindol-2-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.5

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](2-hydroxypiperidin-1-yl)methanone

Homo sapiens

-

above, pH and temperature not specified in the publication

0.00504

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](2-methylpiperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.00682

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](3,4-dihydroisoquinolin-2(1H)-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.135

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](3-hydroxypiperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.5

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](3-hydroxypyrrolidin-1-yl)methanone

Homo sapiens

-

above, pH and temperature not specified in the publication

0.0164

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](3-methylpiperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.0051

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4,4-difluoropiperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.00225

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4-fluoropiperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.037

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4-hydroxypiperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.0286

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4-methylpiperazin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.000423

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](4-methylpiperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.0279

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](morpholin-4-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.0705

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](pyrrolidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.0174

[3-[(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl][4-(hydroxymethyl)piperidin-1-yl]methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.0096

[3-[(4-chlorophenyl)(2-methylphenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.5

[3-[(6-chloropyridin-3-yl)(2-methylphenyl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

above, pH and temperature not specified in the publication

0.5

[3-[(S)-(4-chlorophenyl)(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

above, pH and temperature not specified in the publication

0.00332

[3-[1,3-benzodioxol-5-yl(2-chloropyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

Homo sapiens

-

pH and temperature not specified in the publication

0.00809 - 0.0829

[3-[phenyl(pyridin-3-yl)methoxy]azetidin-1-yl](piperidin-1-yl)methanone

0.001

[[(E)-[1-[4-(2,5-dimethyl-1H-pyrrol-1-yl)phenyl]ethylidene]amino]oxy](naphthalen-1-ylamino)methanone

Homo sapiens

-

pH 8.4, 37°C

0.00908

-

Vmax, substrate: N-(6-methoxypyridin-3-yl)decanamide, pH 8.0, 30°C

0.0213

-

Vmax, substrate: N-(6-methoxypyridin-3-yl)octanamide, pH 8.0, 30°C

7.4

9

assay at

7.3

-

assay at

8

-

assay at

8.4

-

assay at

9

-

assay at

25

assay at

37

22

-

assay at room temperature

37

-

assay at

718570, 719048

-

687528, 694924, 720927, 733500, 733508, 733662, 734378, 734439, 753501

SwissProt

-

-

-

-

-

-

-

-

-

-

primary

highly expressed

-

-

-

-

-

-

-

-

mucosa, urothelium, no FAAH immunoreactivity in other structures of the bladder

-

additional information

7 entries

membrane

endoplasmic reticulum

-

FAAH

5783

endoplasmic reticulum membrane

-

-

FAAH-2, localization of FAAH-2 on the cytoplasmic face of lipid droplets, lipid droplet localization is essential for FAAH-2

-

718570, 719048, 719071, 719302

-

-

additional information

evolution

fatty acid amide hydrolase is an amidase-signature family member

malfunction

enzyme inhibition and deficiency causes increased central and peripheral neuronal levels of anandamide and other FAAs producing physiological effects including analgesia, apoptosis in various cancer cells, 12-14 modulation of memory processes, neuroprotection, epilepsy, feeding, and prevention of neurotoxicity of the human amyloid-beta peptide in Alzheimer's disease. Also anti-depressant, anxiolytic, antiinflammatory, anti-hypertensive, gastrointestinal and sleep-inducing effects are observed

metabolism

fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) are key hydrolytic enzymes of the endocannabinoid system

physiological function

metabolism

physiological function

additional information

6 entries

O00519 pBLAST

FAAH1_HUMAN

579

1

63066

Swiss-Prot

Show Sequence

Secretory Pathway (Reliability: 2)

63000

-

x * 63000, about, SDS-PAGE

?

-

x * 63000, about, SDS-PAGE

additional information

three major cavities in the active site are the membrane access channel, the acyl-chain binding pocket, and the cytosolic port, overview. The core structure of the FAAH monomer adopts an alpha/beta fold with a twisted 11-strand beta-sheet in the center and 24 alpha-helices surrounding the sheet

glycoprotein

-

FAAH is N-glycosylated

no glycoprotein

-

FAAH-2 does not undergo N-glycosylation

purified recombinant His-tagged apo FAAH, hanging drop vapor diffusion method, X-ray diffraction structure determination and analysis at 2.9 A resolution, molecular replacement

additional information

recombinant FAAH-1 partially from HEK-293 cells by membrane preparation

recombinant His-tagged FAAH from Escherichia coli strain by nickel affinity chromatography

cloning from a human brain library as cDNA library, recombinant stable expression in CHO-K1 cells

expressed in COS-7

expression of His-tagged FAAH in Escherichia coli strain

recombinant expression of FAAH-1 in HEK-293 cells

recombinant expression of N-terminal maltose-binding protein fusion enzyme in CHO cells

transient expression of the enzyme in COS7 cells

-

FLAG-tagged FAAH and FAAH-2 expression in HeLa and COS-7 cells, analysis of subcellular localization of full-length and truncated enzymes in transfected cells, overview

-

stable expression of FAAH in CHO cells

-

medicine

there is significant therapeutic potential for FAAH inhibitors as analgesic, neuroprotective, anti-inflammatory and anti-anxiety drugs, and as agents for the treatment of metabolic and sleep disorders

medicine

Wei, B.Q.; Mikkelsen, T.S.; McKinney, M.K.; Lander, E.S.; Cravatt, B.F.

A second fatty acid amide hydrolase with variable distribution among placental mammals

J. Biol. Chem.

281

36569-36578

2006

Homo sapiens (O00519), Homo sapiens (Q6GMR7), Homo sapiens, Mus musculus (O08914), Mus musculus, Rattus norvegicus (P97612)

17015445

690846

Fowler, C.J.; Jonsson, K.O.; Tiger, G.

Fatty acid amide hydrolase: biochemistry, pharmacology, and therapeutic possibilities for an enzyme hydrolyzing anandamide, 2-arachidonoylglycerol, palmitoylethanolamide, and oleamide

Biochem. Pharmacol.

62

517-26

2001

Homo sapiens, Mus musculus, Rattus norvegicus, Sus scrofa

11585048

Giang, D.K.; Cravatt, B.F.

Molecular characterization of human and mouse fatty acid amide hydrolases

Proc. Natl. Acad. Sci. USA

94

2238-2242

1997

Rattus norvegicus, Homo sapiens (O00519), Homo sapiens, Mus musculus (O08914), Mus musculus

9122178

Boger, D.L.; Sato, H.; Lerner, A.E.; Hedrick, M.P.; Fecik, R.A.; Miyauchi, H.; Wilkie, G.D.; Austin, B.J.; Patricelli, M.P.; Cravatt, B.F.

Exceptionally potent inhibitors of fatty acid amide hydrolase: the enzyme responsible for degradation of endogenous oleamide and anandamide

Proc. Natl. Acad. Sci. USA

97

5044-5049

2000

Homo sapiens, Rattus norvegicus

10805767

Karbarz, M.J.; Luo, L.; Chang, L.; Tham, C.S.; Palmer, J.A.; Wilson, S.J.; Wennerholm, M.L.; Brown, S.M.; Scott, B.P.; Apodaca, R.L.; Keith, J.M.; Wu, J.; Breitenbucher, J.G.; Chaplan, S.R.; Webb, M.

Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase

Anesth. Analg.

108

316-329

2009

Rattus norvegicus, Homo sapiens (Q6GMR7), Homo sapiens

19095868

Kaczocha, M.; Glaser, S.T.; Chae, J.; Brown, D.A.; Deutsch, D.G.

Lipid droplets are novel sites of N-acylethanolamine inactivation by fatty acid amide hydrolase-2

J. Biol. Chem.

285

2796-2806

2010

Homo sapiens

19926788

Rakers, C.; Zoerner, A.A.; Engeli, S.; Batkai, S.; Jordan, J.; Tsikas, D.

Stable isotope liquid chromatography-tandem mass spectrometry assay for fatty acid amide hydrolase activity

Anal. Biochem.

421

699-705

2012

Canis lupus familiaris, Homo sapiens

22146559

Tian, G.; Paschetto, K.A.; Gharahdaghi, F.; Gordon, E.; Wilkins, D.E.; Luo, X.; Scott, C.W.

Mechanism of inhibition of fatty acid amide hydrolase by sulfonamide-containing benzothiazoles: long residence time derived from increased kinetic barrier and not exclusively from thermodynamic potency

Biochemistry

50

6867-6878

2011

Homo sapiens, Rattus norvegicus

21728345

Gattinoni, S.; Simone, C.D.; Dallavalle, S.; Fezza, F.; Nannei, R.; Battista, N.; Minetti, P.; Quattrociocchi, G.; Caprioli, A.; Borsini, F.; Cabri, W.; Penco, S.; Merlini, L.; Maccarrone, M.

A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase

Bioorg. Med. Chem. Lett.

20

4406-4411

2010

Homo sapiens

20591666

Roughley, S.D.; Browne, H.; Macias, A.T.; Benwell, K.; Brooks, T.; D'Alessandro, J.; Daniels, Z.; Dugdale, S.; Francis, G.; Gibbons, B.; Hart, T.; Haymes, T.; Kennett, G.; Lightowler, S.; Matassova, N.; Mansell, H.; Merrett, A.; Misra, A.; Padfield, A.; Parsons, R.; Pratt, R.; Robertson, A.; Simmonite, H.; Tan, K.; Walls, S.B.; Wong, M.

Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity

Bioorg. Med. Chem. Lett.

22

901-906

2012

Homo sapiens, Rattus norvegicus

22209458

719302

Zahov, S.; Drews, A.; Hess, M.; Schulze Elfringhoff, A.; Lehr, M.

1-(3-biaryloxy-2-oxopropyl)indole-5-carboxylic acids and related compounds as dual inhibitors of human cytosolic phospholipase A2alpha and fatty acid amide hydrolase

ChemMedChem

6

544-549

2011

Homo sapiens, Rattus norvegicus

21259444

Strittmatter, F.; Gandaglia, G.; Benigni, F.; Bettiga, A.; Rigatti, P.; Montorsi, F.; Gratzke, C.; Stief, C.; Colciago, G.; Hedlund, P.

Expression of fatty acid amide hydrolase (FAAH) in human, mouse, and rat urinary bladder and effects of FAAH inhibition on bladder function in awake rats

Eur. Urol.

61

98-106

2012

Homo sapiens, Mus musculus, Rattus norvegicus, Rattus norvegicus Sprague-Dawley

21930339

719538

Mukhopadhyay, P.; Horvath, B.; Rajesh, M.; Matsumoto, S.; Saito, K.; Batkai, S.; Patel, V.; Tanchian, G.; Gao, R.Y.; Cravatt, B.F.; Hasko, G.; Pacher, P.

Fatty acid amide hydrolase is a key regulator of endocannabinoid-induced myocardial tissue injury

Free Radic. Biol. Med.

50

179-195

2011

Homo sapiens, Mus musculus, Mus musculus C57/BL6J

21070851

Min, X.; Thibault, S.T.; Porter, A.C.; Gustin, D.J.; Carlson, T.J.; Xu, H.; Lindstrom, M.; Xu, G.; Uyeda, C.; Ma, Z.; Li, Y.; Kayser, F.; Walker, N.P.; Wang, Z.

Discovery and molecular basis of potent noncovalent inhibitors of fatty acid amide hydrolase (FAAH)

Proc. Natl. Acad. Sci. USA

108

7379-7384

2011

Homo sapiens (O00519), Rattus norvegicus (P97612)

21502526

Kono, M.; Matsumoto, T.; Imaeda, T.; Kawamura, T.; Fujimoto, S.; Kosugi, Y.; Odani, T.; Shimizu, Y.; Matsui, H.; Shimojo, M.; Kori, M.

Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors

Bioorg. Med. Chem.

22

1468-1478

2014

Homo sapiens (O00519), Rattus norvegicus (P97612), Rattus norvegicus Sprague-Dawley (P97612)

24440478

Korhonen, J.; Kuusisto, A.; van Bruchem, J.; Patel, J.Z.; Laitinen, T.; Navia-Paldanius, D.; Laitinen, J.T.; Savinainen, J.R.; Parkkari, T.; Nevalainen, T.J.

Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL)

Bioorg. Med. Chem.

22

6694-6705

2014

Homo sapiens (O00519)

25282655

Colombano, G.; Albani, C.; Ottonello, G.; Ribeiro, A.; Scarpelli, R.; Tarozzo, G.; Daglian, J.; Jung, K.M.; Piomelli, D.; Bandiera, T.

O-(triazolyl)methyl carbamates as a novel and potent class of fatty acid amide hydrolase (FAAH) inhibitors

ChemMedChem

10

380-395

2015

Homo sapiens (O00519), Homo sapiens, Rattus norvegicus (P97612), Rattus norvegicus Sprague�Dawley (P97612)

25338703

Caruano, J.; Feledziak, M.; Labar, G.; Michaux, C.; Perpete, E.A.; Muccioli, G.G.; Robiette, R.; Marchand-Brynaert, J.

(S)-1-(Pent-4-enoyl)-4-(hydroxymethyl)-azetidin-2-one derivatives as inhibitors of human fatty acid amide hydrolase (hFAAH): synthesis, biological evaluation and molecular modelling

J. Enzyme Inhib. Med. Chem.

29

654-662

2014

Homo sapiens (O00519), Homo sapiens

24102523

Alapafuja, S.O.; Nikas, S.P.; Bharathan, I.T.; Shukla, V.G.; Nasr, M.L.; Bowman, A.L.; Zvonok, N.; Li, J.; Shi, X.; Engen, J.R.; Makriyannis, A.

Sulfonyl fluoride inhibitors of fatty acid amide hydrolase

J. Med. Chem.

55

10074-10089

2012

Homo sapiens (O00519), Homo sapiens, Rattus norvegicus (P97612)

23083016

Dato, F.M.; Maassen, A.; Goldfuss, B.; Pietsch, M.

Characterization of fatty acid amide hydrolase activity by a fluorescence-based assay

Anal. Biochem.

546

50-57

2018

Homo sapiens

29408178

Zahov, S.; Garzinsky, D.; Hanekamp, W.; Lehr, M.

1-Heteroarylpropan-2-ones as inhibitors of fatty acid amide hydrolase Studies on structure-activity relationships and metabolic stability

Bioorg. Med. Chem.

25

825-837

2017

Homo sapiens

27989417

Watabiki, T.; Tsuji, N.; Kiso, T.; Ozawa, T.; Narazaki, F.; Kakimoto, S.

In vitro and in vivo pharmacological characterization of ASP8477 A novel highly selective fatty acid amide hydrolase inhibitor

Eur. J. Pharmacol.

815

42-48

2017

Homo sapiens (B2C6G4), Homo sapiens (O00519), Homo sapiens, Rattus norvegicus (P97612)

29017758

Althaus, J.; Hake, T.; Hanekamp, W.; Lehr, M.

1-(5-Carboxyindazol-1-yl)propan-2-ones as dual inhibitors of cytosolic phospholipase A2? and fatty acid amide hydrolase bioisosteric replacement of the carboxylic acid moiety

J. Enzyme Inhib. Med. Chem.

31

131-140

2016

Homo sapiens

27162011

Sundermann, T.; Hanekamp, W.; Lehr, M.

Structure-activity relationship studies on 1-heteroaryl-3-phenoxypropan-2-ones acting as inhibitors of cytosolic phospholipase A2alpha and fatty acid amide hydrolase replacement of the activated ketone group by other serine traps

J. Enzyme Inhib. Med. Chem.

31

653-663

2016

Homo sapiens

26153239