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3.1.1.1: carboxylesterase

This is an abbreviated version!
For detailed information about carboxylesterase, go to the full flat file.

Word Map on EC 3.1.1.1

Reaction

a carboxylic ester
+
H2O
=
an alcohol
 +
a carboxylate

Synonyms

4-nitrophenyl esterase, ACAT, Acetyl esterase, acetyl xylan esterase, acid retinyl ester hydrolase, AcXE, Acyl coenzyme A:cholesterol acyltransferase, acylcarnitine hydrolase, AF1716, AF1763, AFEST, ali-esterase, aliesterase, alpha-carboxylesterase, alpha-esterase 7, alphaE7, alphaEsterase7, AOPP herbicide carboxylesterase, APE1547, AREH, aspirin hydrolase, Axe1NaM1, Axe1NaM2, Axe1NaM3, B-esterase, Bacillus esterase, BdB1, BioHe, BioHs, Brain carboxylesterase hBr1, BSE, BsE-NP01, BSE01701, butyrate esterase, butyryl esterase, CaE, CaesCCR11, carboxyesterase, Carboxyesterase ES-10, carboxyl ester hydrolase, carboxyl esterase, carboxyl/cholinesterase, carboxylate esterase, carboxylesterase, carboxylesterase 1, carboxylesterase 1A2, carboxylesterase 1C, carboxylesterase 2, carboxylesterase B, carboxylesterase B1, carboxylesterase-1, carboxylesterase-2, Carboxylesterase-5C, carboxylic acid esterase, carboxylic ester hydrolase, carboxylic esterase, Carboxylic-ester hydrolase, CarE, CbE, CCE, CE, CE-1, CE-2, CE1, CE2, CE21p, CE7 AcXE, CEH, CES, CES 1C, CES-2, CES1, CES1-b, CES1-c, CES1A, CES1A1, CES1A2, Ces1c, Ces1d, Ces1e, Ces1g, CES2, CES2A1, Ces3-1, Ces3a, cholesteryl ester hydrolase, cocaine esterase, cocaine:benzoylecgonine esterase, COE, CPT-CE, CXE, CXE1, CXE10, D1CarE5, de-arenethiolase, DEHP, E3 carboxylesterase, E34Tt, EC 3.1.1.21, Egasyn, ES-10, Es-22, ES-HTEL, ES-HVEL, ES-Male, ES-THET, ES10, ES11, ES3, ES4, ES5, ES6, ES7, ES9, EST, EST-3, EST-4, EST-5A, EST-5B, EST-5C, Est-AF, Est0071, Est1, Est1C, EST2, ESt3, Est3 esterase, Est30, Est55, EstA, EstA esterase, EstB, estBB1, EstC, EstC1, esterase, esterase 1F, esterase 2, esterase 2B, esterase 6A, esterase 9A, esterase A, esterase B, esterase B1, esterase D, esterase Sso2518, esterase, carboxyl, Esterase-22, Esterase-31, esterase-6, EStFa, EstGtA2, EstP, EstPS1, EstSt7, EstU1, Fluazifop-P-butyl carboxylesterase, Fluazifop-P-butyl hydrolase, FpbH, fungus-inducible pepper carboxylesterase, general odorant degradation enzyme, GODE, hCE-2, HCE1, HCE2, hCES1, hiCE, HMSE, hormone-sensitive lipase, HSL, human carboxylesterase 1, human carboxylesterase 2, human liver carboxylesterase, ICE, ICXE14, JHE-related, JHER, kidney bean esterase, Kidney microsomal carboxylesterase, LcalphaE7, LIP4, LipA, LipC, Liver microsomal carboxylesterase, malathion carboxylesterase, MAP esterase, MCE, ME, MeIAA esterase, MeSA esterase, methylbutyrase, methylbutyrate esterase, mfCES2v3, Microsomal palmitoyl-CoA hydrolase, monobutyrase, Monocyte/macrophage serine esterase, More, mouse carboxylesterase, MT2282, NaM1, NaM2, NaM3, Non-specific carboxylesterase, nonspecific carboxylesterase, ODE, odorant degradation enzyme, P186_1588, PA3859, PepEST, PF2001, Pf2001 esterase, PI 5.5 esterase, PI 6.1 esterase, pig liver esterase, PLE, PMPMEase, pnbA, PnbA1, PnbA2, polyisoprenylated methylated protein methyl esterase, porcine liver carboxylesterase, PPE, PPMTase, PrbA, prenylated methylated protein methyl esterase, procaine esterase, Proline-beta-naphthylamidase, propionyl esterase, pyrethroid-hydrolysing esterase, Rsp3690, SABP2's methyl salicylate esterase, salicylic acid-binding protein 2, SeE, serine protease-like, serine-type carboxylesterase, SexiCXE10, SiRe0290, SshEstI, SshEstI esterase, Sso P1 carboxylesterase, Sso-EST1, SSO2493, SSO2517, SSoP1 CE, SsoPEst, ST0071, ST2026, STK_00710, Sto-Est, TGH, triacetin esterase, triacylglycerol hydrolase, vitamin A esterase, VmoLac

ECTree

     3 Hydrolases
         3.1 Acting on ester bonds
             3.1.1 Carboxylic-ester hydrolases
                3.1.1.1 carboxylesterase

Inhibitors

Inhibitors on EC 3.1.1.1 - carboxylesterase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(10Z)-hexadecenoic acid
-
-
(2R)-2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile
-
about 30% residual activity at 0.1 mM
(3S)-1-chloro-3-tosylamido-7-amino-2-heptanone
-
73.6% residual activity at 1 mM
(4S)-4,11-diethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
-
-
(4S)-4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl 1,4'-bipiperidine-1'-carboxylate
-
-
(5Z,8Z,11Z,14Z)-eicosatetraenoic acid
-
-
(6Z,9Z,12Z)-octadecatrienoic acid
-
-
(9Z)-octadecenoic acid
-
-
(9Z)-tetradecenoic acid
-
-
(9Z,12Z)-octadecadienoic acid
-
-
(R)-cocaine
-
(S)-naproxen
nearly 80% of the initial activity is lost when 2.5 mM of (S)-naproxen is added to the reaction system
1(R)-cis-alpha(S) deltamethrin
-
1,1'-ethane-1,2-diylbis(1H-indole-2,3-dione)
1,1,1,-trifluoro-3-(hexylsulfinyl)propane-2,2-diol
1,1,1,-trifluoro-3-(hexylsulfonyl)propane-2,2-diol
1,1,1-trifluoro-3-(hexyloxy)propane-2,2-diol
1,1,1-trifluoro-3-(hexyloxy)propane-2,2-diol1,1,1-trifluoro-3-(hexylsulfonyl)propane-2,2-diol
1,1,1-trifluoro-3-(hexylsulfanyl)propan-2-one
1,1,1-trifluoro-3-(hexylsulfinyl)propane-2,2-diol
1,1,1-trifluoro-3-(hexylsulfonyl)propane-2,2-diol
1,1,1-trifluoro-3-(octylsulfanyl)propan-2-one
1,1,1-trifluoro-3-(octylsulfinyl)propane-2,2-diol
1,1,1-trifluoro-3-(octylsulfonyl)propane-2,2-diol
1,1,1-trifluoro-3-octylthiol-propan-2-one
-
-
1,1,1-trifluoro-3-[(2-phenylethyl)sulfanyl]propan-2-one
1,1,1-trifluoro-3-[(2-phenylethyl)sulfonyl]propane-2,2-diol
1,1,1-trifluorododecan-2-one
1,2-bis(2,3,4-trifluorophenyl)ethane-1,2-dione
1,2-bis(2,3,5-trifluorophenyl)ethane-1,2-dione
1,2-bis(2,3-difluorophenyl)ethane-1,2-dione
1,2-bis(2,5-difluorophenyl)-2-hydroxyethanone
1,2-bis(2,6-difluorophenyl)-2-hydroxyethanone
1,2-bis(2-chlorophenyl)ethane-1,2-dione
1,2-bis(3,4,5-trifluorophenyl)ethane-1,2-dione
1,2-bis(3,5-difluorophenyl)-2-hydroxyethanone
1,2-bis(3,5-difluorophenyl)ethane-1,2-dione
1,2-bis(3-methoxyphenyl)ethane-1,2-dione
1,2-bis(3-nitrophenyl)ethane-1,2-dione
1,2-bis(4-bromo-2-methoxyphenyl)ethane-1,2-dione
1,2-bis(4-bromo-3-nitrophenyl)ethane-1,2-dione
1,2-bis(4-bromothiophen-2-yl)ethane-1,2-dione
1,2-bis(4-chlorophenyl)ethane-1,2-dione
1,2-bis(4-fluorophenyl)ethane-1,2-dione
1,2-bis(4-methoxyphenyl)ethane-1,2-dione
1,2-bis(4-methylphenyl)ethane-1,2-dione
1,2-bis(5-bromothiophen-2-yl)ethane-1,2-dione
1,2-di(furan-2-yl)ethane-1,2-dione
1,2-di(naphthalen-2-yl)ethane-1,2-dione
1,2-di(pyridin-2-yl)ethane-1,2-dione
1,2-di(thiophen-2-yl)ethane-1,2-dione
1,2-di(thiophen-3-yl)ethane-1,2-dione
1,2-dicyclohexylethane-1,2-dione
1,2-difluoro-6,6-dimethyl-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
1,2-diphenylethane-1,2-dione
1,4-dibromo-1,4-diphenyl butane-2,3-dione
1-(2,4-dinitrophenyl)-2-phenylethane-1,2-dione
1-(2-bromoethyl)-1H-indole-2,3-dione
1-(2-chlorophenyl)-2-(3,4-dimethoxyphenyl)ethane-1,2-dione
1-(2-iodoethyl)-1H-indole-2,3-dione
1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione
1-(3,4-dimethylphenyl)-2-phenylethane-1,2-dione
1-(4-(4[(2,3-dioxo-2,3-dihydro-1H-indol-1-yl)methyl]benzyl)benzyl)-1H-indole-2,3-dione
1-(4-chlorobenzyl)-1H-indole-2,3-dione
1-(4-chlorophenyl)-2-(4-methylphenyl)ethane-1,2-dione
1-(4-chlorophenyl)-2-phenylethane-1,2-dione
1-(4-methoxyphenyl)-2-phenylethane-1,2-dione
1-(4-methyl-3-nitrophenyl)-2-phenylethane-1,2-dione
1-(4-methylphenyl)-2-phenylethane-1,2-dione
1-(4-nitrophenyl)-2-phenylethane-1,2-dione
1-(pentachlorophenyl)-2-(pentafluorophenyl)ethane-1,2-dione
1-([(2-bromophenyl)amino]methyl)-1H-indole-2,3-dione
1-([(4-chlorophenyl)amino]methyl)-1H-indole-2,3-dione
1-benzyl-1H-indole-2,3-dione
1-butanol
1-chloro-3-tosylamido-4-phenyl-2-butanone
-
-
1-chloro-3-tosylamido-7-amino-2-heptanone
-
-
1-dodecyl-1H-indole-2,3-dione
1-fluoro-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
1-fluoro-6,6-dimethyl-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
1-hexadecanesulfonyl chloride
-
irreversible inhibition
1-hexadecyl-1H-indole-2,3-dione
1-methyl-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
1-phenyl-1H-indole-2,3-dione
1-propanol
1-[(2-naphthylamino)methyl]-1H-indole-2,3-dione
1-[4-(bromomethyl)phenyl]-2-phenylethane-1,2-dione
1-[4-[oxo(phenyl)acetyl]phenyl]-2-phenylethane-1,2-dione
11,12-epoxy-(5Z,8Z,14Z)-eicosatrienoic acid
-
-
11-piperazin-1-yl-dibenzo[b,f][1,4]thiazepine
-
-
13beta,19-dihydroy-3,15-dioxoatis-16-ene-19-O-beta-D-(6'-galloyl)-glucopyranoside
-
13beta,19-dihydroy-3,15-dioxoatis-16-ene-19-O-beta-Dglucopyranoside
-
14,15-epoxy-(5Z,8Z,11Z)-eicosatrienoic acid
-
-
15-deoxy-DELTA12,14-prostaglandin J2
-
-
18beta-11-deoxo-olean-12-en-30-oic acid
-
18beta-11-deoxo-olean-12-en-30-oic acid ethyl ester
-
18beta-11-oxo-olean-12-en-30-oic acid ethyl ester
-
18beta-11-oxo-olean-12-en-30-oic acid methyl ester
-
18beta-11-oxo-olean-12-en-30-oic acid-(20-dimethylamino)ethyl ester
-
18beta-3, 11-dioxo-olean-12-en-30-oic acid
-
18beta-3-O-(beta-carboxypropionyl)-11-deoxo-olean-12-en-30-oic acid ethyl ester
-
18beta-3-O-(beta-carboxypropionyl)-11-oxo-olean-12-en-30-oic acid ethyl ester
-
18beta-3-O-acetyl-11-oxo-olean-12-en-30-oic acid
-
18beta-3-O-acetyl-11-oxo-olean-12-en-30-oic acid-(20-dimethylamino)ethyl ester
-
18beta-3-oxo-11-deoxo-olean-12-en-30-oic acid
-
18beta-glycyrrhetinic acid
-
2,2-dimethyl-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]propanamide
-
-
2,4-dichloro-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]benzamide
-
-
2,4-difluoro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
-
2,5-difluoro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
-
2,6,6-trimethyl-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
2,7,7-trimethyl-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one
-
-
2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one
-
-
2-(4-methoxyphenyl)-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]acetamide
-
-
2-(propan-2-yl)-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
2-butanol
10% (v/v), 52% inhibition; 10% (w/v), 42% inhibition
2-chloro-3,4-dimethoxybenzil
2-fluoro-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
2-fluoro-6,6-dimethyl-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
2-fluorophenanthrene-3,4-dione
-
2-hydroxy-1,2-bis(2,3,4-trifluorophenyl)ethanone
2-hydroxy-1,2-bis(2,3,5-trifluorophenyl)ethanone
2-mercaptoethanol
2-methoxy-6,6-dimethyl-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
2-methyl-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
2-methyl-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]propanamide
-
-
2-propanol
2-[3,4-bis[(diethoxyphosphoryl)oxy]phenyl]-4-oxo-4H-chromene-3,5,7-triyl hexaethyl tris(phosphate)
-
-
2-[3,4-bis[(diethoxyphosphoryl)oxy]phenyl]-4-oxo-4H-chromene-5,7-diyl tetraethyl bis(phosphate)
-
-
2-[3-[(diethoxyphosphoryl)oxy]-4-methoxyphenyl]-4-oxo-3,4-dihydro-2H-chromene-5,7-diyl tetraethyl bis(phosphate)
-
-
2-[4-[(diethoxyphosphoryl)oxy]phenyl]-4-oxo-4H-chromene-5,7-diyl tetraethyl bis(phosphate)
-
-
2-[[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]sulfanyl]ethanesulfonyl fluoride
-
-
22(R)-hydroxycholesterol
-
slight inhibition of CES1, not CES2
24(S),25-epoxycholesterol
-
inhibits only CES1, not CES2
24(S)-hydroxycholesterol
-
slight inhibition of CES1, not CES2
25-hydroxycholesterol
-
slight inhibition of CES1, not CES2
27-Hydroxycholesterol
-
partially noncompetitive inhibitor of recombinant CES1, impaires intracellular CES1 activity following treatment of intact THP1 cells. No inhibition of CES2
3',4',7-trihydroxyisoflavone
-
3',4'-dihydroxyflavone
-
3,3-dimethyl-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]butanamide
-
-
3,4-difluoro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
-
3,4-difluoro-N-(4-(phenylsulfonamido)phenyl)benzene sulfonamide
-
-
3,4-difluoro-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]benzamide
-
-
3,6-dihydroxyflavone
-
3-(butylsulfanyl)-1,1,1-trifluoropropan-2-one
3-(decylsulfanyl)-1,1,1-trifluoropropan-2-one
3-(decylsulfinyl)-1,1,1-trifluoropropane-2,2-diol
3-(decylsulfonyl)-1,1,1-trifluoropropane-2,2-diol
3-(dodecylsulfanyl)-1,1,1-trifluoropropan-2-one
3-(dodecylsulfinyl)-1,1,1-trifluoropropane-2,2-diol
3-(dodecylsulfonyl)-1,1,1-trifluoropropane-2,2-diol
3-butylsulfinyl-1,1,1-trifluoropropane-2,2-diol
3-chloro-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]benzamide
-
-
3-decylsulfinyl-1,1,1-trifluoropropane-2,2-diol
3-decylsulfonyl-1,1,1-trifluoropropane-2,2-diol
3-dodecylsulfinyl-1,1,1-trifluoropropane-2,2-diol
3-dodecylsulfonyl-1,1,1-trifluoropropane-2,2-diol
3-hydroxyflavone
-
3-methyl-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]butanamide
-
-
3-O-acetyl-11-oxo-olean-12-en-30-nitrile
-
3-[4-[(diethoxyphosphoryl)oxy]phenyl]-4-oxo-4H-chromene-5,7-diyl tetraethyl bis(phosphate)
-
-
4,6-dichloro-1H-indole-2,3-dione
4,6-dimethyl-N1,N3-diphenylbenzene-1,3-disulfonamide
-
-
4,7-dichloro-1H-indole-2,3-dione
4-(N-(4-(4-fluorophenylsulfonamido)phenyl)sulfamoyl)-3-methylbenzoic acid
-
-
4-(N-(4-(4-fluorophenylsulfonamido)phenyl)sulfamoyl)-N-methyl benzamide
-
-
4-(N-(4-(4-fluorophenylsulfonamido)phenyl)sulfamoyl)benzoic acid
-
-
4-bromo-N-(4-ethoxyphenyl)benzene sulfonamide
-
-
4-chloro-N-(4-(4-fluorophenylsulfonamido)phenyl)benzene sulfonamide
-
-
4-chloro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
-
4-chloro-N-(4-ethoxyphenyl)benzene sulfonamide
-
-
4-fluoro-N-(4-(4-methoxy phenylsulfonamido)phenyl)benzene sulfonamide
-
-
4-fluoro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
-
4-fluoro-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]benzamide
-
-
4-mercuribenzoate
4-methoxy-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]benzamide
-
-
4-methyl-N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]benzamide
-
-
4-nitrophenyl acetate
-
an inhibition of CaE activity by 4-nitrophenyl acetate is observed at substrate concentration higher than 5 mM
4-[7-[(diethoxyphosphoryl)oxy]-4-oxo-4H-chromen-3-yl]phenyl diethyl phosphate
-
-
4-[7-[(diethoxyphosphoryl)oxy]-5-hydroxy-4-oxo-4H-chromen-2-yl]benzene-1,2-diyl tetraethyl bis(phosphate)
-
-
4-[7-[(diethoxyphosphoryl)oxy]-5-hydroxy-4-oxo-4H-chromen-2-yl]phenyl diethyl phosphate
-
-
4-[7-[(diethoxyphosphoryl)oxy]-5-hydroxy-4-oxo-4H-chromen-3-yl]phenyl diethyl phosphate
-
-
4-[7-[(dimethoxyphosphoryl)oxy]-5-hydroxy-4-oxo-4H-chromen-2-yl]phenyl dimethyl phosphate
-
-
4-[oxo(phenyl)acetyl]benzoic acid
4beta,9alpha,16,20-tetrahydroxy-14(13->12)-abeo-12alphaH-1,6-tigliadiene-3,13-dione
competitive inhibition
4beta,9alpha,20-trihydroxy-14(13->12)-abeo-12alphaH-1,6-tigliadiene-3,13-dione
-
5,5'-dithiobis(2-nitrobenzoic)acid
-
5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
5,6,7-trimethoxybaicalein
-
5,6-dihydroxyflavone
a specific hCE2 inhibitor, exhibits reversible, noncompetitive inhibition, 5,6-dihydroxyflavone displays high specificity toward hCE2 over hCE1
5,7,8-trihydroxyflavone
-
5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one
-
-
5,7-dihydroxyflavone
-
5-bromo-1-(2-methylprop-2-en-1-yl)-1H-indole-2,3-dione
5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl dimethyl phosphate
-
-
5-hydroxy-6-methoxyflavone
-
5-hydroxyflavone
-
5-methoxy-3-(4-phenoxyphenyl)-3H-[1,3,4]oxadiazol-2-one
6,6-dimethyl-2-(propan-2-yl)-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
6,6-dimethyl-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
6,7-dihydroxyflavone
-
6-hydroxyflavone
-
6-methoxyflavone
-
7,7-dimethyl-2-(propan-2-yl)-5,6,7,8-tetrahydrophenanthrene-3,4-dione
-
7,8-dihydroxyflavone
-
7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin
-
i.e. irinotecan or CPT-11, an antitumor prodrug
7-hydroxyflavone
-
7-methoxybaicalein
-
7-oxocholesterol
-
slight inhibition of CES1, not CES2
8-ethyl 3-methyl 4-hydroxy-4-(trifluoromethyl)-1,4-dihydropyrazolo[5,1-c][1,2,4]triazine-3,8-dicarboxylate
-
8-hydroxyquinoline
-
-
8-methyl-1,4-dihydro-2H-naphtho[2,1-c]pyran-9,10-dione
-
8-nitrobaicalein
-
8beta-11-oxo-olean-12-en-30-amide
-
8beta-3-O-acetyl-11-oxo-olean-12-en-30-amide
-
acetone
acetonitrile
Ag2+
strong inhibition
Al3+
inhibits at 0.5-5 mM
Aldicarb
amlodipine
-
about 40% residual activity at 0.1 mM
apigenin 7-O-methyl ether
-
arachidonic acid
-
most potent fatty acid inhibitor of recombinant CES1 acting by a noncompetitive mechanism, overview. The inhibition is reversible by bovine serum albumin
aripiprazole
-
-
ascorbic acid
1 mM, 40% residual activity
asulam
-
91.7% residual activity at 1 mM
atomoxetine
-
-
atorvastatin
-
about 45% residual activity at 0.1 mM
Ba2+
2 mM, 10% inhibition
baicalein
-
bendroflumethiazide
-
about 70% residual activity at 0.1 mM
benzil
bioresmethrin
-
a pyrethroid insecticide
bis(4-cyanophenyl) phosphate
-
-
bis(4-nitrophenyl) phosphate
bis(4-nitrophenyl) phosphoric acid
-
97% inhibition at 1 mM
bis(4-nitrophenyl)phosphate
-
potent inhibitor
bis(p-nitrophenyl) phosphate
bis-4-nitrophenyl phosphate
bis-4-nitrophenylphosphate
-
-
bis-p-nitrophenyl phosphate
O35535, O70177
BNPP, a specific inhibitor of CES, inhibits the hydrolysis of ethyl-FXD in rat skin S9 fraction in a dose-dependent manner, 99% inhibition at 1 mM BNPP
bisdehydrophorbol
-
bisoprolol
-
about 90% residual activity at 0.1 mM
butan-1-ol
27 mM, complete inhibition
butanol
Calycosin
-
Carbaryl
carbofuran
-
-
carvedilol
-
about 17% residual activity at 0.1 mM
cephaloridine
-
competitive inhibitor of 4-nitrophenyl butyrate
cephalothin
-
competitive inhibitor of 4-nitrophenyl butyrate
cetyltrimethylammonium bromide
-
complete inhibition
chloroform
50% (v/v), 2 h incubation, 66% loss of activity
chlorpyrifos
chlorpyrifos-methyl
-
the enzyme is totally inhibited by 0.001 mM chlorpyrifos-methyl
chlorpyrifos-methyl oxon
-
the enzyme is totally inhibited by 0.001 mM chlorpyrifos-methyl oxon
chlorpyrifos-oxon
cholesterol
-
slight inhibition of CES1, not CES2
clopidogrel
-
about 15% residual activity at 0.1 mM
clozapine
-
-
cocaethylene
-
CoCl2
-
1mM, 34% residual activity
Cr3+
inhibits at 0.5-5 mM
CuCl2
-
1 mM, 59% residual activity
curcumin
-
reversible inhibition
CuSO4
-
1 mM, 23% residual activity, isoform E1, 10% residual activity, isoform E2
cyclosarin
-
-
cypermethrin
-
-
decane-5,6-dione
deltamethrin
deoxycholate
-
50% inhibition at 1%
DEPC
histidine modifier
dichlorvos
didehydrolangduin A-20-O-beta-D-glucopyranoside
-
diethyl 4-hydroxy-4-(trifluoromethyl)-1,4-dihydroimidazo[5,1-c][1,2,4]triazine-3,8-dicarboxylate
-
diethyl 4-hydroxy-4-(trifluoromethyl)-1,4-dihydropyrazolo[5,1-c][1,2,4]triazine-3,8-dicarboxylate
-
diethyl 4-nitrophenyl phosphate
diethyl 4-oxo-2-phenyl-4H-chromen-6-yl phosphate
-
-
diethyl 4-oxo-2-phenyl-4H-chromen-7-yl phosphate
-
-
diethyl 5-hydroxy-3-(4-hydroxyphenyl)-4-oxo-4H-chromen-7-yl phosphate
-
-
diethyl 5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl phosphate
-
-
diethyl 7-hydroxy-4-oxo-2-phenyl-4H-chromen-5-yl phosphate
-
-
diethyl coumarylphosphate
-
-
diethyl dicarbonate
Diethyl p-nitrophenyl phosphate
diethyldicarbonate
diethylfluorophosphate
0.01 mM, 30°C, 30 min, 75% inhibition
diethylphosphofluoridate
-
-
diethylpyrocarbonate
5 mM,% inhibition
diethylumbelliferyl phosphate
-
Digitonin
diisopropyl fluorophosphate
diisopropyl phosphofluoridate
-
-
diisopropylfluorophosphate
diltiazem
-
about 23% residual activity at 0.1 mM
Dimethoate
-
-
dimethyl 4-oxo-2-phenyl-4H-chromen-6-yl phosphate
-
-
dimethyl 4-oxo-2-phenyl-4H-chromen-7-yl phosphate
-
-
Dimethyl formamide
-
inactivation
dimethylchlorophosphate
-
dimethylformamide
50% (v/v), 2 h incubation, 72% loss of activity
Dimethylsulfoxide
-
-
dimyristoylphosphatidylcholine
-
88% inhibition
diosmetin
-
dioxane
dipalmitoylphosphatidylcholine
-
91.5% inhibition
diphenyl carbonate
-
-
diphenylamine-2-carboxylate
5 mM, 30°C, 30 min, 77% inhibition
dithiobis-(2-nitrobenzoic acid)
-
weak
dithiothreitol
DMF
-
10% (v/v) and 20% (v/v), strong decrease in activity of wild-type enzyme and mutant enzymes V138G and V138G/L200R
dodecane-6,7-dione
donepezil hydrochloride
-
-
DTNB
-
weak
E600
half-inactivation times of 20 s, at an inhibitor:enzyme molar ratio is 10:1
ebelactone A
-
inhibits more than 80% of the enzyme at 1 mM
ebelactone B
-
complete inhibition at 1 mM
ent-16beta,17-dihydroxyatisan-3-one-19-O-beta-D-(6'-galloyl)-glucopyranoside
-
ent-16beta,17-dihydroxyatisan-3-one-19-O-beta-D-glucopyranoside
-
ent-kaurane-16beta,17-diol-3,12-dione-19-O-beta-D-glucopyranoside
-
ent-kaurane-16beta,17-diol-3-one-19-O-beta-D-(6'-galloyl)-glucopyranoside
-
ent-kaurane-16beta,17-diol-3-one-19-O-beta-D-glucopyranoside
-
eplerenone
-
about 80% residual activity at 0.1 mM
eserine
ethanol
ethyl 3-amino-5-(trifluoromethyl)-1,2,4-triazine-6-carboxylate
-
ethyl 4-hydroxy-4-(trifluoromethyl)-1,4-dihydro[1,2,4]triazolo[5,1-c][1,2,4]triazine-3-carboxylate
-
ethyl 7-hydroxy-7-(trifluoromethyl)-4,7-dihydrotetrazolo[5,1-c][1,2,4]triazine-6-carboxylate
-
ethyl butyrate
-
substrate inhibition
ethyl-4-hydroxy-7-methyl-4-nonaluorobuthyl-1,4-dihydropyrazolo[5,1-c][1,2,4]triazine-3-carboxylate
-
ethyl-4-hydroxy-7-methyl-4-trifluoromethyl-1,4-dihydropyrazolo[5,1-c][1,2,4]triazine-3-carboxylate
-
ethyl-4-hydroxy-7-phenyl-4-nonafluorobutyl-1,4-dihydropyrazolo[5,1-c][1,2,4]triazine-3-carboxylate
-
ethyl-4-hydroxy-7-phenyl-4-pentafluoroethyl-1,4-dihydropyrazolo[5,1-c][1,2,4]triazine-3-carboxylate
-
ethyl-4-hydroxy-7-phenyl-4-trifluoromethyl-1,4-dihydropyrazolo[5,1-c][1,2,4]triazine-3-carboxylate
-
ethyl-7-hydroxy-7-nonafluorobutyl-4,7-dihydrotetrazolo[5,1-c][1,2,4]triazine-6-carboxylate
-
ethyl-7-hydroxy-7-nonafluorobutyl-4,7-dihydro[1,2,4]triazolo[5,1-c][1,2,4]triazine-6-carboxylate
-
eupatilin
-
FeCl2
-
1 mM, 40% residual activity
FeCl3
-
1 mM, 38% residual activity
fischeroside A
-
fischeroside A-16-O-beta-D-glucopyranoside
-
fluoxetine
-
-
formaldehyde
20% (v/v), 2 h incubation, 81% loss of activity
Furosemide
-
about 78% residual activity at 0.1 mM
Galaxolide
genistein
-
glufosinate
-
low to moderate inhibition
-
glycerol
inhibition of mutant enzyme R11G/L36P/V225A/I551L/A564T no matter that it is or is not treated by acetone
glycitein
-
haloperidol
-
-
HEPES
-
inhibition mechanism, competitive
heptane
herbacetin
-
hexadecane-8,9-dione
hexadecanoic acid
-
-
HgCl2
hispidulin
-
imipramine
-
-
ingenol-19-O-beta-D-glucopyranoside
-
iodoacetic acid
irbesartan
-
about 75% residual activity at 0.1 mM
Isopropanol
isorhamnetin
-
isradipine
-
about 18% residual activity at 0.1 mM
kaempferol
-
L-4-tosylamino-2-phenylethyl chloromethyl ketone
-
inhibits more than 80% of the enzyme at 1 mM
L-Leu-chloromethyl ketone
-
60.4% residual activity at 1 mM
langduin F
-
lercanidipine
-
about 78% residual activity at 0.1 mM
Li+
inhibits at 0.5-5 mM
loperamide
lysophosphatidic acid
-
-
malathion
-
-
mercaptoethanol
5 mM, 15% loss of activity (recombinant enzyme expressed in Sulfolobus solfataricus). 5 mM, 25% loss of activity (recombinant enzyme expressed in Escherichia coli as thioredoxin-free form (EcSisEstA I)). 5 mM, 22% loss of activity (recombinant enzyme expressed in Escherichia coli as a thioredoxin-EstA fusion protein (EcSisEstA II))
methanol
methomyl
-
-
methyl 4-hydroxy-4-(nonafluorobutyl)-1,4-dihydro[1,2,4]triazolo[5,1-c][1,2,4]triazine-3-carboxylate
-
methyl 7-(heptafluoropropyl)-7-hydroxy-4,7-dihydrotetrazolo[5,1-c][1,2,4]triazine-6-carboxylate
-
methyl 7-hydroxy-7-(1,1,2,2-tetrafluoroethyl)-4,7-dihydrotetrazolo[5,1-c][1,2,4]triazine-6-carboxylate
-
methyl 7-hydroxy-7-(nonafluorobutyl)-4,7-dihydrotetrazolo[5,1-c][1,2,4]triazine-6-carboxylate
-
methyl paraoxon
methyl-4-hydroxy-7-phenyl-4-nonafluorobutyl-1,4-dihydropyrazolo[5,1-c][1,2,4]triazine-3-carboxylate
-
methyl-7-hydroxy-7-trifluoromethyl-4,7-dihydrotetrazolo[5,1-c][1,2,4]triazine-6-carboxylate
-
mevinphos
-
-
miltirone
-
mono-4-nitrophenyl phosphoric acid ester
-
25% inhibition at 1 mM, no inhibition at 0.1 mM
Monocrotophos
-
-
N,N'-(1,4-phenylene)bis(2,3-dichlorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(2,4,5-trichlorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(2,5-dichlorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(2,6-difluorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(2-fluorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(3,4,5-trifluorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(3,4-dichlorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(3,4-difluorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(3,5-dichlorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(3,5-difluorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(3-bromobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(3-chlorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(3-fluorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(4-bromobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(4-fluoro-2-methylbenzene sulfonamide)
-
-
N,N'-(1,4-phenylene)bis(4-fluorobenzene sulfonamide)
-
-
N,N'-(2,3,5,6-fluoro-1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
-
N,N'-(2,3,5,6-tetrafluoro-1,4-phenylene)bis(4-bromobenzene sulfonamide)
-
-
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(3,4-dichlorobenzene sulfonamide)
-
-
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(3,5-dichlorobenzene sulfonamide)
-
-
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(3-bromobenzene sulfonamide)
-
-
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(3-chlorobenzene sulfonamide)
-
-
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(4-bromobenzene sulfonamide)
-
-
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
-
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(4-fluorobenzene sulfonamide)
-
-
N,N'-(2,5-dibromo-1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
-
N,N'-(2,5-dibromo-1,4-phenylene)bisbenzene sulfonamide
-
-
N,N'-(2,5-dichloro-1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
-
N,N'-(2-chloro-1,4-phenylene)dibenzene sulfonamide
-
-
N,N'-(2-methyl-1,4-phenylene)benzene sulfonamide
-
-
N,N'-(2-methylbenzene-1,4-diyl)dibenzenesulfonamide
-
-
N,N'-(disulfanediyldibenzene-4,1-diyl)dimethanesulfonamide
-
-
N,N'-1,4-phenylenebis-2-naphthalene sulfonamide
-
-
N,N'-9H-fluorene-2,7-diylbis(3,4,5-trifluorobenzenesulfonamide)
-
-
N,N'-9H-fluorene-2,7-diylbis(3-bromobenzenesulfonamide)
-
-
N,N'-9H-fluorene-2,7-diylbis(3-chlorobenzenesulfonamide)
-
-
N,N'-9H-fluorene-2,7-diylbis(4-chlorobenzenesulfonamide)
-
-
N,N'-9H-fluorene-2,7-diyldibenzenesulfonamide
-
-
N,N'-benzene-1,4-diyldibenzenesulfonamide
-
-
N-(4-(4-fluoromethylphenylsulfonamido)phenyl)-2,5-dimethylbenzene sulfonamide
-
-
N-(methoxysuccinyl)-L-Ala-L-Ala-L-Pro-L-Val chloromethyl ketone
-
61.8% residual activity at 1 mM
N-alpha-tosyl-L-Lys chloromethyl ketone
-
98.6% residual activity at 1 mM
N-bromosuccinimide
-
-
n-butanol
-
1 M
N-carbobenzyloxy-L-Phe chloromethyl ketone
-
57% residual activity at 1 mM
n-desmethylclozapine
-
-
N-ethylmaleimide
-
slight inhibition
n-hexane
N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]-2-(thiophen-2-yl)acetamide
-
-
N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]-2-phenoxyacetamide
-
-
N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]-4-(trifluoromethyl)benzamide
-
-
N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]acetamide
-
-
N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]butanamide
-
-
N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]cyclohexanecarboxamide
-
-
N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]hexanamide
-
-
N-[3-[oxo(pyridin-2-yl)acetyl]phenyl]pentanamide
-
-
neostigmine
-
serum enzyme is inhibited, liver enzyme is not affected
NiCl2
-
1 mM, 35% residual activity
nimodipine
-
about 70% residual activity at 0.1 mM
nobiletin
-
O,O'-bis(2-aminoethyl)ethylenglycol-N,N,N',N'-tetraacetic acid
-
-
O-ethyl O-p-nitrophenyl benzene phosphothioate
-
-
octadecane-9,10-dione
octadecanoic acid
-
-
octane-4,5-dione
olanzapine
-
-
omethoate
-
-
organophosphate compounds
-
-
-
organophosphate esters
-
-
-
Organophosphates
-
-
-
oroxylin A
-
oroxyloside A
-
p-chloromercuribenzoate
p-hydroxymercuribenzoate
-
-
p-hydroxymercuribenzoic acid
-
complete inhibition
p-nitrophenol
-
-
p-trimethylammoniumanilinium dichloride
-
serum enzyme is inhibited, liver enzyme is not affected
PAO
cysteine modifier
paraoxon
paraoxon-methyl
-
0.0004 mM, complete inhibition
parathion
Culex sp.
-
diacetylmonoxime protects
Pb2+
inhibits at 0.5-5 mM
PEG 6000
-
complete inhibition
pepstatin A
perphenazine
-
-
phenanthrene-3,4-dione
-
phenol
-
-
phenyl 4-(heptafluoropropyl)-4-hydroxy-1,4-dihydro[1,2,4]triazolo[5,1-c][1,2,4]triazine-3-carboxylate
-
phenyl 7-hydroxy-7-(trifluoromethyl)-4,7-dihydrotetrazolo[5,1-c][1,2,4]triazine-6-carboxylate
-
phenyl-1,2-butanedione
phenyl-1,2-heptanedione
phenyl-1,2-hexanedione
phenyl-1,2-octanedione
phenyl-1,2-pentanedione
phenyl-1,2-propanedione
Phenylarsine oxide
-
10% residual activity at 5 mM
phenylmethanesulfonyl fluoride
0.1 mM, complete inhibition
Phenylmethyl sulfonylfluoride
phenylmethylsulfonyl fluoride
Phenylmethylsulfonylfluoride
Phenylmethylsulphonyl fluoride
-
inhibits at 10 mM
phorbol-13-acetate
-
Phosphamidon
-
-
physostigmine
polyphenol extracts from Arenaria serpyllifolia
-
polyphenol extracts from Rhamnus alaternus
-
polyphenol extracts from Thapsia gargantica
-
prasugrel
-
inhibits isozyme CE2 at high concentrations in vitro but not in vivo
propan-2-ol
Propanol
propoxur
prostaglandin E2
-
-
prostaglandin F2alpha
-
-
quercetin
-
quercetin-3-rhamnoside
-
quetiapine
-
-
reduced glutathione
-
reversible inhibition
S,S,S-tributyl phosphorotrithioate
-
DEF, dynergist DEF can inhibit the activity of carboxylesterase in insect
S,S,S-tributylphosphorotrithionate
-
-
salicylate
-
of 14 recombinant methyl esterase proteins tested, five show preference for methyl salicylate as a substrate and display salicylate inhibition of methyl salicylate esterase activity in vitro, i.e. AtMES1, -2, -4, -7, and -9
scutellarein
-
scutellarin
-
simvastatin
sirolimus
-
about 90% residual activity at 0.1 mM
Sn2+
-
63% inhibition at 25 mM
Sodium cyanide
-
poor inhibition
sodium dodecylsulfate
soman
spironolactone
-
about 70% residual activity at 0.1 mM
sumithion
-
-
tacrolimus
-
about 28% residual activity at 0.1 mM
tangeretin
-
telmisartan
4-nitrophenyl acetate hydrolysis in human iPS cell-derived enterocytes is significantly inhibited by the CES2A1-specific inhibitor telmisartan
tetrachlorvinphos
-
-
tetradecane-7,8-dione
tetradecanoic acid
-
-
tetraethyl 4-oxo-2-phenyl-4H-chromene-5,7-diyl bis(phosphate)
-
-
tetraethyl 5-hydroxy-4-oxo-2-phenyl-4H-chromene-6,7-diyl bis(phosphate)
-
-
tetraisopropyl diphosphoramide
-
67% inhibition at 0.5 mM
thioridazine
-
-
Toluene
20% (v/v), 2 h incubation, 86% loss of activity
Tonalide
tosyl-L-phenylalanine chloromethyl ketone
-
inhibits more than 80% of the enzyme at 1 mM
trans-permethrin
-
a pyrethroid insecticide
trans/cis-permethrin
-
substrate inhibition
triazophos
Trichlorfon
triphenyl phosphate
-
-
tris(p-nitrophenyl)phosphate
-
-
Triton X-100
Tween
5% (v/v), 94% inhibition
Tween 20
Tween 50
10% (v/v), 49% inhibition
-
Tween 60
10% (w/v), 49% inhibition
Tween 80
Tween-20
0.1% v/v, 16% loss of activity. 1% v/v, 33% loss of activity
Tween-80
inhibition of wild-type and mutant enzyme R11G/L36P/V225A/I551L/A564T no matter that they are or are not treated by acetone
Urea
5 mM, 16% loss of activity (recombinant enzyme expressed in Sulfolobus solfataricus). 5 mM, 17% loss of activity (recombinant enzyme expressed in Escherichia coli as thioredoxin-free form (EcSisEstA I)). 5 mM, 10% loss of activity (recombinant enzyme expressed in Escherichia coli as a thioredoxin-EstA fusion protein (EcSisEstA II))
valsartan
-
about 90% residual activity at 0.1 mM
yuexiandajisu D
-
yuexiandajisu E
-
ziprasidone
-
-
ZnCl2
additional information
-