General Information of DTT (ID: TTMF541)

DTT Name Liver carboxylesterase (CES1) DTT Info
Gene Name CES1

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Investigative Drug(s)
1 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [1]
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4 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
PACTIMIBE DM0NZDT Arteriosclerosis BD40 Phase 2/3 [2]
Eldacimibe DML7WP0 Hyperlipidaemia 5C80 Phase 2 [3]
K-604 DMQVN6P Arteriosclerosis BD40 Phase 2 [4]
GR148672X DM7W6YN Acute lymphoblastic leukaemia 2A85 Clinical trial [5]
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21 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Avasimibe DMFG4OM Peripheral vascular disease BD4Z Discontinued in Phase 3 [6]
CI-976 DMBO28J Hyperlipidaemia 5C80 Discontinued in Phase 2 [7]
CL-283796 DM7LIDT Hyperlipidaemia 5C80 Discontinued in Phase 2 [8]
E-5324 DM562BM Hyperlipidaemia 5C80 Discontinued in Phase 2 [9]
Eflucimibe DMZXRF2 Hyperlipidaemia 5C80 Discontinued in Phase 2 [3]
RP-64477 DMTQ3BS Hyperlipidaemia 5C80 Discontinued in Phase 2 [10]
447C88 DMC7M3K Hyperlipidaemia 5C80 Discontinued in Phase 1 [11]
CL-277082 DMSB7WV Arteriosclerosis BD40 Discontinued in Phase 1 [12]
F-1394 DMPC9K3 Arteriosclerosis BD40 Discontinued in Phase 1 [13]
YM-17E DM0FSA9 Hyperlipidaemia 5C80 Discontinued in Phase 1 [14]
YM-750 DMLD2R0 Hyperlipidaemia 5C80 Discontinued in Phase 1 [15]
CEB-925 DMNJXRG Hypercholesterolaemia 5C80.0 Terminated [17]
CI-999 DMV1J0P Arteriosclerosis BD40 Terminated [18]
DuP-129 DMJGCYO Hypercholesterolaemia 5C80.0 Terminated [5]
FR-129169 DM9V6AU Arteriosclerosis BD40 Terminated [19]
FR-145237 DMHV43M Arteriosclerosis BD40 Terminated [20]
Lecimibide DMFEMTG Hyperlipidaemia 5C80 Terminated [21]
NTE-122 DMU3D1K Arteriosclerosis BD40 Terminated [22]
RP-70676 DMHO5AG Hyperlipidaemia 5C80 Terminated [23]
RP-73163 DMO3FYI Arteriosclerosis BD40 Terminated [24]
TEI-6522 DMHS5DX Arteriosclerosis BD40 Terminated [25]
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⏷ Show the Full List of 21 Discontinued Drug(s)
1 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
HL-004 DMRE52S Arteriosclerosis BD40 Preclinical [16]
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113 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(1r)-1,2,2-trimethylpropyl (r)-methylphosphinate DMVE34H Discovery agent N.A. Investigative [26]
(E)-Octadec-9-enoic acid phenylamide DMP7TK0 Discovery agent N.A. Investigative [27]
1,1,1-trifluoro-3-(hexylsulfinyl)propan-2-one DMJ0ZMT Discovery agent N.A. Investigative [28]
1,1,1-trifluoro-3-(hexylsulfonyl)propan-2-one DMWDUCH Discovery agent N.A. Investigative [28]
1,1,1-trifluoro-3-(hexylthio)propan-2-one DMWGSP6 Discovery agent N.A. Investigative [28]
1,1,1-trifluoro-3-(octylsulfinyl)propan-2-one DMLBT0E Discovery agent N.A. Investigative [28]
1,1,1-trifluoro-3-(octylsulfonyl)propan-2-one DMT29SN Discovery agent N.A. Investigative [28]
1,1,1-trifluoro-3-(octylthio)propan-2-one DMU4EJW Discovery agent N.A. Investigative [28]
1,1,1-trifluorododecan-2-one DMW6CQV Discovery agent N.A. Investigative [28]
1,10-phenanthroline-5,6-dione DM5LVD2 Discovery agent N.A. Investigative [29]
1,2-bis(2,3,4-trifluorophenyl)-2-hydroxyethanone DMZSL7H Discovery agent N.A. Investigative [30]
1,2-bis(2,3,4-trifluorophenyl)ethane-1,2-dione DML5ECR Discovery agent N.A. Investigative [30]
1,2-bis(2,3,5-trifluorophenyl)-2-hydroxyethanone DMD9HP8 Discovery agent N.A. Investigative [30]
1,2-bis(2,3,5-trifluorophenyl)ethane-1,2-dione DMZHWAV Discovery agent N.A. Investigative [30]
1,2-bis(2,3,6-trifluorophenyl)ethane-1,2-dione DMWS2HL Discovery agent N.A. Investigative [30]
1,2-bis(2,3-difluorophenyl)-2-hydroxyethanone DMZ0D5W Discovery agent N.A. Investigative [30]
1,2-bis(2,3-fluorophenyl)ethane-1,2-dione DM9Z1NY Discovery agent N.A. Investigative [30]
1,2-bis(2,4-difluorophenyl)-2-hydroxyethanone DMLMCBW Discovery agent N.A. Investigative [30]
1,2-bis(2,4-difluorophenyl)ethane-1,2-dione DMUZHPS Discovery agent N.A. Investigative [30]
1,2-bis(2,5-difluorophenyl)-2-hydroxyethanone DM9EW2F Discovery agent N.A. Investigative [30]
1,2-bis(2,5-difluorophenyl)ethane-1,2-dione DMVLMBQ Discovery agent N.A. Investigative [30]
1,2-bis(2,6-difluorophenyl)-2-hydroxyethanone DMSMVCH Discovery agent N.A. Investigative [30]
1,2-bis(2,6-difluorophenyl)ethane-1,2-dione DM351EA Discovery agent N.A. Investigative [30]
1,2-bis(2-fluorophenyl)-2-hydroxyethanone DMNWM5S Discovery agent N.A. Investigative [30]
1,2-bis(2-fluorophenyl)ethane-1,2-dione DM9FMUE Discovery agent N.A. Investigative [30]
1,2-bis(3,4,5-trifluorophenyl)-2-hydroxyethanone DM0LWAV Discovery agent N.A. Investigative [30]
1,2-bis(3,4,5-trifluorophenyl)ethane-1,2-dione DMPJT3V Discovery agent N.A. Investigative [30]
1,2-bis(3,4-difluorophenyl)-2-hydroxyethanone DMRCUKJ Discovery agent N.A. Investigative [30]
1,2-bis(3,4-difluorophenyl)ethane-1,2-dione DMBZ5RN Discovery agent N.A. Investigative [30]
1,2-bis(3,5-difluorophenyl)-2-hydroxyethanone DMQTPX2 Discovery agent N.A. Investigative [30]
1,2-bis(3,5-difluorophenyl)ethane-1,2-dione DM3K5RI Discovery agent N.A. Investigative [30]
1,2-bis(3-fluorophenyl)-2-hydroxyethanon DM8XGD0 Discovery agent N.A. Investigative [30]
1,2-bis(3-fluorophenyl)ethane-1,2-dione DMM3I1P Discovery agent N.A. Investigative [30]
1,2-bis(4-fluorophenyl)ethane-1,2-dione DM38Q7W Discovery agent N.A. Investigative [30]
1,2-Bis-(2-chloro-phenyl)-ethane-1,2-dione DMZF4IC Discovery agent N.A. Investigative [31]
1,2-Bis-(3-methoxy-phenyl)-ethane-1,2-dione DMWY1QN Discovery agent N.A. Investigative [31]
1,2-Bis-(3-nitro-phenyl)-ethane-1,2-dione DMGSTKZ Discovery agent N.A. Investigative [31]
1,2-Bis-(4-bromo-phenyl)-ethane-1,2-dione DMUW2EJ Discovery agent N.A. Investigative [31]
1,2-Bis-(4-chloro-phenyl)-ethane-1,2-dione DM0E5FH Discovery agent N.A. Investigative [31]
1,2-Bis-(4-methoxy-phenyl)-ethane-1,2-dione DMCGRV7 Discovery agent N.A. Investigative [31]
1,2-Di-naphthalen-2-yl-ethane-1,2-dione DMGXMF0 Discovery agent N.A. Investigative [32]
1,2-Di-p-tolyl-ethane-1,2-dione DMFXB21 Discovery agent N.A. Investigative [31]
1,2-dicyclohexylethane-1,2-dione DM75OR8 Discovery agent N.A. Investigative [29]
1,2-indanedione DMV275G Discovery agent N.A. Investigative [29]
1,2-NAPHTHOQUINONE DMYXELH Discovery agent N.A. Investigative [29]
1-(2-bromoethyl)-1H-indole-2,3-dione DMYF8ES Discovery agent N.A. Investigative [33]
1-(2-iodoethyl)-1H-indole-2,3-dione DM1MSAC Discovery agent N.A. Investigative [33]
1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione DMX71K9 Discovery agent N.A. Investigative [33]
1-(3,4-Dimethyl-phenyl)-2-phenyl-ethane-1,2-dione DMCHILK Discovery agent N.A. Investigative [31]
1-(4-Chloro-phenyl)-2-p-tolyl-ethane-1,2-dione DMOGVZ2 Discovery agent N.A. Investigative [31]
1-(4-Chloro-phenyl)-2-phenyl-ethane-1,2-dione DMCDV1O Discovery agent N.A. Investigative [31]
1-(4-chlorobenzyl)-1H-indole-2,3-dione DMOUPNT Discovery agent N.A. Investigative [33]
1-(4-Methoxy-phenyl)-2-phenyl-ethane-1,2-dione DM5R8KU Discovery agent N.A. Investigative [31]
1-(4-Nitro-phenyl)-2-phenyl-ethane-1,2-dione DMOC67J Discovery agent N.A. Investigative [31]
1-benzyl-1H-indole-2,3-dione DM2UFXE Discovery agent N.A. Investigative [33]
1-butyryl-1H-indole-2,3-dione DMVFCLO Discovery agent N.A. Investigative [33]
1-dodecyl-1H-indole-2,3-dione DMK6BWV Discovery agent N.A. Investigative [33]
1-hexadecyl-1H-indole-2,3-dione DM4OWM6 Discovery agent N.A. Investigative [33]
1-methyl-1H-indole-2,3-dione DMPW75L Discovery agent N.A. Investigative [33]
1-phenyl-1H-indole-2,3-dione DM74RMP Discovery agent N.A. Investigative [33]
1-Phenyl-2-p-tolyl-ethane-1,2-dione DMW9CRT Discovery agent N.A. Investigative [31]
1-Phenyl-propane-1,2-dione DM04SWY Discovery agent N.A. Investigative [31]
1-propionyl-1H-indole-2,3-dione DM1TNWG Discovery agent N.A. Investigative [33]
11,12-dihydro-dibenzo[a,e]cyclooctene-5,6-dione DME0OGM Discovery agent N.A. Investigative [29]
2,2-Dimethoxy-1,2-diphenyl-ethanone DM34IX5 Discovery agent N.A. Investigative [31]
2,2-dimethyl-3-methyleneheptadecane DM7BL04 Discovery agent N.A. Investigative [28]
2-methoxy-3,4-methylenedioxybenzophenone DM93DYT Discovery agent N.A. Investigative [34]
3,4,5,6-Tetrachloro-[1,2]benzoquinone DMSV6K5 Discovery agent N.A. Investigative [31]
3,5-Di-tert-butyl-[1,2]benzoquinone DMWOB7Q Discovery agent N.A. Investigative [31]
3-(butylsulfinyl)-1,1,1-trifluoropropan-2-one DM8PM0E Discovery agent N.A. Investigative [28]
3-(butylthio)-1,1,1-trifluoropropan-2-one DM8T2OX Discovery agent N.A. Investigative [28]
3-(decylsulfinyl)-1,1,1-trifluoropropan-2-one DMWJ6UD Discovery agent N.A. Investigative [28]
3-(decylsulfonyl)-1,1,1-trifluoropropan-2-one DMF27YT Discovery agent N.A. Investigative [28]
3-(decylthio)-1,1,1-trifluoropropan-2-one DM1Y6L8 Discovery agent N.A. Investigative [28]
3-(dodecylsulfinyl)-1,1,1-trifluoropropan-2-one DM7AG6Y Discovery agent N.A. Investigative [28]
3-(dodecylsulfonyl)-1,1,1-trifluoropropan-2-one DMPRCS0 Discovery agent N.A. Investigative [28]
4,5-dichloro-1H-indole-2,3-dione DMX94EK Discovery agent N.A. Investigative [33]
4,6-dichloro-1H-indole-2,3-dione DMHBO17 Discovery agent N.A. Investigative [33]
4,7-dichloro-1H-indole-2,3-dione DMEVK5F Discovery agent N.A. Investigative [33]
4-(2-Oxo-2-phenyl-acetyl)-benzoic acid DMFPNQ9 Discovery agent N.A. Investigative [31]
4-chloro-1H-indole-2,3-dione DM9HXPR Discovery agent N.A. Investigative [33]
4-chloro-7-methyl-1H-indole-2,3-dione DM16P3N Discovery agent N.A. Investigative [33]
4-Piperidino-Piperidine DMONGDX Discovery agent N.A. Investigative [26]
5,6-dinitroacenaphthoquinone DM07HYA Discovery agent N.A. Investigative [29]
5,7-dichloro-1H-indole-2,3-dione DMFHDWG Discovery agent N.A. Investigative [33]
5-(trifluoromethoxy)-1H-indole-2,3-dione DMK3TEV Discovery agent N.A. Investigative [33]
5-chloro-1H-indole-2,3-dione DMQ350F Discovery agent N.A. Investigative [33]
6,7-dichloro-1H-indole-2,3-dione DMZHDFM Discovery agent N.A. Investigative [33]
6-bromo-5-methyl-1H-indole-2,3-dione DMFZ2PI Discovery agent N.A. Investigative [33]
7-(trifluoromethyl)-1H-indole-2,3-dione DM46VT2 Discovery agent N.A. Investigative [33]
7-chloro-1H-indole-2,3-dione DMCZLKA Discovery agent N.A. Investigative [33]
Acenanthrene-9,10-dione DMU9O7K Discovery agent N.A. Investigative [29]
ACENAPHTHOQUINONE DMU3DMH Discovery agent N.A. Investigative [29]
Alpha-D-Mannose DMF5DLW Discovery agent N.A. Investigative [1]
BENZIL DM5Y2M8 Discovery agent N.A. Investigative [28]
Benzoin DM50QMB Discovery agent N.A. Investigative [30]
CHLORANIL DMCHGF1 Discovery agent N.A. Investigative [31]
Dibutyl 2,2,2-trifluoro-1-phenylethyl phosphate DM2G8ON Discovery agent N.A. Investigative [35]
Diethyl 2,2,2-trifluoro-1-phenylethyl phosphate DMDJ9QA Discovery agent N.A. Investigative [35]
Dimethyl 2,2,2-trifluoro-1-phenylethyl phosphate DMTVA49 Discovery agent N.A. Investigative [35]
Heptane-2,3-dione DMCFTB8 Discovery agent N.A. Investigative [31]
KY-382 DMA9VBD Arteriosclerosis BD40 Investigative [5]
N-Methylnaloxonium DMXSJH0 Discovery agent N.A. Investigative [36]
NSC-23180 DMJ91Y7 Discovery agent N.A. Investigative [29]
O-Sialic Acid DMCAR7B Discovery agent N.A. Investigative [26]
Oleic acid anilide DMXCSVH Discovery agent N.A. Investigative [34]
Phenanthrene-9,10-dione DMG8KS9 Discovery agent N.A. Investigative [29]
PYRIPYROPENE A DMCTJAM Discovery agent N.A. Investigative [27]
SCH-48375 DM0J937 Discovery agent N.A. Investigative [37]
SMP-797 DMSI95J Discovery agent N.A. Investigative [38]
Thenoyltrifluoroacetone DM54OKX Discovery agent N.A. Investigative [39]
Thieno[3,2-e][1]benzothiophene-4,5-dione DMT74N6 Discovery agent N.A. Investigative [29]
VULM-1457 DMWRX4T Arteriosclerosis BD40 Investigative [5]
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⏷ Show the Full List of 113 Investigative Drug(s)
Molecule Interaction Atlas

References

1 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
2 Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and b... J Med Chem. 2008 Aug 14;51(15):4823-33.
3 Prospects for drug therapy for hyperlipoproteinaemia. Diabete Metab. 1995 Apr;21(2):139-46.
4 A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels. Atherosclerosis. 2007 Apr;191(2):290-7.
5 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2592).
6 New advances in lipid-modifying therapies for reducing cardiovascular risk. Cardiology. 2002;97(2):59-66.
7 Acyl-coenzyme A:cholesterol-acyltransferase (ACAT) inhibitors modulate monocyte adhesion to aortic endothelial cells. Atherosclerosis. 1995 Jan 6;112(1):7-17.
8 ACAT inhibitors CL 283,546 and CL 283,796 reduce LDL cholesterol without affecting cholesterol absorption in African green monkeys. J Lipid Res. 1995 Jun;36(6):1199-210.
9 Effect of the acyl-CoA:cholesterol acyltransferase inhibitor, E5324, on experimental atherosclerosis in rabbits. Atherosclerosis. 1994 Jun;107(2):187-201.
10 RP 64477: a potent inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase with low systemic bioavailability. Biochem Pharmacol. 1996 Feb 23;51(4):413-21.
11 The tolerability, pharmacokinetics and lack of effect on plasma cholesterol of 447C88, an AcylCoA: Cholesterol Acyl Transferase (ACAT) inhibitor with low bioavailability, in healthy volunteers. Eur JClin Pharmacol. 1995;49(3):243-9.
12 CL 277,082: a novel inhibitor of ACAT-catalyzed cholesterol esterification and cholesterol absorption. J Lipid Res. 1989 May;30(5):681-90.
13 ACAT inhibitor F-1394 prevents intimal hyperplasia induced by balloon injury in rabbits. J Lipid Res. 2001 Apr;42(4):480-8.
14 Pharmacological properties of YM17E, an acyl-CoA:cholesterol acyltransferase inhibitor, and diarrheal effect in beagle dogs. Jpn J Pharmacol. 1997 Jan;73(1):41-50.
15 Effects of an anti-oxidative ACAT inhibitor on apoptosis/necrosis and cholesterol accumulation under oxidative stress in THP-1 cell-derived foam ce... Life Sci. 2008 Jan 2;82(1-2):79-84.
16 ACAT inhibitor HL-004 accelerates the regression of hypercholesterolemia in stroke-prone spontaneously hypertensive rats (SHRSP): stimulation of bile acid production by HL-004. Atherosclerosis. 1997 Aug;133(1):97-104.
17 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010079)
18 Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates. Bioorg Med Chem Lett. 1998 Feb 3;8(3):289-94.
19 Plasma cholesterol reducing effect of FR129169, a novel acyl-CoA:cholesterol acyltransferase inhibitor, in the rat. Jpn J Pharmacol. 1996 Jan;70(1):35-41.
20 Effect of FR145237, a novel ACAT inhibitor, on atherogenesis in cholesterol-fed and WHHL rabbits. Evidence for a direct effect on the arterial wall. Biochim Biophys Acta. 1995 Dec 7;1259(3):254-60.
21 Effect of the acyl-CoA:cholesterol acyltransferase inhibitor DuP 128 on cholesterol absorption and serum cholesterol in humans. Clin Pharmacol Ther. 1994 Jul;56(1):65-74.
22 Cholesterol-lowering effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, on cholesterol diet-fed rats and rabbits. Jpn J Pharmacol. 1998 Nov;78(3):355-64.
23 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002876)
24 Hypolipidaemic properties of a potent and bioavailable alkylsulphinyl-diphenylimidazole ACAT inhibitor (RP 73163) in animals fed diets low in cholesterol. Biochem Pharmacol. 1996 Oct 25;52(8):1177-86.
25 Potent inhibitors of acyl-CoA:cholesterol acyltransferase. Structure-activity relationships of novel N-(4-oxochroman-8-yl)amides. J Med Chem. 1995 Aug 4;38(16):3174-86.
26 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
27 Acyl-CoA: cholesterol acyltransferase inhibitory activities of fatty acid amides isolated from Mylabris phalerate Pallas. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4277-80.
28 Influence of sulfur oxidation state and steric bulk upon trifluoromethyl ketone (TFK) binding kinetics to carboxylesterases and fatty acid amide hy... Bioorg Med Chem. 2008 Feb 15;16(4):2114-30.
29 Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1. J Med Chem. 2007 Nov 15;50(23):5727-34.
30 Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils. Bioorg Med Chem. 2007 Jun 1;15(11):3801-17.
31 Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases. J Med Chem. 2005 Apr 21;48(8):2906-15.
32 Inhibition of carboxylesterases by benzil (diphenylethane-1,2-dione) and heterocyclic analogues is dependent upon the aromaticity of the ring and t... J Med Chem. 2005 Aug 25;48(17):5543-50.
33 Selective inhibition of carboxylesterases by isatins, indole-2,3-diones. J Med Chem. 2007 Apr 19;50(8):1876-85.
34 Phenolic compounds from the roots of Lindera fruticosa. J Nat Prod. 2006 May;69(5):853-5.
35 Synthesis of organophosphates with fluorine-containing leaving groups as serine esterase inhibitors with potential for Alzheimer disease therapeutics. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5528-30.
36 DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41.
37 2-Azetidinones as inhibitors of cholesterol absorption. J Med Chem. 1994 Jun 10;37(12):1733-6.
38 Company report (Dainippon Sumitomo Pharma)
39 Zhang JG, Fariss MW: Thenoyltrifluoroacetone, a potent inhibitor of carboxylesterase activity. Biochem Pharmacol. 2002 Feb 15;63(4):751-4.