General Information of the Protein
Protein ID
PT02186
Protein Name
Liver carboxylesterase 1
Secondarily
Protein Name
Acyl-coenzyme A:cholesterol acyltransferase
Brain carboxylesterase hBr1
Carboxylesterase 1
Cholesteryl ester hydrolase
Cocaine carboxylesterase
Egasyn
HMSE
Methylumbelliferyl-acetate deacetylase 1
Monocyte/macrophage serine esterase
Retinyl ester hydrolase
Serine esterase 1
Triacylglycerol hydrolase
Gene Name
CES1
Secondarily
Gene Name
CES2
SES1
Sequence
MWLRAFILATLSASAAWGHPSSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPLGPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLNIYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFSTGDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLFHRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLKMKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIPMQLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDLIADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPFLKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLKDKEVAFWTNLFAKKAVEKPPQTEHIEL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs (PubMed:7980644, PubMed:9169443, PubMed:9490062, PubMed:18762277). Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester (PubMed:7980644, PubMed:9169443, PubMed:9490062, PubMed:18762277). Hydrolyzes the methyl ester group of cocaine to form benzoylecgonine (PubMed:7980644). Catalyzes the transesterification of cocaine to form cocaethylene (PubMed:7980644). Displays fatty acid ethyl ester synthase activity, catalyzing the ethyl esterification of oleic acid to ethyloleate (PubMed:7980644). Converts monoacylglycerides to free fatty acids and glycerol. Hydrolyzes of 2-arachidonoylglycerol and prostaglandins (PubMed:21049984). Hydrolyzes cellular cholesteryl esters to free cholesterols and promotes reverse cholesterol transport (RCT) by facilitating both the initial and final steps in the process (PubMed:18762277, PubMed:16024911, PubMed:11015575, PubMed:16971496). First of all, allows free cholesterol efflux from macrophages to extracellular cholesterol acceptors and secondly, releases free cholesterol from lipoprotein-delivered cholesteryl esters in the liver for bile acid synthesis or direct secretion into the bile (PubMed:18762277, PubMed:18599737, PubMed:16971496).
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Uniprot ID
Primary ID:
P23141

Secondarily ID:
A6NIM1
A8K3K8
A8K844
E9PAU8
P82127
Q00015
Q13657
Q14062
Q16737
Q16788
Q549X7
Q549X8
Q86UK2
Q96EE8
Q9UC52
Q9UDG8
Q9UK77
Q9ULY2
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Ensembl ID
ENSG00000198848
HGNC ID
HGNC:1863
Subcellular Location
Endoplasmic reticulum lumen
Cytoplasm
Lipid droplet
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000012 , Sf21
Compound ID Compound Name Compound Formula
CP0132869
1-{[4-({4-[(2,3-dioxo-2,3-dihydro-1H-indol-1-yl)methyl]phenyl}methyl)phenyl]methyl}-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C31H22N2O4
 1
1
Ki = 8 nM
   TI
   LI
   LO
   TS
CP0156264
1-dodecyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C20H29NO2
 1
1
Ki = 10 nM
   TI
   LI
   LO
   TS
CP0156260
1-hexadecyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C24H37NO2
 1
1
Ki = 16 nM
   TI
   LI
   LO
   TS
CP0176683
1&#8208;phenylindole&#8208;2,3&#8208;dione (Compound 6)
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C14H9NO2
 1
1
Ki = 23 nM
   TI
   LI
   LO
   TS
CP0112751
1-[(4-chlorophenyl)methyl]-2,3-dihydro-1H-indole-2,3-dione
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C15H10ClNO2
 1
1
Ki = 25 nM
   TI
   LI
   LO
   TS
CP0275191
1-[(3,4-dichlorophenyl)methyl]-2,3-dihydro-1H-indole-2,3-dione
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C15H9Cl2NO2
 1
1
Ki = 31 nM
   TI
   LI
   LO
   TS
CP0176565
5-bromo-1-(2-methylprop-2-en-1-yl)-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C12H10BrNO2
 1
1
Ki = 66 nM
   TI
   LI
   LO
   TS
CP0176682
1-(2-iodoethyl)-2,3-dihydro-1H-indole-2,3-dione
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C10H8INO2
 1
1
Ki = 130 nM
   TI
   LI
   LO
   TS
CP0219837
1,2-Di-naphthalen-2-yl-ethane-1,2-dione
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C22H14O2
 1
1
Ki = 255 nM
   TI
   LI
   LO
   TS
CP0048065
1-(2-bromoethyl)-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C10H8BrNO2
 1
1
Ki = 290 nM
   TI
   LI
   LO
   TS
CP0104526
1-{[(4-bromophenyl)amino]methyl}-2,3-dihydro-1H-indole-2,3-dione
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C15H11BrN2O2
 1
1
Ki = 580 nM
   TI
   LI
   LO
   TS
CP0297233
4,7-dichloro-2,3-dihydro-1H-indole-2,3-dione
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C8H3Cl2NO2
 1
1
Ki = 590 nM
   TI
   LI
   LO
   TS
CP0062390
1-{[(4-chlorophenyl)amino]methyl}-2,3-dihydro-1H-indole-2,3-dione
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C15H11ClN2O2
 1
1
Ki = 610 nM
   TI
   LI
   LO
   TS
CP0141262
4,6-dichloro-2,3-dihydro-1H-indole-2,3-dione
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C8H3Cl2NO2
 1
1
Ki = 890 nM
   TI
   LI
   LO
   TS
CP0033566
5-chloro-2,3-dihydro-1H-indole-2,3-dione
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C8H4ClNO2
 1
1
Ki = 1220 nM
   TI
   LI
   LO
   TS
CP0112757
1-{[(4-tert-butylphenyl)amino]methyl}-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C19H20N2O2
 1
1
Ki = 1420 nM
   TI
   LI
   LO
   TS
CP0176563
1-[2-(2,3-dioxo-2,3-dihydro-1H-indol-1-yl)ethyl]-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C18H12N2O4
 1
1
Ki = 1560 nM
   TI
   LI
   LO
   TS
CP0280272
1-{[(2,4,5-trimethylphenyl)amino]methyl}-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C18H18N2O2
 1
1
Ki = 1620 nM
   TI
   LI
   LO
   TS
CP0082269
1-benzyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C15H11NO2
 1
1
Ki = 1700 nM
   TI
   LI
   LO
   TS
CP0048066
1-{[(4-ethylphenyl)amino]methyl}-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C17H16N2O2
 1
1
Ki = 1880 nM
   TI
   LI
   LO
   TS
CP0048067
1-{[(4-methylphenyl)amino]methyl}-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C16H14N2O2
 1
1
Ki = 2650 nM
   TI
   LI
   LO
   TS
CP0280270
4,5-dichloro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H3Cl2NO2
 1
1
Ki = 3020 nM
   TI
   LI
   LO
   TS
CP0340186
5,7-dichloro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H3Cl2NO2
 1
1
Ki = 3520 nM
   TI
   LI
   LO
   TS
CP0275190
2-(2,3-dioxo-2,3-dihydro-1H-indol-1-yl)-N-(3-methylphenyl)acetamide
   Show/Hide
C17H14N2O3
 1
1
Ki = 4350 nM
   TI
   LI
   LO
   TS
CP0041636
1-methyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H7NO2
 1
1
Ki = 5380 nM
   TI
   LI
   LO
   TS
CP0104529
4-chloro-7-methyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H6ClNO2
 1
1
Ki = 5530 nM
   TI
   LI
   LO
   TS
CP0062398
1-butanoyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C12H11NO3
 1
1
Ki = 7690 nM
   TI
   LI
   LO
   TS
CP0248137
4-chloro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H4ClNO2
 1
1
Ki = 8250 nM
   TI
   LI
   LO
   TS
CP0236213
6,7-dichloro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H3Cl2NO2
 1
1
Ki = 9400 nM
   TI
   LI
   LO
   TS
CP0125598
7-chloro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H4ClNO2
 1
1
Ki = 11400 nM
   TI
   LI
   LO
   TS
CP0156265
7-(trifluoromethyl)-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H4F3NO2
 1
1
Ki = 13100 nM
   TI
   LI
   LO
   TS
CP0055080
5-(trifluoromethoxy)-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H4F3NO3
 1
1
Ki = 16500 nM
   TI
   LI
   LO
   TS
CP0176681
6-bromo-5-methyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H6BrNO2
 1
1
Ki = 16500 nM
   TI
   LI
   LO
   TS
CP0275188
1-propanoyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C11H9NO3
 1
1
Ki = 17500 nM
   TI
   LI
   LO
   TS
CP0141271
1-{[(3,4,5-trimethoxyphenyl)amino]methyl}-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C18H18N2O5
 1
1
Ki = 19500 nM
   TI
   LI
   LO
   TS
CP0280269
5,6-dichloro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H3Cl2NO2
 1
1
Ki = 21000 nM
   TI
   LI
   LO
   TS
CP0062400
1-chloro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H4ClNO2
 1
1
Ki = 22800 nM
   TI
   LI
   LO
   TS
CP0117907
5-iodo-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H4INO2
 1
1
Ki = 26900 nM
   TI
   LI
   LO
   TS
CP0054968
5-bromo-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H4BrNO2
 1
1
Ki = 31700 nM
   TI
   LI
   LO
   TS
CP0141265
5-chloro-7-methyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H6ClNO2
 1
1
Ki = 34100 nM
   TI
   LI
   LO
   TS
CP0141263
1-{[(2-bromophenyl)amino]methyl}-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C15H11BrN2O2
 1
1
Ki = 36000 nM
   TI
   LI
   LO
   TS
CP0156261
1-acetyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C10H7NO3
 1
1
Ki = 36000 nM
   TI
   LI
   LO
   TS
CP0141267
6-chloro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H4ClNO2
 1
1
Ki = 53900 nM
   TI
   LI
   LO
   TS
CP0176564
6-chloro-7-methyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H6ClNO2
 1
1
Ki = 55300 nM
   TI
   LI
   LO
   TS
CP0257171
1,2-Di-furan-2-yl-2-hydroxy-ethanone
   Show/Hide
C10H8O4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0036084
2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H5NO2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0048061
1-(hydroxymethyl)-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H7NO3
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0062386
5-methyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H7NO2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0062388
4-ethyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C10H9NO2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0062394
5-fluoro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H4FNO2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0062396
5-methoxy-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H7NO3
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0104530
2,3-dioxo-2,3-dihydro-1H-indole-7-carboxylic acid
   Show/Hide
C9H5NO4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0104531
5-Nitroisatin
   Show/Hide
C8H4N2O4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0108445
2-(2,3-dioxo-2,3-dihydro-1H-indol-1-yl)acetamide
   Show/Hide
C10H8N2O3
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0112749
1-(thiomorpholin-4-ylmethyl)-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C13H14N2O2S
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0112750
7-fluoro-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C8H4FNO2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0112752
7-methoxy-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H7NO3
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0126950
5,7-dimethyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C10H9NO2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0141264
1-(2-chloroacetyl)-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C10H6ClNO3
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0141268
6-ethyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C10H9NO2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0146494
7-methyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C9H7NO2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0176566
1-[(naphthalen-2-ylamino)methyl]-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C19H14N2O2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0236211
1-(morpholin-4-ylmethyl)-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C13H14N2O3
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0236212
1-(piperidin-1-ylmethyl)-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C14H16N2O2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0275187
2-(2,3-dioxo-2,3-dihydro-1H-indol-1-yl)acetic acid
   Show/Hide
C10H7NO4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0289923
4,7-dimethyl-2,3-dihydro-1H-indole-2,3-dione
   Show/Hide
C10H9NO2
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0289924
2-(2,3-dioxo-2,3-dihydro-1H-indol-1-yl)-N-(4-hydroxyphenyl)acetamide
   Show/Hide
C16H12N2O4
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0859453
(alphaR,1R)-cis-cyano(6-methoxynaphthalen-2-yl)methyl)3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate
   Show/Hide
C21H19Cl2NO3
 1
1
Km = 300 nM
   TI
   LI
   LO
   TS
CP0873907
(alphaS,1R)-trans-cyano(6-methoxynaphthalen-2-yl)methyl)3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate
   Show/Hide
C21H19Cl2NO3
 1
1
Km = 700 nM
   TI
   LI
   LO
   TS
CP0913993
(alphaS,1S)-cis-(cyano(6-methoxynaphthalen-2-yl)methyl)3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate
   Show/Hide
C21H19Cl2NO3
 1
1
Km = 1400 nM
   TI
   LI
   LO
   TS
CP0874414
cyano(6-methoxynaphthalen-2-yl)methyl 2,2,3,3-tetramethylcyclopropanecarboxylate
   Show/Hide
C21H23NO3
 1
1
Km = 1500 nM
   TI
   LI
   LO
   TS
CP0902207
(alphaR,1S)-cis-cyano(6-methoxynaphthalen-2-yl)methyl)3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate
   Show/Hide
C21H19Cl2NO3
 1
1
Km = 1500 nM
   TI
   LI
   LO
   TS
CP0848960
(alphaR,1R)-trans-cyano(6-methoxynaphthalen-2-yl)methyl)3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate
   Show/Hide
C21H19Cl2NO3
 1
1
Km = 1700 nM
   TI
   LI
   LO
   TS
CP0848961
(alphaR,1S)-trans-cyano(6-methoxynaphthalen-2-yl)methyl)3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate
   Show/Hide
C21H19Cl2NO3
 1
1
Km = 1900 nM
   TI
   LI
   LO
   TS
CP0913991
(alphaS,1S)-trans-cyano(6-methoxynaphthalen-2-yl)methyl)3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate
   Show/Hide
C21H19Cl2NO3
 1
1
Km = 2400 nM
   TI
   LI
   LO
   TS
CP0879694
trans-Resmethrin
   Show/Hide
C22H26O3
 1
1
Km = 6720 nM
   TI
   LI
   LO
   TS
CP0859452
SID26754480
   Show/Hide
C21H20Cl2O3
 1
1
Km = 9800 nM
   TI
   LI
   LO
   TS
CP0897258
(RS)-cis-Permethrin
   Show/Hide
C21H20Cl2O3
 1
1
Km = 9800 nM
   TI
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   TS
CP0846183
(RR)-trans-Permethrin
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C21H20Cl2O3
 1
1
Km = 23800 nM
   TI
   LI
   LO
   TS
CP0873906
(SS)-trans-Permethrin
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C21H20Cl2O3
 1
1
Km = 23800 nM
   TI
   LI
   LO
   TS
CP0041251
methyl (2R)-2-phenyl-2-[(2R)-piperidin-2-yl]acetate
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C14H19NO2
 1
1
Km = 43800 nM
   TI
   LI
   LO
   TS
CP0066112
CLOPIDOGREL
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C16H16ClNO2S
 1
1
Km = 55700 nM
   TI
   LI
   LO
   TS
CP0452756
(S)-Phenyl-(S)-piperidin-2-yl-acetic acid methyl ester; hydrochloride
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C14H19NO2
 1
1
Km = 89900 nM
   TI
   LI
   LO
   TS
CP0035807
Cocaine
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C17H21NO4
 1
1
Km = 120000 nM
   TI
   LI
   LO
   TS
CP0859449
p-nitrophenyl butyrate
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C10H11NO4
 1
1
Km = 130000 nM
   TI
   LI
   LO
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CP0084817
Accupril
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C25H30N2O5
 1
1
Km = 134000 nM
   TI
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   TS
CP0046621
3-[4-[3-(3,4,5-trimethoxybenzoyl)oxypropyl]-1,4-diazepan-1-yl]propyl 3,4,5-trimethoxybenzoate
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C31H44N2O10
 1
1
Km = 154000 nM
   TI
   LI
   LO
   TS
CP0036725
Oseltamivir
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C16H28N2O4
 1
1
Km = 177000 nM
   TI
   LI
   LO
   TS
CP0429214
3-[2-(1-Ethoxycarbonyl-3-phenyl-propylamino)-propionyl]-1-methyl-2-oxo-imidazolidine-4-carboxylic acid
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C20H27N3O6
 1
1
Km = 287000 nM
   TI
   LI
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CP0662099
4-nitrophenyl acetate
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C8H7NO4
 1
1
Km = 359000 nM
   TI
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   TS
CP0888733
5'-Phe-Floxuridine
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C18H20FN3O6
 1
1
Km = 460000 nM
   TI
   LI
   LO
   TS
CP0234575
US9199927, camostat
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C20H22N4O5
 1
1
Km = 707000 nM
   TI
   LI
   LO
   TS
CP0066691
1H-1-Benzazepine-1-acetic acid, 3-((1-(ethoxycarbonyl)-3-phenylpropyl)amino)-2,3,4,5-tetrahydro-2-oxo-, (S-(R*,R*))-
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C24H28N2O5
 1
1
Km = 734000 nM
   TI
   LI
   LO
   TS
CP0848964
Temocapril
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C23H28N2O5S2
 1
1
Km = 786000 nM
   TI
   LI
   LO
   TS
CP0298219
(4-methyl-2-oxidanylidene-chromen-7-yl) ethanoate
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C12H10O4
 1
1
Km = 800000 nM
   TI
   LI
   LO
   TS
CP0848966
5'-Leu-Floxuridine
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C15H22FN3O6
 1
1
Km = 970000 nM
   TI
   LI
   LO
   TS
CP0858321
cilazapril
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C22H31N3O5
 1
1
Km = 1295000 nM
   TI
   LI
   LO
   TS
CP0699868
Capecitabine
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C15H22FN3O6
 1
1
Km = 1300000 nM
   TI
   LI
   LO
   TS
CP0076378
(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
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C33H38N4O6
 1
1
Km = 1453000 nM
   TI
   LI
   LO
   TS
CP0859450
Delapril
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C26H32N2O5
 1
1
Km = 1502000 nM
   TI
   LI
   LO
   TS
CP0125124
1-Methyl-4-phenyl-piperidine-4-carboxylic acid ethyl ester
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C15H21NO2
 1
1
Km = 1900000 nM
   TI
   LI
   LO
   TS
CP0873905
(S)-3-amino-4-(((2R,3S,5R)-5-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3-hydroxytetrahydrofuran-2-yl)methoxy)-4-oxobutanoic acid
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C13H16FN3O8
 1
1
Km = 3000000 nM
   TI
   LI
   LO
   TS
CP0846184
(S)-((2R,3S,5R)-5-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3-hydroxytetrahydrofuran-2-yl)methyl 2-amino-3-methylbutanoate
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C14H20FN3O6
 1
1
Km = 3580000 nM
   TI
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   TS
CP0859454
Diacetylmorphine
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C21H23NO5
 1
1
Km = 6300000 nM
   TI
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   TS
CP0401523
6-Acetylmorphine
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C19H21NO4
 1
1
Km = 8300000 nM
   TI
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   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0079374
1,2-diphenylethane-1,2-dione
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C14H10O2
 6
1 IC50 = 27 nM
2 IC50 = 43 nM
3 IC50 = 370 nM
4 Ki = 44.67 nM
5 Ki = 45 nM
6 Ki = 45.1 nM
CP0176683
1&#8208;phenylindole&#8208;2,3&#8208;dione (Compound 6)
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C14H9NO2
 1
1 Ki = 23 nM
CP0112751
1-[(4-chlorophenyl)methyl]-2,3-dihydro-1H-indole-2,3-dione
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C15H10ClNO2
 1
1 Ki = 25 nM
CP0102783
1,2-Bis-(4-bromo-thiophen-2-yl)-ethane-1,2-dione
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C10H4Br2O2S2
 1
1 Ki = 30.2 nM
CP0222311
1,2-Di-pyridin-2-yl-ethane-1,2-dione
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C12H8N2O2
 1
1 Ki = 125.89 nM
CP0150351
1,2-Bis-(5-bromo-thiophen-2-yl)-ethane-1,2-dione
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C10H4Br2O2S2
 1
1 Ki = 208.93 nM
CP0198631
1,2-Di-thiophen-2-yl-ethane-1,2-dione
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C10H6O2S2
 1
1 Ki = 213.8 nM
CP0219837
1,2-Di-naphthalen-2-yl-ethane-1,2-dione
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C22H14O2
 1
1 Ki = 257.04 nM
CP0078039
1,2-Di-thiophen-3-yl-ethane-1,2-dione
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C10H6O2S2
 1
1 Ki = 363.08 nM
CP0333970
1,2-Di-furan-2-yl-ethane-1,2-dione
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C10H6O4
 1
1 Ki = 1174.9 nM
CP0051792
2-hydroxy-1,2-diphenylethan-1-one
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C14H12O2
 1
1 Ki = 7210 nM
Clinical Information about the Protein
Target 1 ( Liver carboxylesterase (CES1) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Synthesis disorder [ICD-11: 5C52-5C59]
2 Arteriosclerosis [ICD-11: BD40]
3 Peripheral vascular disease [ICD-11: BD4Z]
4 Hyperlipidaemia [ICD-11: 5C80]
Approved Drug(s) 1 Approved Drug  1
1 Cholic Acid Approved
Synthesis disorder
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 PACTIMIBE Phase 2/3
Arteriosclerosis
2 K-604 Phase 2
Arteriosclerosis
Discontinued Drug(s) 8 Discontinued Drugs  8
1 Avasimibe Discontinued in Phase 3
Peripheral vascular disease
2 CI-976 Discontinued in Phase 2
Hyperlipidaemia
3 E-5324 Discontinued in Phase 2
Hyperlipidaemia
4 Eflucimibe Discontinued in Phase 2
Hyperlipidaemia
5 CL-277082 Discontinued in Phase 1
Arteriosclerosis
6 Lecimibide Terminated
Hyperlipidaemia
7 RP-73163 Terminated
Arteriosclerosis
8 TEI-6522 Terminated
Arteriosclerosis