Target Information
Target General Information | Top | |||||
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Target ID |
T76369
(Former ID: TTDR00274)
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Target Name |
Liver carboxylesterase (CES1)
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Synonyms |
Serine esterase 1; Monocyte/macrophage serine esterase; Human carboxylesterase 1; HMSE; HCE1; CES1; Brain carboxylesterase hBr1; Acyl coenzyme A:cholesterol acyltransferase
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Gene Name |
CES1
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Peroxisomal disease [ICD-11: 5C57] | |||||
2 | Synthesis disorder [ICD-11: 5C52-5C59] | |||||
Function |
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl coa ester.
Click to Show/Hide
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BioChemical Class |
Carboxylic ester hydrolase
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UniProt ID | ||||||
EC Number |
EC 3.1.1.1
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Sequence |
MWLRAFILATLSASAAWGHPSSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPL
GPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLN IYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFST GDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLF HRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLK MKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIP MQLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDL IADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPF LKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLK DKEVAFWTNLFAKKAVEKPPQTEHIEL Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
ADReCS ID | BADD_A00333 | |||||
HIT2.0 ID | T59DDI |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
1 | Cholic Acid | Drug Info | Approved | Synthesis disorder | [2] | |
Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
1 | PACTIMIBE | Drug Info | Phase 2/3 | Arteriosclerosis | [3] | |
2 | Eldacimibe | Drug Info | Phase 2 | Hyperlipidaemia | [4] | |
3 | K-604 | Drug Info | Phase 2 | Arteriosclerosis | [5] | |
4 | GR148672X | Drug Info | Clinical trial | Acute lymphoblastic leukaemia | [6] | |
Discontinued Drug(s) | [+] 21 Discontinued Drugs | + | ||||
1 | Avasimibe | Drug Info | Discontinued in Phase 3 | Peripheral vascular disease | [7] | |
2 | CI-976 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [8] | |
3 | CL-283796 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [9] | |
4 | E-5324 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [10] | |
5 | Eflucimibe | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [11] | |
6 | RP-64477 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [12] | |
7 | 447C88 | Drug Info | Discontinued in Phase 1 | Hyperlipidaemia | [13] | |
8 | CL-277082 | Drug Info | Discontinued in Phase 1 | Arteriosclerosis | [14] | |
9 | F-1394 | Drug Info | Discontinued in Phase 1 | Arteriosclerosis | [15] | |
10 | YM-17E | Drug Info | Discontinued in Phase 1 | Hyperlipidaemia | [16] | |
11 | YM-750 | Drug Info | Discontinued in Phase 1 | Hyperlipidaemia | [17] | |
12 | CEB-925 | Drug Info | Terminated | Hypercholesterolaemia | [19] | |
13 | CI-999 | Drug Info | Terminated | Arteriosclerosis | [20] | |
14 | DuP-129 | Drug Info | Terminated | Hypercholesterolaemia | [21] | |
15 | FR-129169 | Drug Info | Terminated | Arteriosclerosis | [22] | |
16 | FR-145237 | Drug Info | Terminated | Arteriosclerosis | [23] | |
17 | Lecimibide | Drug Info | Terminated | Hyperlipidaemia | [24] | |
18 | NTE-122 | Drug Info | Terminated | Arteriosclerosis | [25] | |
19 | RP-70676 | Drug Info | Terminated | Hyperlipidaemia | [26] | |
20 | RP-73163 | Drug Info | Terminated | Arteriosclerosis | [27] | |
21 | TEI-6522 | Drug Info | Terminated | Arteriosclerosis | [28] | |
Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
1 | HL-004 | Drug Info | Preclinical | Arteriosclerosis | [18] | |
Mode of Action | [+] 2 Modes of Action | + | ||||
Inhibitor | [+] 123 Inhibitor drugs | + | ||||
1 | Cholic Acid | Drug Info | [1] | |||
2 | PACTIMIBE | Drug Info | [29] | |||
3 | K-604 | Drug Info | [31] | |||
4 | GR148672X | Drug Info | [32] | |||
5 | Avasimibe | Drug Info | [33] | |||
6 | CI-976 | Drug Info | [34] | |||
7 | Eflucimibe | Drug Info | [30] | |||
8 | YM-750 | Drug Info | [43] | |||
9 | CEB-925 | Drug Info | [45] | |||
10 | CI-999 | Drug Info | [46] | |||
11 | DuP-129 | Drug Info | [32] | |||
12 | NTE-122 | Drug Info | [50] | |||
13 | (1r)-1,2,2-trimethylpropyl (r)-methylphosphinate | Drug Info | [54] | |||
14 | (E)-Octadec-9-enoic acid phenylamide | Drug Info | [55] | |||
15 | 1,1,1-trifluoro-3-(hexylsulfinyl)propan-2-one | Drug Info | [56] | |||
16 | 1,1,1-trifluoro-3-(hexylsulfonyl)propan-2-one | Drug Info | [56] | |||
17 | 1,1,1-trifluoro-3-(hexylthio)propan-2-one | Drug Info | [56] | |||
18 | 1,1,1-trifluoro-3-(octylsulfinyl)propan-2-one | Drug Info | [56] | |||
19 | 1,1,1-trifluoro-3-(octylsulfonyl)propan-2-one | Drug Info | [56] | |||
20 | 1,1,1-trifluoro-3-(octylthio)propan-2-one | Drug Info | [56] | |||
21 | 1,1,1-trifluorododecan-2-one | Drug Info | [56] | |||
22 | 1,10-phenanthroline-5,6-dione | Drug Info | [57] | |||
23 | 1,2-bis(2,3,4-trifluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
24 | 1,2-bis(2,3,4-trifluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
25 | 1,2-bis(2,3,5-trifluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
26 | 1,2-bis(2,3,5-trifluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
27 | 1,2-bis(2,3,6-trifluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
28 | 1,2-bis(2,3-difluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
29 | 1,2-bis(2,3-fluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
30 | 1,2-bis(2,4-difluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
31 | 1,2-bis(2,4-difluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
32 | 1,2-bis(2,5-difluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
33 | 1,2-bis(2,5-difluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
34 | 1,2-bis(2,6-difluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
35 | 1,2-bis(2,6-difluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
36 | 1,2-bis(2-fluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
37 | 1,2-bis(2-fluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
38 | 1,2-bis(3,4,5-trifluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
39 | 1,2-bis(3,4,5-trifluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
40 | 1,2-bis(3,4-difluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
41 | 1,2-bis(3,4-difluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
42 | 1,2-bis(3,5-difluorophenyl)-2-hydroxyethanone | Drug Info | [58] | |||
43 | 1,2-bis(3,5-difluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
44 | 1,2-bis(3-fluorophenyl)-2-hydroxyethanon | Drug Info | [58] | |||
45 | 1,2-bis(3-fluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
46 | 1,2-bis(4-fluorophenyl)ethane-1,2-dione | Drug Info | [58] | |||
47 | 1,2-Bis-(2-chloro-phenyl)-ethane-1,2-dione | Drug Info | [59] | |||
48 | 1,2-Bis-(3-methoxy-phenyl)-ethane-1,2-dione | Drug Info | [59] | |||
49 | 1,2-Bis-(3-nitro-phenyl)-ethane-1,2-dione | Drug Info | [59] | |||
50 | 1,2-Bis-(4-bromo-phenyl)-ethane-1,2-dione | Drug Info | [59] | |||
51 | 1,2-Bis-(4-chloro-phenyl)-ethane-1,2-dione | Drug Info | [59] | |||
52 | 1,2-Bis-(4-methoxy-phenyl)-ethane-1,2-dione | Drug Info | [59] | |||
53 | 1,2-Di-naphthalen-2-yl-ethane-1,2-dione | Drug Info | [60] | |||
54 | 1,2-Di-p-tolyl-ethane-1,2-dione | Drug Info | [59] | |||
55 | 1,2-dicyclohexylethane-1,2-dione | Drug Info | [57] | |||
56 | 1,2-indanedione | Drug Info | [57] | |||
57 | 1,2-NAPHTHOQUINONE | Drug Info | [57] | |||
58 | 1-(2-bromoethyl)-1H-indole-2,3-dione | Drug Info | [61] | |||
59 | 1-(2-iodoethyl)-1H-indole-2,3-dione | Drug Info | [61] | |||
60 | 1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione | Drug Info | [61] | |||
61 | 1-(3,4-Dimethyl-phenyl)-2-phenyl-ethane-1,2-dione | Drug Info | [59] | |||
62 | 1-(4-Chloro-phenyl)-2-p-tolyl-ethane-1,2-dione | Drug Info | [59] | |||
63 | 1-(4-Chloro-phenyl)-2-phenyl-ethane-1,2-dione | Drug Info | [59] | |||
64 | 1-(4-chlorobenzyl)-1H-indole-2,3-dione | Drug Info | [61] | |||
65 | 1-(4-Methoxy-phenyl)-2-phenyl-ethane-1,2-dione | Drug Info | [59] | |||
66 | 1-(4-Nitro-phenyl)-2-phenyl-ethane-1,2-dione | Drug Info | [59] | |||
67 | 1-benzyl-1H-indole-2,3-dione | Drug Info | [61] | |||
68 | 1-butyryl-1H-indole-2,3-dione | Drug Info | [61] | |||
69 | 1-dodecyl-1H-indole-2,3-dione | Drug Info | [61] | |||
70 | 1-hexadecyl-1H-indole-2,3-dione | Drug Info | [61] | |||
71 | 1-methyl-1H-indole-2,3-dione | Drug Info | [61] | |||
72 | 1-phenyl-1H-indole-2,3-dione | Drug Info | [61] | |||
73 | 1-Phenyl-2-p-tolyl-ethane-1,2-dione | Drug Info | [59] | |||
74 | 1-Phenyl-propane-1,2-dione | Drug Info | [59] | |||
75 | 1-propionyl-1H-indole-2,3-dione | Drug Info | [61] | |||
76 | 11,12-dihydro-dibenzo[a,e]cyclooctene-5,6-dione | Drug Info | [57] | |||
77 | 2,2-Dimethoxy-1,2-diphenyl-ethanone | Drug Info | [59] | |||
78 | 2,2-dimethyl-3-methyleneheptadecane | Drug Info | [56] | |||
79 | 2-methoxy-3,4-methylenedioxybenzophenone | Drug Info | [62] | |||
80 | 3,4,5,6-Tetrachloro-[1,2]benzoquinone | Drug Info | [59] | |||
81 | 3,5-Di-tert-butyl-[1,2]benzoquinone | Drug Info | [59] | |||
82 | 3-(butylsulfinyl)-1,1,1-trifluoropropan-2-one | Drug Info | [56] | |||
83 | 3-(butylthio)-1,1,1-trifluoropropan-2-one | Drug Info | [56] | |||
84 | 3-(decylsulfinyl)-1,1,1-trifluoropropan-2-one | Drug Info | [56] | |||
85 | 3-(decylsulfonyl)-1,1,1-trifluoropropan-2-one | Drug Info | [56] | |||
86 | 3-(decylthio)-1,1,1-trifluoropropan-2-one | Drug Info | [56] | |||
87 | 3-(dodecylsulfinyl)-1,1,1-trifluoropropan-2-one | Drug Info | [56] | |||
88 | 3-(dodecylsulfonyl)-1,1,1-trifluoropropan-2-one | Drug Info | [56] | |||
89 | 4,5-dichloro-1H-indole-2,3-dione | Drug Info | [61] | |||
90 | 4,6-dichloro-1H-indole-2,3-dione | Drug Info | [61] | |||
91 | 4,7-dichloro-1H-indole-2,3-dione | Drug Info | [61] | |||
92 | 4-(2-Oxo-2-phenyl-acetyl)-benzoic acid | Drug Info | [59] | |||
93 | 4-chloro-1H-indole-2,3-dione | Drug Info | [61] | |||
94 | 4-chloro-7-methyl-1H-indole-2,3-dione | Drug Info | [61] | |||
95 | 4-Piperidino-Piperidine | Drug Info | [54] | |||
96 | 5,6-dinitroacenaphthoquinone | Drug Info | [57] | |||
97 | 5,7-dichloro-1H-indole-2,3-dione | Drug Info | [61] | |||
98 | 5-(trifluoromethoxy)-1H-indole-2,3-dione | Drug Info | [61] | |||
99 | 5-chloro-1H-indole-2,3-dione | Drug Info | [61] | |||
100 | 6,7-dichloro-1H-indole-2,3-dione | Drug Info | [61] | |||
101 | 6-bromo-5-methyl-1H-indole-2,3-dione | Drug Info | [61] | |||
102 | 7-(trifluoromethyl)-1H-indole-2,3-dione | Drug Info | [61] | |||
103 | 7-chloro-1H-indole-2,3-dione | Drug Info | [61] | |||
104 | Acenanthrene-9,10-dione | Drug Info | [57] | |||
105 | ACENAPHTHOQUINONE | Drug Info | [57] | |||
106 | Alpha-D-Mannose | Drug Info | [1] | |||
107 | BENZIL | Drug Info | [56] | |||
108 | Benzoin | Drug Info | [58] | |||
109 | CHLORANIL | Drug Info | [59] | |||
110 | Dibutyl 2,2,2-trifluoro-1-phenylethyl phosphate | Drug Info | [63] | |||
111 | Diethyl 2,2,2-trifluoro-1-phenylethyl phosphate | Drug Info | [63] | |||
112 | Dimethyl 2,2,2-trifluoro-1-phenylethyl phosphate | Drug Info | [63] | |||
113 | Heptane-2,3-dione | Drug Info | [59] | |||
114 | N-Methylnaloxonium | Drug Info | [64] | |||
115 | NSC-23180 | Drug Info | [57] | |||
116 | O-Sialic Acid | Drug Info | [54] | |||
117 | Oleic acid anilide | Drug Info | [62] | |||
118 | Phenanthrene-9,10-dione | Drug Info | [57] | |||
119 | PYRIPYROPENE A | Drug Info | [55] | |||
120 | SCH-48375 | Drug Info | [65] | |||
121 | Thenoyltrifluoroacetone | Drug Info | [67] | |||
122 | Thieno[3,2-e][1]benzothiophene-4,5-dione | Drug Info | [57] | |||
123 | VULM-1457 | Drug Info | [32] | |||
Modulator | [+] 17 Modulator drugs | + | ||||
1 | Eldacimibe | Drug Info | [30] | |||
2 | CL-283796 | Drug Info | [35], [36] | |||
3 | E-5324 | Drug Info | [37] | |||
4 | RP-64477 | Drug Info | [38] | |||
5 | 447C88 | Drug Info | [39] | |||
6 | CL-277082 | Drug Info | [40] | |||
7 | F-1394 | Drug Info | [41] | |||
8 | YM-17E | Drug Info | [42] | |||
9 | HL-004 | Drug Info | [44] | |||
10 | FR-129169 | Drug Info | [47] | |||
11 | FR-145237 | Drug Info | [48] | |||
12 | Lecimibide | Drug Info | [49] | |||
13 | RP-70676 | Drug Info | [51] | |||
14 | RP-73163 | Drug Info | [52] | |||
15 | TEI-6522 | Drug Info | [53] | |||
16 | KY-382 | Drug Info | [32] | |||
17 | SMP-797 | Drug Info | [66] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
1 | Drug metabolism - other enzymes | |||||
2 | Metabolic pathways | |||||
PID Pathway | [+] 1 PID Pathways | + | ||||
1 | E2F transcription factor network | |||||
WikiPathways | [+] 6 WikiPathways | + | ||||
1 | NRF2 pathway | |||||
2 | Nuclear Receptors Meta-Pathway | |||||
3 | Heroin metabolism | |||||
4 | Irinotecan Pathway | |||||
5 | Fluoropyrimidine Activity | |||||
6 | Phase I biotransformations, non P450 |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
REF 2 | 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. (Ligand id: 609). | |||||
REF 3 | ClinicalTrials.gov (NCT00151788) Efficacy and Safety of the ACAT Inhibitor CS-505 (Pactimibe) for Reducing the Progression of Carotid Artery Disease. This Study is Also Known as CAPTIVATE.. U.S. National Institutes of Health. | |||||
REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003592) | |||||
REF 5 | ClinicalTrials.gov (NCT00851500) A Trial of the Safety and Efficacy of K-604 for the Treatment of Atherosclerosis. U.S. National Institutes of Health. | |||||
REF 6 | 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. (Ligand id: 6701). | |||||
REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008778) | |||||
REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001196) | |||||
REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004604) | |||||
REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004427) | |||||
REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011031) | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002301) | |||||
REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002257) | |||||
REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001648) | |||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003109) | |||||
REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002618) | |||||
REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003090) | |||||
REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033616) | |||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010079) | |||||
REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010990) | |||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003587) | |||||
REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002683) | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006465) | |||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002283) | |||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008195) | |||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002876) | |||||
REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003588) | |||||
REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004501) | |||||
REF 29 | 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. | |||||
REF 30 | Prospects for drug therapy for hyperlipoproteinaemia. Diabete Metab. 1995 Apr;21(2):139-46. | |||||
REF 31 | 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. | |||||
REF 32 | 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). | |||||
REF 33 | New advances in lipid-modifying therapies for reducing cardiovascular risk. Cardiology. 2002;97(2):59-66. | |||||
REF 34 | Acyl-coenzyme A:cholesterol-acyltransferase (ACAT) inhibitors modulate monocyte adhesion to aortic endothelial cells. Atherosclerosis. 1995 Jan 6;112(1):7-17. | |||||
REF 35 | 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. | |||||
REF 36 | Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36. | |||||
REF 37 | Effect of the acyl-CoA:cholesterol acyltransferase inhibitor, E5324, on experimental atherosclerosis in rabbits. Atherosclerosis. 1994 Jun;107(2):187-201. | |||||
REF 38 | 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. | |||||
REF 39 | 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. | |||||
REF 40 | CL 277,082: a novel inhibitor of ACAT-catalyzed cholesterol esterification and cholesterol absorption. J Lipid Res. 1989 May;30(5):681-90. | |||||
REF 41 | ACAT inhibitor F-1394 prevents intimal hyperplasia induced by balloon injury in rabbits. J Lipid Res. 2001 Apr;42(4):480-8. | |||||
REF 42 | 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. | |||||
REF 43 | 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. | |||||
REF 44 | 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. | |||||
REF 45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010079) | |||||
REF 46 | 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. | |||||
REF 47 | 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. | |||||
REF 48 | 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. | |||||
REF 49 | 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. | |||||
REF 50 | 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. | |||||
REF 51 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002876) | |||||
REF 52 | 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. | |||||
REF 53 | 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. | |||||
REF 54 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
REF 55 | 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. | |||||
REF 56 | 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. | |||||
REF 57 | 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. | |||||
REF 58 | Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils. Bioorg Med Chem. 2007 Jun 1;15(11):3801-17. | |||||
REF 59 | 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. | |||||
REF 60 | 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. | |||||
REF 61 | Selective inhibition of carboxylesterases by isatins, indole-2,3-diones. J Med Chem. 2007 Apr 19;50(8):1876-85. | |||||
REF 62 | Phenolic compounds from the roots of Lindera fruticosa. J Nat Prod. 2006 May;69(5):853-5. | |||||
REF 63 | 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. | |||||
REF 64 | DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41. | |||||
REF 65 | 2-Azetidinones as inhibitors of cholesterol absorption. J Med Chem. 1994 Jun 10;37(12):1733-6. | |||||
REF 66 | Company report (Dainippon Sumitomo Pharma) | |||||
REF 67 | Zhang JG, Fariss MW: Thenoyltrifluoroacetone, a potent inhibitor of carboxylesterase activity. Biochem Pharmacol. 2002 Feb 15;63(4):751-4. |
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