General Information of the Protein
Protein ID
PT01891
Protein Name
Hormone-sensitive lipase
Secondarily
Protein Name
Monoacylglycerol lipase LIPE
Retinyl ester hydrolase
Gene Name
LIPE
Sequence
MEPGSKSVSRSDWQPEPHQRPITPLEPGPEKTPIAQPESKTLQGSNTQQKPASNQRPLTQQETPAQHDAESQKEPRAQQKSASQEEFLAPQKPAPQQSPYIQRVLLTQQEAASQQGPGLGKESITQQEPALRQRHVAQPGPGPGEPPPAQQEAESTPAAQAKPGAKREPSAPTESTSQETPEQSDKQTTPVQGAKSKQGSLTELGFLTKLQELSIQRSALEWKALSEWVTDSESESDVGSSSDTDSPATMGGMVAQGVKLGFKGKSGYKVMSGYSGTSPHEKTSARNHRHYQDTASRLIHNMDLRTMTQSLVTLAEDNIAFFSSQGPGETAQRLSGVFAGVREQALGLEPALGRLLGVAHLFDLDPETPANGYRSLVHTARCCLAHLLHKSRYVASNRRSIFFRTSHNLAELEAYLAALTQLRALVYYAQRLLVTNRPGVLFFEGDEGLTADFLREYVTLHKGCFYGRCLGFQFTPAIRPFLQTISIGLVSFGEHYKRNETGLSVAASSLFTSGRFAIDPELRGAEFERITQNLDVHFWKAFWNITEMEVLSSLANMASATVRVSRLLSLPPEAFEMPLTADPTLTVTISPPLAHTGPGPVLVRLISYDLREGQDSEELSSLIKSNGQRSLELWPRPQQAPRSRSLIVHFHGGGFVAQTSRSHEPYLKSWAQELGAPIISIDYSLAPEAPFPRALEECFFAYCWAIKHCALLGSTGERICLAGDSAGGNLCFTVALRAAAYGVRVPDGIMAAYPATMLQPAASPSRLLSLMDPLLPLSVLSKCVSAYAGAKTEDHSNSDQKALGMMGLVRRDTALLLRDFRLGASSWLNSFLELSGRKSQKMSEPIAEPMRRSVSEAALAQPQGPLGTDSLKNLTLRDLSLRGNSETSSDTPEMSLSAETLSPSTPSDVNFLLPPEDAGEEAEAKNELSPMDRGLGVRAAFPEGFHPRRSSQGATQMPLYSSPIVKNPFMSPLLAPDSMLKSLPPVHIVACALDPMLDDSVMLARRLRNLGQPVTLRVVEDLPHGFLTLAALCRETRQAAELCVERIRLVLTPPAGAGPSGETGAAGVDGGCGGRH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Hydrolase
Function
Lipase with broad substrate specificity, catalyzing the hydrolysis of triacylglycerols (TAGs), diacylglycerols (DAGs), monoacylglycerols (MAGs), cholesteryl esters and retinyl esters (PubMed:8812477, PubMed:15955102, PubMed:15716583, PubMed:19800417). Shows a preferential hydrolysis of DAGs over TAGs and MAGs and preferentially hydrolyzes the fatty acid (FA) esters at the sn-3 position of the glycerol backbone in DAGs (PubMed:19800417). Preferentially hydrolyzes FA esters at the sn-1 and sn-2 positions of the glycerol backbone in TAGs (By similarity). Catalyzes the hydrolysis of 2-arachidonoylglycerol, an endocannabinoid and of 2-acetyl monoalkylglycerol ether, the penultimate precursor of the pathway for de novo synthesis of platelet-activating factor (By similarity). In adipose tissue and heart, it primarily hydrolyzes stored triglycerides to free fatty acids, while in steroidogenic tissues, it principally converts cholesteryl esters to free cholesterol for steroid hormone production (By similarity).
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Uniprot ID
Primary ID:
Q05469

Secondarily ID:
Q3LRT2
Q6NSL7
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Ensembl ID
ENSG00000079435
HGNC ID
HGNC:6621
Subcellular Location
Cell membrane
Membrane
Caveola
Cytoplasm
Cytosol
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: CL000384 , 3T3-L1
Compound ID Compound Name Compound Formula
CP0366445
2-(4-(3-fluorophenyl)piperidine-1-carbonyl)-4-(2-methoxyethyl)-3-methylisoxazol-5(2H)-one
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C19H23FN2O4
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0089605
3-Methyl-4-(2-phenoxy-ethyl)-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C18H22N2O4
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0130731
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid methyl-thiophen-2-ylmethyl-amide
   Show/Hide
C14H18N2O3S
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0053132
4-(2-Methoxy-ethyl)-3-methyl-2-(4-m-tolyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C20H26N2O4
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0162696
2-(4-(3-fluorophenyl)piperidine-1-carbonyl)-4-isopropyl-3-methylisoxazol-5(2H)-one
   Show/Hide
C19H23FN2O3
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0347863
4-Isobutyl-3-methyl-2-(4-phenyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C20H26N2O3
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0362689
4-(2-Methoxy-ethyl)-3-methyl-2-(4-phenyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C19H24N2O4
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0164003
4-Cyclopentyl-3-methyl-2-(4-phenyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
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C21H26N2O3
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0276954
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid furan-2-ylmethyl-methyl-amide
   Show/Hide
C14H18N2O4
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0163555
4-Butyl-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C15H24N2O3
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0360894
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid (2-fluoro-benzyl)-methyl-amide
   Show/Hide
C16H19FN2O3
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0173036
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid (3-fluoro-benzyl)-methyl-amide
   Show/Hide
C16H19FN2O3
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0361036
4-Isopropyl-2-[4-(3-methoxy-phenyl)-piperazine-1-carbonyl]-3-methyl-2H-isoxazol-5-one
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C19H25N3O4
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0052461
4-Isobutyl-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
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C15H24N2O3
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0103269
4-(2-Ethoxy-ethyl)-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C15H24N2O4
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0171544
4-Cyclohexyl-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C17H26N2O3
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0288317
4-Cyclopentyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
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C15H22N2O3
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0119105
3-Methyl-2-(4-methyl-piperidine-1-carbonyl)-4-(tetrahydro-thiopyran-4-yl)-2H-isoxazol-5-one
   Show/Hide
C16H24N2O3S
 1
1
IC50 = 24 nM
   TI
   LI
   LO
   TS
CP0279609
4-Isopropyl-3-methyl-2-(4-phenyl-piperazine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C18H23N3O3
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0362688
4-Cyclohexyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H24N2O3
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0095675
(S)-4-isopropyl-3-methyl-2-(3-methylpiperidine-1-carbonyl)isoxazol-5(2H)-one
   Show/Hide
C14H22N2O3
 1
1
IC50 = 28 nM
   TI
   LI
   LO
   TS
CP0182153
4-Isopropyl-3-methyl-2-(pyrrolidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C12H18N2O3
 1
1
IC50 = 28 nM
   TI
   LI
   LO
   TS
CP0065171
2-(1-(2-chlorophenyl)piperazine-4-carbonyl)-4-isopropyl-3-methylisoxazol-5(2H)-one
   Show/Hide
C18H22ClN3O3
 1
1
IC50 = 31 nM
   TI
   LI
   LO
   TS
CP0193921
4-Isobutyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0245889
4-Isopropyl-3-methyl-2-(4-phenyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C19H24N2O3
 1
1
IC50 = 33 nM
   TI
   LI
   LO
   TS
CP0216362
4-Isopropyl-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0276941
2-(3,3-Dimethyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C15H24N2O3
 1
1
IC50 = 48 nM
   TI
   LI
   LO
   TS
CP0292336
1-(4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carbonyl)-piperidine-4-carboxylic acid ethyl ester
   Show/Hide
C16H24N2O5
 1
1
IC50 = 49 nM
   TI
   LI
   LO
   TS
CP0299703
4-Isopropyl-3-methyl-2-(4-pyrimidin-2-yl-piperazine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H21N5O3
 1
1
IC50 = 51 nM
   TI
   LI
   LO
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CP0367679
2-(1-benzylpiperazine-4-carbonyl)-4-isopropyl-3-methylisoxazol-5(2H)-one
   Show/Hide
C19H25N3O3
 1
1
IC50 = 56 nM
   TI
   LI
   LO
   TS
CP0340097
4-Butyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1
IC50 = 61 nM
   TI
   LI
   LO
   TS
CP0358401
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid benzyl-methyl-amide
   Show/Hide
C16H20N2O3
 1
1
IC50 = 67 nM
   TI
   LI
   LO
   TS
CP0293366
4-Isopropyl-3-methyl-2-[4-(4-methyl-3H-isoxazol-2-yl)-piperidine-1-carbonyl]-2H-isoxazol-5-one
   Show/Hide
C17H25N3O4
 1
1
IC50 = 73 nM
   TI
   LI
   LO
   TS
CP0511592
4-Isopropyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
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C13H20N2O3
 1
1
IC50 = 75 nM
   TI
   LI
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CP0110236
4-tert-Butyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1
IC50 = 90 nM
   TI
   LI
   LO
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CP0358378
4-Benzyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
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C17H20N2O3
 1
1
IC50 = 90 nM
   TI
   LI
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CP0340099
3-Methyl-2-(piperidine-1-carbonyl)-4-(tetrahydro-thiopyran-4-yl)-2H-isoxazol-5-one
   Show/Hide
C15H22N2O3S
 1
1
IC50 = 98 nM
   TI
   LI
   LO
   TS
CP0089489
2-(2,5-Dihydro-pyrrole-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C12H16N2O3
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0081303
4-(4-Chloro-phenylsulfanyl)-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H17ClN2O3S
 1
1
IC50 = 135 nM
   TI
   LI
   LO
   TS
CP0079352
2-(3,5-Dimethyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C15H24N2O3
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0347455
1-(4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carbonyl)-piperidin-4-one
   Show/Hide
C13H18N2O4
 1
1
IC50 = 150 nM
   TI
   LI
   LO
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CP0502190
3-Methyl-4-phenyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H18N2O3
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0326474
1-(4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carbonyl)-piperidine-3-carboxylic acid ethyl ester
   Show/Hide
C16H24N2O5
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0221894
4-{[(1H-Indol-2-yl)-methyl-amino]-methyl}-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C20H24N4O3
 1
1
IC50 = 177 nM
   TI
   LI
   LO
   TS
CP0044486
4-(2-Methoxy-ethyl)-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C13H20N2O4
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0536670
(R)-4-isopropyl-3-methyl-2-(3-methylpiperidine-1-carbonyl)isoxazol-5(2H)-one
   Show/Hide
C14H22N2O3
 1
1
IC50 = 187 nM
   TI
   LI
   LO
   TS
CP0222002
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid methyl-phenyl-amide
   Show/Hide
C15H18N2O3
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0289076
3-Methyl-4-phenylsulfanyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H18N2O3S
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0055468
3-Methyl-2-(piperidine-1-carbonyl)-4-(tetrahydro-pyran-4-yl)-2H-isoxazol-5-one
   Show/Hide
C15H22N2O4
 1
1
IC50 = 200 nM
   TI
   LI
   LO
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CP0367680
2-(Azepane-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1
IC50 = 215 nM
   TI
   LI
   LO
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CP0184100
4-Isopropyl-3-methyl-2-(4-p-tolyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C20H26N2O3
 1
1
IC50 = 246 nM
   TI
   LI
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CP0153162
4-Isopropyl-3-methyl-2-(thiomorpholine-4-carbonyl)-2H-isoxazol-5-one
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C12H18N2O3S
 1
1
IC50 = 290 nM
   TI
   LI
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CP0221895
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid methyl-phenethyl-amide
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C17H22N2O3
 1
1
IC50 = 300 nM
   TI
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CP0348095
4-Ethyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C12H18N2O3
 1
1
IC50 = 325 nM
   TI
   LI
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CP0216352
4-(1,1-Dioxo-hexahydro-1lambda*6*-thiopyran-4-yl)-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C15H22N2O5S
 1
1
IC50 = 380 nM
   TI
   LI
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CP0216357
4-Isopropyl-3-methyl-2-(2-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1
IC50 = 400 nM
   TI
   LI
   LO
   TS
CP0361037
2-(4-Hydroxy-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C13H20N2O4
 1
1
IC50 = 450 nM
   TI
   LI
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CP0347861
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid diethylamide
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C12H20N2O3
 1
1
IC50 = 600 nM
   TI
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CP0038386
3,4-Dimethyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
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C11H16N2O3
 1
1
IC50 = 655 nM
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CP0360691
2-(3-(hydroxymethyl)piperidine-1-carbonyl)-4-isopropyl-3-methylisoxazol-5(2H)-one
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C14H22N2O4
 1
1
IC50 = 800 nM
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   LI
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CP0222001
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid (4-fluoro-benzyl)-methyl-amide
   Show/Hide
C16H19FN2O3
 1
1
IC50 = 1000 nM
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CP0288331
4-(4-Chloro-benzenesulfonyl)-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
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C16H17ClN2O5S
 1
1
IC50 = 1270 nM
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CP0044487
2-(4-Hydroxy-4-phenyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C19H24N2O4
 1
1
IC50 > 1000 nM
   TI
   LI
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CP0052421
4-Isopropyl-3-methyl-2-(morpholine-4-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C12H18N2O4
 1
1
IC50 > 1000 nM
   TI
   LI
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CP0097397
2-(3,4-Dihydro-2H-quinoline-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C17H20N2O3
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
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CP0160252
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid methyl-(4-methyl-benzyl)-amide
   Show/Hide
C17H22N2O3
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0171038
2-(4-Benzoyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C20H24N2O4
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0173065
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid benzyl-methyl-amide
   Show/Hide
C15H24N2O3
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0221896
2-(4-Benzyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C20H26N2O3
 1
1
IC50 > 1000 nM
   TI
   LI
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   TS
CP0268866
4-Isopropyl-3-methyl-2-(4-methyl-piperazine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C13H21N3O3
 1
1
IC50 > 1000 nM
   TI
   LI
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CP0310964
2-(2,5-Dimethyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C15H24N2O3
 1
1
IC50 > 1000 nM
   TI
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CP0363775
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid (4-chloro-phenyl)-methyl-amide
   Show/Hide
C15H17ClN2O3
 1
1
IC50 > 1000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0163555
4-Butyl-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C15H24N2O3
 1
1 IC50 = 1 nM
CP0361036
4-Isopropyl-2-[4-(3-methoxy-phenyl)-piperazine-1-carbonyl]-3-methyl-2H-isoxazol-5-one
   Show/Hide
C19H25N3O4
 1
1 IC50 = 1 nM
CP0130731
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid methyl-thiophen-2-ylmethyl-amide
   Show/Hide
C14H18N2O3S
 1
1 IC50 = 2 nM
CP0511592
4-Isopropyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C13H20N2O3
 1
1 IC50 = 2 nM
CP0052461
4-Isobutyl-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C15H24N2O3
 1
1 IC50 = 3 nM
CP0095675
(S)-4-isopropyl-3-methyl-2-(3-methylpiperidine-1-carbonyl)isoxazol-5(2H)-one
   Show/Hide
C14H22N2O3
 2
1 IC50 = 3 nM
2 IC50 = 170 nM
CP0103269
4-(2-Ethoxy-ethyl)-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C15H24N2O4
 1
1 IC50 = 3 nM
CP0089605
3-Methyl-4-(2-phenoxy-ethyl)-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C18H22N2O4
 1
1 IC50 = 4 nM
CP0171544
4-Cyclohexyl-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C17H26N2O3
 1
1 IC50 = 4 nM
CP0276954
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid furan-2-ylmethyl-methyl-amide
   Show/Hide
C14H18N2O4
 1
1 IC50 = 4 nM
CP0360894
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid (2-fluoro-benzyl)-methyl-amide
   Show/Hide
C16H19FN2O3
 1
1 IC50 = 4 nM
CP0173036
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid (3-fluoro-benzyl)-methyl-amide
   Show/Hide
C16H19FN2O3
 1
1 IC50 = 5 nM
CP0193921
4-Isobutyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1 IC50 = 5 nM
CP0358378
4-Benzyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C17H20N2O3
 1
1 IC50 = 5 nM
CP0358401
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid benzyl-methyl-amide
   Show/Hide
C16H20N2O3
 1
1 IC50 = 5 nM
CP0081303
4-(4-Chloro-phenylsulfanyl)-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H17ClN2O3S
 1
1 IC50 = 6 nM
CP0119105
3-Methyl-2-(4-methyl-piperidine-1-carbonyl)-4-(tetrahydro-thiopyran-4-yl)-2H-isoxazol-5-one
   Show/Hide
C16H24N2O3S
 1
1 IC50 = 6 nM
CP0216362
4-Isopropyl-3-methyl-2-(4-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1 IC50 = 6 nM
CP0279609
4-Isopropyl-3-methyl-2-(4-phenyl-piperazine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C18H23N3O3
 1
1 IC50 = 6 nM
CP0288317
4-Cyclopentyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C15H22N2O3
 1
1 IC50 = 6 nM
CP0289076
3-Methyl-4-phenylsulfanyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H18N2O3S
 1
1 IC50 = 6 nM
CP0292336
1-(4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carbonyl)-piperidine-4-carboxylic acid ethyl ester
   Show/Hide
C16H24N2O5
 1
1 IC50 = 6 nM
CP0222002
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid methyl-phenyl-amide
   Show/Hide
C15H18N2O3
 1
1 IC50 = 7 nM
CP0276941
2-(3,3-Dimethyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C15H24N2O3
 1
1 IC50 = 7 nM
CP0340097
4-Butyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1 IC50 = 7 nM
CP0153162
4-Isopropyl-3-methyl-2-(thiomorpholine-4-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C12H18N2O3S
 1
1 IC50 = 8 nM
CP0173065
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid benzyl-methyl-amide
   Show/Hide
C15H24N2O3
 1
1 IC50 = 9 nM
CP0044486
4-(2-Methoxy-ethyl)-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C13H20N2O4
 1
1 IC50 = 10 nM
CP0347863
4-Isobutyl-3-methyl-2-(4-phenyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C20H26N2O3
 1
1 IC50 = 10 nM
CP0340099
3-Methyl-2-(piperidine-1-carbonyl)-4-(tetrahydro-thiopyran-4-yl)-2H-isoxazol-5-one
   Show/Hide
C15H22N2O3S
 1
1 IC50 = 11 nM
CP0362688
4-Cyclohexyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H24N2O3
 1
1 IC50 = 11 nM
CP0362689
4-(2-Methoxy-ethyl)-3-methyl-2-(4-phenyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C19H24N2O4
 1
1 IC50 = 11 nM
CP0162696
2-(4-(3-fluorophenyl)piperidine-1-carbonyl)-4-isopropyl-3-methylisoxazol-5(2H)-one
   Show/Hide
C19H23FN2O3
 1
1 IC50 = 12 nM
CP0245889
4-Isopropyl-3-methyl-2-(4-phenyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C19H24N2O3
 1
1 IC50 = 12 nM
CP0038386
3,4-Dimethyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C11H16N2O3
 1
1 IC50 = 13 nM
CP0110236
4-tert-Butyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1 IC50 = 14 nM
CP0502190
3-Methyl-4-phenyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H18N2O3
 1
1 IC50 = 14 nM
CP0182153
4-Isopropyl-3-methyl-2-(pyrrolidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C12H18N2O3
 1
1 IC50 = 15 nM
CP0221894
4-{[(1H-Indol-2-yl)-methyl-amino]-methyl}-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C20H24N4O3
 1
1 IC50 = 17 nM
CP0363775
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid (4-chloro-phenyl)-methyl-amide
   Show/Hide
C15H17ClN2O3
 1
1 IC50 = 17 nM
CP0348095
4-Ethyl-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C12H18N2O3
 1
1 IC50 = 18 nM
CP0366445
2-(4-(3-fluorophenyl)piperidine-1-carbonyl)-4-(2-methoxyethyl)-3-methylisoxazol-5(2H)-one
   Show/Hide
C19H23FN2O4
 1
1 IC50 = 20 nM
CP0536670
(R)-4-isopropyl-3-methyl-2-(3-methylpiperidine-1-carbonyl)isoxazol-5(2H)-one
   Show/Hide
C14H22N2O3
 1
1 IC50 = 20 nM
CP0053132
4-(2-Methoxy-ethyl)-3-methyl-2-(4-m-tolyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C20H26N2O4
 1
1 IC50 = 23 nM
CP0164003
4-Cyclopentyl-3-methyl-2-(4-phenyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C21H26N2O3
 1
1 IC50 = 24 nM
CP0293366
4-Isopropyl-3-methyl-2-[4-(4-methyl-3H-isoxazol-2-yl)-piperidine-1-carbonyl]-2H-isoxazol-5-one
   Show/Hide
C17H25N3O4
 1
1 IC50 = 28 nM
CP0326474
1-(4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carbonyl)-piperidine-3-carboxylic acid ethyl ester
   Show/Hide
C16H24N2O5
 1
1 IC50 = 28 nM
CP0065171
2-(1-(2-chlorophenyl)piperazine-4-carbonyl)-4-isopropyl-3-methylisoxazol-5(2H)-one
   Show/Hide
C18H22ClN3O3
 1
1 IC50 = 30 nM
CP0288331
4-(4-Chloro-benzenesulfonyl)-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H17ClN2O5S
 1
1 IC50 = 35 nM
CP0184100
4-Isopropyl-3-methyl-2-(4-p-tolyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C20H26N2O3
 1
1 IC50 = 37 nM
CP0052421
4-Isopropyl-3-methyl-2-(morpholine-4-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C12H18N2O4
 1
1 IC50 = 52 nM
CP0216352
4-(1,1-Dioxo-hexahydro-1lambda*6*-thiopyran-4-yl)-3-methyl-2-(piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C15H22N2O5S
 1
1 IC50 = 55 nM
CP0097397
2-(3,4-Dihydro-2H-quinoline-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C17H20N2O3
 1
1 IC50 = 60 nM
CP0367680
2-(Azepane-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1 IC50 = 62 nM
CP0367679
2-(1-benzylpiperazine-4-carbonyl)-4-isopropyl-3-methylisoxazol-5(2H)-one
   Show/Hide
C19H25N3O3
 1
1 IC50 = 65 nM
CP0299703
4-Isopropyl-3-methyl-2-(4-pyrimidin-2-yl-piperazine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C16H21N5O3
 1
1 IC50 = 67 nM
CP0055468
3-Methyl-2-(piperidine-1-carbonyl)-4-(tetrahydro-pyran-4-yl)-2H-isoxazol-5-one
   Show/Hide
C15H22N2O4
 1
1 IC50 = 71 nM
CP0089489
2-(2,5-Dihydro-pyrrole-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C12H16N2O3
 1
1 IC50 = 72 nM
CP0216357
4-Isopropyl-3-methyl-2-(2-methyl-piperidine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C14H22N2O3
 1
1 IC50 = 93 nM
CP0221896
2-(4-Benzyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C20H26N2O3
 1
1 IC50 = 102 nM
CP0222001
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid (4-fluoro-benzyl)-methyl-amide
   Show/Hide
C16H19FN2O3
 1
1 IC50 = 111 nM
CP0361037
2-(4-Hydroxy-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C13H20N2O4
 1
1 IC50 = 166 nM
CP0221895
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid methyl-phenethyl-amide
   Show/Hide
C17H22N2O3
 1
1 IC50 = 180 nM
CP0360691
2-(3-(hydroxymethyl)piperidine-1-carbonyl)-4-isopropyl-3-methylisoxazol-5(2H)-one
   Show/Hide
C14H22N2O4
 1
1 IC50 = 180 nM
CP0347455
1-(4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carbonyl)-piperidin-4-one
   Show/Hide
C13H18N2O4
 1
1 IC50 = 200 nM
CP0171038
2-(4-Benzoyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C20H24N2O4
 1
1 IC50 = 250 nM
CP0268866
4-Isopropyl-3-methyl-2-(4-methyl-piperazine-1-carbonyl)-2H-isoxazol-5-one
   Show/Hide
C13H21N3O3
 1
1 IC50 = 314 nM
CP0079352
2-(3,5-Dimethyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C15H24N2O3
 1
1 IC50 = 326 nM
CP0160252
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid methyl-(4-methyl-benzyl)-amide
   Show/Hide
C17H22N2O3
 1
1 IC50 = 408 nM
CP0310964
2-(2,5-Dimethyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C15H24N2O3
 1
1 IC50 = 460 nM
CP0167187
4-hydroxy-piperidine-1-carboxylic acid 4-(5-trifluoromethylpyridin-2-yloxy)-phenyl ester
   Show/Hide
C18H17F3N2O4
 1
1 IC50 = 500 nM
CP0347861
4-Isopropyl-3-methyl-5-oxo-5H-isoxazole-2-carboxylic acid diethylamide
   Show/Hide
C12H20N2O3
 1
1 IC50 = 1400 nM
CP0044487
2-(4-Hydroxy-4-phenyl-piperidine-1-carbonyl)-4-isopropyl-3-methyl-2H-isoxazol-5-one
   Show/Hide
C19H24N2O4
 1
1 IC50 > 1000 nM
Clinical Information about the Protein
Target 1 ( Hormone sensitive lipase (LIPE) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Infestations of lice and scabies [ICD-11: 1G00.Z]
2 Pancreatitis [ICD-11: DC31-DC34]
Approved Drug(s) 1 Approved Drug  1
1 BENZYL BENZOATE Approved
Infestations of lice and scabies
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PMID15026062C41 Clinical trial
Pancreatitis