General Information of the Protein
Protein ID
PT04933
Protein Name
Diacylglycerol lipase-alpha
Secondarily
Protein Name
Neural stem cell-derived dendrite regulator
Sn1-specific diacylglycerol lipase alpha
Gene Name
DAGLA
Secondarily
Gene Name
C11orf11
KIAA0659
NSDDR
Sequence
MPGIVVFRRRWSVGSDDLVLPAIFLFLLHTTWFVILSVVLFGLVYNPHEACSLNLVDHGRGYLGILLSCMIAEMAIIWLSMRGGILYTEPRDSMQYVLYVRLAILVIEFIYAIVGIVWLTQYYTSCNDLTAKNVTLGMVVCNWVVILSVCITVLCVFDPTGRTFVKLRATKRRQRNLRTYNLRHRLEEGQATSWSRRLKVFLCCTRTKDSQSDAYSEIAYLFAEFFRDLDIVPSDIIAGLVLLRQRQRAKRNAVLDEANNDILAFLSGMPVTRNTKYLDLKNSQEMLRYKEVCYYMLFALAAYGWPMYLMRKPACGLCQLARSCSCCLCPARPRFAPGVTIEEDNCCGCNAIAIRRHFLDENMTAVDIVYTSCHDAVYETPFYVAVDHDKKKVVISIRGTLSPKDALTDLTGDAERLPVEGHHGTWLGHKGMVLSAEYIKKKLEQEMVLSQAFGRDLGRGTKHYGLIVVGHSLGAGTAAILSFLLRPQYPTLKCFAYSPPGGLLSEDAMEYSKEFVTAVVLGKDLVPRIGLSQLEGFRRQLLDVLQRSTKPKWRIIVGATKCIPKSELPEEVEVTTLASTRLWTHPSDLTIALSASTPLYPPGRIIHVVHNHPAEQCCCCEQEEPTYFAIWGDNKAFNEVIISPAMLHEHLPYVVMEGLNKVLENYNKGKTALLSAAKVMVSPTEVDLTPELIFQQQPLPTGPPMPTGLALELPTADHRNSSVRSKSQSEMSLEGFSEGRLLSPVVAAAARQDPVELLLLSTQERLAAELQARRAPLATMESLSDTESLYSFDSRRSSGFRSIRGSPSLHAVLERDEGHLFYIDPAIPEENPSLSSRTELLAADSLSKHSQDTQPLEAALGSGGVTPERPPSAAANDEEEEVGGGGGGPASRGELALHNGRLGDSPSPQVLEFAEFIDSLFNLDSKSSSFQDLYCMVVPESPTSDYAEGPKSPSQQEILLRAQFEPNLVPKPPRLFAGSADPSSGISLSPSFPLSSSGELMDLTPTGLSSQECLAADKIRTSTPTGHGASPAKQDELVISAR
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Hydrolase
Function
Serine hydrolase that hydrolyzes arachidonic acid-esterified diacylglycerols (DAGs) to produce the principal endocannabinoid, 2-arachidonoylglycerol (2-AG) (PubMed:14610053, PubMed:26668358, PubMed:23502535). Preferentially hydrolyzes sn-1 fatty acids from diacylglycerols (DAG) that contain arachidonic acid (AA) esterified at the sn-2 position to biosynthesize 2-AG (PubMed:14610053, PubMed:26668358, PubMed:23502535). Has negligible activity against other lipids including monoacylglycerols and phospholipids (PubMed:14610053). Plays a key role in regulating 2-AG signaling in the central nervous system (CNS). Regulates 2-AG involved in retrograde suppression at central synapses. Supports axonal growth during development and adult neurogenesis. Plays a role for eCB signaling in the physiological regulation of anxiety and depressive behaviors. Regulates also neuroinflammatory responses in the brain, in particular, LPS-induced microglial activation (By similarity).
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Uniprot ID
Primary ID:
Q9Y4D2

Secondarily ID:
A0A024R517
A7E233
Q6WQJ0
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Ensembl ID
ENSG00000134780
HGNC ID
HGNC:1165
Subcellular Location
Cell membrane
Postsynaptic density membrane
Early endosome membrane
Cell projection
Dendritic spine membrane
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: CL000053 , COS-7
Compound ID Compound Name Compound Formula
CP0423365
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-formamido-3-methylpentanoate
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C29H53NO5
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0439729
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-formamido-3-methylbutanoate
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C28H51NO5
 1
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
CP0485042
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-formamidopropanoate
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C26H47NO5
 1
1
IC50 = 43 nM
   TI
   LI
   LO
   TS
CP0433844
5-oxo-L-Proline-(1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl Ester
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C27H47NO5
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0511846
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-acetamido-3-methylpentanoate
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C30H55NO5
 1
1
IC50 = 430 nM
   TI
   LI
   LO
   TS
CP0506288
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-acetamido-3-methylbutanoate
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C29H53NO5
 1
1
IC50 = 460 nM
   TI
   LI
   LO
   TS
CP0465926
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] 3-formamidopropanoate
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C26H47NO5
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0423366
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] 2-acetamidoacetate
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C26H47NO5
 1
1
IC50 = 800 nM
   TI
   LI
   LO
   TS
CP0489860
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-1-formylpyrrolidine-2-carboxylate
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C28H49NO5
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0485066
(1R)-1-{[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]methyl}dodecyl N-formylglycinate
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C25H45NO5
 1
1
IC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0135864
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2R)-2-formamido-4-methylpentanoate
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C29H53NO5
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0423377
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-amino-4-methylpentanoate
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C28H53NO4
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0423378
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-3-phenyl-2-(phenylmethoxycarbonylamino)propanoate
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C39H57NO6
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0439254
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-formamido-3-phenylpropanoate
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C32H51NO5
 1
1
IC50 = 25000 nM
   TI
   LI
   LO
   TS
CP0439255
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] 2-(phenylmethoxycarbonylamino)acetate
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C32H51NO6
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0439730
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-4-methyl-2-[(2-methylpropan-2-yl)oxycarbonylamino]pentanoate
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C33H61NO6
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0465929
(3S,4S)-3-Hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one
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C22H42O3
 1
1
IC50 = 25000 nM
   TI
   LI
   LO
   TS
CP0465931
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-4-methyl-2-(phenylmethoxycarbonylamino)pentanoate
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C36H59NO6
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0465932
4-Methylpentanoic Acid (1S)-1-[[(2S,3S-3-Hexyl-4-oxo-2-oxetanyl]methyl]dodecyl Ester
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C28H52O4
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0485044
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2R)-4-methyl-2-(phenylmethoxycarbonylamino)pentanoate
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C36H59NO6
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0500741
[(2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl] (2S)-2-amino-3-phenylpropanoate
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C31H51NO4
 1
1
IC50 = 25000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0437875
1-[6-(4-methylphenyl)-[1,3]oxazolo[4,5-b]pyridin-2-yl]-6-phenylhexan-1-one
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C25H24N2O2
 1
1 IC50 = 12.59 nM
CP0191477
2-[(2,2-dimethyl-3,4-dihydrochromen-6-yl)sulfonyl-[(4-phenoxyphenyl)methyl]amino]acetic acid
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C26H27NO6S
 1
1 IC50 = 18 nM
CP0316088
(cyclohexylideneamino) N-[6-[(cyclohexylideneamino)oxycarbonylamino]hexyl]carbamate
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C20H34N4O4
 1
1 IC50 = 65000 nM
Clinical Information about the Protein
Target 1 ( Diacylglycerol lipase alpha (DAGLA) )
Target Type Patented-recorded Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06149 Diacylglycerol lipase-alpha Mus musculus, Mouse