General Information of the Protein
Protein ID
PT06149
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
Kiaa0659
Nsddr
Sequence
MPGIVVFRRRWSVGSDDLVLPAIFLFLLHTTWFVILSVVLFGLVYNPHEACSLNLVDHGRGYLGILLSCMIAEMAIIWLSMRGGILYTEPRDSMQYVLYVRLAILVIEFIYAIVGIVWLTQYYTSCNDLTAKNVTLGMVVCNWVVILSVCITVLCVFDPTGRTFVKLRATKRRQRNLRTYNLRHRLEEGQATSWSRRLKVFLCCTRTKDSQSDAYSEIAYLFAEFFRDLDIVPSDIIAGLVLLRQRQRAKRNAVLDEANNDILAFLSGMPVTRNTKYLDLKNSHEMLRYKEVCYYMLFALAAYGWPMYLMRKPTCGLCQLARSCSCCLCPARPRFAPGVTIEEDNCCGCNAIAIRRHFLDENMTAVDIVYTSCHDAVYETPFYVAVDHDKKKVVISIRGTLSPKDALTDLTGDAERLPVEGHRGTWLGHKGMVLSAEYIKKKLEQEMVLSQAFGRDLGRGTKHYGLIVVGHSLGAGTAAILSFLLRPQYPTLKCFAYSPPGGLLSEDAMEYSKEFVTAVVLGKDLVPRIGLSQLEGFRRQLLDVLQRSTKPKWRIIVGATKCIPKSELPEDQVEVTTLASTRLWTHPSDLTIALSASTPLYPPGRIIHVVHNHPAEQCCCCEQEEPTYFAIWGDNKAFNEVIISPAMLHEHLPYVVMEGLNKVLENYNKGKTALLSAAKVMVSPTEVDLTPELIFQQQPLPTGPPLPTGLALELPATEHRNSSVRSKSQSEMSLEGFSEGRLLSPVAAASAARQDPVELLLLSTQERLAAELQSRRAPLATMESLSDTESLYSFDSRRSSGFRSIRGSPSLHAVLERDEGHLFYIDPAIPEENPSLSSRTELLAADSLSKHSQDTQPLEAALGSGGVTPERPPSATIEEEEAAGGSEGGGVAPRGELALHNGRLGDSPSPQVLEFAEFIDSLFNLDSKSSSFQDLYCMMVPESPTSDYTEGPKSPSQQEILLRAQFEPNLVPKPPRLFAGSAEPSSGISLSPSFPLSSSGELMDLTPTGLSSQECLATDKIRTSTPTGHGASPTKQDDLVISAR
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Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Hydrolase
Function
Serine hydrolase that hydrolyzes arachidonic acid-esterified diacylglycerols (DAGs) to produce the principal endocannabinoid (eCB), 2-arachidonoylglycerol (2-AG) (PubMed:17584991, PubMed:23103940). Preferentially hydrolyzes sn-1 fatty acids from diacylglycerols (DAG) that contain arachidonic acid (AA) esterified at the sn-2 position to biosynthesize 2-AG. Has negligible activity against other lipids including monoacylglycerols and phospholipids (PubMed:17584991). Plays a key role in regulating 2-AG signaling in the central nervous system (CNS) (PubMed:20159446, PubMed:20147530, PubMed:25466252, PubMed:26668358, PubMed:26779719). Controls the activity of 2-AG as a retrograde messenger at neuronal synapses (PubMed:20159446, PubMed:20147530, PubMed:26668358). Supports axonal growth during development and adult neurogenesis (PubMed:20147530). Plays a role for eCB signaling in the physiological regulation of anxiety and depressive behaviors (PubMed:25466252). Regulates also neuroinflammatory responses in the brain, in particular, LPS-induced microglial activation (PubMed:26779719).
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Uniprot ID
Primary ID:
Q6WQJ1

Secondarily ID:
A8WFL4
Q6ZQ76
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Ensembl ID
ENSG00000134780
Subcellular Location
Cell membrane
Cell projection
Dendritic spine membrane
Postsynaptic density membrane
Early endosome 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: CL000025 , HEK-293T
Compound ID Compound Name Compound Formula
CP0110020
(2-benzylpiperidin-1-yl)-[4-(4-phenylphenyl)triazol-1-yl]methanone
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C27H26N4O
 2
1
IC50 < 1 nM
   TI
   LI
   LO
   TS
2
Ki = 0.35 nM
   TI
   LI
   LO
   TS
CP0302766
[(2R,5R)-2-benzyl-5-prop-2-ynoxypiperidin-1-yl]-[4-[bis(4-fluorophenyl)-hydroxymethyl]triazol-2-yl]methanone
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C31H28F2N4O3
 2
1
IC50 < 1 nM
   TI
   LI
   LO
   TS
2
Ki = 0.27 nM
   TI
   LI
   LO
   TS
CP0437875
1-[6-(4-methylphenyl)-[1,3]oxazolo[4,5-b]pyridin-2-yl]-6-phenylhexan-1-one
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C25H24N2O2
 2
1
IC50 = 2.512 nM
   TI
   LI
   LO
   TS
2
Ki = 0.23 nM
   TI
   LI
   LO
   TS
CP0508076
[(2R)-2-benzylpiperidin-1-yl]-[4-[bis(4-fluorophenyl)-hydroxymethyl]triazol-2-yl]methanone
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C28H26F2N4O2
 2
1
IC50 = 3.02 nM
   TI
   LI
   LO
   TS
2
Ki = 10.4 nM
   TI
   LI
   LO
   TS
CP0533202
[(2R)-2-benzylpiperidin-1-yl]-[4-[bis(4-fluorophenyl)-hydroxymethyl]triazol-1-yl]methanone
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C28H26F2N4O2
 2
1
IC50 = 3.802 nM
   TI
   LI
   LO
   TS
2
Ki = 339 nM
   TI
   LI
   LO
   TS
CP0518330
[(2R)-2-benzylpiperidin-1-yl]-[4-[bis(4-fluorophenyl)-hydroxymethyl]imidazol-1-yl]methanone
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C29H27F2N3O2
 1
1
IC50 > 31622.78 nM
   TI
   LI
   LO
   TS
CP0492195
[(2R)-2-benzylpiperidin-1-yl]-[3-[bis(4-fluorophenyl)-hydroxymethyl]pyrazol-1-yl]methanone
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C29H27F2N3O2
 1
1
Ki = 10800 nM
   TI
   LI
   LO
   TS
CP0494009
[(2R)-2-benzylpiperidin-1-yl]-[3-[bis(4-fluorophenyl)-hydroxymethyl]-1,2,4-triazol-1-yl]methanone
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C28H26F2N4O2
 1
1
Ki = 13770 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT04933 Diacylglycerol lipase-alpha Homo sapiens, Human