Skip to content
PsychedeliaDokholyan Laboratory
TargetUnclassified

Diacylglycerol lipase-alpha

Matched no rule. Shown as-is rather than assigned a class by guesswork. Values below are reported as measured; because this is not a molecular target, they are not treated as affinities anywhere on this site.

Measurements
17
Compounds
8
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

DGLA_HUMANDAGLAHomo sapiens

Diacylglycerol lipase-alpha

Serine hydrolase that hydrolyzes arachidonic acid-esterified diacylglycerols (DAGs) to produce the principal endocannabinoid, 2-arachidonoylglycerol (2-AG)14610053,23502535,26668358. Preferentially hydrolyzes sn-1 fatty acids from diacylglycerols (DAG) that contain arachidonic acid (AA) esterified at the sn-2 position to biosynthesize 2-AG14610053,23502535,26668358. Has negligible activity against other lipids including monoacylglycerols and phospholipids14610053. 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. Also regulates neuroinflammatory responses in the brain, in particular, LPS-induced microglial activation (By similarity)

Quoted from UniProt’s FUNCTION annotation for Q9Y4D2 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
DAGLB0.9150.0000.9000.187
FAAH0.8980.0000.0000.894
NAPEPLD0.8940.0000.0000.894
MGLL0.8870.0000.0000.884
ABHD60.8310.0000.0000.827
CNR10.8170.0000.0000.817
GRM50.8110.0000.0000.805
ABHD120.7910.0000.0000.782
ABHD40.7140.0000.0000.714
GPR550.7000.0000.0000.700

Where it sits in the cell

UniProt, curated Cell membrane · Postsynaptic density membrane · Early endosome membrane · Cell projection, dendritic spine membrane

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • brain12.3 nTPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

Brain

cerebral cortex — 12.3 nTPM, from DAGLAcerebellum — 7.8 nTPM, from DAGLAhippocampal formation — 4.3 nTPM, from DAGLAamygdala — 3.6 nTPM, from DAGLAhypothalamus — 2.9 nTPM, from DAGLAthalamus — no resolved target expressed herebasal ganglia — 4.2 nTPM, from DAGLAmedulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: pituitary gland 2.2, midbrain 1.9, spinal cord 0.7, retina 0.5.

Body

heart — 2.1 nTPM, from DAGLAsmooth muscle — 1.2 nTPM, from DAGLAlung — 1.5 nTPM, from DAGLAliver — 0.2 nTPM, from DAGLAkidney — 1.4 nTPM, from DAGLAstomach — 1.4 nTPM, from DAGLAduodenum — 2.0 nTPM, from DAGLAsmall intestine — 2.2 nTPM, from DAGLAcolon — 2.9 nTPM, from DAGLAadrenal gland — 1.0 nTPM, from DAGLAthyroid gland — 1.0 nTPM, from DAGLApancreas — 3.8 nTPM, from DAGLAurinary bladder — 0.5 nTPM, from DAGLAskeletal muscle — 2.8 nTPM, from DAGLAspleen — 1.6 nTPM, from DAGLAsalivary gland — 3.7 nTPM, from DAGLA
012 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of DAGLA transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 10

  • cerebral cortex12.3 nTPM
  • cerebellum7.8 nTPM
  • hippocampal formation4.3 nTPM
  • basal ganglia4.2 nTPM
  • amygdala3.6 nTPM
  • hypothalamus2.9 nTPM
  • pituitary gland2.2 nTPM
  • midbrain1.9 nTPM
  • spinal cord0.7 nTPM
  • retina0.5 nTPM

Peripheral and autonomic · 16

  • pancreas3.8 nTPM
  • salivary gland3.7 nTPM
  • colon2.9 nTPM
  • skeletal muscle2.8 nTPM
  • small intestine2.2 nTPM
  • heart muscle2.1 nTPM
  • duodenum2.0 nTPM
  • spleen1.6 nTPM
  • lung1.5 nTPM
  • kidney1.4 nTPM
  • stomach 11.4 nTPM
  • smooth muscle1.2 nTPM
  • adrenal gland1.0 nTPM
  • thyroid gland1.0 nTPM
  • urinary bladder0.5 nTPM
  • liver0.2 nTPM

Transcript is not protein. These are RNA levels for DAGLA, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 9

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Diacylglycerol lipase-alphaUnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424973
Diacylglycerol lipase-alphaUnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424973
Diacylglycerol lipase-alphaUnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424973
Diacylglycerol lipase-alphaUnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424973
Diacylglycerol lipase-alphaUnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424973
Diacylglycerol lipase-alphaUnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424973
Diacylglycerol lipase-alphaUnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424973
Diacylglycerol lipase-alphaUnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424973
Diacylglycerol lipase-alphaUnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5096648

Other measurements 8

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Diacylglycerol lipase-alphaUnclassifiedEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424975
Diacylglycerol lipase-alphaUnclassifiedEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424975
Diacylglycerol lipase-alphaUnclassifiedEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424975
Diacylglycerol lipase-alphaUnclassifiedEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424974
Diacylglycerol lipase-alphaUnclassifiedEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424974
Diacylglycerol lipase-alphaUnclassifiedEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424974
Diacylglycerol lipase-alphaUnclassifiedEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424974
Diacylglycerol lipase-alphaUnclassifiedEmax— no normalized value— value does not convert to pXHomo sapiensCHEMBL4424974
← All targets