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PsychedeliaDokholyan Laboratory
TargetAdenosine receptors

Adenosine receptor A2a

A1, A2A, A2B, A3.

Measurements
27
Compounds
14
Binding constants
8
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

AA2AR_HUMANADORA2AHomo sapiens

Adenosine receptor A2a

Receptor for adenosine (By similarity). The activity of this receptor is mediated by G proteins which activate adenylyl cyclase (By similarity)

Quoted from UniProt’s FUNCTION annotation for P29274 (reviewed).

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
DRD20.9970.8060.0000.987
GNAS0.9950.9260.9000.395
GRM50.9760.3000.0000.968
GNAQ0.9590.1150.9000.578
CNR10.9560.6340.0000.884
GNAL0.9490.2970.9000.337
NTRK20.9400.0000.7000.809
ADORA2B0.9370.3250.9000.153
GNB10.9280.9260.0000.070
POMC0.9230.0940.9000.211

Where it sits in the cell

  • Plasma membrane
  • Vesiclesadditional
  • Primary ciliumadditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 2 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Brain inhibitory neurons15.4 nCPM
  • Pericytes3.9 nCPM

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.

  • brain108.6 nTPM
  • lymphoid tissue50.4 nTPM
  • bone marrow38.3 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 — 7.6 nTPM, from ADORA2Acerebellum — 9.6 nTPM, from ADORA2Ahippocampal formation — 8.3 nTPM, from ADORA2Aamygdala — 6.1 nTPM, from ADORA2Ahypothalamus — 6.8 nTPM, from ADORA2Athalamus — no resolved target expressed herebasal ganglia — 108.6 nTPM, from ADORA2Amedulla 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: midbrain 7.9, pituitary gland 6.5, spinal cord 4.2, retina 1.9.

Body

heart — 13.2 nTPM, from ADORA2Asmooth muscle — 0.9 nTPM, from ADORA2Alung — 14.2 nTPM, from ADORA2Aliver — 13.8 nTPM, from ADORA2Akidney — 19.9 nTPM, from ADORA2Astomach — 3.8 nTPM, from ADORA2Aduodenum — 6.2 nTPM, from ADORA2Asmall intestine — 6.6 nTPM, from ADORA2Acolon — 4.1 nTPM, from ADORA2Aadrenal gland — 5.5 nTPM, from ADORA2Athyroid gland — 4.2 nTPM, from ADORA2Apancreas — 2.2 nTPM, from ADORA2Aurinary bladder — 4.9 nTPM, from ADORA2Askeletal muscle — 2.4 nTPM, from ADORA2Aspleen — 14.5 nTPM, from ADORA2Asalivary gland — 3.0 nTPM, from ADORA2A
0109 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 ADORA2A 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

  • basal ganglia108.6 nTPM
  • cerebellum9.6 nTPM
  • hippocampal formation8.3 nTPM
  • midbrain7.9 nTPM
  • cerebral cortex7.6 nTPM
  • hypothalamus6.8 nTPM
  • pituitary gland6.5 nTPM
  • amygdala6.1 nTPM
  • spinal cord4.2 nTPM
  • retina1.9 nTPM

Peripheral and autonomic · 16

  • kidney19.9 nTPM
  • spleen14.5 nTPM
  • lung14.2 nTPM
  • liver13.8 nTPM
  • heart muscle13.2 nTPM
  • small intestine6.6 nTPM
  • duodenum6.2 nTPM
  • adrenal gland5.5 nTPM
  • urinary bladder4.9 nTPM
  • thyroid gland4.2 nTPM
  • colon4.1 nTPM
  • stomach 13.8 nTPM
  • salivary gland3.0 nTPM
  • skeletal muscle2.4 nTPM
  • pancreas2.2 nTPM
  • smooth muscle0.9 nTPM

Transcript is not protein. These are RNA levels for ADORA2A, 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.

Equilibrium binding constants 8

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Adenosine receptor A2aAdenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739262
Adenosine receptor A2aAdenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214

Functional readouts 16

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

TargetClassTypeValue (nM)pXOrganismAssay
Adenosine receptor A2aAdenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291726
Adenosine receptor A2aAdenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291726
Adenosine receptor A2aAdenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909214
Adenosine receptor A2aAdenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291726
Adenosine receptor A2aAdenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291726
Adenosine receptor A2aAdenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291726
Adenosine receptor A2aAdenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291726
Adenosine receptor A2aAdenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291726
Adenosine receptor A2aAdenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291726
Adenosine receptor A2aAdenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291726

Other measurements 3

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
Adenosine receptor A2aAdenosine receptorskon— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739262
Adenosine receptor A2aAdenosine receptorsk_off— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739262
Adenosine receptor A2aAdenosine receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL889380
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