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PsychedeliaDokholyan Laboratory
TargetAdenosine receptors

Adenosine receptor A3

A1, A2A, A2B, A3.

Measurements
28
Compounds
13
Binding constants
7
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

AA3R_HUMANADORA3Homo sapiens

Adenosine receptor A3

G protein-coupled receptor (GPCR) for adenosine that plays significant roles in various physiological processes including immune regulation, cardioprotection and neuroprotection38627384,40825947,9837869. Also acts as a receptor for adenosines containing N(6)-methylated adenine (m6A) post-transcriptional modification, which are derived from the degradation of RNAs (mRNAs, rRNAs and tRNAs): activated by N(6)-methyladenosine (m6A), N(6),N(6)-dimethyladenosine (m6,6A) and N(6)-isopentenyladenosine (i6A)33472058,39511145. Preferentially couples to the inhibitory G protein (Gi), leading to the suppression of adenylate cyclase activity and a reduction in intracellular cyclic AMP levels33472058,38627384. Upon adenosine binding, mediates cardioprotection in cardiomyocytes through anti-apoptotic effects primarily via the ERK1/2 pathway as well as the PI3K pathway9837869. In the central nervous system, participates in the modulation of synaptic plasticity, including long-term potentiation (LTP) and long-term depression (LTD) in the hippocampus (By similarity). In lung mast cells, receptor activation contributes to the type I allergic response by facilitating mast cell degranulation and histamine release (By similarity). Highly expressed in inflammatory cells such as neutrophils and mast cells, inhibits neutrophil degranulation and reduces superoxide production, thereby modulating inflammatory responses9164961
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase8234299

Quoted from UniProt’s FUNCTION annotation for P0DMS8 (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
GNAI20.9220.1250.9000.179
GNAI10.9200.1250.9000.160
KNG10.9150.0000.9000.186
GNAI30.9100.1250.9000.056
ADORA10.9070.0000.9000.101
GPR340.6750.0000.0000.422
LTBP20.6590.0490.0000.654
LTBP30.6570.0490.0000.655
LTBP10.6530.0490.0000.651
ADA0.6490.0000.0000.649

Where it sits in the cell

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 3 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Late spermatids4.7 nCPM
  • Early spermatids2.9 nCPM
  • Mast cells1.2 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.

  • brain19.8 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 — 6.5 nTPM, from ADORA3cerebellum — 0.9 nTPM, from ADORA3hippocampal formation — 6.4 nTPM, from ADORA3amygdala — 6.4 nTPM, from ADORA3hypothalamus — 6.1 nTPM, from ADORA3thalamus — no resolved target expressed herebasal ganglia — 4.3 nTPM, from ADORA3medulla 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: spinal cord 19.8, midbrain 9.9, pituitary gland 2.6, retina 0.9.

Body

heart — 3.3 nTPM, from ADORA3smooth muscle — 4.5 nTPM, from ADORA3lung — 3.5 nTPM, from ADORA3liver — 3.1 nTPM, from ADORA3kidney — 1.4 nTPM, from ADORA3stomach — 2.8 nTPM, from ADORA3duodenum — 4.2 nTPM, from ADORA3small intestine — 8.9 nTPM, from ADORA3colon — 6.2 nTPM, from ADORA3adrenal gland — 14.2 nTPM, from ADORA3thyroid gland — 1.4 nTPM, from ADORA3pancreas — 1.8 nTPM, from ADORA3urinary bladder — 4.0 nTPM, from ADORA3skeletal muscle — 0.6 nTPM, from ADORA3spleen — 4.4 nTPM, from ADORA3salivary gland — 2.7 nTPM, from ADORA3
020 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 ADORA3 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

  • spinal cord19.8 nTPM
  • midbrain9.9 nTPM
  • cerebral cortex6.5 nTPM
  • hippocampal formation6.4 nTPM
  • amygdala6.4 nTPM
  • hypothalamus6.1 nTPM
  • basal ganglia4.3 nTPM
  • pituitary gland2.6 nTPM
  • cerebellum0.9 nTPM
  • retina0.9 nTPM

Peripheral and autonomic · 16

  • adrenal gland14.2 nTPM
  • small intestine8.9 nTPM
  • colon6.2 nTPM
  • smooth muscle4.5 nTPM
  • spleen4.4 nTPM
  • duodenum4.2 nTPM
  • urinary bladder4.0 nTPM
  • lung3.5 nTPM
  • heart muscle3.3 nTPM
  • liver3.1 nTPM
  • stomach 12.8 nTPM
  • salivary gland2.7 nTPM
  • pancreas1.8 nTPM
  • kidney1.4 nTPM
  • thyroid gland1.4 nTPM
  • skeletal muscle0.6 nTPM

Transcript is not protein. These are RNA levels for ADORA3, 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 7

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

TargetClassTypeValue (nM)pXOrganismAssay
Adenosine receptor A3Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215

Functional readouts 21

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

TargetClassTypeValue (nM)pXOrganismAssay
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291727
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291727
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291728
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291728
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291728
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291728
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291728
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291727
Adenosine receptor A3Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909215
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291727
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291727
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291727
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291727
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291727
Adenosine receptor A3Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291727
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