Skip to content
PsychedeliaDokholyan Laboratory
TargetAdenosine receptors

Adenosine receptor A1

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

AA1R_HUMANADORA1Homo sapiens

Adenosine receptor A1

Receptor for adenosine29925945. The activity of this receptor is mediated by G proteins such as GNAI2 which inhibit adenylyl cyclase

Quoted from UniProt’s FUNCTION annotation for P30542 (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
GNAI20.9940.9320.9000.188
GNB10.9410.9090.0000.379
GNAI10.9310.1250.9000.256
KNG10.9280.0000.9000.313
GNAI30.9200.1250.9000.162
ADORA30.9070.0000.9000.101
SLC29A10.8800.0450.0000.880
ADA0.8310.2260.0000.791
GNG20.8160.8160.0000.000
ADORA2A0.7840.3940.0000.646

Where it sits in the cell

  • Plasma membrane
  • 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 11 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Podocytes138.9 nCPM
  • Müller glia60.9 nCPM
  • Oligodendrocytes55.1 nCPM
  • Oligodendrocyte progenitor cells54.5 nCPM
  • Pancreatic duct cells30.8 nCPM
  • Astrocytes30.3 nCPM
  • Sertoli cells28.8 nCPM
  • Brain excitatory neurons21.9 nCPM
  • Adipocytes20.5 nCPM
  • Breast secretory cells19.9 nCPM
  • Retinal amacrine cells19.7 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.

  • brain42.6 nTPM
  • testis20.2 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 — 38.3 nTPM, from ADORA1cerebellum — 19.0 nTPM, from ADORA1hippocampal formation — 37.0 nTPM, from ADORA1amygdala — 39.5 nTPM, from ADORA1hypothalamus — 23.7 nTPM, from ADORA1thalamus — no resolved target expressed herebasal ganglia — 42.6 nTPM, from ADORA1medulla 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 42.0, midbrain 40.6, retina 4.5, pituitary gland 1.7.

Body

heart — 10.7 nTPM, from ADORA1smooth muscle — 0.4 nTPM, from ADORA1lung — 1.6 nTPM, from ADORA1liver — 0.3 nTPM, from ADORA1kidney — 9.3 nTPM, from ADORA1stomach — 1.0 nTPM, from ADORA1duodenum — 0.9 nTPM, from ADORA1small intestine — 1.1 nTPM, from ADORA1colon — 1.0 nTPM, from ADORA1adrenal gland — 0.2 nTPM, from ADORA1thyroid gland — 2.1 nTPM, from ADORA1pancreas — 12.4 nTPM, from ADORA1urinary bladder — 1.5 nTPM, from ADORA1skeletal muscle — 1.6 nTPM, from ADORA1spleen — 6.0 nTPM, from ADORA1salivary gland — 6.0 nTPM, from ADORA1
043 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 ADORA1 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 ganglia42.6 nTPM
  • spinal cord42.0 nTPM
  • midbrain40.6 nTPM
  • amygdala39.5 nTPM
  • cerebral cortex38.3 nTPM
  • hippocampal formation37.0 nTPM
  • hypothalamus23.7 nTPM
  • cerebellum19.0 nTPM
  • retina4.5 nTPM
  • pituitary gland1.7 nTPM

Peripheral and autonomic · 16

  • pancreas12.4 nTPM
  • heart muscle10.7 nTPM
  • kidney9.3 nTPM
  • spleen6.0 nTPM
  • salivary gland6.0 nTPM
  • thyroid gland2.1 nTPM
  • lung1.6 nTPM
  • skeletal muscle1.6 nTPM
  • urinary bladder1.5 nTPM
  • small intestine1.1 nTPM
  • stomach 11.0 nTPM
  • colon1.0 nTPM
  • duodenum0.9 nTPM
  • smooth muscle0.4 nTPM
  • liver0.3 nTPM
  • adrenal gland0.2 nTPM

Transcript is not protein. These are RNA levels for ADORA1, 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 A1Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739260
Adenosine receptor A1Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213

Functional readouts 16

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

TargetClassTypeValue (nM)pXOrganismAssay
Adenosine receptor A1Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291724
Adenosine receptor A1Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291724
Adenosine receptor A1Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909213
Adenosine receptor A1Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291724
Adenosine receptor A1Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291724
Adenosine receptor A1Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291724
Adenosine receptor A1Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291724
Adenosine receptor A1Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291724
Adenosine receptor A1Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291724
Adenosine receptor A1Adenosine receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291724

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 A1Adenosine receptorskon— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739260
Adenosine receptor A1Adenosine receptorsk_off— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739260
Adenosine receptor A1Adenosine receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL889379
← All targets