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Target Report Card

Target Name and Classification

Target ID CHEMBL251
Target Type SINGLE PROTEIN
Preferred Name Adenosine A2a receptor
Synonyms ADORA2 | ADORA2A | Adenosine receptor A2a
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > small molecule receptor (family a gpcr) > nucleotide-like receptor (family a gpcr) > adenosine receptor

Target Components

Component Description Relationship Accession
Adenosine receptor A2a SINGLE PROTEIN P29274

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111329 Adenosine receptor PROTEIN FAMILY
CHEMBL2096679 Adenosine receptors; A1 & A2 SELECTIVITY GROUP
CHEMBL2095213 Adenosine receptors; A2a & A3 SELECTIVITY GROUP
CHEMBL2094257 Adenosine A2 receptor PROTEIN FAMILY
CHEMBL2096982 Adenosine receptors; A1 & A2a SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL3989695 REGADENOSON Adenosine A2a receptor agonist 4 DailyMed
CHEMBL431770 ISTRADEFYLLINE Adenosine A2a receptor antagonist 3 PubMed
CHEMBL240624 PRELADENANT Adenosine A2a receptor antagonist 3 PubMed PubMed
CHEMBL1950554 BINODENOSON Adenosine A2a receptor agonist 3 PubMed
CHEMBL1950649 APADENOSON Adenosine A2a receptor agonist 3 PubMed PubMed
CHEMBL2105747 TOZADENANT Adenosine A2a receptor antagonist 3 Other PubMed PubMed
CHEMBL447664 VIPADENANT Adenosine A2a receptor antagonist 2 PubMed PubMed
CHEMBL1096896 UK432097 Adenosine A2a receptor agonist 2 PubMed PubMed
CHEMBL1950553 SONEDENOSON Adenosine A2a receptor agonist 2 PubMed
CHEMBL1950651 EVODENOSON Adenosine A2a receptor agonist 2 PubMed
CHEMBL3545163 AMP579 Adenosine A2a receptor agonist 2 PubMed
CHEMBL3545288 V81444 Adenosine A2a receptor antagonist 2 Other PubMed
CHEMBL3545409 BVT.115959 Adenosine A2a receptor agonist 2 PubMed
CHEMBL197669 ST1535 Adenosine A2a receptor antagonist 1 PubMed PubMed
CHEMBL3545009 PBF-509 Adenosine A2a receptor antagonist 1 Other
CHEMBL3545271 PBF-999 Adenosine A2a receptor antagonist 1 Other
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000128271
Ensembl ENSG00000128271
GO Cellular Component GO:0005882 (intermediate filament)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0012505 (endomembrane system)
GO:0014069 (postsynaptic density)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030424 (axon)
GO:0030425 (dendrite)
GO:0030673 (axolemma)
GO:0032279 (asymmetric synapse)
GO:0042734 (presynaptic membrane)
GO:0043025 (neuronal cell body)
GO:0045211 (postsynaptic membrane)
GO:0048786 (presynaptic active zone)
GO:0099055 (integral component of postsynaptic membrane)
GO:0099056 (integral component of presynaptic membrane)
GO Molecular Function GO:0001609 (G-protein coupled adenosine receptor activity)
GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0005515 (protein binding)
GO:0019899 (enzyme binding)
GO:0031802 (type 5 metabotropic glutamate receptor binding)
GO:0042802 (identical protein binding)
GO:0046982 (protein heterodimerization activity)
GO:0051393 (alpha-actinin binding)
GO Biological Process GO:0001963 (synaptic transmission, dopaminergic)
GO:0001973 (adenosine receptor signaling pathway)
GO:0001975 (response to amphetamine)
GO:0006171 (cAMP biosynthetic process)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006469 (negative regulation of protein kinase activity)
GO:0006909 (phagocytosis)
GO:0006915 (apoptotic process)
GO:0006954 (inflammatory response)
GO:0006968 (cellular defense response)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007188 (adenylate cyclase-modulating G-protein coupled receptor signaling pathway)
GO:0007189 (adenylate cyclase-activating G-protein coupled receptor signaling pathway)
GO:0007205 (protein kinase C-activating G-protein coupled receptor signaling pathway)
GO:0007267 (cell-cell signaling)
GO:0007271 (synaptic transmission, cholinergic)
GO:0007417 (central nervous system development)
GO:0007596 (blood coagulation)
GO:0007600 (sensory perception)
GO:0007626 (locomotory behavior)
GO:0008015 (blood circulation)
GO:0008285 (negative regulation of cell proliferation)
GO:0014049 (positive regulation of glutamate secretion)
GO:0014057 (positive regulation of acetylcholine secretion, neurotransmission)
GO:0014061 (regulation of norepinephrine secretion)
GO:0031000 (response to caffeine)
GO:0032230 (positive regulation of synaptic transmission, GABAergic)
GO:0035249 (synaptic transmission, glutamatergic)
GO:0035810 (positive regulation of urine volume)
GO:0035815 (positive regulation of renal sodium excretion)
GO:0040013 (negative regulation of locomotion)
GO:0042311 (vasodilation)
GO:0042493 (response to drug)
GO:0042755 (eating behavior)
GO:0043116 (negative regulation of vascular permeability)
GO:0043154 (negative regulation of cysteine-type endopeptidase activity involved in apoptotic process)
GO:0043279 (response to alkaloid)
GO:0043524 (negative regulation of neuron apoptotic process)
GO:0044267 (cellular protein metabolic process)
GO:0045938 (positive regulation of circadian sleep/wake cycle, sleep)
GO:0046636 (negative regulation of alpha-beta T cell activation)
GO:0048143 (astrocyte activation)
GO:0048167 (regulation of synaptic plasticity)
GO:0048812 (neuron projection morphogenesis)
GO:0050714 (positive regulation of protein secretion)
GO:0050728 (negative regulation of inflammatory response)
GO:0051881 (regulation of mitochondrial membrane potential)
GO:0051899 (membrane depolarization)
GO:0051924 (regulation of calcium ion transport)
GO:0051968 (positive regulation of synaptic transmission, glutamatergic)
GO:0060079 (excitatory postsynaptic potential)
GO:0060080 (inhibitory postsynaptic potential)
GO:0060134 (prepulse inhibition)
GO:2001235 (positive regulation of apoptotic signaling pathway)
Wikipedia Adenosine_A2A_receptor

Target Cross References - Protein

canSAR P29274
Human Protein Atlas ENSG00000128271
IntAct P29274
Guide to Pharmacology 19
MICAD NBK22976 (Adenosine A2A receptor)
NBK23199 (Adenosine A2A receptor)
Open Targets ENSG00000128271
PharmGKB PA24584
Pharos P29274 (Tclin)
Reactome R-HSA-187024 (NGF-independant TRKA activation.)
R-HSA-417973 (Adenosine P1 receptors.)
R-HSA-418555 (G alpha (s) signalling events.)
R-HSA-5683826 (Surfactant metabolism.)
UniProt B2R7E0 P29274

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR001513 (Adeno_A2A_rcpt.)
IPR001634 (Adenosn_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)

Target Cross References - Structure

PDBe 2YDO 2YDV 3EML 3PWH 3QAK 3REY 3RFM 3UZA 3UZC 3VG9 3VGA 4EIY 4UG2 4UHR 5G53 5IU4 5IU7 5IU8 5IUA 5IUB 5JTB 5K2A 5K2B 5K2C More...
CREDO 2YDO 2YDV 3EML 3PWH 3QAK 3REY 3RFM 3UZA 3UZC 3VG9 3VGA 4EIY 4UG2 4UHR 5G53 5IU4 5IU7 5IU8 5IUA 5IUB 5JTB 5K2A 5K2B 5K2C More...
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