A2A receptor

Target id: 19

Nomenclature: A2A receptor

Family: Adenosine receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for A2A receptor in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 412 22q11.23 ADORA2A adenosine A2a receptor 38,68,104
Mouse 7 410 10 Adora2a adenosine A2a receptor 81
Rat 7 410 20p12 Adora2a adenosine A2a receptor 17
Previous and Unofficial Names
RDC8 | A2-AR | adenosine receptor A2a
Database Links
Specialist databases
GPCRDB aa2ar_human (Hs), aa2ar_mouse (Mm), aa2ar_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Human A2A adenosine receptor bound to an antagonist
PDB Id:  4EIY
Ligand:  ZM-241385
Resolution:  1.8Å
Species:  Human
References:  76
Image of receptor 3D structure from RCSB PDB
Description:  A2A receptor (thermostabilised) bound to its natural ligand adenosine
PDB Id:  2YDO
Ligand:  adenosine   This ligand is endogenous
Resolution:  3.0Å
Species:  Human
References:  70
Image of receptor 3D structure from RCSB PDB
Description:  Thermostabilised human A2A receptor with NECA bound
PDB Id:  2YDV
Ligand:  NECA
Resolution:  2.6Å
Species:  Human
References:  69
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with PSB36
PDB Id:  5N2R
Ligand:  PSB36
Resolution:  2.8Å
Species:  Human
References:  15
Image of receptor 3D structure from RCSB PDB
Description:  Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein.
PDB Id:  6GDG
Ligand:  NECA
Resolution:  3.8Å
Species:  Human
References:  44
Natural/Endogenous Ligands
adenosine

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]CGS 21680 Hs Full agonist 7.7 – 7.8 pKd 52,137
pKd 7.7 – 7.8 (Kd 2.2x10-8 – 1.6x10-8 M) [52,137]
[3H]NECA Hs Full agonist 7.7 pKd 62
pKd 7.7 [62]
apadenoson Hs Agonist 9.3 pKi 103
pKi 9.3 (Ki 5x10-10 M) [103]
(R,S)-PHPNECA Hs Full agonist 8.5 pKi 136
pKi 8.5 [136]
2-hexynyl-NECA Hs Full agonist 8.2 – 8.3 pKi 27,64,136
pKi 8.2 – 8.3 [27,64,136]
compound 4g [PMID: 22220592] Hs Agonist 8.1 pKi 19
pKi 8.1 (Ki 7.76x10-9 M) [19]
NECA Rn Agonist 8.0 pKi 78
pKi 8.0 (Ki 9.7x10-9 M) [78]
UK-432,097 Hs Agonist 7.7 – 8.3 pKi 46,140
pKi 7.7 – 8.3 [46,140]
NECA Hs Full agonist 6.9 – 8.7 pKi 9,27,42,59,64,141
pKi 6.9 – 8.7 [9,27,42,59,64,141]
CGS 21680 Rn Agonist 7.7 pKi 75
pKi 7.7 (Ki 1.9x10-8 M) [75]
CGS 21680 Hs Full agonist 6.7 – 8.1 pKi 9,27,42,51,59,62,64,97
pKi 6.7 – 8.1 (Ki 1.99x10-7 – 7.94x10-9 M) [9,27,42,51,59,62,64,97]
2-chloroadenosine Rn Agonist 7.1 pKi 23
pKi 7.1 (Ki 7.6x10-8 M) [23]
CV-1808 Hs Full agonist 7.1 pKi 27,64
pKi 7.1 [27,64]
adenosine Rn Agonist 6.8 pKi 141
pKi 6.8 (Ki 1.5x10-7 M) [141]
2-chloroadenosine Hs Full agonist 6.7 – 6.8 pKi 59,64
pKi 6.7 – 6.8 [59,64]
TCPA Hs Agonist 6.7 pKi 6
pKi 6.7 (Ki 2.1x10-7 M) [6]
(R)-PIA Rn Agonist 6.7 pKi 23
pKi 6.7 (Ki 2.2x10-7 M) [23]
binodenoson Hs Agonist 6.6 pKi 51
pKi 6.6 (Ki 2.7x10-7 M) [51]
regadenoson Hs Agonist 6.5 pKi 51
pKi 6.5 (Ki 2.9x10-7 M) [51]
adenosine Hs Agonist 6.5 pKi 34-35,141
pKi 6.5 (Ki 3.1x10-7 M) [34-35,141]
CGS 24012 Hs Full agonist 6.4 pKi 59
pKi 6.4 [59]
N(6)-cyclohexyladenosine Rn Agonist 6.3 pKi 23
pKi 6.3 (Ki 4.6x10-7 M) [23]
Cl-IB-MECA Rn Agonist 6.3 pKi 75
pKi 6.3 (Ki 4.7x10-7 M) [75]
PENECA Hs Full agonist 6.2 pKi 136
pKi 6.2 [136]
cyclopentyladenosine Hs Full agonist 6.1 pKi 42,51,62
pKi 6.1 [42,51,62]
(R)-PIA Hs Full agonist 6.0 – 6.2 pKi 27,42,59,62,64
pKi 6.0 – 6.2 [27,42,59,62,64]
CCPA Rn Agonist 6.0 pKi 75
pKi 6.0 (Ki 9.5x10-7 M) [75]
cyclopentyladenosine Rn Agonist 6.0 pKi 75
pKi 6.0 (Ki 9.5x10-7 M) [75]
MRS3558 Rn Agonist 6.0 pKi 75
pKi 6.0 (Ki 1.08x10-6 M) [75]
piclidenoson Hs Full agonist 5.6 – 6.3 pKi 51,59,62
pKi 5.6 – 6.3 [51,59,62]
HEMADO Hs Agonist 5.9 pKi 63,136
pKi 5.9 (Ki 1.2x10-6 M) [63,136]
N(6)-cyclohexyladenosine Hs Full agonist 5.9 pKi 27,64
pKi 5.9 [27,64]
GR79236 Hs Agonist 5.9 pKi 51
pKi 5.9 (Ki 1.3x10-6 M) [51]
CV-1674 Hs Full agonist 5.8 pKi 64
pKi 5.8 [64]
tecadenoson Pig Agonist 5.6 pKi 51,89
pKi 5.6 (Ki 2.315x10-6 M) [51,89]
MRS3558 Hs Agonist 5.6 pKi 51
pKi 5.6 (Ki 2.33x10-6 M) [51]
CCPA Hs Full agonist 5.6 pKi 51,62
pKi 5.6 [51,62]
metrifudil Hs Full agonist 5.5 pKi 64
pKi 5.5 [64]
AB-MECA Hs Full agonist 5.4 pKi 62
pKi 5.4 [62]
APNEA Hs Full agonist 5.3 pKi 64
pKi 5.3 [64]
Cl-IB-MECA Hs Agonist 5.3 pKi 51
pKi 5.3 (Ki 5.36x10-6 M) [51]
(S)-PIA Hs Full agonist 5.0 – 5.1 pKi 27,62
pKi 5.0 – 5.1 [27,62]
Cl-IB-MECA Mm Agonist ~5.0 pKi 75
pKi ~5.0 (Ki ~1x10-5 M) [75]
BAY 60-6583 Hs Agonist <5.0 pKi 66
pKi <5.0 (Ki >1x10-5 M) [66]
GS9667 Hs Agonist <5.0 pKi 32
pKi <5.0 (Ki >1x10-5 M) [32]
MRS5151 Hs Agonist <5.0 pKi 84
pKi <5.0 (Ki >1x10-5 M) [84]
MRS5151 Mm Agonist <5.0 pKi 84
pKi <5.0 (Ki >1x10-5 M) [84]
MRS3558 Mm Agonist 5.0 pKi 75
pKi 5.0 (Ki 1.04x10-5 M) [75]
View species-specific agonist tables
Agonist Comments
The INN-assigned compound evodenoson is an agonist of the A2A receptor but affinity data is not available.
Note that for tecadenoson, there is inconsistency between the two referenced articles (from the same group) as to the species origin of the ADORA2A used to generate the Ki value which is presented as identical in both articles. We have used the earlier paper as precedent, which indicates the use of the porcine receptor.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]ZM-241385 Rn Antagonist 9.2 pKd 102
pKd 9.2 [102]
[3H]ZM 241385 Hs Antagonist 8.7 – 9.1 pKd 4,41
pKd 8.7 – 9.1 (Kd 1.8x10-9 – 8x10-10 M) [4,41]
[3H]SCH 58261 Hs Antagonist 8.6 – 9.0 pKd 64,100
pKd 8.6 – 9.0 [64,100]
[3H]XAC Hs Antagonist 8.0 pKd 59
pKd 8.0 [59]
SCH442416 Hs Antagonist 8.4 – 10.3 pKi 123,126
pKi 8.4 – 10.3 [123,126]
MRS1093 Hs Antagonist 9.2 pKi 56
pKi 9.2 [56]
preladenant Hs Antagonist 9.1 pKi 88
pKi 9.1 (Ki 9x10-10 M) [88]
ZM-241385 Hs Antagonist 8.8 – 9.1 pKi 100
pKi 8.8 – 9.1 [100]
vipadenant Hs Antagonist 8.9 pKi 45
pKi 8.9 (Ki 1.3x10-9 M) [45]
SCH 58261 Hs Antagonist 8.3 – 9.2 pKi 27,64,100
pKi 8.3 – 9.2 [27,64,100]
xanthine amine congener Hs Antagonist 8.4 – 9.0 pKi 27,62
pKi 8.4 – 9.0 [27,62]
CGS 15943 Hs Antagonist 7.7 – 9.4 pKi 27,59,62,100
pKi 7.7 – 9.4 [27,59,62,100]
istradefylline Rn Antagonist 8.4 – 8.7 pKi 109,122
pKi 8.4 – 8.7 (Ki 4.46x10-9 – 2.2x10-9 M) [109,122]
tozadenant Hs Antagonist 8.3 pKi 24
pKi 8.3 (Ki 5x10-9 M) [24]
ST-1535 Hs Antagonist 8.2 pKi 85
pKi 8.2 (Ki 6.6x10-9 M) [85]
MSX-2 Rn Antagonist 8.1 pKi 90,117
pKi 8.1 (Ki 8.04x10-9 M) [90,117]
MSX-2 Hs Antagonist 7.8 – 8.3 pKi 117
pKi 7.8 – 8.3 (Ki 1.45x10-8 – 5.38x10-9 M) [117]
KF 17837S Hs Antagonist 7.7 pKi 27
pKi 7.7 [27]
istradefylline Hs Antagonist 7.0 – 7.9 pKi 11,36
pKi 7.0 – 7.9 (Ki 9.12x10-8 – 1.2x10-8 M) [11,36]
CSC Rn Antagonist 7.3 pKi 50
pKi 7.3 (Ki 5.4x10-8 M) [50]
DPCPX Hs Antagonist 6.6 – 7.2 pKi 27,62,64,100,139
pKi 6.6 – 7.2 [27,62,64,100,139]
MRE 3008F20 Hs Antagonist 6.8 pKi 51,129-130
pKi 6.8 [51,129-130]
LUF5981 Hs Antagonist 6.7 pKi 11
pKi 6.7 (Ki 1.94x10-7 M) [11]
rolofylline Hs Antagonist 6.2 – 7.0 pKi 57,105
pKi 6.2 – 7.0 (Ki 6.37x10-7 – 1.08x10-7 M) [57,105]
DPCPX Rn Antagonist 6.3 – 6.8 pKi 60,90
pKi 6.3 – 6.8 (Ki 5x10-7 – 1.57x10-7 M) [60,90]
derenofylline Hs Antagonist 6.4 pKi 55
pKi 6.4 (Ki 3.98x10-7 M) [55]
rolofylline Rn Antagonist 6.3 – 6.4 pKi 58,106
pKi 6.3 – 6.4 (Ki 5.1x10-7 – 3.8x10-7 M) [58,106]
KF26777 Hs Antagonist 6.3 pKi 112
pKi 6.3 (Ki 4.7x10-7 M) [112]
MRS1754 Hs Antagonist 6.3 pKi 61
pKi 6.3 (Ki 5.03x10-7 M) [61]
PSB36 Rn Antagonist 6.3 pKi 139
pKi 6.3 (Ki 5.52x10-7 M) [139]
MRS1754 Rn Antagonist 6.2 pKi 61
pKi 6.2 (Ki 6.12x10-7 M) [61]
CPX Hs Antagonist 6.2 pKi 59
pKi 6.2 [59]
ATL802 Hs Antagonist 6.2 pKi 61
pKi 6.2 (Ki 6.54x10-7 M) [61]
CPFPX Rn Antagonist 6.1 pKi 47
pKi 6.1 (Ki 8.12x10-7 M) [47]
CPFPX Hs Antagonist 6.0 pKi 47
pKi 6.0 (Ki 9.4x10-7 M) [47]
PSB36 Hs Antagonist 6.0 pKi 139
pKi 6.0 (Ki 9.8x10-7 M) [139]
MRE 2029F20 Hs Antagonist <6.0 pKi 5
pKi <6.0 (Ki >1x10-6 M) [5]
galangin Hs Antagonist 6.0 pKi 56
pKi 6.0 [56]
LAS38096 Hs Antagonist <6.0 pKi 29,134
pKi <6.0 (Ki >1x10-6 M) [29,134]
FK-453 Hs Antagonist 5.9 pKi 51
pKi 5.9 (Ki 1.3x10-6 M) [51]
PSB-11 Hs Antagonist 5.9 pKi 101
pKi 5.9 (Ki 1.28x10-6 M) [101]
MRS1523 Rn Antagonist 5.7 pKi 75
pKi 5.7 (Ki 2.05x10-6 M) [75]
PSB-11 Rn Antagonist 5.7 pKi 101
pKi 5.7 (Ki 2.1x10-6 M) [101]
tonapofylline Rn Antagonist 5.6 pKi 57
pKi 5.6 (Ki 2.44x10-6 M) [57]
PSB-10 Hs Antagonist 5.6 pKi 101
pKi 5.6 (Ki 2.7x10-6 M) [101]
MRS1041 Hs Antagonist 5.5 pKi 56
pKi 5.5 [56]
MRS1042 Hs Antagonist 5.5 pKi 56
pKi 5.5 [56]
flavone Hs Antagonist 5.5 pKi 56
pKi 5.5 [56]
theophylline Hs Antagonist 5.2 – 5.8 pKi 27,49,62,129
pKi 5.2 – 5.8 [27,49,62,129]
CVT-6883 Hs Antagonist 5.5 pKi 31
pKi 5.5 (Ki 3.28x10-6 M) [31]
MRS1523 Hs Antagonist 5.4 pKi 75
pKi 5.4 (Ki 3.66x10-6 M) [75]
PSB-10 Rn Antagonist 5.2 pKi 92
pKi 5.2 (Ki 6.04x10-6 M) [92]
MRS928 Hs Antagonist 5.2 pKi 56
pKi 5.2 [56]
tonapofylline Hs Antagonist 5.2 pKi 57
pKi 5.2 (Ki 6.41x10-6 M) [57]
caffeine Hs Antagonist 4.6 – 5.6 pKi 1,49,64
pKi 4.6 – 5.6 [1,49,64]
ATL802 Mm Antagonist 5.1 pKi 61
pKi 5.1 (Ki 8.393x10-6 M) [61]
MRS1191 Hs Antagonist <5.0 pKi 75
pKi <5.0 (Ki >1x10-5 M) [75]
MRS1191 Rn Antagonist <5.0 pKi 75
pKi <5.0 (Ki >1x10-5 M) [75]
VUF5574 Rn Antagonist >5.0 pKi 127
pKi >5.0 (Ki <1x10-5 M) [127]
PSB603 Hs Antagonist <5.0 pKi 8
pKi <5.0 (Ki >1x10-5 M) [8]
PSB603 Rn Antagonist <5.0 pKi 8
pKi <5.0 (Ki >1x10-5 M) [8]
MRS1065 Hs Antagonist 4.9 pKi 56
pKi 4.9 [56]
morin Hs Antagonist 4.8 pKi 56
pKi 4.8 [56]
theophylline Rn Antagonist 4.6 – 4.7 pKi 49,91
pKi 4.6 – 4.7 (Ki 2.53x10-5 – 2.2x10-5 M) [49,91]
PSB1115 Rn Antagonist 4.6 pKi 91
pKi 4.6 (Ki 2.4x10-5 M) [91]
MRS1086 Hs Antagonist 4.6 pKi 56
pKi 4.6 [56]
MRS1132 Hs Antagonist 4.6 pKi 56
pKi 4.6 [56]
MRS1066 Hs Antagonist 4.5 pKi 56
pKi 4.5 [56]
caffeine Rn Antagonist 4.3 – 4.5 pKi 22,49,90
pKi 4.3 – 4.5 (Ki 4.8x10-5 – 3.25x10-5 M) [22,49,90]
sakuranetin