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A3 receptor

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 21

Nomenclature: A3 receptor

Family: Adenosine receptors

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 318 1p13.2 ADORA3 adenosine A3 receptor 1,67,77,80
Mouse 7 319 3 46.45 cM Adora3 adenosine A3 receptor 107
Rat 7 320 2q34 Adora3 adenosine A3 receptor 111
Previous and Unofficial Names Click here for help
Adenosine receptor A3 | TGPCR1 | A3AR | ARA3
Database Links Click here for help
Specialist databases
GPCRDB aa3r_human (Hs), aa3r_mouse (Mm), aa3r_rat (Rn)
Other databases
Alphafold
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
adenosine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]AB-MECA Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 9.0 – 9.1 pKd 73,95
pKd 9.0 – 9.1 (Kd 1x10-9 – 6x10-10 M) [73,95]
[3H]HEMADO Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 9.0 pKd 54
pKd 9.0 [54]
[125I]AB-MECA Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Full agonist 8.9 pKd 72
pKd 8.9 [72]
[3H]NECA Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Full agonist 7.9 – 8.2 pKd 25,55
pKd 7.9 – 8.2 [25,55]
[125I]APNEA Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 7.8 pKd 111
pKd 7.8 [111]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Mm Agonist 9.7 pKi 60
pKi 9.7 (Ki 1.8x10-10 M) [60]
MRS3558 Small molecule or natural product Click here for species-specific activity table Hs Agonist 9.5 pKi 45
pKi 9.5 (Ki 2.9x10-10 M) [45]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Rn Agonist 9.5 pKi 60
pKi 9.5 (Ki 3.3x10-10 M) [60]
(R,S)-PHPNECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.4 pKi 99
pKi 9.4 [99]
2-phenylethylyl-adenosine derivative Small molecule or natural product Hs Agonist 9.4 pKi 98
pKi 9.4 (Ki 4.4x10-10 M) [98]
MRS3558 Small molecule or natural product Click here for species-specific activity table Rn Agonist 9.0 pKi 60
pKi 9.0 (Ki 1x10-9 M) [60]
HEMADO Small molecule or natural product Click here for species-specific activity table Hs Agonist 9.0 pKi 54,99
pKi 9.0 (Ki 1.1x10-9 M) [54,99]
piclidenoson Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Full agonist 8.7 – 9.2 pKi 25,31,55,95
pKi 8.7 – 9.2 [25,31,55,95]
MRS3558 Small molecule or natural product Click here for species-specific activity table Mm Agonist 8.8 pKi 60
pKi 8.8 (Ki 1.49x10-9 M) [60]
MRS5151 Small molecule or natural product Click here for species-specific activity table Hs Agonist 8.6 pKi 65
pKi 8.6 (Ki 2.38x10-9 M) [65]
compound 6c [PMID: 34435786] Small molecule or natural product Hs Agonist 8.6 pKi 58
pKi 8.6 (Ki 2.4x10-9 M) [58]
2-hexynyl-NECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.6 pKi 99
pKi 8.6 [99]
MRS5698 Small molecule or natural product Hs Agonist 8.5 pKi 88
pKi 8.5 [88]
Cl-IB-MECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 – 8.9 pKi 10,46,51
pKi 8.0 – 8.9 [10,46,51]
CP608,039 Small molecule or natural product Click here for species-specific activity table Hs Agonist 8.2 pKi 89
pKi 8.2 (Ki 5.8x10-9 M) [89]
PENECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 pKi 99
pKi 8.2 [99]
I-ABA Small molecule or natural product Hs Full agonist 8.0 pKi 80
pKi 8.0 [80]
MRE 3008F20 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 pKi 95
pKi 8.0 [95]
NECA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.5 – 8.4 pKi 9,32,46,80,95,102
pKi 7.5 – 8.4 [9,32,46,80,95,102]
AB-MECA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.7 pKi 55,95
pKi 7.7 [55,95]
MRS5151 Small molecule or natural product Click here for species-specific activity table Mm Agonist 7.6 pKi 65
pKi 7.6 (Ki 2.44x10-8 M) [65]
(R)-PIA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.1 – 8.1 pKi 32,46,55,80,95
pKi 7.1 – 8.1 [32,46,55,80,95]
CCPA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 45,55
pKi 7.4 [45,55]
apadenoson Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.3 pKi 45
pKi 7.3 (Ki 4.5x10-8 M) [45]
cyclopentyladenosine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.0 – 7.4 pKi 32,45,55,80
pKi 7.0 – 7.4 [32,45,55,80]
(S)-PIA Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.3 – 7.4 pKi 55,80,95
pKi 6.3 – 7.4 [55,80,95]
MPC-MECA Small molecule or natural product Hs Full agonist 6.8 pKi 95
pKi 6.8 [95]
NECA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 6.6 – 6.9 pKi 63,72
pKi 6.6 – 6.9 [63,72]
N(6)-cyclohexyladenosine Small molecule or natural product Click here for species-specific activity table Rn Agonist 6.8 pKi 90
pKi 6.8 (Ki 1.76x10-7 M) [90]
(R)-PIA Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.6 – 6.8 pKi 16,72
pKi 6.6 – 6.8 [16,72]
CCPA Small molecule or natural product Click here for species-specific activity table Rn Agonist 6.6 pKi 60
pKi 6.6 (Ki 2.37x10-7 M) [60]
CGS 21680 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.0 – 7.2 pKi 9,32,45,55,95
pKi 6.0 – 7.2 [9,32,45,55,95]
adenosine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 6.5 pKi 28-29,102
pKi 6.5 (Ki 2.9x10-7 M) [28-29,102]
CGS 21680 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Agonist 6.2 pKi 60
pKi 6.2 (Ki 5.84x10-7 M) [60]
TCPA Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.2 pKi 6
pKi 6.2 (Ki 6x10-7 M) [6]
binodenoson Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.0 pKi 45
pKi 6.0 (Ki 9.03x10-7 M) [45]
GS9667 Small molecule or natural product Click here for species-specific activity table Hs Agonist <6.0 pKi 22
pKi <6.0 (Ki >1x10-6 M) [22]
N(6)-cyclohexyladenosine Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.0 pKi 78
pKi 6.0 (Ki 1.025x10-6 M) [78]
2-chloroadenosine Small molecule or natural product Click here for species-specific activity table Rn Agonist 5.7 pKi 90
pKi 5.7 (Ki 1.89x10-6 M) [90]
2'-Me-CCPA Small molecule or natural product Rn Agonist 5.3 pKi 27
pKi 5.3 (Ki 5x10-6 M) [27]
adenosine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Agonist 5.2 pKi 102
pKi 5.2 (Ki 6.5x10-6 M) [102]
BAY 60-6583 Small molecule or natural product Click here for species-specific activity table Hs Agonist <5.0 pKi 56
pKi <5.0 (Ki >1x10-5 M) [56]
regadenoson Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist <5.0 pKi 45
pKi <5.0 (Ki >1x10-5 M) [45]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]MRE 3008F20 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.1 pKd 4,95
pKd 9.1 [4,95]
PSB-11 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKd 68
pKd 8.3 (Kd 4.9x10-9 M) [68]
[3H]PSB-11 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.3 pKd 68
pKd 8.3 [68]
KF26777 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.7 pKi 79
pKi 9.7 (Ki 2x10-10 M) [79]
PSB-10 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.4 pKi 70
pKi 9.4 (Ki 4.41x10-10 M) [70]
MRE 3010F20 Small molecule or natural product Hs Antagonist 9.3 pKi 95
pKi 9.3 [95]
MRE 3008F20 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 – 9.5 pKi 45,94-95
pKi 9.0 – 9.5 [45,94-95]
MRS1220 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 9.2 pKi 46,53,85,105
pKi 8.2 – 9.2 (Ki 6.31x10-9 – 6.3x10-10 M) [46,53,85,105]
PSB-11 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 74
pKi 8.6 (Ki 2.34x10-9 M) [74]
MRS1177 Small molecule or natural product Hs Antagonist 8.5 pKi 53
pKi 8.5 [53]
VUF5574 Small molecule or natural product Hs Antagonist 8.4 pKi 92
pKi 8.4 (Ki 4.03x10-9 M) [92]
MRS1186 Small molecule or natural product Hs Antagonist 8.1 pKi 53
pKi 8.1 [53]
MRS1505 Small molecule or natural product Hs Antagonist 8.1 pKi 59
pKi 8.1 [59]
LUF7602 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.0 pKi 104
pKi 8.0 (Ki 1x10-8 M) [104]
Description: Displacement of [3H]PSB-11 binding from the hA3AR (in membranes from stably transfected CHO cells) following preincubation for 4 h,
VUF8504 Small molecule or natural product Hs Antagonist 7.8 pKi 91
pKi 7.8 [91]
xanthine amine congener Small molecule or natural product Ligand has a PDB structure Rn Antagonist 7.7 pKi 72
pKi 7.7 [72]
I-ABOPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 80
pKi 7.7 [80]
MRS1476 Small molecule or natural product Hs Antagonist 7.7 pKi 59
pKi 7.7 [59]
MRS1523 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 59
pKi 7.7 (Ki 1.99x10-8 M) [59]
MRS1191 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 46-47,60
pKi 7.5 [46-47,60]
MRS1486 Small molecule or natural product Hs Antagonist 7.5 pKi 59
pKi 7.5 [59]
CGS 15943 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.0 – 7.9 pKi 53,55,73,95
pKi 7.0 – 7.9 [53,55,73,95]
BW-A1433 Small molecule or natural product Rn Antagonist 7.4 pKi 72
pKi 7.4 [72]
BW-A1433 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.3 pKi 80
pKi 7.3 [80]
xanthine amine congener Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 – 7.4 pKi 55,80,95
pKi 7.0 – 7.4 [55,80,95]
MRS1097 Small molecule or natural product Hs Antagonist 7.0 pKi 46,93
pKi 7.0 [46,93]
MRS1523 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.9 pKi 60
pKi 6.9 (Ki 1.13x10-7 M) [60]
VUF8507 Small molecule or natural product Hs Antagonist 6.7 pKi 91
pKi 6.7 [91]
derenofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pKi 48
pKi 6.7 (Ki 2x10-7 M) [48]
MRS1042 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 49
pKi 6.5 [49]
MRS1041 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 pKi 49
pKi 6.4 [49]
MRS1754 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 52
pKi 6.2 (Ki 5.7x10-7 M) [52]
MRS1067 Small molecule or natural product Hs Antagonist 6.2 pKi 46,49
pKi 6.2 [46,49]
LUF5981 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 12
pKi 6.2 (Ki 6.37x10-7 M) [12]
MRS1523 Small molecule or natural product Click here for species-specific activity table Mm Antagonist 6.1 pKi 60
pKi 6.1 (Ki 7.31x10-7 M) [60]
ZM-241385 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.1 pKi 45
pKi 6.1 (Ki 7.43x10-7 M) [45]
MRS1093 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 pKi 49
pKi 6.1 [49]
MRS1088 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 pKi 49
pKi 6.1 [49]
DPCPX Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 – 6.6 pKi 2,38,55,80,95,100
pKi 5.4 – 6.6 (Ki 3.96x10-6 – 2.43x10-7 M) [2,38,55,80,95,100]
MRE 2029F20 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.0 pKi 5
pKi <6.0 (Ki >1x10-6 M) [5]
vipadenant Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 6.0 pKi 34
pKi 6.0 (Ki 1.005x10-6 M) [34]
ST-1535 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.0 pKi 66
pKi <6.0 (Ki >1x10-6 M) [66]
preladenant Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist <6.0 pKi 69
pKi <6.0 (Ki >1x10-6 M) [69]
ATL802 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <6.0 pKi 52
pKi <6.0 (Ki >1x10-6 M) [52]
DPCPX Small molecule or natural product Click here for species-specific activity table Rn Antagonist 4.4 – 7.6 pKi 2,72,100
pKi 4.4 – 7.6 [2,72,100]
LAS38096 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 20,97
pKi 6.0 (Ki 1.043x10-6 M) [20,97]
CVT-6883 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 21
pKi 6.0 (Ki 1.07x10-6 M) [21]
SCH 58261 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 45
pKi 5.9 (Ki 1.2x10-6 M) [45]
MRS928 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 49
pKi 5.9 [49]
MRS1191 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.8 pKi 59-60
pKi 5.8 [59-60]
dexniguldipine Small molecule or natural product Hs Antagonist 5.7 pKi 93
pKi 5.7 [93]
PSB36 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 pKi 100
pKi 5.6 (Ki 2.3x10-6 M) [100]
galangin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.5 pKi 49
pKi 5.5 [49]
sakuranetin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.5 pKi 49
pKi 5.5 [49]
nicardipine Small molecule or natural product Approved drug Hs Antagonist 5.5 pKi 93
pKi 5.5 [93]
rolofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 pKi 50
pKi 5.4 (Ki 4.39x10-6 M) [50]
istradefylline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.3 pKi 30
pKi 5.3 (Ki 4.47x10-6 M) [30]
PSB36 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.2 pKi 100
pKi 5.2 (Ki 6.5x10-6 M) [100]
SCH442416 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 45
pKi <5.0 (Ki >1x10-5 M) [45]
PSB603 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 8
pKi <5.0 (Ki >1x10-5 M) [8]
PSB1115 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist <5.0 pKi 38
pKi <5.0 (Ki >1x10-5 M) [38]
tonapofylline Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 50
pKi <5.0 (Ki >1x10-5 M) [50]
FK-453 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.0 pKi 45
pKi 5.0 (Ki 1x10-5 M) [45]
CSC Small molecule or natural product Click here for species-specific activity table Rn Antagonist <5.0 pKi 90
pKi <5.0 (Ki >1x10-5 M) [90]
MSX-2 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 82
pKi <5.0 (Ki >1x10-5 M) [82]
ATL802 Small molecule or natural product Click here for species-specific activity table Mm Antagonist <5.0 pKi 52
pKi <5.0 (Ki >1x10-5 M) [52]
caffeine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 4.9 pKi 43
pKi 4.9 (Ki 1.33x10-5 M) [43]
flavone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 4.8 pKi 49
pKi 4.8 [49]
theophylline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 4.1 – 4.7 pKi 43,55
pKi 4.1 – 4.7 (Ki 8.64x10-5 – 2.23x10-5 M) [43,55]
flavanone Small molecule or natural product Hs Antagonist 4.3 pKi 49
pKi 4.3 [49]
visnagin Small molecule or natural product Click here for species-specific activity table