A<sub>3</sub> receptor | Adenosine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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A3 receptor

target has curated data in GtoImmuPdb

Target id: 21

Nomenclature: A3 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

Gene and Protein Information
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 1,66,76,79
Mouse 7 319 3 F2.3 Adora3 adenosine A3 receptor 106
Rat 7 320 2q34 Adora3 adenosine A3 receptor 110
Previous and Unofficial Names
Adenosine receptor A3 | TGPCR1 | A3AR | ARA3
Database Links
Specialist databases
GPCRDB aa3r_human (Hs), aa3r_mouse (Mm), aa3r_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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 Value Parameter Reference
[125I]AB-MECA Hs Full agonist 9.0 – 9.1 pKd 72,94
pKd 9.0 – 9.1 (Kd 1x10-9 – 6x10-10 M) [72,94]
[3H]HEMADO Hs Full agonist 9.0 pKd 54
pKd 9.0 [54]
[125I]AB-MECA Rn Full agonist 8.9 pKd 71
pKd 8.9 [71]
[3H]NECA Hs Full agonist 7.9 – 8.2 pKd 25,55
pKd 7.9 – 8.2 [25,55]
[125I]APNEA Hs Full agonist 7.8 pKd 110
pKd 7.8 [110]
Cl-IB-MECA Mm Agonist 9.7 pKi 59
pKi 9.7 (Ki 1.8x10-10 M) [59]
MRS3558 Hs Agonist 9.5 pKi 45
pKi 9.5 (Ki 2.9x10-10 M) [45]
Cl-IB-MECA Rn Agonist 9.5 pKi 59
pKi 9.5 (Ki 3.3x10-10 M) [59]
(R,S)-PHPNECA Hs Full agonist 9.4 pKi 98
pKi 9.4 [98]
2-phenylethylyl-adenosine derivative Hs Agonist 9.4 pKi 97
pKi 9.4 (Ki 4.4x10-10 M) [97]
MRS3558 Rn Agonist 9.0 pKi 59
pKi 9.0 (Ki 1x10-9 M) [59]
HEMADO Hs Agonist 9.0 pKi 54,98
pKi 9.0 (Ki 1.1x10-9 M) [54,98]
piclidenoson Hs Full agonist 8.7 – 9.2 pKi 25,31,55,94
pKi 8.7 – 9.2 [25,31,55,94]
MRS3558 Mm Agonist 8.8 pKi 59
pKi 8.8 (Ki 1.49x10-9 M) [59]
MRS5151 Hs Agonist 8.6 pKi 64
pKi 8.6 (Ki 2.38x10-9 M) [64]
2-hexynyl-NECA Hs Full agonist 8.6 pKi 98
pKi 8.6 [98]
MRS5698 Hs Agonist 8.5 pKi 87
pKi 8.5 [87]
Cl-IB-MECA Hs Full agonist 8.0 – 8.9 pKi 10,46,51
pKi 8.0 – 8.9 [10,46,51]
CP608,039 Hs Agonist 8.2 pKi 88
pKi 8.2 (Ki 5.8x10-9 M) [88]
PENECA Hs Full agonist 8.2 pKi 98
pKi 8.2 [98]
I-ABA Hs Full agonist 8.0 pKi 79
pKi 8.0 [79]
MRE 3008F20 Hs Full agonist 8.0 pKi 94
pKi 8.0 [94]
NECA Hs Full agonist 7.5 – 8.4 pKi 9,32,46,79,94,101
pKi 7.5 – 8.4 [9,32,46,79,94,101]
AB-MECA Hs Full agonist 7.7 pKi 55,94
pKi 7.7 [55,94]
MRS5151 Mm Agonist 7.6 pKi 64
pKi 7.6 (Ki 2.44x10-8 M) [64]
(R)-PIA Hs Full agonist 7.1 – 8.1 pKi 32,46,55,79,94
pKi 7.1 – 8.1 [32,46,55,79,94]
CCPA Hs Full agonist 7.4 pKi 45,55
pKi 7.4 [45,55]
apadenoson Hs Agonist 7.3 pKi 45
pKi 7.3 (Ki 4.5x10-8 M) [45]
cyclopentyladenosine Hs Full agonist 7.0 – 7.4 pKi 32,45,55,79
pKi 7.0 – 7.4 [32,45,55,79]
(S)-PIA Hs Full agonist 6.3 – 7.4 pKi 55,79,94
pKi 6.3 – 7.4 [55,79,94]
MPC-MECA Hs Full agonist 6.8 pKi 94
pKi 6.8 [94]
NECA Rn Full agonist 6.6 – 6.9 pKi 62,71
pKi 6.6 – 6.9 [62,71]
N(6)-cyclohexyladenosine Rn Agonist 6.8 pKi 89
pKi 6.8 (Ki 1.76x10-7 M) [89]
(R)-PIA Rn Full agonist 6.6 – 6.8 pKi 16,71
pKi 6.6 – 6.8 [16,71]
CCPA Rn Agonist 6.6 pKi 59
pKi 6.6 (Ki 2.37x10-7 M) [59]
CGS 21680 Hs Full agonist 6.0 – 7.2 pKi 9,32,45,55,94
pKi 6.0 – 7.2 [9,32,45,55,94]
adenosine Hs Agonist 6.5 pKi 28-29,101
pKi 6.5 (Ki 2.9x10-7 M) [28-29,101]
CGS 21680 Rn Agonist 6.2 pKi 59
pKi 6.2 (Ki 5.84x10-7 M) [59]
TCPA Hs Agonist 6.2 pKi 6
pKi 6.2 (Ki 6x10-7 M) [6]
binodenoson Hs Agonist 6.0 pKi 45
pKi 6.0 (Ki 9.03x10-7 M) [45]
GS9667 Hs Agonist <6.0 pKi 22
pKi <6.0 (Ki >1x10-6 M) [22]
N(6)-cyclohexyladenosine Hs Agonist 6.0 pKi 77
pKi 6.0 (Ki 1.025x10-6 M) [77]
2-chloroadenosine Rn Agonist 5.7 pKi 89
pKi 5.7 (Ki 1.89x10-6 M) [89]
2'-Me-CCPA Rn Agonist 5.3 pKi 27
pKi 5.3 (Ki 5x10-6 M) [27]
adenosine Rn Agonist 5.2 pKi 101
pKi 5.2 (Ki 6.5x10-6 M) [101]
BAY 60-6583 Hs Agonist <5.0 pKi 56
pKi <5.0 (Ki >1x10-5 M) [56]
regadenoson Hs Agonist <5.0 pKi 45
pKi <5.0 (Ki >1x10-5 M) [45]
adenosine Hs Agonist - - 101
[101]
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 Hs Antagonist 9.1 pKd 4,94
pKd 9.1 [4,94]
PSB-11 Hs Antagonist 8.3 pKd 67
pKd 8.3 (Kd 4.9x10-9 M) [67]
[3H]PSB-11 Hs Antagonist 8.3 pKd 67
pKd 8.3 [67]
KF26777 Hs Antagonist 9.7 pKi 78
pKi 9.7 (Ki 2x10-10 M) [78]
PSB-10 Hs Antagonist 9.4 pKi 69
pKi 9.4 (Ki 4.41x10-10 M) [69]
MRE 3010F20 Hs Antagonist 9.3 pKi 94
pKi 9.3 [94]
MRE 3008F20 Hs Antagonist 9.0 – 9.5 pKi 45,93-94
pKi 9.0 – 9.5 [45,93-94]
MRS1220 Hs Antagonist 8.2 – 9.2 pKi 46,53,84,104
pKi 8.2 – 9.2 (Ki 6.31x10-9 – 6.3x10-10 M) [46,53,84,104]
PSB-11 Hs Antagonist 8.6 pKi 73
pKi 8.6 (Ki 2.34x10-9 M) [73]
MRS1177 Hs Antagonist 8.5 pKi 53
pKi 8.5 [53]
VUF5574 Hs Antagonist 8.4 pKi 91
pKi 8.4 (Ki 4.03x10-9 M) [91]
MRS1186 Hs Antagonist 8.1 pKi 53
pKi 8.1 [53]
MRS1505 Hs Antagonist 8.1 pKi 58
pKi 8.1 [58]
LUF7602 Hs Antagonist 8.0 pKi 103
pKi 8.0 (Ki 1x10-8 M) [103]
Description: Displacement of [3H]PSB-11 binding from the hA3AR (in membranes from stably transfected CHO cells) following preincubation for 4 h,
VUF8504 Hs Antagonist 7.8 pKi 90
pKi 7.8 [90]
xanthine amine congener Rn Antagonist 7.7 pKi 71
pKi 7.7 [71]
I-ABOPX Hs Antagonist 7.7 pKi 79
pKi 7.7 [79]
MRS1476 Hs Antagonist 7.7 pKi 58
pKi 7.7 [58]
MRS1523 Hs Antagonist 7.7 pKi 58
pKi 7.7 (Ki 1.99x10-8 M) [58]
MRS1191 Hs Antagonist 7.5 pKi 46-47,59
pKi 7.5 [46-47,59]
MRS1486 Hs Antagonist 7.5 pKi 58
pKi 7.5 [58]
CGS 15943 Hs Antagonist 7.0 – 7.9 pKi 53,55,72,94
pKi 7.0 – 7.9 [53,55,72,94]
BW-A1433 Rn Antagonist 7.4 pKi 71
pKi 7.4 [71]
BW-A1433 Hs Antagonist 7.3 pKi 79
pKi 7.3 [79]
xanthine amine congener Hs Antagonist 7.0 – 7.4 pKi 55,79,94
pKi 7.0 – 7.4 [55,79,94]
MRS1097 Hs Antagonist 7.0 pKi 46,92
pKi 7.0 [46,92]
MRS1523 Rn Antagonist 6.9 pKi 59
pKi 6.9 (Ki 1.13x10-7 M) [59]
VUF8507 Hs Antagonist 6.7 pKi 90
pKi 6.7 [90]
derenofylline Hs Antagonist 6.7 pKi 48
pKi 6.7 (Ki 2x10-7 M) [48]
MRS1042 Hs Antagonist 6.5 pKi 49
pKi 6.5 [49]
MRS1041 Hs Antagonist 6.4 pKi 49
pKi 6.4 [49]
MRS1754 Hs Antagonist 6.2 pKi 52
pKi 6.2 (Ki 5.7x10-7 M) [52]
MRS1067 Hs Antagonist 6.2 pKi 46,49
pKi 6.2 [46,49]
LUF5981 Hs Antagonist 6.2 pKi 12
pKi 6.2 (Ki 6.37x10-7 M) [12]
MRS1523 Mm Antagonist 6.1 pKi 59
pKi 6.1 (Ki 7.31x10-7 M) [59]
ZM-241385 Hs Antagonist 6.1 pKi 45
pKi 6.1 (Ki 7.43x10-7 M) [45]
MRS1093 Hs Antagonist 6.1 pKi 49
pKi 6.1 [49]
MRS1088 Hs Antagonist 6.1 pKi 49
pKi 6.1 [49]
DPCPX Hs Antagonist 5.4 – 6.6 pKi 2,38,55,79,94,99
pKi 5.4 – 6.6 (Ki 3.96x10-6 – 2.43x10-7 M) [2,38,55,79,94,99]
MRE 2029F20 Hs Antagonist <6.0 pKi 5
pKi <6.0 (Ki >1x10-6 M) [5]
vipadenant Hs Antagonist 6.0 pKi 34
pKi 6.0 (Ki 1.005x10-6 M) [34]
ST-1535 Hs Antagonist <6.0 pKi 65
pKi <6.0 (Ki >1x10-6 M) [65]
preladenant Hs Antagonist <6.0 pKi 68
pKi <6.0 (Ki >1x10-6 M) [68]
ATL802 Hs Antagonist <6.0 pKi 52
pKi <6.0 (Ki >1x10-6 M) [52]
DPCPX Rn Antagonist 4.4 – 7.6 pKi 2,71,99
pKi 4.4 – 7.6 [2,71,99]
LAS38096 Hs Antagonist 6.0 pKi 20,96
pKi 6.0 (Ki 1.043x10-6 M) [20,96]
CVT-6883 Hs Antagonist 6.0 pKi 21
pKi 6.0 (Ki 1.07x10-6 M) [21]
SCH 58261 Hs Antagonist 5.9 pKi 45
pKi 5.9 (Ki 1.2x10-6 M) [45]
MRS928 Hs Antagonist 5.9 pKi 49
pKi 5.9 [49]
MRS1191 Rn Antagonist 5.8 pKi 58-59
pKi 5.8 [58-59]
dexniguldipine Hs Antagonist 5.7 pKi 92
pKi 5.7 [92]
PSB36 Hs Antagonist 5.6 pKi 99
pKi 5.6 (Ki 2.3x10-6 M) [99]
galangin Hs Antagonist 5.5 pKi 49
pKi 5.5 [49]
sakuranetin Hs Antagonist 5.5 pKi 49
pKi 5.5 [49]
nicardipine Hs Antagonist 5.5 pKi 92
pKi 5.5 [92]
rolofylline Hs Antagonist 5.4 pKi 50
pKi 5.4 (Ki 4.39x10-6 M) [50]
istradefylline Hs Antagonist 5.3 pKi 30
pKi 5.3 (Ki 4.47x10-6 M) [30]
PSB36 Rn Antagonist 5.2 pKi 99
pKi 5.2 (Ki 6.5x10-6 M) [99]
SCH442416 Hs Antagonist <5.0 pKi 45
pKi <5.0 (Ki >1x10-5 M) [45]
PSB603 Hs Antagonist <5.0 pKi 8
pKi <5.0 (Ki >1x10-5 M) [8]
PSB1115 Hs Antagonist <5.0 pKi 38
pKi <5.0 (Ki >1x10-5 M) [38]
tonapofylline Hs Antagonist <5.0 pKi 50
pKi <5.0 (Ki >1x10-5 M) [50]
FK-453 Hs Antagonist 5.0 pKi 45
pKi 5.0 (Ki 1x10-5 M) [45]
CSC Rn Antagonist <5.0 pKi 89
pKi <5.0 (Ki >1x10-5 M) [89]
MSX-2 Hs Antagonist <5.0 pKi 81
pKi <5.0 (Ki >1x10-5 M) [81]
ATL802 Mm Antagonist <5.0 pKi 52
pKi <5.0 (Ki >1x10-5 M) [52]
caffeine Hs Antagonist 4.9 pKi 43
pKi 4.9 (Ki 1.33x10-5 M) [43]
flavone Hs Antagonist 4.8 pKi 49
pKi 4.8 [49]
theophylline 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 Hs Antagonist 4.3 pKi 49
pKi 4.3