Target Information

Target General Infomation
Target ID
T36059
Former ID
TTDS00189
Target Name
Adenosine A3 receptor
Gene Name
ADORA3
Synonyms
A3 Adenosine receptor; A3AR; Adenosine 3 receptor; Adenosine receptor A3A; ADORA3
Target Type
Clinical Trial
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Hepatocellular carcinoma; Hepatitis C virus infection [ICD9: 001-139, 070.4, 070.5, 070.70, 155, 573.3; ICD10: A00-B99, B17.1, B18.2, C22.0, K75.9]
Ischemia [ICD9: 459.89; ICD10: I99.8]
Inflammation [ICD10: E08-E13, E10.2, E11, E11.2, E13.2, I73.9, I80-I82, N00-N29, G89]
Multiple scierosis [ICD9: 340; ICD10: G35]
Malaria [ICD10: B54]
Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. possible role in reproduction.
BioChemical Class
GPCR rhodopsin
Target Validation
T36059
UniProt ID
P0DMS8
Sequence
MPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYFIVSLALADIA
VGVLVMPLAIVVSLGITIHFYSCLFMTCLLLIFTHASIMSLLAIAVDRYLRVKLTVRYKR
VTTHRRIWLALGLCWLVSFLVGLTPMFGWNMKLTSEYHRNVTFLSCQFVSVMRMDYMVYF
SFLTWIFIPLVVMCAIYLDIFYIIRNKLSLNLSNSKETGAFYGREFKTAKSLFLVLFLFA
LSWLPLSIINCIIYFNGEVPQLVLYMGILLSHANSMMNPIVYAYKIKKFKETYLLILKAC
VVCHPSDSLDTSIEKNSE
Drugs and Mode of Action
Drug(s) IB-MECA Drug Info Phase 3 Cancer [1], [2], [3]
Tonapofylline Drug Info Phase 2/3 Discovery agent [4], [5]
NITD609 Drug Info Phase 2 Malaria [6]
CF102 Drug Info Phase 1/2 Hepatocellular carcinoma; Hepatitis C virus infection [7]
GBR-12909 Drug Info Phase 1 Discovery agent [8]
SCH-442416 Drug Info Phase 1 Discovery agent [9], [10]
CF502 Drug Info Preclinical Inflammation [11], [7]
CF602 Drug Info Preclinical Inflammation [7]
BEMESETRON Drug Info Discontinued in Phase 3 Discovery agent [12]
DIZOCILPINE Drug Info Terminated Cerebrovascular ischaemia [13], [14]
METHYLTHIOADENOSINE Drug Info Terminated Multiple scierosis [15]
METRIFUDIL Drug Info Terminated Discovery agent [16], [17]
Inhibitor (+)-BUTACLAMOL Drug Info [18]
(2R,3S)-3-(6-Amino-purin-9-yl)-nonan-2-ol Drug Info [19]
1,2-dihydro-2-oxoquinazoline-4-carboxyanilide Drug Info [20]
1-(2-(diethylamino)quinazolin-4-yl)-3-phenylurea Drug Info [21]
1-Allyl-3,7-dihydro-purine-2,6-dione Drug Info [22]
1-Benzyl-1H-1,3,4b,9-tetraaza-fluorene-2,4-dione Drug Info [23]
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione Drug Info [22]
1-Butyl-3,7-dihydro-purine-2,6-dione Drug Info [22]
1-Cyclopentyl-3,7-dihydro-purine-2,6-dione Drug Info [22]
1-Phenethyl-3,7-dihydro-purine-2,6-dione Drug Info [22]
1-phenyl-3-(2-(pyridin-2-yl)quinazolin-4-yl)urea Drug Info [21]
1-phenyl-3-(2-(pyridin-3-yl)quinazolin-4-yl)urea Drug Info [21]
1-phenyl-3-(3-(pyridin-2-yl)isoquinolin-1-yl)urea Drug Info [21]
1-phenyl-3-(quinazolin-4-yl)urea Drug Info [21]
1-Prop-2-ynyl-3,7-dihydro-purine-2,6-dione Drug Info [22]
1-Propyl-3,7-dihydro-purine-2,6-dione Drug Info [22]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine Drug Info [24]
2,6,8-triphenyl-9H-purine Drug Info [25]
2,6-bis(4-chlorophenyl)-9H-purine Drug Info [25]
2,6-bis(4-methoxyphenyl)-9H-purine Drug Info [25]
2,6-bis(4-tolyl)-9H-purine Drug Info [25]
2,6-diphenyl-1-deazapurine Drug Info [26]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine Drug Info [26]
2,6-diphenyl-8-ethyl-1-deazapurine Drug Info [26]
2,6-diphenyl-8-methyl-1-deazapurine Drug Info [26]
2,6-diphenyl-8-tButyl-1-deazapurine Drug Info [26]
2,6-diphenyl-9H-purine Drug Info [25]
2,6-dphenyl-8-propyl-1-deazapurine Drug Info [26]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [27]
2-(1H-imidazo[4,5-c]pyridin-2-yl)quinoxaline Drug Info [28]
2-(2''-indolylethyloxy)adenosine Drug Info [29]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine Drug Info [29]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine Drug Info [29]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine Drug Info [29]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine Drug Info [29]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine Drug Info [29]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine Drug Info [29]
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine Drug Info [29]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine Drug Info [29]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine Drug Info [29]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine Drug Info [29]
2-(3''-(benzoimidazole-1''-yl)ethyloxy)adenosine Drug Info [29]
2-(3''-(benzotriazole-1''-yl)ethyloxy)adenosine Drug Info [29]
2-(3''-indolylethyloxy)adenosine Drug Info [29]
2-(3''-pyrrolylethyloxy)adenosine Drug Info [29]
2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [28]
2-(4-chlorophenyl)-6-phenyl-9H-purine Drug Info [25]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline Drug Info [28]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine Drug Info [30]
2-(4-methoxyphenyl)-6-phenyl-9H-purine Drug Info [25]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [27]
2-(4-nitro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [28]
2-(5-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [28]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine Drug Info [30]
2-(hex-1-ynyl)-N6-methoxyadenosine Drug Info [30]
2-acetylaminoquinazoline-4-carboxyanilide Drug Info [20]
2-aminoquinazoline-4-carboxy-(4-bromophenyl)amide Drug Info [20]
2-aminoquinazoline-4-carboxyanilide Drug Info [20]
2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine Drug Info [31]
2-benzoylaminoquinazoline-4-carboxyanilide Drug Info [20]
2-benzyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Drug Info [32]
2-chloro-2'-C-methyl-tecadenoson Drug Info [33]
2-chloro-N6-cyclopentyladenosine Drug Info [33]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info [34]
2-ethynyl-N6-methoxyadenosine Drug Info [30]
2-Phenyl-2H-pyrazolo[4,3-c]quinoline Drug Info [35]
2-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one Drug Info [36]
2-phenylpropoxyadenosine Drug Info [29]
2-tolyl-6-phenyl-9H-purine Drug Info [25]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine Drug Info [30]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine Drug Info [30]
3,5,7-Triethoxy-2-phenyl-chromen-4-one Drug Info [37]
3,5,7-Trimethoxy-2-phenyl-chromen-4-one Drug Info [38]
3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one Drug Info [27]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info [39]
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione Drug Info [22]
3-noradamantyl-1,3-dipropylxanthine Drug Info [40]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [41]
4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one Drug Info [37]
4-Methoxy-2-phenyl-2H-pyrazolo[4,3-c]quinoline Drug Info [35]
4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide Drug Info [42]
5,6,7-Trimethyl-2-p-tolyl-chromen-4-one Drug Info [38]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol Drug Info [43]
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol Drug Info [26]
5-Butyl-8-phenyl-3H-[1,2,4]triazolo[5,1-i]purine Drug Info [44]
6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine Drug Info [29]
6-guanidino-2-(3''-indolylethyloxy)adenosine Drug Info [29]
6-Hydroxy-5,7-dimethyl-beta-carboline Drug Info [43]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine Drug Info [45]
8-Bromo-9-(sec-butyl)-9H-adenine Drug Info [45]
8-Bromo-9-cyclobutyl-9H-adenine Drug Info [45]
8-Bromo-9-cyclohexyl-9H-adenine Drug Info [45]
8-Bromo-9-cyclopentyl-9H-adenine Drug Info [45]
8-bromo-9-isobutyl-9H-purin-6-amine Drug Info [46]
8-Bromo-9-isopropyl-9H-adenine Drug Info [45]
8-Hydroxy-5,7,9-trimethyl-delta-carboline Drug Info [43]
8-Hydroxy-7,9-dimethyl-delta-carboline Drug Info [43]
8-PHENYL THEOPHYLLINE Drug Info [39]
8-propyl-2,6-diphenyl-9H-purine Drug Info [25]
9-Cyclopentyl-9H-adenine Drug Info [45]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine Drug Info [47]
9H-purine derivative Drug Info [18]
BEMESETRON Drug Info [18]
CIRSIMARITIN Drug Info [38]
Cyclohexyl-(2-phenoxy-9H-purin-6-yl)-amine Drug Info [48]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine Drug Info [48]
DIZOCILPINE Drug Info [18]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate Drug Info [49]
GALANGIN Drug Info [38]
GBR-12909 Drug Info [18]
GLUTAMATE Drug Info [18]
GNF-PF-2224 Drug Info [50]
Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide Drug Info [51]
KAINATE Drug Info [18]
L-249313 Drug Info [52]
LUF-5417 Drug Info [49]
LUF-5433 Drug Info [49]
LUF-5767 Drug Info [51]
LUF-5816 Drug Info [26]
LUF-5956 Drug Info [25]
LUF-5957 Drug Info [25]
LUF-5962 Drug Info [25]
LUF-5978 Drug Info [26]
LUF-5980 Drug Info [26]
LUF-5981 Drug Info [26]
MESULERGINE Drug Info [18]
METHOCTRAMINE Drug Info [18]
METHYLTHIOADENOSINE Drug Info [53]
METRIFUDIL Drug Info [54]
N*2*-Benzyl-N*6*-cyclohexyl-9H-purine-2,6-diamine Drug Info [48]
N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine Drug Info [48]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info [48]
N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info [48]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide Drug Info [51]
N-(2,6-diphenylpyrimidin-4-yl)acetamide Drug Info [51]
N-(2,6-diphenylpyrimidin-4-yl)benzamide Drug Info [51]
N-(2,6-diphenylpyrimidin-4-yl)butyramide Drug Info [51]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide Drug Info [51]
N-(2,6-diphenylpyrimidin-4-yl)propionamide Drug Info [51]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide Drug Info [55]
N-(4,5-diphenylpyrimidin-2-yl)acetamide Drug Info [51]
N-(4,6-diphenylpyrimidin-2-yl)-4-chlorobenzamide Drug Info [51]
N-(4,6-diphenylpyrimidin-2-yl)propionamide Drug Info [51]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide Drug Info [49]
N6-((+/-)-endo-norborn-2-yl)adenosine Drug Info [24]
N6-(3-Iodobenzyl)-2'-O-methyladenosine Drug Info [56]
N6-CYCLOPENTYLADENOSINE Drug Info [57]
N6-methoxy-2-phenylethynyladenosine Drug Info [30]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine Drug Info [30]
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine Drug Info [30]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine Drug Info [30]
N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine Drug Info [30]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine Drug Info [30]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine Drug Info [30]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine Drug Info [30]
NECA Drug Info [58]
NIPECOTIC ACID Drug Info [18]
NITD609 Drug Info [59]
NSC-19028 Drug Info [38]
NSC-407228 Drug Info [38]
OSIP-339391 Drug Info [46]
R-N6-(phenylisopropyl)adenosine Drug Info [29]
REVERSINE Drug Info [48]
SB-298 Drug Info [60]
SCH-442416 Drug Info [61]
SEROTONIN Drug Info [18]
Tonapofylline Drug Info [49]
VUF-8504 Drug Info [21]
VUF-8507 Drug Info [21]
[1,2,4]triazolo[1,5-a]quinoxalin-4(5H)-one Drug Info [62]
Agonist (R)-PIA Drug Info [63]
(R,S)-PHPNECA Drug Info [64]
(S)-PIA Drug Info [65]
2'-Me-CCPA Drug Info [66]
2-chloroadenosine Drug Info [67]
2-phenylethylyl-adenosine derivative Drug Info [68]
3-IB-MECA Drug Info [69]
AB-MECA Drug Info [65]
BAY 60-6583 Drug Info [70]
CF102 Drug Info [7]
CF502 Drug Info [7]
CF602 Drug Info [7]
CP608,039 Drug Info [71]
HEMADO Drug Info [72]
I-ABA Drug Info [73]
IB-MECA Drug Info [74]
MPC-MECA Drug Info [65]
MRE 3008F20 Drug Info [65]
MRS5151 Drug Info [75]
MRS5698 Drug Info [76]
N(6)-cyclohexyladenosine Drug Info [77]
PENECA Drug Info [64]
TCPA Drug Info [78]
[125I]AB-MECA Drug Info [65]
[125I]APNEA Drug Info [79]
[3H]HEMADO Drug Info [72]
[3H]NECA Drug Info [80]
Antagonist ACN-1052 Drug Info [81]
ATL802 Drug Info [82]
CSC Drug Info [67]
flavone Drug Info [37]
I-ABOPX Drug Info [73]
KF26777 Drug Info [83]
MRE 2029F20 Drug Info [84]
MRE 3010F20 Drug Info [65]
MRS-1220 Drug Info [85]
MRS1041 Drug Info [37]
MRS1042 Drug Info [37]
MRS1067 Drug Info [86]
MRS1088 Drug Info [37]
MRS1093 Drug Info [37]
MRS1097 Drug Info [87]
MRS1177 Drug Info [88]
MRS1186 Drug Info [88]
MRS1191 Drug Info [81]
MRS1476 Drug Info [89]
MRS1486 Drug Info [89]
MRS1505 Drug Info [89]
MRS1523 Drug Info [89]
MRS928 Drug Info [37]
PSB-10 Drug Info [90]
PSB-11 Drug Info [91]
PSB36 Drug Info [92]
PSB603 Drug Info [60]
sakuranetin Drug Info [37]
visnagin Drug Info [37]
VUF5574 Drug Info [93]
xanthine amine congener Drug Info [65]
[3H]MRE 3008F20 Drug Info [94]
[3H]PSB-11 Drug Info [91]
Enhancer LUF-5833 Drug Info [81]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
Reactome Adenosine P1 receptors
G alpha (i) signalling events
WikiPathways Nucleotide GPCRs
GPCRs, Class A Rhodopsin-like
GPCRs, Other
References
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REF 2CF101, an agonist to the A3 adenosine receptor, enhances the chemotherapeutic effect of 5-fluorouracil in a colon carcinoma murine model. Neoplasia. 2005 Jan;7(1):85-90.
REF 3Methotrexate enhances the anti-inflammatory effect of CF101 via up-regulation of the A3 adenosine receptor expression. Arthritis Res Ther. 2006;8(6):R169.
REF 4ClinicalTrials.gov (NCT00709865) Phase 2b Study to Assess the Safety and Tolerability of IV Tonapofylline in Subjects With Acute Decompensated Heart Failure (ADHF) and Renal Insufficiency. U.S. National Institutes of Health.
REF 5(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5605).
REF 6Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035252)
REF 72011 Pipeline of Can-Fite BioPharm.
REF 8ClinicalTrials.gov (NCT00218049) Interaction Between Vanoxerine (GBR 12909) and Cocaine in Cocaine Dependent Individuals. U.S. National Institutes of Health.
REF 9ClinicalTrials.gov (NCT00531193) Using PET Scans to Study Brain Receptor Occupancy of BIIB014 in Healthy Male Volunteers. U.S. National Institutes of Health.
REF 10(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3283).
REF 11(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5601).
REF 12Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000675)
REF 13(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2403).
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REF 17Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006749)
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