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]
Inflammation [ICD10: E08-E13, E10.2, E11, E11.2, E13.2, I73.9, I80-I82, N00-N29, G89]
Ischemia [ICD9: 459.89; ICD10: I99.8]
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
Sequence
MPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYFIVSLALADIA
VGVLVMPLAIVVSLGITIHFYSCLFMTCLLLIFTHASIMSLLAIAVDRYLRVKLTVRYKR
VTTHRRIWLALGLCWLVSFLVGLTPMFGWNMKLTSEYHRNVTFLSCQFVSVMRMDYMVYF
SFLTWIFIPLVVMCAIYLDIFYIIRNKLSLNLSNSKETGAFYGREFKTAKSLFLVLFLFA
LSWLPLSIINCIIYFNGEVPQLVLYMGILLSHANSMMNPIVYAYKIKKFKETYLLILKAC
VVCHPSDSLDTSIEKNSE
Drugs and Mode of Action
Drug(s) IB-MECA Drug Info Phase 3 Cancer [467554], [527444], [528521]
Tonapofylline Drug Info Phase 2/3 Discovery agent [522369], [540973]
NITD609 Drug Info Phase 2 Malaria [549327]
CF102 Drug Info Phase 1/2 Hepatocellular carcinoma; Hepatitis C virus infection [550529]
GBR-12909 Drug Info Phase 1 Discovery agent [521723]
SCH-442416 Drug Info Phase 1 Discovery agent [522117], [540246]
CF502 Drug Info Preclinical Inflammation [540970], [550529]
CF602 Drug Info Preclinical Inflammation [550529]
BEMESETRON Drug Info Discontinued in Phase 3 Discovery agent [544703]
DIZOCILPINE Drug Info Terminated Cerebrovascular ischaemia [539532], [544717]
METHYLTHIOADENOSINE Drug Info Terminated Multiple scierosis [544778]
METRIFUDIL Drug Info Terminated Discovery agent [467595], [546171]
Inhibitor (+)-BUTACLAMOL Drug Info [527823]
(2R,3S)-3-(6-Amino-purin-9-yl)-nonan-2-ol Drug Info [533722]
1,2-dihydro-2-oxoquinazoline-4-carboxyanilide Drug Info [529186]
1-(2-(diethylamino)quinazolin-4-yl)-3-phenylurea Drug Info [528290]
1-Allyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
1-Benzyl-1H-1,3,4b,9-tetraaza-fluorene-2,4-dione Drug Info [526388]
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
1-Butyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
1-Cyclopentyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
1-Phenethyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
1-phenyl-3-(2-(pyridin-2-yl)quinazolin-4-yl)urea Drug Info [528290]
1-phenyl-3-(2-(pyridin-3-yl)quinazolin-4-yl)urea Drug Info [528290]
1-phenyl-3-(3-(pyridin-2-yl)isoquinolin-1-yl)urea Drug Info [528290]
1-phenyl-3-(quinazolin-4-yl)urea Drug Info [528290]
1-Prop-2-ynyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
1-Propyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine Drug Info [530035]
2,6,8-triphenyl-9H-purine Drug Info [528192]
2,6-bis(4-chlorophenyl)-9H-purine Drug Info [528192]
2,6-bis(4-methoxyphenyl)-9H-purine Drug Info [528192]
2,6-bis(4-tolyl)-9H-purine Drug Info [528192]
2,6-diphenyl-1-deazapurine Drug Info [528673]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine Drug Info [528673]
2,6-diphenyl-8-ethyl-1-deazapurine Drug Info [528673]
2,6-diphenyl-8-methyl-1-deazapurine Drug Info [528673]
2,6-diphenyl-8-tButyl-1-deazapurine Drug Info [528673]
2,6-diphenyl-9H-purine Drug Info [528192]
2,6-dphenyl-8-propyl-1-deazapurine Drug Info [528673]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [529313]
2-(1H-imidazo[4,5-c]pyridin-2-yl)quinoxaline Drug Info [527933]
2-(2''-indolylethyloxy)adenosine Drug Info [528748]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(benzoimidazole-1''-yl)ethyloxy)adenosine Drug Info [528748]
2-(3''-(benzotriazole-1''-yl)ethyloxy)adenosine Drug Info [528748]
2-(3''-indolylethyloxy)adenosine Drug Info [528748]
2-(3''-pyrrolylethyloxy)adenosine Drug Info [528748]
2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [527933]
2-(4-chlorophenyl)-6-phenyl-9H-purine Drug Info [528192]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline Drug Info [527933]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine Drug Info [528684]
2-(4-methoxyphenyl)-6-phenyl-9H-purine Drug Info [528192]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [529313]
2-(4-nitro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [527933]
2-(5-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info [527933]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine Drug Info [528684]
2-(hex-1-ynyl)-N6-methoxyadenosine Drug Info [528684]
2-acetylaminoquinazoline-4-carboxyanilide Drug Info [529186]
2-aminoquinazoline-4-carboxy-(4-bromophenyl)amide Drug Info [529186]
2-aminoquinazoline-4-carboxyanilide Drug Info [529186]
2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine Drug Info [528559]
2-benzoylaminoquinazoline-4-carboxyanilide Drug Info [529186]
2-benzyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Drug Info [528969]
2-chloro-2'-C-methyl-tecadenoson Drug Info [529098]
2-chloro-N6-cyclopentyladenosine Drug Info [529098]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info [529419]
2-ethynyl-N6-methoxyadenosine Drug Info [528684]
2-Phenyl-2H-pyrazolo[4,3-c]quinoline Drug Info [527649]
2-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one Drug Info [530372]
2-phenylpropoxyadenosine Drug Info [528748]
2-tolyl-6-phenyl-9H-purine Drug Info [528192]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine Drug Info [528684]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine Drug Info [528684]
3,5,7-Triethoxy-2-phenyl-chromen-4-one Drug Info [534145]
3,5,7-Trimethoxy-2-phenyl-chromen-4-one Drug Info [534098]
3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one Drug Info [529313]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info [533542]
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione Drug Info [526332]
3-noradamantyl-1,3-dipropylxanthine Drug Info [528544]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one Drug Info [534145]
4-Methoxy-2-phenyl-2H-pyrazolo[4,3-c]quinoline Drug Info [527649]
4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide Drug Info [526099]
5,6,7-Trimethyl-2-p-tolyl-chromen-4-one Drug Info [534098]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol Drug Info [529305]
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol Drug Info [528673]
5-Butyl-8-phenyl-3H-[1,2,4]triazolo[5,1-i]purine Drug Info [527055]
6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine Drug Info [528748]
6-guanidino-2-(3''-indolylethyloxy)adenosine Drug Info [528748]
6-Hydroxy-5,7-dimethyl-beta-carboline Drug Info [529305]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine Drug Info [530014]
8-Bromo-9-(sec-butyl)-9H-adenine Drug Info [530014]
8-Bromo-9-cyclobutyl-9H-adenine Drug Info [530014]
8-Bromo-9-cyclohexyl-9H-adenine Drug Info [530014]
8-Bromo-9-cyclopentyl-9H-adenine Drug Info [530014]
8-bromo-9-isobutyl-9H-purin-6-amine Drug Info [530966]
8-Bromo-9-isopropyl-9H-adenine Drug Info [530014]
8-Hydroxy-5,7,9-trimethyl-delta-carboline Drug Info [529305]
8-Hydroxy-7,9-dimethyl-delta-carboline Drug Info [529305]
8-PHENYL THEOPHYLLINE Drug Info [533542]
8-propyl-2,6-diphenyl-9H-purine Drug Info [528192]
9-Cyclopentyl-9H-adenine Drug Info [530014]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine Drug Info [526104]
9H-purine derivative Drug Info [527823]
BEMESETRON Drug Info [527823]
CIRSIMARITIN Drug Info [534098]
Cyclohexyl-(2-phenoxy-9H-purin-6-yl)-amine Drug Info [527647]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine Drug Info [527647]
DIZOCILPINE Drug Info [527823]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate Drug Info [530752]
GALANGIN Drug Info [534098]
GBR-12909 Drug Info [527823]
GLUTAMATE Drug Info [527823]
GNF-PF-2224 Drug Info [531209]
Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide Drug Info [527331]
KAINATE Drug Info [527823]
L-249313 Drug Info [525676]
LUF-5417 Drug Info [530752]
LUF-5433 Drug Info [530752]
LUF-5767 Drug Info [527331]
LUF-5816 Drug Info [528673]
LUF-5956 Drug Info [528192]
LUF-5957 Drug Info [528192]
LUF-5962 Drug Info [528192]
LUF-5978 Drug Info [528673]
LUF-5980 Drug Info [528673]
LUF-5981 Drug Info [528673]
MESULERGINE Drug Info [527823]
METHOCTRAMINE Drug Info [527823]
METHYLTHIOADENOSINE Drug Info [527040]
METRIFUDIL Drug Info [527473]
N*2*-Benzyl-N*6*-cyclohexyl-9H-purine-2,6-diamine Drug Info [527647]
N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine Drug Info [527647]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info [527647]
N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info [527647]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)acetamide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)benzamide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)butyramide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide Drug Info [527331]
N-(2,6-diphenylpyrimidin-4-yl)propionamide Drug Info [527331]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide Drug Info [530694]
N-(4,5-diphenylpyrimidin-2-yl)acetamide Drug Info [527331]
N-(4,6-diphenylpyrimidin-2-yl)-4-chlorobenzamide Drug Info [527331]
N-(4,6-diphenylpyrimidin-2-yl)propionamide Drug Info [527331]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide Drug Info [530752]
N6-((+/-)-endo-norborn-2-yl)adenosine Drug Info [530035]
N6-(3-Iodobenzyl)-2'-O-methyladenosine Drug Info [528886]
N6-CYCLOPENTYLADENOSINE Drug Info [527930]
N6-methoxy-2-phenylethynyladenosine Drug Info [528684]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine Drug Info [528684]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine Drug Info [528684]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine Drug Info [528684]
NECA Drug Info [525473]
NIPECOTIC ACID Drug Info [527823]
NITD609 Drug Info [531146]
NSC-19028 Drug Info [534098]
NSC-407228 Drug Info [534098]
OSIP-339391 Drug Info [530966]
R-N6-(phenylisopropyl)adenosine Drug Info [528748]
REVERSINE Drug Info [527647]
SB-298 Drug Info [530243]
SCH-442416 Drug Info [531130]
SEROTONIN Drug Info [527823]
Tonapofylline Drug Info [530752]
VUF-8504 Drug Info [528290]
VUF-8507 Drug Info [528290]
[1,2,4]triazolo[1,5-a]quinoxalin-4(5H)-one Drug Info [527915]
Agonist (R)-PIA Drug Info [534039]
(R,S)-PHPNECA Drug Info [526375]
(S)-PIA Drug Info [525758]
2'-Me-CCPA Drug Info [534615]
2-chloroadenosine Drug Info [533853]
2-phenylethylyl-adenosine derivative Drug Info [530458]
3-IB-MECA Drug Info [537920]
AB-MECA Drug Info [525758]
BAY 60-6583 Drug Info [528950]
CF102 Drug Info [550529]
CF502 Drug Info [550529]
CF602 Drug Info [550529]
CP608,039 Drug Info [526692]
HEMADO Drug Info [528546]
I-ABA Drug Info [533946]
IB-MECA Drug Info [535470]
MPC-MECA Drug Info [525758]
MRE 3008F20 Drug Info [525758]
MRS5151 Drug Info [529435]
MRS5698 Drug Info [531894]
N(6)-cyclohexyladenosine Drug Info [534114]
PENECA Drug Info [526375]
TCPA Drug Info [526590]
[125I]AB-MECA Drug Info [525758]
[125I]APNEA Drug Info [526745]
[3H]HEMADO Drug Info [528546]
[3H]NECA Drug Info [526188]
Antagonist ACN-1052 Drug Info [543555]
ATL802 Drug Info [525731]
CSC Drug Info [533853]
flavone Drug Info [534145]
I-ABOPX Drug Info [533946]
KF26777 Drug Info [526356]
MRE 2029F20 Drug Info [526981]
MRE 3010F20 Drug Info [525758]
MRS-1220 Drug Info [534925]
MRS1041 Drug Info [534145]
MRS1042 Drug Info [534145]
MRS1067 Drug Info [534506]
MRS1088 Drug Info [534145]
MRS1093 Drug Info [534145]
MRS1097 Drug Info [534159]
MRS1177 Drug Info [534241]
MRS1186 Drug Info [534241]
MRS1191 Drug Info [543555]
MRS1476 Drug Info [534684]
MRS1486 Drug Info [534684]
MRS1505 Drug Info [534684]
MRS1523 Drug Info [534684]
MRS928 Drug Info [534145]
PSB-10 Drug Info [526390]
PSB-11 Drug Info [526260]
PSB36 Drug Info [528362]
PSB603 Drug Info [530243]
sakuranetin Drug Info [534145]
visnagin Drug Info [534145]
VUF5574 Drug Info [525784]
xanthine amine congener Drug Info [525758]
[3H]MRE 3008F20 Drug Info [525709]
[3H]PSB-11 Drug Info [526260]
Enhancer LUF-5833 Drug Info [543555]
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
Ref 467554(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: 422).
Ref 467595(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: 426).
Ref 521723ClinicalTrials.gov (NCT00218049) Interaction Between Vanoxerine (GBR 12909) and Cocaine in Cocaine Dependent Individuals. U.S. National Institutes of Health.
Ref 522117ClinicalTrials.gov (NCT00531193) Using PET Scans to Study Brain Receptor Occupancy of BIIB014 in Healthy Male Volunteers. U.S. National Institutes of Health.
Ref 522369ClinicalTrials.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 527444CF101, 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 528521Methotrexate enhances the anti-inflammatory effect of CF101 via up-regulation of the A3 adenosine receptor expression. Arthritis Res Ther. 2006;8(6):R169.
Ref 539532(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).
Ref 540246(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 540970(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 540973(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 544703Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000675)
Ref 544717Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000713)
Ref 544778Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000987)
Ref 546171Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006749)
Ref 549327Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035252)
Ref 5505292011 Pipeline of Can-Fite BioPharm.
Ref 525473J Med Chem. 1999 Apr 22;42(8):1384-92.5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.
Ref 525676Bioorg Med Chem Lett. 2000 Jan 3;10(1):31-4.The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family.
Ref 525709Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors. Bioorg Med Chem Lett. 2000 Feb 7;10(3):209-11.
Ref 525731Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. J Med Chem. 2000 Mar 23;43(6):1165-72.
Ref 525758[(3)H]MRE 3008F20: a novel antagonist radioligand for the pharmacological and biochemical characterization of human A(3) adenosine receptors. Mol Pharmacol. 2000 May;57(5):968-75.
Ref 525784J Med Chem. 2000 Jun 1;43(11):2227-38.Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.
Ref 526099Bioorg Med Chem Lett. 2001 Aug 6;11(15):2017-9.Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
Ref 526104Bioorg Med Chem Lett. 2001 Jul 23;11(14):1931-4.Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.
Ref 526188Inhibition of human mast cell activation with the novel selective adenosine A(2B) receptor antagonist 3-isobutyl-8-pyrrolidinoxanthine (IPDX)(2). Biochem Pharmacol. 2001 Nov 1;62(9):1163-73.
Ref 526260[(3)H]8-Ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one ([(3)H]PSB-11), a novel high-affinity antagonist radioligand for human A(3) adenosine receptors. Bioorg Med Chem Lett. 2002 Feb 11;12(3):501-3.
Ref 526332J Med Chem. 2002 May 23;45(11):2131-8.Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
Ref 526356KF26777 (2-(4-bromophenyl)-7,8-dihydro-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one dihydrochloride), a new potent and selective adenosine A3 receptor antagonist. Eur J Pharmacol. 2002 May 31;444(3):133-41.
Ref 526375N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands. J Med Chem. 2002 Jul 18;45(15):3271-9.
Ref 526388J Med Chem. 2002 Aug 1;45(16):3337-44.Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.
Ref 526390Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists. J Med Chem. 2002 Aug 1;45(16):3440-50.
Ref 526590N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor. J Med Chem. 2003 Apr 10;46(8):1492-503.
Ref 526692Novel N6-substituted adenosine 5'-N-methyluronamides with high selectivity for human adenosine A3 receptors reduce ischemic myocardial injury. Am J Physiol Heart Circ Physiol. 2003 Dec;285(6):H2780-7. Epub 2003 Aug 14.
Ref 526745Molecular cloning and characterization of an adenosine receptor: the A3 adenosine receptor. Proc Natl Acad Sci U S A. 1992 Aug 15;89(16):7432-6.
Ref 526981Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists. J Med Chem. 2004 Mar 11;47(6):1434-47.
Ref 527040J Med Chem. 2004 Apr 22;47(9):2243-55.Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative.
Ref 527055Bioorg Med Chem Lett. 2004 May 17;14(10):2443-6.Facile synthesis of fused 1,2,4-triazolo[1,5-c]pyrimidine derivatives as human adenosine A3 receptor ligands.
Ref 527331J Med Chem. 2004 Dec 16;47(26):6529-40.2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
Ref 527473J Med Chem. 2005 Mar 24;48(6):1745-58.(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
Ref 527647J Med Chem. 2005 Jul 28;48(15):4910-8."Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
Ref 527649J Med Chem. 2005 Jul 28;48(15):5001-8.New 2-arylpyrazolo[4,3-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists.
Ref 527823J Med Chem. 2005 Nov 3;48(22):6887-96.2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Ref 527915J Med Chem. 2005 Dec 15;48(25):7932-45.1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.
Ref 527930J Med Chem. 2005 Dec 29;48(26):8103-7.Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.
Ref 527933J Med Chem. 2005 Dec 29;48(26):8253-60.2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching.
Ref 528192J Med Chem. 2006 May 18;49(10):2861-7.2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
Ref 528290J Med Chem. 2006 Jul 13;49(14):4085-97.Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models.
Ref 528362Improving potency, selectivity, and water solubility of adenosine A1 receptor antagonists: xanthines modified at position 3 and related pyrimido[1,2,3-cd]purinediones. ChemMedChem. 2006 Aug;1(8):891-902.
Ref 528544J Med Chem. 2006 Nov 30;49(24):7119-31.Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Ref 528546[3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor. Eur J Pharmacol. 2007 Feb 5;556(1-3):14-8. Epub 2006 Oct 27.
Ref 528559J Med Chem. 2006 Dec 14;49(25):7373-83.2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.
Ref 528673J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Ref 528684J Med Chem. 2007 Mar 22;50(6):1222-30. Epub 2007 Feb 20.N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor.
Ref 528748J Med Chem. 2007 Apr 19;50(8):1810-27. Epub 2007 Mar 23.Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.
Ref 528886Bioorg Med Chem. 2007 Aug 15;15(16):5440-7. Epub 2007 May 26.Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands.
Ref 528950Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion. J Mol Cell Cardiol. 2007 Sep;43(3):262-71. Epub 2007 May 24.
Ref 528969J Med Chem. 2007 Aug 23;50(17):4061-74. Epub 2007 Aug 1.New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Ref 529098Bioorg Med Chem. 2008 Jan 1;16(1):336-53. Epub 2007 Sep 22.5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivityfor A1 receptor from different species.
Ref 529186J Med Chem. 2007 Dec 27;50(26):6596-606. Epub 2007 Nov 30.Scouting human A3 adenosine receptor antagonist binding mode using a molecular simplification approach: from triazoloquinoxaline to a pyrimidine skeleton as a key study.
Ref 529305Bioorg Med Chem. 2008 Apr 1;16(7):3825-30. Epub 2008 Jan 30.Synthesis of eudistomin D analogues and its effects on adenosine receptors.
Ref 529313J Med Chem. 2008 Mar 27;51(6):1764-70. Epub 2008 Feb 13.Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.
Ref 529419Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3. Epub 2008 Mar 30.Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
Ref 529435Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2813-9.
Ref 530014Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Ref 530035J Med Chem. 2009 Apr 23;52(8):2393-406.N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
Ref 530243J Med Chem. 2009 Jul 9;52(13):3994-4006.1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Ref 530372J Med Chem. 2009 Dec 10;52(23):7640-52.2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a new scaffold to obtain potent and selective human A3 adenosine receptor antagonists: new insights into the receptor-antagonist recognition.
Ref 530458Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor. J Med Chem. 2009 Dec 10;52(23):7897-900.
Ref 530694Bioorg Med Chem Lett. 2010 Mar 1;20(5):1697-700. Epub 2010 Jan 20.Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists.
Ref 530752Bioorg Med Chem. 2010 Mar 15;18(6):2195-203. Epub 2010 Feb 4.2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
Ref 530966Eur J Med Chem. 2010 Aug;45(8):3459-71. Epub 2010 May 7.Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 531130Bioorg Med Chem Lett. 2010 Oct 1;20(19):5690-4. Epub 2010 Aug 10.Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.
Ref 531146Science. 2010 Sep 3;329(5996):1175-80.Spiroindolones, a potent compound class for the treatment of malaria.
Ref 531209Bioorg Med Chem. 2010 Nov 15;18(22):7890-9. Epub 2010 Sep 22.Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.
Ref 531894Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions. J Med Chem. 2012 May 24;55(10):4847-60.
Ref 533542J Med Chem. 1982 Mar;25(3):197-207.Adenosine receptors: targets for future drugs.
Ref 533722J Med Chem. 1995 May 12;38(10):1720-35.Structure-activity relationships of 9-alkyladenine and ribose-modified adenosine derivatives at rat A3 adenosine receptors.
Ref 533853A binding site model and structure-activity relationships for the rat A3 adenosine receptor. Mol Pharmacol. 1994 Jun;45(6):1101-11.
Ref 533946Molecular cloning and characterization of the human A3 adenosine receptor. Proc Natl Acad Sci U S A. 1993 Nov 1;90(21):10365-9.
Ref 534039Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors. Pharmacology. 1993;46(2):91-100.
Ref 534098J Med Chem. 1996 Feb 2;39(3):781-8.Interactions of flavonoids and other phytochemicals with adenosine receptors.
Ref 534114Inhibition of TNF-alpha expression by adenosine: role of A3 adenosine receptors. J Immunol. 1996 May 1;156(9):3435-42.
Ref 534145J Med Chem. 1996 Jun 7;39(12):2293-301.Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Ref 534159J Med Chem. 1996 Jul 19;39(15):2980-9.Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
Ref 534241Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. J Med Chem. 1996 Oct 11;39(21):4142-8.
Ref 534506Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.
Ref 5346152'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies. J Med Chem. 1998 May 7;41(10):1708-15.
Ref 534684Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists. J Med Chem. 1998 Aug 13;41(17):3186-201.
Ref 534925A(3) adenosine receptor activation attenuates neutrophil function and neutrophil-mediated reperfusion injury. Am J Physiol. 1999 Nov;277(5 Pt 2):H1895-905.
Ref 535470A3 adenosine receptor as a target for cancer therapy. Anticancer Drugs. 2002 Jun;13(5):437-43.
Ref 537920A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. FEBS Lett. 1993 Dec 20;336(1):57-60.
Ref 543555(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. (Target id: 21).
Ref 5505292011 Pipeline of Can-Fite BioPharm.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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