General Information of Drug Therapeutic Target (DTT) (ID: TTM2AOE)

DTT Name Adenosine A2a receptor (ADORA2A)
Synonyms Adenosine receptor A2a; ADORA2; A2a Adenosine receptor; A(2A) adenosine receptor
Gene Name ADORA2A
DTT Type
Successful target
[1]
Related Disease
Orthostatic hypotension [ICD-11: BA21]
Parkinsonism [ICD-11: 8A00]
Radionuclide imaging [ICD-11: N.A.]
BioChemical Class
GPCR rhodopsin
UniProt ID
AA2AR_HUMAN
TTD ID
T77365
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAAADIAVGVLAI
PFAITISTGFCAACHGCLFIACFVLVLTQSSIFSLLAIAIDRYIAIRIPLRYNGLVTGTR
AKGIIAICWVLSFAIGLTPMLGWNNCGQPKEGKNHSQGCGEGQVACLFEDVVPMNYMVYF
NFFACVLVPLLLMLGVYLRIFLAARRQLKQMESQPLPGERARSTLQKEVHAAKSLAIIVG
LFALCWLPLHIINCFTFFCPDCSHAPLWLMYLAIVLSHTNSVVNPFIYAYRIREFRQTFR
KIIRSHVLRQQEPFKAAGTSARVLAAHGSDGEQVSLRLNGHPPGVWANGSAPHPERRPNG
YALGLVSGGSAQESQGNTGLPDVELLSHELKGVCPEPPGLDDPLAQDGAGVS
Function The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. Receptor for adenosine.
KEGG Pathway
Rap1 signaling pathway (hsa04015 )
Calcium signaling pathway (hsa04020 )
cAMP signaling pathway (hsa04024 )
Neuroactive ligand-receptor interaction (hsa04080 )
Vascular smooth muscle contraction (hsa04270 )
Parkinson's disease (hsa05012 )
Alcoholism (hsa05034 )
Reactome Pathway
Adenosine P1 receptors (R-HSA-417973 )
G alpha (s) signalling events (R-HSA-418555 )
Surfactant metabolism (R-HSA-5683826 )
NGF-independant TRKA activation (R-HSA-187024 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
3 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Caffeine DMKBJWP Orthostatic hypotension BA21 Approved [1], [2]
Istradefylline DM20VSK Parkinson disease 8A00.0 Approved [3]
Regadenoson DM76VHG Radionuclide imaging N.A. Approved [4]
------------------------------------------------------------------------------------
21 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Apadenoson DMD8QTC Coronary artery disease BA80 Phase 3 [5]
Binodenoson DMVHF8G Hypertension BA00-BA04 Phase 3 [6]
Tozadenant DMATC14 Parkinson disease 8A00.0 Phase 3 [7]
AMP-579 DMJ4GPR Hyperlipidaemia 5C80 Phase 2 [8]
AZD4635 DM8SVIY Prostate cancer 2C82.0 Phase 2 [9]
BIIB014 DMH7RJ1 Parkinson disease 8A00.0 Phase 2 [10]
Dexefaroxan DMTY4KN Parkinson disease 8A00.0 Phase 2 [11]
MRE-0094 DMQR23W Diabetic foot ulcer BD54 Phase 2 [12]
SCH 420814 DMMWCZS Parkinson disease 8A00.0 Phase 2 [10]
Tonapofylline DMBH316 Acute and chronic heart failure BD1Z Phase 2 [13]
UK-432097 DM2O4MI Chronic obstructive pulmonary disease CA22 Phase 2 [14]
AB928 DMDOXMN Metastatic colorectal cancer 2B91 Phase 1/2 [9]
ATL-313 DM75QY9 Arteriosclerosis BD40 Phase 1/2 [15]
OPA-6566 DMELJIV Glaucoma/ocular hypertension 9C61 Phase 1/2 [16]
PBF509 DMGFPQ0 Non-small-cell lung cancer 2C25.Y Phase 1/2 [9]
V81444 DMPWHU6 Parkinson disease 8A00.0 Phase 1/2 [17]
EOS100850 DMQ6GUY Solid tumour/cancer 2A00-2F9Z Phase 1 [18]
GW-328267 DMM1RB6 Allergic rhinitis CA08.0 Phase 1 [19]
KF-17837 DMQ6DLZ Parkinson disease 8A00.0 Phase 1 [20]
PBF-999 DMBSQH9 Huntington disease 8A01.10 Phase 1 [21]
SCH-442416 DMQ2K1V N. A. N. A. Phase 1 [22]
------------------------------------------------------------------------------------
⏷ Show the Full List of 21 Clinical Trial Drug(s)
8 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PF-1913539 DMXEU14 Alzheimer disease 8A20 Discontinued in Phase 3 [23], [24]
BVT-115959 DM43JK0 Pain MG30-MG3Z Discontinued in Phase 2 [25]
Lu-AA47070 DML86MJ Parkinson disease 8A00.0 Discontinued in Phase 1 [26]
T-62 DMQVLZH Neuropathic pain 8E43.0 Discontinued in Phase 1 [27]
ARISTEROMYCIN DMRXB74 N. A. N. A. Terminated [28]
Methylthioadenosine DMC8J6F Multiple sclerosis 8A40 Terminated [29]
METRIFUDIL DMS5CZ4 N. A. N. A. Terminated [30]
ZM-241385 DMWQ38G N. A. N. A. Terminated [31]
------------------------------------------------------------------------------------
⏷ Show the Full List of 8 Discontinued Drug(s)
220 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl DM4FSTL Discovery agent N.A. Investigative [32]
(2R,3S)-3-(6-Amino-purin-9-yl)-nonan-2-ol DM852Z6 Discovery agent N.A. Investigative [33]
(3-amino-5-bromobenzofuran-2-yl)(phenyl)methanone DMP2G5W Discovery agent N.A. Investigative [34]
(E,E)-8-(4-Phenylbutadien-1-yl)caffeine DMPIUKZ Discovery agent N.A. Investigative [35]
(E,E)-8-[4-(3-Bromophenyl)butadien-1-yl]caffeine DMPEV7S Discovery agent N.A. Investigative [35]
(E,E)-8-[4-(3-Chlorophenyl)butadien-1-yl]caffeine DMY4W25 Discovery agent N.A. Investigative [35]
(E,E)-8-[4-(3-Fluorophenyl)butadien-1-yl]caffeine DMPHJO2 Discovery agent N.A. Investigative [35]
(S)-DHPA DMQSC21 Discovery agent N.A. Investigative [36]
(Z)-8-(3-chlorostyryl)caffeine DMOB9E4 Discovery agent N.A. Investigative [35]
1,3,7-Tripropyl-3,7-dihydro-purine-2,6-dione DMNCJ5R Discovery agent N.A. Investigative [37]
1,3,8-Trimethyl-3,7-dihydro-purine-2,6-dione DMOZEKU Discovery agent N.A. Investigative [38]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione DMEV8G2 Discovery agent N.A. Investigative [39]
1,3-Diallyl-7-methyl-3,7-dihydro-purine-2,6-dione DM4G2IE Discovery agent N.A. Investigative [37]
1,3-Dibenzyl-3,7-dihydro-purine-2,6-dione DM2WSG5 Discovery agent N.A. Investigative [37]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione DMKYE16 Discovery agent N.A. Investigative [39]
1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione DMZ80CT Discovery agent N.A. Investigative [37]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione DMUL2B3 Discovery agent N.A. Investigative [39]
1,4-diaminoanthracene-9,10-dione DMIHYKG Discovery agent N.A. Investigative [34]
1-Allyl-3,7-dimethyl-3,7-dihydro-purine-2,6-dione DMZE5GX Discovery agent N.A. Investigative [37]
1-amino-2,4-bis(phenylthio)anthracene-9,10-dione DMRAN9T Discovery agent N.A. Investigative [34]
1-amino-2-phenoxyanthracene-9,10-dione DMWCXM4 Discovery agent N.A. Investigative [34]
1-amino-4-chloroanthracene-9,10-dione DMJMDNX Discovery agent N.A. Investigative [34]
1-amino-4-methoxyanthracene-9,10-dione DM7X5BP Discovery agent N.A. Investigative [34]
1-aminoanthracene-9,10-dione DMGU76I Discovery agent N.A. Investigative [34]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione DMSNK98 Discovery agent N.A. Investigative [40]
1-Ethyl-3-methyl-3,7-dihydro-purine-2,6-dione DMSFINY Discovery agent N.A. Investigative [37]
1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione DMSTH24 Discovery agent N.A. Investigative [40]
1-METHYLXANTHINE DM2WQ1E Discovery agent N.A. Investigative [39]
1-Phenyl-3-(4-pyridin-2-yl-thiazol-2-yl)-urea DMJ723D Discovery agent N.A. Investigative [41]
1H-Imidazo[4,5-c]quinolin-4-ylamine HCl DMME09C Discovery agent N.A. Investigative [32]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine DMMESIU Discovery agent N.A. Investigative [42]
2,6,8-triphenyl-9H-purine DM4IFPQ Discovery agent N.A. Investigative [43]
2,6-diphenyl-1-deazapurine DMW2VZ1 Discovery agent N.A. Investigative [44]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine DMY3C78 Discovery agent N.A. Investigative [44]
2,6-diphenyl-8-ethyl-1-deazapurine DM0C8BW Discovery agent N.A. Investigative [44]
2,6-diphenyl-8-methyl-1-deazapurine DMI79FV Discovery agent N.A. Investigative [44]
2,6-diphenyl-8-tButyl-1-deazapurine DM6D1BQ Discovery agent N.A. Investigative [44]
2,6-diphenyl-9H-purine DM5SXYI Discovery agent N.A. Investigative [43]
2,6-Diphenyl-pyrimidin-4-ylamine DM3JURW Discovery agent N.A. Investigative [45]
2,6-dphenyl-8-propyl-1-deazapurine DM8F9KO Discovery agent N.A. Investigative [44]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline DM0Y2P1 Discovery agent N.A. Investigative [46]
2-(2''-indolylethyloxy)adenosine DMCLIN8 Discovery agent N.A. Investigative [47]
2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine DMXGWOT Discovery agent N.A. Investigative [48]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine DMD8Q3E Discovery agent N.A. Investigative [47]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine DMITEND Discovery agent N.A. Investigative [47]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine DMXRHOY Discovery agent N.A. Investigative [47]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine DMR8PGZ Discovery agent N.A. Investigative [47]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine DME3IN1 Discovery agent N.A. Investigative [47]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine DM6BIOP Discovery agent N.A. Investigative [47]
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine DMFP0IW Discovery agent N.A. Investigative [47]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine DMWA0MN Discovery agent N.A. Investigative [47]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine DMGRC24 Discovery agent N.A. Investigative [47]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine DML39UW Discovery agent N.A. Investigative [47]
2-(3''-(benzoimidazole-1''-yl)ethyloxy)adenosine DMLDOH6 Discovery agent N.A. Investigative [47]
2-(3''-indolylethyloxy)adenosine DMXRAE3 Discovery agent N.A. Investigative [47]
2-(3''-pyrrolylethyloxy)adenosine DMNCP8Y Discovery agent N.A. Investigative [47]
2-(4-chlorophenyl)-6-phenyl-9H-purine DMAPWNR Discovery agent N.A. Investigative [43]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline DMTAVU5 Discovery agent N.A. Investigative [49]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine DM1C864 Discovery agent N.A. Investigative [50]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline DMDXIN1 Discovery agent N.A. Investigative [46]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine DMSIJ17 Discovery agent N.A. Investigative [50]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol DMRBX1D Discovery agent N.A. Investigative [51]
2-(hex-1-ynyl)-N6-methoxyadenosine DM7YLTS Discovery agent N.A. Investigative [50]
2-amino-3-(m-tolylamino)naphthalene-1,4-dione DM2GJZE Discovery agent N.A. Investigative [34]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile DMVN0EC Discovery agent N.A. Investigative [52]
2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile DM53T8Q Discovery agent N.A. Investigative [52]
2-Amino-4,6-diphenyl-nicotinonitrile DMO69TS Discovery agent N.A. Investigative [52]
2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile DM1MOB9 Discovery agent N.A. Investigative [45]
2-Amino-4,6-diphenyl-pyrimidine DMI9YGU Discovery agent N.A. Investigative [45]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile DMP4NHD Discovery agent N.A. Investigative [52]
2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile DMRVTJ1 Discovery agent N.A. Investigative [52]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile DMUYTXS Discovery agent N.A. Investigative [52]
2-amino-6-phenyl-4-p-tolylnicotinonitrile DMAXESK Discovery agent N.A. Investigative [53]
2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile DM7M9CL Discovery agent N.A. Investigative [52]
2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide DM320RW Discovery agent N.A. Investigative [54]
2-chloro-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine DMPCRLY Discovery agent N.A. Investigative [55]
2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine DMC5OQ3 Discovery agent N.A. Investigative [55]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine DM6CZAN Discovery agent N.A. Investigative [32]
2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine DM0BHKM Discovery agent N.A. Investigative [55]
2-ethyl-4-(furan-3-yl)thieno[3,2-d]pyrimidine DMR0IEK Discovery agent N.A. Investigative [55]
2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine DMWFR16 Discovery agent N.A. Investigative [55]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine DMWCGE8 Discovery agent N.A. Investigative [55]
2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine DMIRSQO Discovery agent N.A. Investigative [55]
2-ethynyl-N6-methoxyadenosine DM2D78W Discovery agent N.A. Investigative [50]
2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine DMIMRCH Discovery agent N.A. Investigative [56]
2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine DM9MIC5 Discovery agent N.A. Investigative [56]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine DMDC6XP Discovery agent N.A. Investigative [32]
2-phenyl-2H-pyrazolo[3,4-c]quinolin-4-amine DM5WOSM Discovery agent N.A. Investigative [56]
2-phenylpropoxyadenosine DMZQCEP Discovery agent N.A. Investigative [47]
2-tolyl-6-phenyl-9H-purine DM1HABS Discovery agent N.A. Investigative [43]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine DMKC1GI Discovery agent N.A. Investigative [50]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine DMTNQZU Discovery agent N.A. Investigative [50]
3-Benzyl-7-methyl-[1,8]naphthyridin-4-ol DMHQ467 Discovery agent N.A. Investigative [57]
3-Benzyl-7-methyl-[1,8]naphthyridine-4-thiol DM12RH3 Discovery agent N.A. Investigative [57]
3-Isopropyl-1-methyl-3,7-dihydro-purine-2,6-dione DMYKVRF Discovery agent N.A. Investigative [37]
3-noradamantyl-1,3-dipropylxanthine DMFHYAE Discovery agent N.A. Investigative [58]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [59]
4-(ethylthio)-6-phenyl-1,3,5-triazin-2-amine DM0GCEK Discovery agent N.A. Investigative [53]
4-(furan-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine DMY7035 Discovery agent N.A. Investigative [60]
4-(furan-2-yl)thieno[3,2-d]pyrimidin-2-amine DM7LVKP Discovery agent N.A. Investigative [54]
4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine DMK3J8Q Discovery agent N.A. Investigative [55]
4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile DM7X59V Discovery agent N.A. Investigative [45]
4-amino-2-p-tolylisoindoline-1,3-dione DMOJTZD Discovery agent N.A. Investigative [34]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol DMZLOVB Discovery agent N.A. Investigative [61]
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol DM4TIXY Discovery agent N.A. Investigative [44]
5-Azido-6-benzyl-2-methyl-[1,8]naphthyridine DMURTHE Discovery agent N.A. Investigative [57]
5-Butyl-8-phenyl-3H-[1,2,4]triazolo[5,1-i]purine DM2EPFZ Discovery agent N.A. Investigative [62]
6-(furan-2-yl)-9H-purin-2-amine DMOYCBH Discovery agent N.A. Investigative [60]
6-Furan-2-yl-9-phenethyl-9H-purin-2-ylamine DMOLIW4 Discovery agent N.A. Investigative [63]
6-Furan-2-yl-9-phenyl-9H-purin-2-ylamine DMSJP6T Discovery agent N.A. Investigative [63]
6-guanidino-2-(3''-indolylethyloxy)adenosine DMM86PK Discovery agent N.A. Investigative [47]
7-Allyl-1,3-dimethyl-3,7-dihydro-purine-2,6-dione DMPRBO1 Discovery agent N.A. Investigative [37]
7-Allyl-1,3-dipropyl-3,7-dihydro-purine-2,6-dione DMHJ6TU Discovery agent N.A. Investigative [37]
7-Isopropyl-7H-adenine DMVSF0O Discovery agent N.A. Investigative [36]
7-Propyl-7H-adenine DM4I0B1 Discovery agent N.A. Investigative [36]
8-Br-adenine DMVPIYG Discovery agent N.A. Investigative [36]
8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine DMMQ79W Discovery agent N.A. Investigative [36]
8-Bromo-9-(2-butyl)-9H-adenine DM5DCPF Discovery agent N.A. Investigative [36]
8-Bromo-9-(2-hydroxypropyl)-9H-adenine DMKW2PE Discovery agent N.A. Investigative [36]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine DMA258T Discovery agent N.A. Investigative [36]
8-Bromo-9-(but-3-enyl)-9H-adenine DMXNF3V Discovery agent N.A. Investigative [36]
8-Bromo-9-(sec-butyl)-9H-adenine DMSQPFM Discovery agent N.A. Investigative [36]
8-Bromo-9-cyclobutyl-9H-adenine DMUTV76 Discovery agent N.A. Investigative [36]
8-Bromo-9-cyclohexyl-9H-adenine DMLVCON Discovery agent N.A. Investigative [36]
8-Bromo-9-cyclopentyl-9H-adenine DMCK0O1 Discovery agent N.A. Investigative [36]
8-Bromo-9-ethyl-9H-adenine DM4YAD6 Discovery agent N.A. Investigative [36]
8-bromo-9-isobutyl-9H-purin-6-amine DMZF3UN Discovery agent N.A. Investigative [51]
8-Bromo-9-isopropyl-9H-adenine DMIN9HC Discovery agent N.A. Investigative [36]
8-Bromo-9-methyl-9H-adenine DM1DS3B Discovery agent N.A. Investigative [36]
8-Bromo-9-phenylethyl-9H-adenine DMB7EWZ Discovery agent N.A. Investigative [36]
8-Bromo-9-propyl-9H-adenine DMRIPU5 Discovery agent N.A. Investigative [36]
8-PHENYL THEOPHYLLINE DMFGUCY Discovery agent N.A. Investigative [32]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione DMHQGOC Discovery agent N.A. Investigative [40]
8-propyl-2,6-diphenyl-9H-purine DMT6YUF Discovery agent N.A. Investigative [43]
9-(2-Hydroxyethyl)-9H-adenine DMYUMHG Discovery agent N.A. Investigative [36]
9-(2-Hydroxypropyl)-9H-adenine DM2UQ0R Discovery agent N.A. Investigative [36]
9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine DMDYZCH Discovery agent N.A. Investigative [54]
9-(3-Hydroxypropyl)-9H-adenine DM80MTI Discovery agent N.A. Investigative [36]
9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine DM4X18V Discovery agent N.A. Investigative [54]
9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine DMURKL9 Discovery agent N.A. Investigative [54]
9-(sec-Butyl)-9H-adenine DMFKVPA Discovery agent N.A. Investigative [36]
9-Allyl-8-bromo-9H-adenine DM8VZIY Discovery agent N.A. Investigative [36]
9-benzyl-6-(furan-2-yl)-9H-purin-2-amine DMO6CB7 Discovery agent N.A. Investigative [54]
9-Benzyl-8-bromo-9H-adenine DMMWGVI Discovery agent N.A. Investigative [36]
9-BENZYL-9H-ADENINE DMONCUL Discovery agent N.A. Investigative [36]
9-But-3-enyl-9H-adenine DMSWQY7 Discovery agent N.A. Investigative [36]
9-Butyl-9H-adenine DMZQLBD Discovery agent N.A. Investigative [36]
9-Cyclobutyl-9H-adenine DM04QWX Discovery agent N.A. Investigative [36]
9-Cycloheptyl-9H-adenine DMP8VM2 Discovery agent N.A. Investigative [36]
9-Cyclopentyl-9H-adenine DMSGU2L Discovery agent N.A. Investigative [36]
9-Cyclopropyl-9H-adenine DMAFCZL Discovery agent N.A. Investigative [36]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine DMRVS2D Discovery agent N.A. Investigative [64]
9-Ethyl-9H-adenine DMWV8YX Discovery agent N.A. Investigative [36]
9-Isopropyl-9H-adenine DMBQLAI Discovery agent N.A. Investigative [36]
9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine DMO4CSP Discovery agent N.A. Investigative [65]
9-Methyl-9H-adenine DM6DOVL Discovery agent N.A. Investigative [36]
9-Phenylethyl-9H-adenine DMO17J0 Discovery agent N.A. Investigative [36]
9-Propyl-9H-adenine DMQTEPY Discovery agent N.A. Investigative [36]
Alloxazine DM7U2BE Discovery agent N.A. Investigative [65]
CGS 21680 DMZ0TGY Discovery agent N.A. Investigative [66]
Cyclohexyl-(2-phenoxy-9H-purin-6-yl)-amine DM84ZX5 Discovery agent N.A. Investigative [67]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine DMLREDJ Discovery agent N.A. Investigative [67]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate DMK4T5Y Discovery agent N.A. Investigative [13]
FR-166124 DMPCBXT Discovery agent N.A. Investigative [68]
Galangin DM5TQ2O Discovery agent N.A. Investigative [69]
GNF-PF-2224 DM26UKN Discovery agent N.A. Investigative [70]
GNF-PF-2700 DMC56YJ Discovery agent N.A. Investigative [51]
isobutylmethylxanthine DM46F5X Discovery agent N.A. Investigative [37]
Isoguanosine DMAFLCJ Discovery agent N.A. Investigative [71]
Kuanoniamine D DMAVM94 Discovery agent N.A. Investigative [72]
LUF-5417 DMUPQED Discovery agent N.A. Investigative [13]
LUF-5433 DME4O5D Discovery agent N.A. Investigative [13]
LUF-5437 DM0DRO8 Discovery agent N.A. Investigative [41]
LUF-5767 DMP08QO Discovery agent N.A. Investigative [73]
LUF-5956 DMG4YWM Discovery agent N.A. Investigative [43]
LUF-5957 DMJFMH9 Discovery agent N.A. Investigative [43]
LUF-5962 DMR6LIE Discovery agent N.A. Investigative [43]
LUF-5978 DMCTM3L Discovery agent N.A. Investigative [44]
LUF-5980 DMGOIF5 Discovery agent N.A. Investigative [44]
LUF-5981 DMHO3XL Discovery agent N.A. Investigative [44]
Methyl 7-methoxy-4-phenylbenzofuran-2-ylcarbamate DMBLW1A Discovery agent N.A. Investigative [74]
MSX-3 DMF9HYI Parkinson disease 8A00.0 Investigative [75]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine DM3C8PJ Discovery agent N.A. Investigative [67]
N-(2,6-diphenylpyrimidin-4-yl)-2-ethylbutyramide DMK5AU4 Discovery agent N.A. Investigative [73]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide DM6HGK4 Discovery agent N.A. Investigative [73]
N-(2,6-diphenylpyrimidin-4-yl)acetamide DMQ0DMU Discovery agent N.A. Investigative [73]
N-(2,6-diphenylpyrimidin-4-yl)butyramide DM5EF71 Discovery agent N.A. Investigative [73]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide DMWPZCS Discovery agent N.A. Investigative [73]
N-(2,6-diphenylpyrimidin-4-yl)propionamide DM89NGE Discovery agent N.A. Investigative [73]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide DMLTROU Discovery agent N.A. Investigative [76]
N-(3-Phenyl-[1,2,4]thiadiazol-5-yl)-benzamide DM4IA92 Discovery agent N.A. Investigative [41]
N-(4,6-diphenylpyrimidin-2-yl)propionamide DMJZ2IP Discovery agent N.A. Investigative [73]
N-(4-Pyridin-2-yl-thiazol-2-yl)-benzamide DMHBWM9 Discovery agent N.A. Investigative [41]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide DMTF8US Discovery agent N.A. Investigative [13]
N-(7-methoxy-4-phenylbenzofuran-2-yl)acetamide DMH42L8 Discovery agent N.A. Investigative [74]
N6-((+/-)-endo-norborn-2-yl)adenosine DM30KXV Discovery agent N.A. Investigative [42]
N6-(4-hydroxybenzyl)adenine riboside DM5Q71U Discovery agent N.A. Investigative [77]
N6-cyclopentyladenosine DMD6AJO Discovery agent N.A. Investigative [13]
N6-methoxy-2-phenylethynyladenosine DMDG59X Discovery agent N.A. Investigative [50]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine DMSEL5W Discovery agent N.A. Investigative [50]
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine DMP7246 Discovery agent N.A. Investigative [50]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine DM8LR62 Discovery agent N.A. Investigative [50]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine DMQ5K8R Discovery agent N.A. Investigative [50]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine DM9H3W8 Discovery agent N.A. Investigative [50]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine DMRBS50 Discovery agent N.A. Investigative [50]
N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine DM0WMKJ Discovery agent N.A. Investigative [78]
N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine DMVNLPF Discovery agent N.A. Investigative [78]
PD-115199 DMQ4LRZ Discovery agent N.A. Investigative [79]
Phenyl 7-methoxy-4-phenylbenzofuran-2-ylcarbamate DMWN9XU Discovery agent N.A. Investigative [74]
Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol DMDV1SN Discovery agent N.A. Investigative [80]
PSB-0788 DM0FKV9 Discovery agent N.A. Investigative [81]
PSB-09120 DMAFHLX Discovery agent N.A. Investigative [81]
PSB-601 DMBIK7D Discovery agent N.A. Investigative [81]
R-N6-(phenylisopropyl)adenosine DM2N3BA Discovery agent N.A. Investigative [47]
SB-298 DMU2J3K Discovery agent N.A. Investigative [81]
SCH-63390 DMAUB9F Discovery agent N.A. Investigative [82]
ST-1535 DMUTC9Z Discovery agent N.A. Investigative [52]
[3H]CCPA DMHDGB3 Discovery agent N.A. Investigative [83]
[3H]NECA DMAO9SH Discovery agent N.A. Investigative [84]
[3H]OSIP339391 DM4BY5J Discovery agent N.A. Investigative [51]
------------------------------------------------------------------------------------
⏷ Show the Full List of 220 Investigative Drug(s)

References

1 Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.
2 Adenosine receptor antagonists intensify the benzodiazepine withdrawal signs in mice. Pharmacol Rep. 2006 Sep-Oct;58(5):643-51.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
5 URL: 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: 3290).
6 Coronary circulation responses to binodenoson, a selective adenosine A2A receptor agonist. Am J Cardiol. 2007 Jun 1;99(11):1507-12.
7 Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Lancet Neurol. 2014 Aug;13(8):767-76.
8 Adenosine A1/A2a receptor agonist AMP-579 induces acute and delayed preconditioning against in vivo myocardial stunning. Am J Physiol Heart Circ Physiol. 2004 Dec;287(6):H2746-53.
9 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
10 Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54.
11 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
12 Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
13 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.
14 Structure of an agonist-bound human A2A adenosine receptor. Science. 2011 Apr 15;332(6027):322-7.
15 Effect of novel A2A adenosine receptor agonist ATL 313 on Clostridium difficile toxin A-induced murine ileal enteritis. Infect Immun. 2006 May;74(5):2606-12.
16 Clinical pipeline report, company report or official report of Acucela.
17 Adenosine A2A receptor antagonists in Parkinson's disease: progress in clinical trials from the newly approved istradefylline to drugs in early development and those already discontinued. CNS Drugs. 2014 May;28(5):455-74.
18 National Cancer Institute Drug Dictionary (drug name EOS100850).
19 ADENOSINE RECEPTORS AS TARGETS FOR THERAPEUTIC INTERVENTION IN ASTHMA AND CHRONIC OBSTRUCTIVE PULMONARY DISEASE
20 Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine. J Med Chem. 1993 Nov 12;36(23):3731-3.
21 Clinical pipeline report, company report or official report of Palobiofarma.
22 Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using p... J Med Chem. 2000 Nov 16;43(23):4359-62.
23 Blockade of A2A adenosine receptors prevents basic fibroblast growth factor-induced reactive astrogliosis in rat striatal primary astrocytes. Glia. 2003 Aug;43(2):190-4.
24 Adenosine A2A receptor antagonists are potential antidepressants: evidence based on pharmacology and A2A receptor knockout mice. Br J Pharmacol. 2001 Sep;134(1):68-77.
25 Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308.
26 The novel adenosine A2A antagonist Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade. Pharmacol Biochem Behav. 2012 Jan;100(3):498-505.
27 Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
28 Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. J Med Chem. 2000 Jun 1;43(11):2196-203.
29 Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique aden... J Med Chem. 2004 Apr 22;47(9):2243-55.
30 N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. J Med Chem. 1999 Sep 9;42(18):3463-77.
31 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 ... J Med Chem. 2009 Dec 10;52(23):7640-52.
32 1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. J Med Chem. 1991 Mar;34(3):1202-6.
33 Structure-activity relationships of 9-alkyladenine and ribose-modified adenosine derivatives at rat A3 adenosine receptors. J Med Chem. 1995 May 12;38(10):1720-35.
34 Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists. J Med Chem. 2010 Feb 25;53(4):1799-809.
35 Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues. Bioorg Med Chem. 2008 Sep 15;16(18):8676-84.
36 8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands. Bioorg Med Chem. 2009 Apr 1;17(7):2812-22.
37 Analogues of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors. J Med Chem. 1986 Jul;29(7):1305-8.
38 1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors. J Med Chem. 1985 Apr;28(4):487-92.
39 Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. J Med Chem. 1988 Oct;31(10):2034-9.
40 Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic... J Med Chem. 2004 Feb 12;47(4):1031-43.
41 Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists. J Med Chem. 2001 Mar 1;44(5):749-62.
42 N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine recept... J Med Chem. 2009 Apr 23;52(8):2393-406.
43 2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. J Med Chem. 2006 May 18;49(10):2861-7.
44 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34.
45 A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. Bioorg Med Chem. 2008 Mar 15;16(6):2741-52.
46 Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists. J Med Chem. 2008 Mar 27;51(6):1764-70.
47 Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor. J Med Chem. 2007 Apr 19;50(8):1810-27.
48 Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. J Med Chem. 2008 Feb 14;51(3):400-6.
49 2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database search... J Med Chem. 2005 Dec 29;48(26):8253-60.
50 N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor. J Med Chem. 2007 Mar 22;50(6):1222-30.
51 Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods. Eur J Med Chem. 2010 Aug;45(8):3459-71.
52 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem. 2008 Aug 14;51(15):4449-55.
53 Identification of non-furan containing A2A antagonists using database mining and molecular similarity approaches. Bioorg Med Chem Lett. 2006 Dec 1;16(23):5993-7.
54 Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpu... Bioorg Med Chem Lett. 2008 May 1;18(9):2924-9.
55 Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3.
56 New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluati... J Med Chem. 2007 Aug 23;50(17):4061-74.
57 1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4604-10.
58 Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7119-31.
59 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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
60 Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines. J Med Chem. 2009 Jan 8;52(1):33-47.
61 Synthesis of eudistomin D analogues and its effects on adenosine receptors. Bioorg Med Chem. 2008 Apr 1;16(7):3825-30.
62 Facile synthesis of fused 1,2,4-triazolo[1,5-c]pyrimidine derivatives as human adenosine A3 receptor ligands. Bioorg Med Chem Lett. 2004 May 17;14(10):2443-6.
63 6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2119-22.
64 Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1931-4.
65 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 pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.
66 Effects of CGS 21680, a selective adenosine A2A receptor agonist, on allergic airways inflammation in the rat. Eur J Pharmacol. 2002 Mar 8;438(3):183-8.
67 Reversine and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem. 2005 Jul 28;48(15):4910-8.
68 Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist. Bioorg Med Chem Lett. 1999 Jul 19;9(14):1979-84.
69 Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. J Med Chem. 1997 Aug 1;40(16):2588-95.
70 Synthesis and theoretical studies on energetics of novel N- and O- perfluoroalkyl triazole tagged thienopyrimidines--their potential as adenosine r... Eur J Med Chem. 2010 May;45(5):1739-45.
71 High selectivity of novel isoguanosine analogues for the adenosine A1 receptor. Bioorg. Med. Chem. Lett. 1(9):481-486 (1991).
72 Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp. J Nat Prod. 1998 Feb;61(2):301-5.
73 2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. J Med Chem. 2004 Dec 16;47(26):6529-40.
74 Synthetic studies on selective adenosine A2A receptor antagonists: synthesis and structure-activity relationships of novel benzofuran derivatives. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1090-3.
75 URL: 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: 5610).
76 Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1697-700.
77 Neuroprotective principles from Gastrodia elata. J Nat Prod. 2007 Apr;70(4):571-4.
78 N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A... Eur J Med Chem. 2008 Aug;43(8):1639-47.
79 (E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists. J Med Chem. 1992 Jun 12;35(12):2342-5.
80 Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2916-9.
81 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with... J Med Chem. 2009 Jul 9;52(13):3994-4006.
82 Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A... J Med Chem. 1998 Jun 4;41(12):2126-33.
83 5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 ... Bioorg Med Chem. 2008 Jan 1;16(1):336-53.
84 Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. J Med Chem. 1988 Jun;31(6):1179-83.