General Information of Drug Therapeutic Target (DTT) (ID: TTK25J1)

DTT Name Adenosine A1 receptor (ADORA1)
Synonyms Adenosine receptor A1; A(1) adenosine receptor
Gene Name ADORA1
DTT Type
Successful target
[1]
BioChemical Class
GPCR rhodopsin
UniProt ID
AA1R_HUMAN
TTD ID
T92072
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGA
LVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVT
PRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYM
VYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALIL
FLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFL
KIWNDHFRCQPAPPIDEDLPEERPDD
Function The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Receptor for adenosine.
KEGG Pathway
cGMP-PKG signaling pathway (hsa04022 )
cAMP signaling pathway (hsa04024 )
Sphingolipid signaling pathway (hsa04071 )
Neuroactive ligand-receptor interaction (hsa04080 )
Morphine addiction (hsa05032 )
Reactome Pathway
G alpha (i) signalling events (R-HSA-418594 )
Adenosine P1 receptors (R-HSA-417973 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Caffeine DMKBJWP Allergic rhinitis CA08.0 Approved [1]
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14 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Rolofylline DMSZPR3 Heart failure BD10-BD13 Phase 3 [2]
AMP-579 DMJ4GPR Hyperlipidaemia 5C80 Phase 2 [3]
Apaxifylline DMQMV9F Cognitive impairment 6D71 Phase 2 [4]
BAY 1067197 DM4JGNH Heart failure BD10-BD13 Phase 2 [5]
Capadenoson DMYWO62 Atrial fibrillation BC81.3 Phase 2 [6]
DTI-0009 DMV84OK Atrial fibrillation BC81.3 Phase 2 [7]
SELODENOSON DMQM3IX Cardiac arrhythmias BC9Z Phase 2 [7]
SLV320 DM867BJ Heart failure BD10-BD13 Phase 2 [8]
Tonapofylline DMBH316 Acute and chronic heart failure BD1Z Phase 2 [9]
INO-8875 DMKNA94 Glaucoma/ocular hypertension 9C61 Phase 1/2 [10]
AST-004 DM5WMG7 Stroke 8B20 Phase 1 [11]
GS 9667 DMI319T Hypertriglyceridemia 5C80.1 Phase 1 [12]
KF-17837 DMQ6DLZ Parkinson disease 8A00.0 Phase 1 [13]
SCH-442416 DMQ2K1V N. A. N. A. Phase 1 [14]
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⏷ Show the Full List of 14 Clinical Trial Drug(s)
1 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID27387065-Compound-6 DMD4CIU N. A. N. A. Patented [15]
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14 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
CVT-124 DM753RT Autoimmune diabetes 5A10 Discontinued in Phase 3 [16]
N-0861 DMNX0JH Cardiac disease BA00-BE2Z Discontinued in Phase 3 [17]
Tecadenoson DM9T6MS Atrial fibrillation BC81.3 Discontinued in Phase 3 [16]
BRL-61063 DMV3Y8R Allergy 4A80-4A85 Discontinued in Phase 2 [18]
FK-352 DMHIUGT Hypertension BA00-BA04 Discontinued in Phase 2 [19]
FK-453 DMH3DXY Renal failure GB60-GB6Z Discontinued in Phase 2 [20]
FK-838 DMS87T9 Hypertension BA00-BA04 Discontinued in Phase 2 [21]
GW-493838 DMZ2OBD Neuropathic pain 8E43.0 Discontinued in Phase 2 [6]
GR-79236 DM9C1LQ Diabetic complication 5A2Y Discontinued in Phase 1 [22]
SDZ-WAG-994 DMFLOT4 Hypertension BA00-BA04 Discontinued in Phase 1 [23]
ARISTEROMYCIN DMRXB74 N. A. N. A. Terminated [25]
METHYLTHIOADENOSINE DMC8J6F Multiple sclerosis 8A40 Terminated [26]
METRIFUDIL DMS5CZ4 N. A. N. A. Terminated [27]
ZM-241385 DMWQ38G N. A. N. A. Terminated [28]
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⏷ Show the Full List of 14 Discontinued Drug(s)
1 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY 60-6583 DMTEJV1 Myocardial ischemia BA6Z Preclinical [24]
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280 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(1-Phenyl-propyl)-(9-phenyl-9H-purin-6-yl)-amine DMZU2VG Discovery agent N.A. Investigative [29]
(1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl DM4FSTL Discovery agent N.A. Investigative [30]
(2-Chloro-9-methyl-9H-purin-6-yl)-phenyl-amine DMCE1SU Discovery agent N.A. Investigative [29]
(9-Methyl-9H-purin-6-yl)-phenyl-amine DMWJNFC Discovery agent N.A. Investigative [29]
(E)-8-(3-chlorostyryl)-caffeine DMQT15Z Discovery agent N.A. Investigative [31]
(R,S)-PHPNECA DMQO71C Discovery agent N.A. Investigative [32]
(S)-PIA DM04BHI Discovery agent N.A. Investigative [33]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione DMEV8G2 Discovery agent N.A. Investigative [34]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione DMKYE16 Discovery agent N.A. Investigative [34]
1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione DMZ80CT Discovery agent N.A. Investigative [34]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione DMUL2B3 Discovery agent N.A. Investigative [34]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione DMSNK98 Discovery agent N.A. Investigative [35]
1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione DMSTH24 Discovery agent N.A. Investigative [36]
1-METHYLXANTHINE DM2WQ1E Discovery agent N.A. Investigative [34]
1-Propyl-3,7-dihydro-purine-2,6-dione DML5J94 Discovery agent N.A. Investigative [37]
1H-Imidazo[4,5-c]quinolin-4-ylamine HCl DMME09C Discovery agent N.A. Investigative [30]
2'-Me-tecadenoson DMY2GXT Discovery agent N.A. Investigative [38]
2,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide DMO4FSH Discovery agent N.A. Investigative [39]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine DMMESIU Discovery agent N.A. Investigative [40]
2,6,8-triphenyl-9H-purine DM4IFPQ Discovery agent N.A. Investigative [41]
2,6-bis(4-tolyl)-9H-purine DM41RZX Discovery agent N.A. Investigative [41]
2,6-dimethyl-8-ethyl-1-deazapurine DMRZJU5 Discovery agent N.A. Investigative [42]
2,6-diphenyl-1-deazapurine DMW2VZ1 Discovery agent N.A. Investigative [42]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine DMY3C78 Discovery agent N.A. Investigative [42]
2,6-diphenyl-8-ethyl-1-deazapurine DM0C8BW Discovery agent N.A. Investigative [42]
2,6-diphenyl-8-methyl-1-deazapurine DMI79FV Discovery agent N.A. Investigative [42]
2,6-diphenyl-8-tButyl-1-deazapurine DM6D1BQ Discovery agent N.A. Investigative [42]
2,6-diphenyl-9H-purine DM5SXYI Discovery agent N.A. Investigative [41]
2,6-Diphenyl-pyrimidin-4-ylamine DM3JURW Discovery agent N.A. Investigative [43]
2,6-dphenyl-8-propyl-1-deazapurine DM8F9KO Discovery agent N.A. Investigative [42]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline DM0Y2P1 Discovery agent N.A. Investigative [44]
2-(2''-indolylethyloxy)adenosine DMCLIN8 Discovery agent N.A. Investigative [45]
2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine DMXGWOT Discovery agent N.A. Investigative [46]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine DMD8Q3E Discovery agent N.A. Investigative [45]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine DMITEND Discovery agent N.A. Investigative [45]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine DMXRHOY Discovery agent N.A. Investigative [45]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine DMR8PGZ Discovery agent N.A. Investigative [45]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine DME3IN1 Discovery agent N.A. Investigative [45]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine DM6BIOP Discovery agent N.A. Investigative [45]
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine DMFP0IW Discovery agent N.A. Investigative [45]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine DMWA0MN Discovery agent N.A. Investigative [45]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine DMGRC24 Discovery agent N.A. Investigative [45]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine DML39UW Discovery agent N.A. Investigative [45]
2-(3''-indolylethyloxy)adenosine DMXRAE3 Discovery agent N.A. Investigative [45]
2-(3''-pyrrolylethyloxy)adenosine DMNCP8Y Discovery agent N.A. Investigative [45]
2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline DM7BHYS Discovery agent N.A. Investigative [47]
2-(4-chlorophenyl)-6-phenyl-9H-purine DMAPWNR Discovery agent N.A. Investigative [41]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline DMTAVU5 Discovery agent N.A. Investigative [47]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine DM1C864 Discovery agent N.A. Investigative [48]
2-(4-methoxyphenyl)-6-phenyl-9H-purine DMXTHOV Discovery agent N.A. Investigative [41]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline DMDXIN1 Discovery agent N.A. Investigative [44]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine DMSIJ17 Discovery agent N.A. Investigative [48]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol DMRBX1D Discovery agent N.A. Investigative [49]
2-(6-Cyclopentylamino-purin-9-yl)-ethanol DMTI1VO Discovery agent N.A. Investigative [29]
2-(hex-1-ynyl)-N6-methoxyadenosine DM7YLTS Discovery agent N.A. Investigative [48]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile DMVN0EC Discovery agent N.A. Investigative [50]
2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile DM53T8Q Discovery agent N.A. Investigative [50]
2-Amino-4,6-diphenyl-nicotinonitrile DMO69TS Discovery agent N.A. Investigative [50]
2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile DM1MOB9 Discovery agent N.A. Investigative [43]
2-Amino-4,6-diphenyl-pyrimidine DMI9YGU Discovery agent N.A. Investigative [43]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile DMP4NHD Discovery agent N.A. Investigative [50]
2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile DMRVTJ1 Discovery agent N.A. Investigative [50]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile DMUYTXS Discovery agent N.A. Investigative [50]
2-amino-6-phenyl-4-p-tolylnicotinonitrile DMAXESK Discovery agent N.A. Investigative [51]
2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile DM7M9CL Discovery agent N.A. Investigative [50]
2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide DM320RW Discovery agent N.A. Investigative [52]
2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine DMBSDIV Discovery agent N.A. Investigative [53]
2-chloro-2'-C-methyl-tecadenoson DMD3ZNP Discovery agent N.A. Investigative [38]
2-chloro-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine DMPCRLY Discovery agent N.A. Investigative [54]
2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine DMC5OQ3 Discovery agent N.A. Investigative [54]
2-chloroadenosine DMYPQEW Discovery agent N.A. Investigative [55]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine DM6CZAN Discovery agent N.A. Investigative [30]
2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine DM0BHKM Discovery agent N.A. Investigative [54]
2-ethyl-4-(furan-3-yl)thieno[3,2-d]pyrimidine DMR0IEK Discovery agent N.A. Investigative [54]
2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine DMWFR16 Discovery agent N.A. Investigative [54]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine DMWCGE8 Discovery agent N.A. Investigative [54]
2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine DMIRSQO Discovery agent N.A. Investigative [54]
2-ethynyl-N6-methoxyadenosine DM2D78W Discovery agent N.A. Investigative [48]
2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one DM3AFXM Discovery agent N.A. Investigative [56]
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(5H)-one DM1NK2M 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 [30]
2-phenyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one DMFE2R1 Discovery agent N.A. Investigative [56]
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 [45]
2-tolyl-6-phenyl-9H-purine DM1HABS Discovery agent N.A. Investigative [41]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine DMKC1GI Discovery agent N.A. Investigative [48]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine DMTNQZU Discovery agent N.A. Investigative [48]
3,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide DM4RNOE Discovery agent N.A. Investigative [39]
3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one DMI2RH1 Discovery agent N.A. Investigative [44]
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-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide DMAWC7S Discovery agent N.A. Investigative [39]
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 [51]
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 [52]
4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine DMK3J8Q Discovery agent N.A. Investigative [54]
4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile DM7X59V Discovery agent N.A. Investigative [43]
4-Bromo-N-(4-phenyl-thiazol-2-yl)-benzamide DMJFY9Z Discovery agent N.A. Investigative [39]
4-Chloro-7-methyl-2-phenyl-[1,8]naphthyridine DM9SVEB Discovery agent N.A. Investigative [61]
4-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide DMVKU4L Discovery agent N.A. Investigative [39]
4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one DM8642Z Discovery agent N.A. Investigative [62]
4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide DMFKN1M Discovery agent N.A. Investigative [39]
4-Methyl-N-(4-phenyl-thiazol-2-yl)-benzamide DMSF5DR Discovery agent N.A. Investigative [39]
4-Nitro-N-(4-phenyl-thiazol-2-yl)-benzamide DMKZUWY Discovery agent N.A. Investigative [39]
4-tert-Butyl-N-(4-phenyl-thiazol-2-yl)-benzamide DMLFZ6Q Discovery agent N.A. Investigative [39]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol DMZLOVB Discovery agent N.A. Investigative [63]
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol DM4TIXY Discovery agent N.A. Investigative [42]
5-Cl-5-deoxy-(+/-)-ENBA DM109IL Discovery agent N.A. Investigative [40]
6-(furan-2-yl)-9H-purin-2-amine DMOYCBH Discovery agent N.A. Investigative [60]
6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine DME4GBS Discovery agent N.A. Investigative [45]
6-guanidino-2-(3''-indolylethyloxy)adenosine DMM86PK Discovery agent N.A. Investigative [45]
7-(3,6,9,12-tetraoxatricos-22-enyl)theophylline DMNQW2B Discovery agent N.A. Investigative [64]
7-Bromo-2-phenyl-[1,8]naphthyridin-4-ol DMG8ZJA Discovery agent N.A. Investigative [65]
7-Chloro-2-phenyl-[1,8]naphthyridin-4-ol DM9TZH4 Discovery agent N.A. Investigative [65]
7-Dimethylamino-2-phenyl-[1,8]naphthyridin-4-ol DMNEAU0 Discovery agent N.A. Investigative [65]
7-Methyl-2-propyl-[1,8]naphthyridin-4-ol DMGB9IE Discovery agent N.A. Investigative [65]
8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine DMMQ79W Discovery agent N.A. Investigative [66]
8-Bromo-9-(2-butyl)-9H-adenine DM5DCPF Discovery agent N.A. Investigative [66]
8-Bromo-9-(2-hydroxypropyl)-9H-adenine DMKW2PE Discovery agent N.A. Investigative [66]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine DMA258T Discovery agent N.A. Investigative [66]
8-Bromo-9-(but-3-enyl)-9H-adenine DMXNF3V Discovery agent N.A. Investigative [66]
8-Bromo-9-(sec-butyl)-9H-adenine DMSQPFM Discovery agent N.A. Investigative [66]
8-Bromo-9-cyclobutyl-9H-adenine DMUTV76 Discovery agent N.A. Investigative [66]
8-Bromo-9-cyclohexyl-9H-adenine DMLVCON Discovery agent N.A. Investigative [66]
8-Bromo-9-cyclopentyl-9H-adenine DMCK0O1 Discovery agent N.A. Investigative [66]
8-Bromo-9-ethyl-9H-adenine DM4YAD6 Discovery agent N.A. Investigative [66]
8-bromo-9-isobutyl-9H-purin-6-amine DMZF3UN Discovery agent N.A. Investigative [49]
8-Bromo-9-isopropyl-9H-adenine DMIN9HC Discovery agent N.A. Investigative [66]
8-Bromo-9-methyl-9H-adenine DM1DS3B Discovery agent N.A. Investigative [66]
8-Bromo-9-phenylethyl-9H-adenine DMB7EWZ Discovery agent N.A. Investigative [66]
8-Bromo-9-propyl-9H-adenine DMRIPU5 Discovery agent N.A. Investigative [66]
8-cyclohexyl-6-(4-tolyl)-2-phenyl-9H-purine DM79VQM Discovery agent N.A. Investigative [41]
8-cyclopentyltheophylline DMMITAJ Discovery agent N.A. Investigative [67]
8-PHENYL THEOPHYLLINE DMFGUCY Discovery agent N.A. Investigative [30]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione DMHQGOC Discovery agent N.A. Investigative [68]
8-Phenyl-3,7-dihydro-purine-2,6-dione DMJB1NI Discovery agent N.A. Investigative [68]
8-propyl-2,6-diphenyl-9H-purine DMT6YUF Discovery agent N.A. Investigative [41]
9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine DMDYZCH Discovery agent N.A. Investigative [52]
9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine DM4X18V Discovery agent N.A. Investigative [52]
9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine DMURKL9 Discovery agent N.A. Investigative [52]
9-Allyl-8-bromo-9H-adenine DM8VZIY Discovery agent N.A. Investigative [66]
9-benzyl-6-(furan-2-yl)-9H-purin-2-amine DMO6CB7 Discovery agent N.A. Investigative [52]
9-Benzyl-8-bromo-9H-adenine DMMWGVI Discovery agent N.A. Investigative [66]
9-Cyclobutyl-9H-adenine DM04QWX Discovery agent N.A. Investigative [66]
9-Cyclopentyl-9H-adenine DMSGU2L Discovery agent N.A. Investigative [29]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine DMRVS2D Discovery agent N.A. Investigative [69]
9-Ethyl-9H-adenine DMWV8YX Discovery agent N.A. Investigative [66]
9-Isopropyl-9H-adenine DMBQLAI Discovery agent N.A. Investigative [66]
9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine DMO4CSP Discovery agent N.A. Investigative [70]
9-Methyl-9H-adenine DM6DOVL Discovery agent N.A. Investigative [26]
9-Phenyl-9H-purin-6-ylamine DM73O2A Discovery agent N.A. Investigative [29]
9-Propyl-9H-adenine DMQTEPY Discovery agent N.A. Investigative [66]
A-987306 DMU34BK Discovery agent N.A. Investigative [71]
Anthoptilide C DMRQVW9 Discovery agent N.A. Investigative [72]
AS100 DMXZ8S9 Discovery agent N.A. Investigative [73]
AS70 DM9CIJP Discovery agent N.A. Investigative [73]
AS99 DMZ7FJN Discovery agent N.A. Investigative [73]
ATL802 DMYMCQA Discovery agent N.A. Investigative [74]
Cirsimarin DMM10TG Discovery agent N.A. Investigative [75]
CP608,039 DMTKO7P Discovery agent N.A. Investigative [76]
CPFPX DMFE5GX Discovery agent N.A. Investigative [77]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine DMLREDJ Discovery agent N.A. Investigative [78]
Cyclohexyl-(9-ethyl-9H-purin-6-yl)-amine DM1F7I5 Discovery agent N.A. Investigative [29]
Cyclohexyl-(9-methyl-9H-purin-6-yl)-amine DMIUCSW Discovery agent N.A. Investigative [29]
Cyclopentyl-(9-cyclopentyl-9H-purin-6-yl)-amine DMBDTFQ Discovery agent N.A. Investigative [29]
Cyclopentyl-(9-ethyl-9H-purin-6-yl)-amine DMQ6BS2 Discovery agent N.A. Investigative [29]
Cyclopentyl-(9-methyl-9H-purin-6-yl)-amine DM9DHNZ Discovery agent N.A. Investigative [29]
Cyclopentyl-(9-phenyl-9H-purin-6-yl)-amine DMBJV90 Discovery agent N.A. Investigative [29]
DEPX DM4JM50 Discovery agent N.A. Investigative [79]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate DMK4T5Y Discovery agent N.A. Investigative [9]
flavone DMEQH6J Discovery agent N.A. Investigative [62]
FR-166124 DMPCBXT Discovery agent N.A. Investigative [80]
FR194921 DMISP7G Discovery agent N.A. Investigative [81]
GNF-PF-2224 DM26UKN Discovery agent N.A. Investigative [82]
GNF-PF-2700 DMC56YJ Discovery agent N.A. Investigative [49]
Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide DMJOZYG Discovery agent N.A. Investigative [83]
isobutylmethylxanthine DM46F5X Discovery agent N.A. Investigative [84]
Isoguanosine DMAFLCJ Discovery agent N.A. Investigative [85]
KF26777 DMPBDW0 Discovery agent N.A. Investigative [86]
Kuanoniamine D DMAVM94 Discovery agent N.A. Investigative [87]
L-249313 DMEK65F Discovery agent N.A. Investigative [13]
L-97-1 intravenous DMYDR2N Sepsis 1G40-1G41 Investigative [88]
LUF-5417 DMUPQED Discovery agent N.A. Investigative [9]
LUF-5433 DME4O5D Discovery agent N.A. Investigative [9]
LUF-5735 DM89FBX Discovery agent N.A. Investigative [83]
LUF-5737 DMXFD3S Discovery agent N.A. Investigative [83]
LUF-5764 DMQ3VHR Discovery agent N.A. Investigative [83]
LUF-5767 DMP08QO Discovery agent N.A. Investigative [83]
LUF-5816 DMQZDMH Discovery agent N.A. Investigative [42]
LUF-5853 DMZQU90 Discovery agent N.A. Investigative [43]
LUF-5956 DMG4YWM Discovery agent N.A. Investigative [41]
LUF-5957 DMJFMH9 Discovery agent N.A. Investigative [41]
LUF-5962 DMR6LIE Discovery agent N.A. Investigative [41]
LUF-5978 DMCTM3L Discovery agent N.A. Investigative [42]
LUF-5980 DMGOIF5 Discovery agent N.A. Investigative [42]
LUF-5981 DMHO3XL Discovery agent N.A. Investigative [42]
LUF-6258 DM0K75N Discovery agent N.A. Investigative [89]
LUF5831 DMYZGIK Discovery agent N.A. Investigative [90]
MRE 2029F20 DMUK1PA Discovery agent N.A. Investigative [91]
MRE 3008F20 DM72US0 Discovery agent N.A. Investigative [76]
MRS1041 DMBXKYR Discovery agent N.A. Investigative [62]
MRS1042 DMVT865 Discovery agent N.A. Investigative [62]
MRS1062 DM50QBR Discovery agent N.A. Investigative [62]
MRS1065 DMYAHU3 Discovery agent N.A. Investigative [62]
MRS1084 DMKELWG Discovery agent N.A. Investigative [62]
MRS1086 DM1K5E2 Discovery agent N.A. Investigative [62]
MRS1093 DM801AO Discovery agent N.A. Investigative [62]
MRS1132 DMY4C0G Discovery agent N.A. Investigative [62]
MRS1191 DM9WX3C Discovery agent N.A. Investigative [88]
MRS1523 DM4AONZ Discovery agent N.A. Investigative [88]
MRS5151 DM1GUTC Discovery agent N.A. Investigative [92]
MRS923 DMMN42V Discovery agent N.A. Investigative [62]
MRS928 DMKJ9WM Discovery agent N.A. Investigative [62]
N(6)-cyclohexyladenosine DMHINE0 Discovery agent N.A. Investigative [93]
N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine DM1K2A4 Discovery agent N.A. Investigative [78]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine DM3C8PJ Discovery agent N.A. Investigative [78]
N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine DMCOPR3 Discovery agent N.A. Investigative [78]
N-(2,6-diphenylpyrimidin-4-yl)-2-ethylbutyramide DMK5AU4 Discovery agent N.A. Investigative [83]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide DM6HGK4 Discovery agent N.A. Investigative [83]
N-(2,6-diphenylpyrimidin-4-yl)acetamide DMQ0DMU Discovery agent N.A. Investigative [83]
N-(2,6-diphenylpyrimidin-4-yl)benzamide DMBW752 Discovery agent N.A. Investigative [83]
N-(2,6-diphenylpyrimidin-4-yl)butyramide DM5EF71 Discovery agent N.A. Investigative [83]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide DMWPZCS Discovery agent N.A. Investigative [83]
N-(2,6-diphenylpyrimidin-4-yl)propionamide DM89NGE Discovery agent N.A. Investigative [83]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide DMLTROU Discovery agent N.A. Investigative [94]
N-(4,5-diphenylpyrimidin-2-yl)acetamide DM34R10 Discovery agent N.A. Investigative [83]
N-(4,6-diphenylpyrimidin-2-yl)-2-ethylbutyramide DMDP1QG Discovery agent N.A. Investigative [83]
N-(4,6-diphenylpyrimidin-2-yl)-3-chlorobenzamide DMQVPK9 Discovery agent N.A. Investigative [83]
N-(4,6-diphenylpyrimidin-2-yl)-3-methylbutyramide DMOAPJ1 Discovery agent N.A. Investigative [83]
N-(4,6-diphenylpyrimidin-2-yl)benzamide DMA214F Discovery agent N.A. Investigative [83]
N-(4,6-diphenylpyrimidin-2-yl)propionamide DMJZ2IP Discovery agent N.A. Investigative [83]
N-(4-Phenyl-thiazol-2-yl)-benzamide DMPA91F Discovery agent N.A. Investigative [39]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide DMTF8US Discovery agent N.A. Investigative [9]
N6-((+/-)-endo-norborn-2-yl)adenosine DM30KXV Discovery agent N.A. Investigative [40]
N6-CYCLOPENTYLADENOSINE DMD6AJO Discovery agent N.A. Investigative [38]
N6-methoxy-2-phenylethynyladenosine DMDG59X Discovery agent N.A. Investigative [48]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine DMSEL5W Discovery agent N.A. Investigative [48]
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine DMP7246 Discovery agent N.A. Investigative [48]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine DM8LR62 Discovery agent N.A. Investigative [48]
N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine DM1KA9R Discovery agent N.A. Investigative [48]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine DMQ5K8R Discovery agent N.A. Investigative [48]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine DM9H3W8 Discovery agent N.A. Investigative [48]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine DMRBS50 Discovery agent N.A. Investigative [48]
N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine DM0WMKJ Discovery agent N.A. Investigative [95]
N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine DMVNLPF Discovery agent N.A. Investigative [95]
P-IODOAMPHETAMINE DMHLBZR Discovery agent N.A. Investigative [96]
Paeoniflorin DMJ5TAU Parkinson disease 8A00.0 Investigative [88]
PD-115199 DMQ4LRZ Discovery agent N.A. Investigative [97]
PD-81723 DM5SYTW Discovery agent N.A. Investigative [98]
PENECA DMIDSJ9 Discovery agent N.A. Investigative [32]
Pentanoic acid (4,6-diphenylpyrimidin-2-yl)amide DM3S790 Discovery agent N.A. Investigative [83]
Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol DMDV1SN Discovery agent N.A. Investigative [99]
Phenyl-(9-phenyl-9H-purin-6-yl)-amine DMIQ18W Discovery agent N.A. Investigative [29]
PSB-0788 DM0FKV9 Discovery agent N.A. Investigative [100]
PSB-10 DMXDWO7 Discovery agent N.A. Investigative [101]
PSB-11 DMGK2PC Discovery agent N.A. Investigative [101]
PSB-1115 DMOH2VC Discovery agent N.A. Investigative [100]
PSB-601 DMBIK7D Discovery agent N.A. Investigative [100]
PSB36 DMBGM1E Discovery agent N.A. Investigative [102]
PSB603 DM6QERS Discovery agent N.A. Investigative [100]
R-N6-(phenylisopropyl)adenosine DM2N3BA Discovery agent N.A. Investigative [103]
sakuranetin DMUAQYZ Discovery agent N.A. Investigative [62]
SB-298 DMU2J3K Discovery agent N.A. Investigative [100]
SCH-63390 DMAUB9F Discovery agent N.A. Investigative [104]
ST-1535 DMUTC9Z Discovery agent N.A. Investigative [70]
TCPA DMTF4VI Discovery agent N.A. Investigative [105]
VCP-28 DMG1YZQ Discovery agent N.A. Investigative [106]
VUF-8507 DMQFWV7 Discovery agent N.A. Investigative [107]
VUF5574 DMUA751 Discovery agent N.A. Investigative [108]
WRC-0571 DM1U29V Discovery agent N.A. Investigative [109]
xanthine amine congener DMGYVFD Discovery agent N.A. Investigative [84]
[3H]CCPA DMHDGB3 Discovery agent N.A. Investigative [103]
[3H]DPCPX DM9GY7O Discovery agent N.A. Investigative [110]
[3H]HEMADO DMEO6AH Discovery agent N.A. Investigative [111]
[3H]NECA DMAO9SH Discovery agent N.A. Investigative [112]
[3H]OSIP339391 DM4BY5J Discovery agent N.A. Investigative [49]
------------------------------------------------------------------------------------
⏷ Show the Full List of 280 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Parkinson's disease 8A00.0 Substantia nigra tissue 7.60E-01 -0.12 -0.48
Asthma CA23 Nasal and bronchial airway 1.74E-01 -0.13 -0.36
Neonatal sepsis 1G41 Whole blood 7.48E-02 -0.09 -0.3
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References

1 Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.
2 Association between the PDE4D gene and ischaemic stroke in the Chinese Han population. Clin Sci (Lond). 2009 Aug 17;117(7):265-72.
3 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.
4 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004779)
5 Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Current Issue vol. 111 no. 12 Celine Valant, 4614-4619.
6 A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008 Dec;17(12):1901-10.
7 Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308.
8 Role of matrix metalloproteinases and their tissue inhibitors as potential biomarkers of left ventricular remodelling in the athlete's heart. Clin Sci (Lond). 2009 Jul 16;117(4):157-64.
9 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.
10 INO-8875, a highly selective A1 adenosine receptor agonist: evaluation of chronotropic, dromotropic, and hemodynamic effects in rats. J Pharmacol Exp Ther. 2013 Jan;344(1):59-67.
11 Adenosine A1R/A3R (Adenosine A1 and A3 Receptor) Agonist AST-004 Reduces Brain Infarction in a Nonhuman Primate Model of Stroke. Stroke. 2022 Jan;53(1):238-248.
12 Reduction of free fatty acids, safety, and pharmacokinetics of oral GS-9667, an A(1) adenosine receptor partial agonist. J Clin Pharmacol. 2013 Apr;53(4):385-92.
13 2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic gluc... J Med Chem. 2001 Jan 18;44(2):170-9.
14 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.
15 Carbonic anhydrase inhibitors: a review on the progress of patent literature (2011-2016).Expert Opin Ther Pat. 2016 Aug;26(8):947-56.
16 CV Therapeutics. Company report from CV Therapeutics, Inc. CV Therapeutics. 2009.
17 N-0861 selectively antagonizes adenosine A1 receptors in vivo. Eur J Pharmacol. 1992 May 27;216(1):9-16.
18 Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. J Med Chem. 1994 Feb 18;37(4):476-85.
19 Adenosine A1 receptor antagonist improves intradialytic hypotension. Kidney Int. 2006 Mar;69(5):877-83.
20 Cardiovascular and renal effects of blocking A1 adenosine receptors. J Cardiovasc Pharmacol. 1993 May;21(5):822-8.
21 An orally active adenosine A1 receptor antagonist, FK838, increases renal excretion and maintains glomerular filtration rate in furosemide-resistan... Br J Pharmacol. 2003 Aug;139(8):1383-8.
22 Effect of the adenosine A1 receptor agonist GR79236 on trigeminal nociception with blink reflex recordings in healthy human subjects. Cephalalgia. 2003 May;23(4):287-92.
23 The cardiac effects of a novel A1-adenosine receptor agonist in guinea pig isolated heart. J Pharmacol Exp Ther. 1994 Dec;271(3):1371-82.
24 Protein 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.
25 Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. J Med Chem. 2000 Jun 1;43(11):2196-203.
26 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.
27 N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. J Med Chem. 1999 Sep 9;42(18):3463-77.
28 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.
29 N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor. J Med Chem. 1991 Sep;34(9):2877-82.
30 1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. J Med Chem. 1991 Mar;34(3):1202-6.
31 Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists. J Med Chem. 1993 May 14;36(10):1333-42.
32 N(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.
33 A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding. J Biol Chem. 1994 Jan 28;269(4):2373-6.
34 Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. J Med Chem. 1988 Oct;31(10):2034-9.
35 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.
36 Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-,... J Med Chem. 1989 Jun;32(6):1231-7.
37 Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. J Med Chem. 2002 May 23;45(11):2131-8.
38 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.
39 Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor. Bioorg Med Chem Lett. 2001 Aug 6;11(15):2017-9.
40 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.
41 2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. J Med Chem. 2006 May 18;49(10):2861-7.
42 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34.
43 A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. Bioorg Med Chem. 2008 Mar 15;16(6):2741-52.
44 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.
45 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.
46 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.
47 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.
48 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.
49 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.
50 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem. 2008 Aug 14;51(15):4449-55.
51 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.
52 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.
53 2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. J Med Chem. 2006 Dec 14;49(25):7373-83.
54 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.
55 Identification of the adenine binding site of the human A1 adenosine receptor. J Biol Chem. 1999 Feb 5;274(6):3617-21.
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 A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives. J Med Chem. 2000 Jul 27;43(15):2814-23.
62 Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301.
63 Synthesis of eudistomin D analogues and its effects on adenosine receptors. Bioorg Med Chem. 2008 Apr 1;16(7):3825-30.
64 Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. Bioorg Med Chem. 2010 Mar 15;18(6):2081-2088.
65 Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. J Med Chem. 2004 Jun 3;47(12):3019-31.
66 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.
67 Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors. Biochem Pharmacol. 1998 Dec 1;56(11):1437-45.
68 Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationshi... J Med Chem. 1993 Oct 29;36(22):3341-9.
69 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.
70 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.
71 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
72 Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali. J Nat Prod. 2000 Mar;63(3):318-21.
73 Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors. Biochem Pharmacol. 2005 Nov 25;70(11):1601-12.
74 Anilide 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.
75 Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis. J Nat Prod. 1997 Jun;60(6):638-41.
76 Adenosine receptors as therapeutic targets. Nat Rev Drug Discov. 2006 Mar;5(3):247-64.
77 Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging. J Med Chem. 2002 Nov 7;45(23):5150-6.
78 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.
79 125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors. J Med Chem. 1988 Apr;31(4):745-51.
80 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.
81 Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors. J Pharmacol Sci. 2004 Sep;96(1):42-52.
82 Minoxidil-induced hair growth is mediated by adenosine in cultured dermal papilla cells: possible involvement of sulfonylurea receptor 2B as a target of minoxidil. J Invest Dermatol. 2001 Dec;117(6):1594-600.
83 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.
84 Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor. J Biol Chem. 1994 Dec 23;269(51):32077-84.
85 High selectivity of novel isoguanosine analogues for the adenosine A1 receptor. Bioorg. Med. Chem. Lett. 1(9):481-486 (1991).
86 KF26777 (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.
87 Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp. J Nat Prod. 1998 Feb;61(2):301-5.
88 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. (Target id: 18).
89 Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. J Med Chem. 2010 Apr 22;53(8):3028-37.
90 Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist. Br J Pharmacol. 2006 Mar;147(5):533-41.
91 Design, 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.
92 Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2813-9.
93 Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors. Pharmacology. 1993;46(2):91-100.
94 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.
95 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.
96 Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective a... J Med Chem. 1992 Oct 30;35(22):4143-9.
97 (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.
98 Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of t... J Med Chem. 2008 Sep 25;51(18):5875-9.
99 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.
100 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.
101 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors. Bioorg Med Chem. 2003 Feb 6;11(3):347-56.
102 Antinociceptive effects of novel A2B adenosine receptor antagonists. J Pharmacol Exp Ther. 2004 Jan;308(1):358-66.
103 Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):1-9.
104 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.
105 N6-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.
106 Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists. Bioorg Med Chem. 2010 May 1;18(9):3078-87.
107 Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. J Med Chem. 2000 Jun 1;43(11):2227-38.
108 A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. J Med Chem. 1998 Oct 8;41(21):3987-93.
109 Characterization of 8-(N-methylisopropyl)amino-N6-(5'-endohydroxy- endonorbornyl)-9-methyladenine (WRC-0571), a highly potent and selective, non-xanthine antagonist of A1 adenosine receptors. J Pharmacol Exp Ther. 1996 Feb;276(2):490-9.
110 Inhibition 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.
111 [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor. Eur J Pharmacol. 2007 Feb 5;556(1-3):14-8.
112 Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. J Med Chem. 1988 Jun;31(6):1179-83.