Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTJFY5U)

• DTT Name: Adenosine A3 receptor (ADORA3)
• Synonyms: Adenosine receptor A3A; Adenosine receptor A3; Adenosine 3 receptor; A3AR; A3 Adenosine receptor
• Gene Name: ADORA3
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: AA3R_HUMAN
• TTD ID: T36059
• Sequence:
  MPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYFIVSLALADIA
  VGVLVMPLAIVVSLGITIHFYSCLFMTCLLLIFTHASIMSLLAIAVDRYLRVKLTVRYKR
  VTTHRRIWLALGLCWLVSFLVGLTPMFGWNMKLTSEYHRNVTFLSCQFVSVMRMDYMVYF
  SFLTWIFIPLVVMCAIYLDIFYIIRNKLSLNLSNSKETGAFYGREFKTAKSLFLVLFLFA
  LSWLPLSIINCIIYFNGEVPQLVLYMGILLSHANSMMNPIVYAYKIKKFKETYLLILKAC
  VVCHPSDSLDTSIEKNSE
• Function: The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. Isoform 2: Receptor for adenosine.
• KEGG Pathway:
  cGMP-PKG signaling pathway (hsa04022)
  Sphingolipid signaling pathway (hsa04071)
  Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Adenosine P1 receptors (R-HSA-417973)

Molecular Interaction Atlas (MIA) of This DTT

6 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
IB-MECA	DM9G5XD	Psoriasis vulgaris	EA90	Phase 3	[1]
CF102	DMP56WJ	Hepatocellular carcinoma	2C12.02	Phase 2	[2]
NITD609	DMQHBSX	Malaria	1F40-1F45	Phase 2	[3]
Tonapofylline	DMBH316	Acute and chronic heart failure	BD1Z	Phase 2	[4]
AST-004	DM5WMG7	Stroke	8B20	Phase 1	[5]
SCH-442416	DMQ2K1V	N. A.	N. A.	Phase 1	[6]

4 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BEMESETRON	DMSPJX9	N. A.	N. A.	Discontinued in Phase 3	[7]
DIZOCILPINE	DMMGYXR	Cerebrovascular ischaemia	8B1Z	Terminated	[7]
METHYLTHIOADENOSINE	DMC8J6F	Multiple sclerosis	8A40	Terminated	[9]
METRIFUDIL	DMS5CZ4	N. A.	N. A.	Terminated	[10]

3 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 60-6583	DMTEJV1	Myocardial ischemia	BA6Z	Preclinical	[8]
CF502	DMQSJ20	Inflammation	1A00-CA43.1	Preclinical	[2]
CF602	DM0ULO2	Inflammation	1A00-CA43.1	Preclinical	[2]

209 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+)-BUTACLAMOL	DMX6UYN	Discovery agent	N.A.	Investigative	[7]
(2R,3S)-3-(6-Amino-purin-9-yl)-nonan-2-ol	DM852Z6	Discovery agent	N.A.	Investigative	[11]
(E)-8-(3-chlorostyryl)-caffeine	DMQT15Z	Discovery agent	N.A.	Investigative	[12]
(R,S)-PHPNECA	DMQO71C	Discovery agent	N.A.	Investigative	[13]
(S)-PIA	DM04BHI	Discovery agent	N.A.	Investigative	[14]
1,2-dihydro-2-oxoquinazoline-4-carboxyanilide	DM542I9	Discovery agent	N.A.	Investigative	[15]
1-(2-(diethylamino)quinazolin-4-yl)-3-phenylurea	DMU5BOW	Discovery agent	N.A.	Investigative	[16]
1-Allyl-3,7-dihydro-purine-2,6-dione	DML54H2	Discovery agent	N.A.	Investigative	[17]
1-Benzyl-1H-1,3,4b,9-tetraaza-fluorene-2,4-dione	DMYGZ8V	Discovery agent	N.A.	Investigative	[18]
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione	DMMRV21	Discovery agent	N.A.	Investigative	[17]
1-Butyl-3,7-dihydro-purine-2,6-dione	DMOE2ZV	Discovery agent	N.A.	Investigative	[17]
1-Cyclopentyl-3,7-dihydro-purine-2,6-dione	DMEMQFH	Discovery agent	N.A.	Investigative	[17]
1-Phenethyl-3,7-dihydro-purine-2,6-dione	DMA29SX	Discovery agent	N.A.	Investigative	[17]
1-phenyl-3-(2-(pyridin-2-yl)quinazolin-4-yl)urea	DM9SKYC	Discovery agent	N.A.	Investigative	[16]
1-phenyl-3-(2-(pyridin-3-yl)quinazolin-4-yl)urea	DMQKB6W	Discovery agent	N.A.	Investigative	[16]
1-phenyl-3-(3-(pyridin-2-yl)isoquinolin-1-yl)urea	DMJNAX5	Discovery agent	N.A.	Investigative	[16]
1-phenyl-3-(quinazolin-4-yl)urea	DMZOEQY	Discovery agent	N.A.	Investigative	[16]
1-Prop-2-ynyl-3,7-dihydro-purine-2,6-dione	DMCBX7R	Discovery agent	N.A.	Investigative	[17]
1-Propyl-3,7-dihydro-purine-2,6-dione	DML5J94	Discovery agent	N.A.	Investigative	[17]
2'-Me-CCPA	DMDFPGB	Discovery agent	N.A.	Investigative	[19]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine	DMMESIU	Discovery agent	N.A.	Investigative	[20]
2,6,8-triphenyl-9H-purine	DM4IFPQ	Discovery agent	N.A.	Investigative	[21]
2,6-bis(4-chlorophenyl)-9H-purine	DMYQNK0	Discovery agent	N.A.	Investigative	[21]
2,6-bis(4-methoxyphenyl)-9H-purine	DMC2N80	Discovery agent	N.A.	Investigative	[21]
2,6-bis(4-tolyl)-9H-purine	DM41RZX	Discovery agent	N.A.	Investigative	[21]
2,6-diphenyl-1-deazapurine	DMW2VZ1	Discovery agent	N.A.	Investigative	[22]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine	DMY3C78	Discovery agent	N.A.	Investigative	[22]
2,6-diphenyl-8-ethyl-1-deazapurine	DM0C8BW	Discovery agent	N.A.	Investigative	[22]
2,6-diphenyl-8-methyl-1-deazapurine	DMI79FV	Discovery agent	N.A.	Investigative	[22]
2,6-diphenyl-8-tButyl-1-deazapurine	DM6D1BQ	Discovery agent	N.A.	Investigative	[22]
2,6-diphenyl-9H-purine	DM5SXYI	Discovery agent	N.A.	Investigative	[21]
2,6-dphenyl-8-propyl-1-deazapurine	DM8F9KO	Discovery agent	N.A.	Investigative	[22]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline	DM0Y2P1	Discovery agent	N.A.	Investigative	[23]
2-(1H-imidazo[4,5-c]pyridin-2-yl)quinoxaline	DMXA20E	Discovery agent	N.A.	Investigative	[24]
2-(2''-indolylethyloxy)adenosine	DMCLIN8	Discovery agent	N.A.	Investigative	[25]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine	DMD8Q3E	Discovery agent	N.A.	Investigative	[25]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine	DMITEND	Discovery agent	N.A.	Investigative	[25]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine	DMXRHOY	Discovery agent	N.A.	Investigative	[25]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine	DMR8PGZ	Discovery agent	N.A.	Investigative	[25]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine	DME3IN1	Discovery agent	N.A.	Investigative	[25]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine	DM6BIOP	Discovery agent	N.A.	Investigative	[25]
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine	DMFP0IW	Discovery agent	N.A.	Investigative	[25]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine	DMWA0MN	Discovery agent	N.A.	Investigative	[25]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine	DMGRC24	Discovery agent	N.A.	Investigative	[25]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine	DML39UW	Discovery agent	N.A.	Investigative	[25]
2-(3''-(benzoimidazole-1''-yl)ethyloxy)adenosine	DMLDOH6	Discovery agent	N.A.	Investigative	[25]
2-(3''-(benzotriazole-1''-yl)ethyloxy)adenosine	DM1KCUV	Discovery agent	N.A.	Investigative	[25]
2-(3''-indolylethyloxy)adenosine	DMXRAE3	Discovery agent	N.A.	Investigative	[25]
2-(3''-pyrrolylethyloxy)adenosine	DMNCP8Y	Discovery agent	N.A.	Investigative	[25]
2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline	DM7BHYS	Discovery agent	N.A.	Investigative	[24]
2-(4-chlorophenyl)-6-phenyl-9H-purine	DMAPWNR	Discovery agent	N.A.	Investigative	[21]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline	DMTAVU5	Discovery agent	N.A.	Investigative	[24]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine	DM1C864	Discovery agent	N.A.	Investigative	[26]
2-(4-methoxyphenyl)-6-phenyl-9H-purine	DMXTHOV	Discovery agent	N.A.	Investigative	[21]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline	DMDXIN1	Discovery agent	N.A.	Investigative	[23]
2-(4-nitro-1H-benzo[d]imidazol-2-yl)quinoxaline	DMBJICP	Discovery agent	N.A.	Investigative	[24]
2-(5-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline	DM0ZB89	Discovery agent	N.A.	Investigative	[24]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine	DMSIJ17	Discovery agent	N.A.	Investigative	[26]
2-(hex-1-ynyl)-N6-methoxyadenosine	DM7YLTS	Discovery agent	N.A.	Investigative	[26]
2-acetylaminoquinazoline-4-carboxyanilide	DM0NJYZ	Discovery agent	N.A.	Investigative	[15]
2-aminoquinazoline-4-carboxy-(4-bromophenyl)amide	DMJW4CS	Discovery agent	N.A.	Investigative	[15]
2-aminoquinazoline-4-carboxyanilide	DMQJYX7	Discovery agent	N.A.	Investigative	[15]
2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine	DMBSDIV	Discovery agent	N.A.	Investigative	[27]
2-benzoylaminoquinazoline-4-carboxyanilide	DMGEFQP	Discovery agent	N.A.	Investigative	[15]
2-benzyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one	DM6E04T	Discovery agent	N.A.	Investigative	[28]
2-chloro-2'-C-methyl-tecadenoson	DMD3ZNP	Discovery agent	N.A.	Investigative	[29]
2-chloroadenosine	DMYPQEW	Discovery agent	N.A.	Investigative	[12]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine	DMWCGE8	Discovery agent	N.A.	Investigative	[30]
2-ethynyl-N6-methoxyadenosine	DM2D78W	Discovery agent	N.A.	Investigative	[26]
2-Phenyl-2H-pyrazolo[4,3-c]quinoline	DMAHI7G	Discovery agent	N.A.	Investigative	[31]
2-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one	DMQXCIK	Discovery agent	N.A.	Investigative	[32]
2-phenylethylyl-adenosine derivative	DMW3F5C	Discovery agent	N.A.	Investigative	[33]
2-phenylpropoxyadenosine	DMZQCEP	Discovery agent	N.A.	Investigative	[25]
2-tolyl-6-phenyl-9H-purine	DM1HABS	Discovery agent	N.A.	Investigative	[21]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine	DMKC1GI	Discovery agent	N.A.	Investigative	[26]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine	DMTNQZU	Discovery agent	N.A.	Investigative	[26]
3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one	DMI2RH1	Discovery agent	N.A.	Investigative	[23]
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione	DMKYPUW	Discovery agent	N.A.	Investigative	[17]
3-noradamantyl-1,3-dipropylxanthine	DMFHYAE	Discovery agent	N.A.	Investigative	[34]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[35]
4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one	DM8642Z	Discovery agent	N.A.	Investigative	[36]
4-Methoxy-2-phenyl-2H-pyrazolo[4,3-c]quinoline	DM97B2G	Discovery agent	N.A.	Investigative	[31]
4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide	DMFKN1M	Discovery agent	N.A.	Investigative	[37]
5,6,7-Trimethyl-2-p-tolyl-chromen-4-one	DM6VPF4	Discovery agent	N.A.	Investigative	[38]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol	DMZLOVB	Discovery agent	N.A.	Investigative	[39]
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol	DM4TIXY	Discovery agent	N.A.	Investigative	[22]
5-Butyl-8-phenyl-3H-[1,2,4]triazolo[5,1-i]purine	DM2EPFZ	Discovery agent	N.A.	Investigative	[40]
6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine	DME4GBS	Discovery agent	N.A.	Investigative	[25]
6-guanidino-2-(3''-indolylethyloxy)adenosine	DMM86PK	Discovery agent	N.A.	Investigative	[25]
6-Hydroxy-5,7-dimethyl-beta-carboline	DM0CVTI	Discovery agent	N.A.	Investigative	[39]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine	DMA258T	Discovery agent	N.A.	Investigative	[41]
8-Bromo-9-(sec-butyl)-9H-adenine	DMSQPFM	Discovery agent	N.A.	Investigative	[41]
8-Bromo-9-cyclobutyl-9H-adenine	DMUTV76	Discovery agent	N.A.	Investigative	[41]
8-Bromo-9-cyclohexyl-9H-adenine	DMLVCON	Discovery agent	N.A.	Investigative	[41]
8-Bromo-9-cyclopentyl-9H-adenine	DMCK0O1	Discovery agent	N.A.	Investigative	[41]
8-bromo-9-isobutyl-9H-purin-6-amine	DMZF3UN	Discovery agent	N.A.	Investigative	[42]
8-Bromo-9-isopropyl-9H-adenine	DMIN9HC	Discovery agent	N.A.	Investigative	[41]
8-Hydroxy-5,7,9-trimethyl-delta-carboline	DMG4W2C	Discovery agent	N.A.	Investigative	[39]
8-Hydroxy-7,9-dimethyl-delta-carboline	DMFL46R	Discovery agent	N.A.	Investigative	[39]
8-PHENYL THEOPHYLLINE	DMFGUCY	Discovery agent	N.A.	Investigative	[43]
8-propyl-2,6-diphenyl-9H-purine	DMT6YUF	Discovery agent	N.A.	Investigative	[21]
9-Cyclopentyl-9H-adenine	DMSGU2L	Discovery agent	N.A.	Investigative	[41]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine	DMRVS2D	Discovery agent	N.A.	Investigative	[44]
9H-purine derivative	DMF1XLZ	Discovery agent	N.A.	Investigative	[7]
AB-MECA	DMQPHFU	Discovery agent	N.A.	Investigative	[14]
ACN-1052	DM3E4QR	Glaucoma/ocular hypertension	9C61	Investigative	[45]
ATL802	DMYMCQA	Discovery agent	N.A.	Investigative	[46]
CIRSIMARITIN	DMA3N9R	Discovery agent	N.A.	Investigative	[38]
CP608,039	DMTKO7P	Discovery agent	N.A.	Investigative	[47]
Cyclohexyl-(2-phenoxy-9H-purin-6-yl)-amine	DM84ZX5	Discovery agent	N.A.	Investigative	[48]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine	DMLREDJ	Discovery agent	N.A.	Investigative	[48]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate	DMK4T5Y	Discovery agent	N.A.	Investigative	[4]
flavone	DMEQH6J	Discovery agent	N.A.	Investigative	[36]
Galangin	DM5TQ2O	Discovery agent	N.A.	Investigative	[38]
GNF-PF-2224	DM26UKN	Discovery agent	N.A.	Investigative	[49]
Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide	DMJOZYG	Discovery agent	N.A.	Investigative	[50]
I-ABA	DMIJ2GV	Discovery agent	N.A.	Investigative	[51]
I-ABOPX	DM5X0JS	Discovery agent	N.A.	Investigative	[51]
isobutylmethylxanthine	DM46F5X	Discovery agent	N.A.	Investigative	[43]
KF26777	DMPBDW0	Discovery agent	N.A.	Investigative	[52]
L-249313	DMEK65F	Discovery agent	N.A.	Investigative	[53]
LUF-5417	DMUPQED	Discovery agent	N.A.	Investigative	[4]
LUF-5433	DME4O5D	Discovery agent	N.A.	Investigative	[4]
LUF-5767	DMP08QO	Discovery agent	N.A.	Investigative	[50]
LUF-5816	DMQZDMH	Discovery agent	N.A.	Investigative	[22]
LUF-5833	DMDHUL8	Ischemia	8B10-8B11	Investigative	[45]
LUF-5956	DMG4YWM	Discovery agent	N.A.	Investigative	[21]
LUF-5957	DMJFMH9	Discovery agent	N.A.	Investigative	[21]
LUF-5962	DMR6LIE	Discovery agent	N.A.	Investigative	[21]
LUF-5978	DMCTM3L	Discovery agent	N.A.	Investigative	[22]
LUF-5980	DMGOIF5	Discovery agent	N.A.	Investigative	[22]
LUF-5981	DMHO3XL	Discovery agent	N.A.	Investigative	[22]
MESULERGINE	DMKGWAH	Discovery agent	N.A.	Investigative	[7]
METHOCTRAMINE	DMH2CKX	Discovery agent	N.A.	Investigative	[7]
MPC-MECA	DMONDP1	Discovery agent	N.A.	Investigative	[14]
MRE 2029F20	DMUK1PA	Discovery agent	N.A.	Investigative	[54]
MRE 3008F20	DM72US0	Discovery agent	N.A.	Investigative	[14]
MRE 3010F20	DMMFJA8	Discovery agent	N.A.	Investigative	[14]
MRS-1220	DMT6JH9	Discovery agent	N.A.	Investigative	[55]
MRS1041	DMBXKYR	Discovery agent	N.A.	Investigative	[36]
MRS1042	DMVT865	Discovery agent	N.A.	Investigative	[36]
MRS1067	DMAEW9M	Discovery agent	N.A.	Investigative	[56]
MRS1088	DMSKWL7	Discovery agent	N.A.	Investigative	[36]
MRS1093	DM801AO	Discovery agent	N.A.	Investigative	[36]
MRS1097	DMLOHAZ	Discovery agent	N.A.	Investigative	[57]
MRS1177	DMBXTPU	Discovery agent	N.A.	Investigative	[58]
MRS1186	DMGJ0IE	Discovery agent	N.A.	Investigative	[58]
MRS1191	DM9WX3C	Discovery agent	N.A.	Investigative	[45]
MRS1476	DMLQYN7	Discovery agent	N.A.	Investigative	[59]
MRS1486	DMFJHMQ	Discovery agent	N.A.	Investigative	[59]
MRS1505	DM3Q5NO	Discovery agent	N.A.	Investigative	[59]
MRS1523	DM4AONZ	Discovery agent	N.A.	Investigative	[59]
MRS5151	DM1GUTC	Discovery agent	N.A.	Investigative	[60]
MRS5698	DMDF6WG	Discovery agent	N.A.	Investigative	[61]
MRS928	DMKJ9WM	Discovery agent	N.A.	Investigative	[36]
N(6)-cyclohexyladenosine	DMHINE0	Discovery agent	N.A.	Investigative	[62]
N*2*-Benzyl-N*6*-cyclohexyl-9H-purine-2,6-diamine	DM41TQB	Discovery agent	N.A.	Investigative	[48]
N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine	DM1K2A4	Discovery agent	N.A.	Investigative	[48]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine	DM3C8PJ	Discovery agent	N.A.	Investigative	[48]
N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine	DMCOPR3	Discovery agent	N.A.	Investigative	[48]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide	DM6HGK4	Discovery agent	N.A.	Investigative	[50]
N-(2,6-diphenylpyrimidin-4-yl)acetamide	DMQ0DMU	Discovery agent	N.A.	Investigative	[50]
N-(2,6-diphenylpyrimidin-4-yl)benzamide	DMBW752	Discovery agent	N.A.	Investigative	[50]
N-(2,6-diphenylpyrimidin-4-yl)butyramide	DM5EF71	Discovery agent	N.A.	Investigative	[50]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide	DMWPZCS	Discovery agent	N.A.	Investigative	[50]
N-(2,6-diphenylpyrimidin-4-yl)propionamide	DM89NGE	Discovery agent	N.A.	Investigative	[50]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide	DMLTROU	Discovery agent	N.A.	Investigative	[63]
N-(4,5-diphenylpyrimidin-2-yl)acetamide	DM34R10	Discovery agent	N.A.	Investigative	[50]
N-(4,6-diphenylpyrimidin-2-yl)-4-chlorobenzamide	DM1PSR7	Discovery agent	N.A.	Investigative	[50]
N-(4,6-diphenylpyrimidin-2-yl)propionamide	DMJZ2IP	Discovery agent	N.A.	Investigative	[50]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide	DMTF8US	Discovery agent	N.A.	Investigative	[4]
N6-((+/-)-endo-norborn-2-yl)adenosine	DM30KXV	Discovery agent	N.A.	Investigative	[20]
N6-(3-Iodobenzyl)-2'-O-methyladenosine	DM2W9NO	Discovery agent	N.A.	Investigative	[64]
N6-CYCLOPENTYLADENOSINE	DMD6AJO	Discovery agent	N.A.	Investigative	[65]
N6-methoxy-2-phenylethynyladenosine	DMDG59X	Discovery agent	N.A.	Investigative	[26]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine	DMSEL5W	Discovery agent	N.A.	Investigative	[26]
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine	DMP7246	Discovery agent	N.A.	Investigative	[26]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine	DM8LR62	Discovery agent	N.A.	Investigative	[26]
N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine	DM1KA9R	Discovery agent	N.A.	Investigative	[26]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine	DMQ5K8R	Discovery agent	N.A.	Investigative	[26]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine	DM9H3W8	Discovery agent	N.A.	Investigative	[26]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine	DMRBS50	Discovery agent	N.A.	Investigative	[26]
NIPECOTIC ACID	DMPV450	Discovery agent	N.A.	Investigative	[7]
NSC-407228	DMKJWGP	Discovery agent	N.A.	Investigative	[38]
PENECA	DMIDSJ9	Discovery agent	N.A.	Investigative	[13]
PSB-10	DMXDWO7	Discovery agent	N.A.	Investigative	[66]
PSB-11	DMGK2PC	Discovery agent	N.A.	Investigative	[67]
PSB36	DMBGM1E	Discovery agent	N.A.	Investigative	[68]
PSB603	DM6QERS	Discovery agent	N.A.	Investigative	[69]
R-N6-(phenylisopropyl)adenosine	DM2N3BA	Discovery agent	N.A.	Investigative	[70]
REVERSINE	DMWDNOK	Discovery agent	N.A.	Investigative	[48]
sakuranetin	DMUAQYZ	Discovery agent	N.A.	Investigative	[36]
SB-298	DMU2J3K	Discovery agent	N.A.	Investigative	[69]
SEROTONIN	DMOFCRY	Discovery agent	N.A.	Investigative	[7]
TCPA	DMTF4VI	Discovery agent	N.A.	Investigative	[71]
visnagin	DMCSHE8	Discovery agent	N.A.	Investigative	[36]
VUF-8504	DM8OTAG	Discovery agent	N.A.	Investigative	[16]
VUF-8507	DMQFWV7	Discovery agent	N.A.	Investigative	[16]
VUF5574	DMUA751	Discovery agent	N.A.	Investigative	[72]
xanthine amine congener	DMGYVFD	Discovery agent	N.A.	Investigative	[14]
[1,2,4]triazolo[1,5-a]quinoxalin-4(5H)-one	DMPV0QN	Discovery agent	N.A.	Investigative	[73]
[125I]AB-MECA	DM8EQFL	Discovery agent	N.A.	Investigative	[14]
[125I]APNEA	DM95A4Z	Discovery agent	N.A.	Investigative	[74]
[3H]CCPA	DMHDGB3	Discovery agent	N.A.	Investigative	[29]
[3H]HEMADO	DMEO6AH	Discovery agent	N.A.	Investigative	[75]
[3H]kainate	DMMK7XU	Discovery agent	N.A.	Investigative	[7]
[3H]NECA	DMAO9SH	Discovery agent	N.A.	Investigative	[76]
[3H]OSIP339391	DM4BY5J	Discovery agent	N.A.	Investigative	[42]
[3H]PSB-11	DMFDCJK	Discovery agent	N.A.	Investigative	[67]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Liver cancer	2C82	Liver tissue	6.30E-08	-0.73	-1.4
Asthma	CA23	Nasal and bronchial airway	1.35E-12	0.28	0.71

References

• [1] A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. FEBS Lett. 1993 Dec 20;336(1):57-60.
• [2] 2011 Pipeline of Can-Fite BioPharm.
• [3] Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80.
• [4] 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.
• [5] 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.
• [6] Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5690-4.
• [7] 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.
• [8] 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.
• [9] 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.
• [10] (N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists. J Med Chem. 2005 Mar 24;48(6):1745-58.
• [11] 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.
• [12] A binding site model and structure-activity relationships for the rat A3 adenosine receptor. Mol Pharmacol. 1994 Jun;45(6):1101-11.
• [13] 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.
• [14] [(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.
• [15] Scouting human A3 adenosine receptor antagonist binding mode using a molecular simplification approach: from triazoloquinoxaline to a pyrimidine sk... J Med Chem. 2007 Dec 27;50(26):6596-606.
• [16] Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models. J Med Chem. 2006 Jul 13;49(14):4085-97.
• [17] 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.
• [18] Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists. J Med Chem. 2002 Aug 1;45(16):3337-44.
• [19] 2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies. J Med Chem. 1998 May 7;41(10):1708-15.
• [20] 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.
• [21] 2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. J Med Chem. 2006 May 18;49(10):2861-7.
• [22] 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34.
• [23] 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.
• [24] 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.
• [25] 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.
• [26] 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.
• [27] 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.
• [28] 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.
• [29] 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.
• [30] 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.
• [31] New 2-arylpyrazolo[4,3-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. J Med Chem. 2005 Jul 28;48(15):5001-8.
• [32] 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.
• [33] Synthesis 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.
• [34] 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.
• [35] 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.
• [36] Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301.
• [37] 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.
• [38] Interactions of flavonoids and other phytochemicals with adenosine receptors. J Med Chem. 1996 Feb 2;39(3):781-8.
• [39] Synthesis of eudistomin D analogues and its effects on adenosine receptors. Bioorg Med Chem. 2008 Apr 1;16(7):3825-30.
• [40] 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.
• [41] 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.
• [42] 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.
• [43] Adenosine receptors: targets for future drugs. J Med Chem. 1982 Mar;25(3):197-207.
• [44] 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.
• [45] 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: 21).
• [46] 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.
• [47] Novel 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.
• [48] 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.
• [49] Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands. Bioorg Med Chem. 2010 Nov 15;18(22):7890-9.
• [50] 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.
• [51] Molecular cloning and characterization of the human A3 adenosine receptor. Proc Natl Acad Sci U S A. 1993 Nov 1;90(21):10365-9.
• [52] 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.
• [53] The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family. Bioorg Med Chem Lett. 2000 Jan 3;10(1):31-4.
• [54] 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.
• [55] A(3) adenosine receptor activation attenuates neutrophil function and neutrophil-mediated reperfusion injury. Am J Physiol. 1999 Nov;277(5 Pt 2):H1895-905.
• [56] Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.
• [57] Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors. J Med Chem. 1996 Jul 19;39(15):2980-9.
• [58] Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. J Med Chem. 1996 Oct 11;39(21):4142-8.
• [59] Structure-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.
• [60] 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.
• [61] Structure-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.
• [62] Inhibition of TNF-alpha expression by adenosine: role of A3 adenosine receptors. J Immunol. 1996 May 1;156(9):3435-42.
• [63] 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.
• [64] Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands. Bioorg Med Chem. 2007 Aug 15;15(16):5440-7.
• [65] Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprote... J Med Chem. 2005 Dec 29;48(26):8103-7.
• [66] Imidazo[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.
• [67] [(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.
• [68] Improving 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.
• [69] 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.
• [70] Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors. Pharmacology. 1993;46(2):91-100.
• [71] 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.
• [72] Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. J Med Chem. 2000 Jun 1;43(11):2227-38.
• [73] 1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological eva... J Med Chem. 2005 Dec 15;48(25):7932-45.
• [74] Molecular 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.
• [75] [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor. Eur J Pharmacol. 2007 Feb 5;556(1-3):14-8.
• [76] 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.