Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTNE7KG)

• DTT Name: Adenosine A2b receptor (ADORA2B)
• Synonyms: Adenosine receptor A2b; A2b Adenosine receptor
• Gene Name: ADORA2B
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: AA2BR_HUMAN
• TTD ID: T86679
• Sequence:
  MLLETQDALYVALELVIAALSVAGNVLVCAAVGTANTLQTPTNYFLVSLAAADVAVGLFA
  IPFAITISLGFCTDFYGCLFLACFVLVLTQSSIFSLLAVAVDRYLAICVPLRYKSLVTGT
  RARGVIAVLWVLAFGIGLTPFLGWNSKDSATNNCTEPWDGTTNESCCLVKCLFENVVPMS
  YMVYFNFFGCVLPPLLIMLVIYIKIFLVACRQLQRTELMDHSRTTLQREIHAAKSLAMIV
  GIFALCWLPVHAVNCVTLFQPAQGKNKPKWAMNMAILLSHANSVVNPIVYAYRNRDFRYT
  FHKIISRYLLCQADVKSGNGQAGVQPALGVGL
• 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)
  Neuroactive ligand-receptor interaction (hsa04080)
  Vascular smooth muscle contraction (hsa04270)
  Alcoholism (hsa05034)
• Reactome Pathway:
  G alpha (s) signalling events (R-HSA-418555)
  Surfactant metabolism (R-HSA-5683826)
  Adenosine P1 receptors (R-HSA-417973)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Adenosine	DMM2NSK	Paroxysmal supraventricular tachycardia	BC81.Z	Approved	[1]
Vidarabine	DM0N85H	Hepatosplenic T-cell lymphoma		Approved	[1]

8 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
A295	DM55GO2	Aggressive cancer	2A00-2F9Z	IND submitted	[2]
Tonapofylline	DMBH316	Acute and chronic heart failure	BD1Z	Phase 2	[3]
YT-146	DM3YVKQ	Hypertension	BA00-BA04	Phase 2	[4]
AB928	DMDOXMN	Metastatic colorectal cancer	2B91	Phase 1/2	[5]
CVT-6883	DMY84TW	Asthma	CA23	Phase 1	[6]
KF-17837	DMQ6DLZ	Parkinson disease	8A00.0	Phase 1	[7]
PBF-1129	DMOPGXM	Non-small-cell lung cancer	2C25.Y	Phase 1	[5]
Xanthine	DMFBOQ7	Apnea	MD11.0	Phase 1	[8]

3 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	[9]
METHYLTHIOADENOSINE	DMC8J6F	Multiple sclerosis	8A40	Terminated	[12]
ZM-241385	DMWQ38G	N. A.	N. A.	Terminated	[13]

2 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 60-6583	DMTEJV1	Myocardial ischemia	BA6Z	Preclinical	[10]
LAS-101057	DMFBMXD	Asthma	CA23	Preclinical	[11]

132 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	[14]
(E)-8-(3-chlorostyryl)-caffeine	DMQT15Z	Discovery agent	N.A.	Investigative	[15]
(R,S)-PHPNECA	DMQO71C	Discovery agent	N.A.	Investigative	[16]
(S)-PIA	DM04BHI	Discovery agent	N.A.	Investigative	[17]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione	DMEV8G2	Discovery agent	N.A.	Investigative	[18]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione	DMKYE16	Discovery agent	N.A.	Investigative	[18]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione	DMUL2B3	Discovery agent	N.A.	Investigative	[18]
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione	DMMRV21	Discovery agent	N.A.	Investigative	[19]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione	DMSNK98	Discovery agent	N.A.	Investigative	[20]
1-METHYLXANTHINE	DM2WQ1E	Discovery agent	N.A.	Investigative	[18]
1-Propyl-3,7-dihydro-purine-2,6-dione	DML5J94	Discovery agent	N.A.	Investigative	[19]
1H-Imidazo[4,5-c]quinolin-4-ylamine HCl	DMME09C	Discovery agent	N.A.	Investigative	[14]
2'-Me-tecadenoson	DMY2GXT	Discovery agent	N.A.	Investigative	[21]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine	DMMESIU	Discovery agent	N.A.	Investigative	[22]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine	DMY3C78	Discovery agent	N.A.	Investigative	[23]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol	DMRBX1D	Discovery agent	N.A.	Investigative	[24]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile	DMVN0EC	Discovery agent	N.A.	Investigative	[25]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile	DMP4NHD	Discovery agent	N.A.	Investigative	[25]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile	DMUYTXS	Discovery agent	N.A.	Investigative	[25]
2-chloro-2'-C-methyl-tecadenoson	DMD3ZNP	Discovery agent	N.A.	Investigative	[21]
2-chloroadenosine	DMYPQEW	Discovery agent	N.A.	Investigative	[26]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine	DM6CZAN	Discovery agent	N.A.	Investigative	[14]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine	DMWCGE8	Discovery agent	N.A.	Investigative	[27]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine	DMDC6XP	Discovery agent	N.A.	Investigative	[14]
3-isobutyl-8-pyrrolidinoxanthine	DM9GM1H	Discovery agent	N.A.	Investigative	[28]
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione	DMKYPUW	Discovery agent	N.A.	Investigative	[19]
3-noradamantyl-1,3-dipropylxanthine	DMFHYAE	Discovery agent	N.A.	Investigative	[29]
4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one	DM8642Z	Discovery agent	N.A.	Investigative	[30]
8-(3-Fluoro-phenyl)-9-methyl-9H-purin-6-ylamine	DMLQPVH	Discovery agent	N.A.	Investigative	[31]
8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine	DMMQ79W	Discovery agent	N.A.	Investigative	[32]
8-Bromo-9-(2-butyl)-9H-adenine	DM5DCPF	Discovery agent	N.A.	Investigative	[32]
8-Bromo-9-(2-hydroxypropyl)-9H-adenine	DMKW2PE	Discovery agent	N.A.	Investigative	[32]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine	DMA258T	Discovery agent	N.A.	Investigative	[32]
8-Bromo-9-(sec-butyl)-9H-adenine	DMSQPFM	Discovery agent	N.A.	Investigative	[32]
8-Bromo-9-cyclobutyl-9H-adenine	DMUTV76	Discovery agent	N.A.	Investigative	[32]
8-Bromo-9-cyclopentyl-9H-adenine	DMCK0O1	Discovery agent	N.A.	Investigative	[32]
8-Bromo-9-ethyl-9H-adenine	DM4YAD6	Discovery agent	N.A.	Investigative	[32]
8-bromo-9-isobutyl-9H-purin-6-amine	DMZF3UN	Discovery agent	N.A.	Investigative	[24]
8-Bromo-9-isopropyl-9H-adenine	DMIN9HC	Discovery agent	N.A.	Investigative	[32]
8-Bromo-9-methyl-9H-adenine	DM1DS3B	Discovery agent	N.A.	Investigative	[32]
8-Bromo-9-propyl-9H-adenine	DMRIPU5	Discovery agent	N.A.	Investigative	[32]
8-PHENYL THEOPHYLLINE	DMFGUCY	Discovery agent	N.A.	Investigative	[31]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione	DMHQGOC	Discovery agent	N.A.	Investigative	[20]
9-(sec-Butyl)-9H-adenine	DMFKVPA	Discovery agent	N.A.	Investigative	[32]
9-Allyl-8-bromo-9H-adenine	DM8VZIY	Discovery agent	N.A.	Investigative	[32]
9-Cyclobutyl-9H-adenine	DM04QWX	Discovery agent	N.A.	Investigative	[32]
9-Isopropyl-9H-adenine	DMBQLAI	Discovery agent	N.A.	Investigative	[32]
9-Propyl-9H-adenine	DMQTEPY	Discovery agent	N.A.	Investigative	[32]
AB-MECA	DMQPHFU	Discovery agent	N.A.	Investigative	[33]
AB-NECA	DME8G7F	Discovery agent	N.A.	Investigative	[17]
Alloxazine	DM7U2BE	Discovery agent	N.A.	Investigative	[34]
APNEA	DMW45GK	Discovery agent	N.A.	Investigative	[9]
AS100	DMXZ8S9	Discovery agent	N.A.	Investigative	[35]
AS16	DMP0A17	Discovery agent	N.A.	Investigative	[35]
AS70	DM9CIJP	Discovery agent	N.A.	Investigative	[35]
AS74	DMZPHKG	Discovery agent	N.A.	Investigative	[35]
AS94	DM7WJ6F	Discovery agent	N.A.	Investigative	[35]
AS95	DMN3E9Q	Discovery agent	N.A.	Investigative	[35]
AS96	DML6I8J	Discovery agent	N.A.	Investigative	[35]
AS99	DMZ7FJN	Discovery agent	N.A.	Investigative	[35]
ATL-801	DMAZ0EQ	Non-insulin dependent diabetes	5A11	Investigative	[15]
ATL-844	DM6V9SC	Asthma	CA23	Investigative	[15]
ATL802	DMYMCQA	Discovery agent	N.A.	Investigative	[36]
BETA-HYDROXYETHYL THEOPHYLLINE	DMGP9MN	Discovery agent	N.A.	Investigative	[24]
CGS 21680	DMZ0TGY	Discovery agent	N.A.	Investigative	[37]
CGS 24012	DMRU8G7	Discovery agent	N.A.	Investigative	[38]
CPFPX	DMFE5GX	Discovery agent	N.A.	Investigative	[39]
CV-1674	DM9AL7W	Discovery agent	N.A.	Investigative	[9]
CV-1808	DM07VRS	Discovery agent	N.A.	Investigative	[40]
CVT-6694	DMYC1DW	Discovery agent	N.A.	Investigative	[24]
CVT-7124	DM53VA8	Discovery agent	N.A.	Investigative	[24]
DEPX	DM4JM50	Discovery agent	N.A.	Investigative	[17]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate	DMK4T5Y	Discovery agent	N.A.	Investigative	[3]
flavone	DMEQH6J	Discovery agent	N.A.	Investigative	[30]
GNF-PF-2224	DM26UKN	Discovery agent	N.A.	Investigative	[41]
GNF-PF-2700	DMC56YJ	Discovery agent	N.A.	Investigative	[24]
I-ABOPX	DM5X0JS	Discovery agent	N.A.	Investigative	[17]
isobutylmethylxanthine	DM46F5X	Discovery agent	N.A.	Investigative	[42]
Isoguanosine	DMAFLCJ	Discovery agent	N.A.	Investigative	[43]
KF 17837S	DM7W9MT	Discovery agent	N.A.	Investigative	[40]
KF26777	DMPBDW0	Discovery agent	N.A.	Investigative	[44]
LUF-5816	DMQZDMH	Discovery agent	N.A.	Investigative	[23]
LUF-5978	DMCTM3L	Discovery agent	N.A.	Investigative	[23]
LUF-5980	DMGOIF5	Discovery agent	N.A.	Investigative	[23]
LUF-5981	DMHO3XL	Discovery agent	N.A.	Investigative	[23]
MRE 2029F20	DMUK1PA	Discovery agent	N.A.	Investigative	[45]
MRE 3008F20	DM72US0	Discovery agent	N.A.	Investigative	[46]
MRS1041	DMBXKYR	Discovery agent	N.A.	Investigative	[30]
MRS1042	DMVT865	Discovery agent	N.A.	Investigative	[30]
MRS1065	DMYAHU3	Discovery agent	N.A.	Investigative	[30]
MRS1084	DMKELWG	Discovery agent	N.A.	Investigative	[30]
MRS1086	DM1K5E2	Discovery agent	N.A.	Investigative	[30]
MRS1088	DMSKWL7	Discovery agent	N.A.	Investigative	[30]
MRS1093	DM801AO	Discovery agent	N.A.	Investigative	[30]
MRS1132	DMY4C0G	Discovery agent	N.A.	Investigative	[30]
MRS1191	DM9WX3C	Discovery agent	N.A.	Investigative	[15]
MRS1523	DM4AONZ	Discovery agent	N.A.	Investigative	[15]
MRS1706	DM5I7PL	Discovery agent	N.A.	Investigative	[36]
MRS5151	DM1GUTC	Discovery agent	N.A.	Investigative	[47]
MRS923	DMMN42V	Discovery agent	N.A.	Investigative	[30]
MRS928	DMKJ9WM	Discovery agent	N.A.	Investigative	[30]
N(6)-cyclohexyladenosine	DMHINE0	Discovery agent	N.A.	Investigative	[26]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide	DMLTROU	Discovery agent	N.A.	Investigative	[48]
N6-((+/-)-endo-norborn-2-yl)adenosine	DM30KXV	Discovery agent	N.A.	Investigative	[22]
N6-CYCLOPENTYLADENOSINE	DMD6AJO	Discovery agent	N.A.	Investigative	[49]
PD-115199	DMQ4LRZ	Discovery agent	N.A.	Investigative	[50]
PENECA	DMIDSJ9	Discovery agent	N.A.	Investigative	[16]
PSB-0788	DM0FKV9	Discovery agent	N.A.	Investigative	[51]
PSB-09120	DMAFHLX	Discovery agent	N.A.	Investigative	[51]
PSB-10	DMXDWO7	Discovery agent	N.A.	Investigative	[52]
PSB-11	DMGK2PC	Discovery agent	N.A.	Investigative	[52]
PSB-1115	DMOH2VC	Discovery agent	N.A.	Investigative	[51]
PSB-601	DMBIK7D	Discovery agent	N.A.	Investigative	[24]
PSB36	DMBGM1E	Discovery agent	N.A.	Investigative	[53]
PSB603	DM6QERS	Discovery agent	N.A.	Investigative	[51]
R-N6-(phenylisopropyl)adenosine	DM2N3BA	Discovery agent	N.A.	Investigative	[26]
sakuranetin	DMUAQYZ	Discovery agent	N.A.	Investigative	[30]
SB-298	DMU2J3K	Discovery agent	N.A.	Investigative	[51]
ST-1535	DMUTC9Z	Discovery agent	N.A.	Investigative	[34]
TCPA	DMTF4VI	Discovery agent	N.A.	Investigative	[54]
visnagin	DMCSHE8	Discovery agent	N.A.	Investigative	[30]
VUF5574	DMUA751	Discovery agent	N.A.	Investigative	[55]
xanthine amine congener	DMGYVFD	Discovery agent	N.A.	Investigative	[56]
XCC	DM8PADV	Discovery agent	N.A.	Investigative	[57]
[125I]ABOPX	DMZBNK9	Discovery agent	N.A.	Investigative	[17]
[125I]ZM-241385	DME53D6	Discovery agent	N.A.	Investigative	[58]
[3H]CCPA	DMHDGB3	Discovery agent	N.A.	Investigative	[21]
[3H]DPCPX	DM9GY7O	Discovery agent	N.A.	Investigative	[59]
[3H]HEMADO	DMEO6AH	Discovery agent	N.A.	Investigative	[60]
[3H]NECA	DMAO9SH	Discovery agent	N.A.	Investigative	[33]
[3H]OSIP339391	DM4BY5J	Discovery agent	N.A.	Investigative	[59]
[3H]ZM 241385	DMKU4YQ	Discovery agent	N.A.	Investigative	[56]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Apnea	CA23	Hyperplastic tonsil	8.57E-02	-0.76	-0.62
Asthma	CA23	Nasal and bronchial airway	7.89E-02	0.09	0.11
Parkinson's disease	8A00.0	Substantia nigra tissue	7.34E-01	-0.01	-0.06

References

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