Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T77365 Target Info
Target Name Adenosine A2a receptor (ADORA2A)
Synonyms
Adenosine receptor A2a; ADORA2; A2a Adenosine receptor; A(2A) adenosine receptor
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Target Type Successful Target
Gene Name ADORA2A
Biochemical Class GPCR rhodopsin
UniProt ID
AA2AR_HUMAN
Co-Targets of This Target  Top
Co-Target Name Adenosine A1 receptor (ADORA1) Successful Target
UniProt ID AA1R_HUMAN
Gene Name ADORA1
Synonyms
Adenosine receptor A1; A(1) adenosine receptor
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Representative Drug(s) SCH-442416 Drug Info Ki = 1.111 nM Click to Show More [1]
2 Tonapofylline Drug Info Ki = 7 nM [2]
3 Tonapofylline Drug Info Ki = 7.4 nM [3]
4 BIIB014 Drug Info Ki = 68 nM [6]
5 Apadenoson Drug Info Ki = 77 nM [7]
6 SCH 420814 Drug Info Ki = 295 nM [9]
7 GW-328267 Drug Info Ki = 369 nM [7]
8 Istradefylline Drug Info Ki = 841 nM [10]
Co-Target Name Monoamine oxidase type B (MAO-B) Successful Target
UniProt ID AOFB_HUMAN
Gene Name MAOB
Synonyms
MAO-B; Amine oxidase [flavin-containing] B
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Representative Drug(s) Istradefylline Drug Info Ki = 27 nM [4]
Co-Target Name Adenosine A2b receptor (ADORA2B) Successful Target
UniProt ID AA2BR_HUMAN
Gene Name ADORA2B
Synonyms
Adenosine receptor A2b; A2b Adenosine receptor
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Representative Drug(s) GW-328267 Drug Info EC50 = 51 nM Click to Show More [5]
2 BIIB014 Drug Info Ki = 63 nM [6]
3 Tonapofylline Drug Info Ki = 90 nM [3]
4 Tonapofylline Drug Info Ki = 90 nM [8]
5 Tozadenant Drug Info Ki = 700 nM [7]
6 SCH 420814 Drug Info Ki ~ 1000 nM [9]
Co-Target Name Adenosine A3 receptor (ADORA3) Clinical trial Target
UniProt ID AA3R_HUMAN
Gene Name ADORA3
Synonyms
Adenosine receptor A3A; Adenosine receptor A3; Adenosine 3 receptor; A3AR; A3 Adenosine receptor
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Representative Drug(s) GW-328267 Drug Info EC50 = 4.2 nM Click to Show More [5]
2 Regadenoson Drug Info Ki ~ 10 nM [11]
3 Apadenoson Drug Info Ki = 45 nM [7]
4 SCH 420814 Drug Info Ki ~ 1000 nM [9]
References  Top
REF 1 Scaffold decoration at positions 5 and 8 of 1,2,4-triazolo[1,5-c]pyrimidines to explore the antagonist profiling on adenosine receptors: a preliminary structure-activity relationship study. J Med Chem. 2014 Jul 24;57(14):6210-25.
REF 2 Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7132-9.
REF 3 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.
REF 4 Discovery of monoamine oxidase inhibitors by medicinal chemistry approaches. Med. Chem. Commun. 2019;10:10-25.
REF 5 Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1219-24.
REF 6 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.
REF 7 Adenosine A2A receptor as a drug discovery target. J Med Chem. 2014 May 8;57(9):3623-50.
REF 8 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.
REF 9 Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. J Med Chem. 2013 Jun 13;56(11):4580-96.
REF 10 1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases. Bioorg Med Chem. 2013 Dec 1;21(23):7435-52.
REF 11 2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists. J Med Chem. 2004 Sep 9;47(19):4766-73.

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