Co-Target(s) Information

Content Navigation (  All   None )                                      
Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T92072 Target Info
Target Name Adenosine A1 receptor (ADORA1)
Synonyms
Adenosine receptor A1; A(1) adenosine receptor
    Click to Show/Hide
Target Type Successful Target
Gene Name ADORA1
Biochemical Class GPCR rhodopsin
UniProt ID
AA1R_HUMAN
Co-Targets of This Target  Top
Co-Target Name Adenosine A2a receptor (ADORA2A) Successful Target
UniProt ID AA2AR_HUMAN
Gene Name ADORA2A
Synonyms
Adenosine receptor A2a; ADORA2; A2a Adenosine receptor; A(2A) adenosine receptor
    Click to Show/Hide
Representative Drug(s) SCH-442416 Drug Info Ki = 0.048 nM Click to Show More [1]
2 KF-17837 Drug Info IC50 = 1 nM [2]
3 Rolofylline Drug Info Ki = 108 nM [5]
4 Rolofylline Drug Info Ki = 108 nM [6]
5 SLV320 Drug Info Ki = 398 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
    Click to Show/Hide
Representative Drug(s) Tonapofylline Drug Info Ki = 90 nM Click to Show More [3]
2 Tonapofylline Drug Info Ki = 90 nM [4]
3 Rolofylline Drug Info Ki = 108 nM [6]
4 Rolofylline Drug Info Ki = 269 nM [5]
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
    Click to Show/Hide
Representative Drug(s) SLV320 Drug Info Ki = 200 nM Click to Show More [4]
2 GS 9667 Drug Info Ki ~ 1000 nM [7]
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 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.
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 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 5 Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties. Medchemcomm. 2018 May 14;9(6):951-62.
REF 6 Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine. J Med Chem. 1997 Jun 6;40(12):1773-8.
REF 7 Design and in Vivo Characterization of A 1 Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series. J Med Chem. 2019 Feb 14;62(3):1502-1522.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.