Target Information
Target General Information | Top | |||||
---|---|---|---|---|---|---|
Target ID |
T86679
(Former ID: TTDS00188)
|
|||||
Target Name |
Adenosine A2b receptor (ADORA2B)
|
|||||
Synonyms |
Adenosine receptor A2b; A2b Adenosine receptor
Click to Show/Hide
|
|||||
Gene Name |
ADORA2B
|
|||||
Target Type |
Successful target
|
[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Herpes simplex infection [ICD-11: 1F00] | |||||
2 | Supraventricular tachyarrhythmia [ICD-11: BC81] | |||||
Function |
The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. Receptor for adenosine.
Click to Show/Hide
|
|||||
BioChemical Class |
GPCR rhodopsin
|
|||||
UniProt ID | ||||||
Sequence |
MLLETQDALYVALELVIAALSVAGNVLVCAAVGTANTLQTPTNYFLVSLAAADVAVGLFA
IPFAITISLGFCTDFYGCLFLACFVLVLTQSSIFSLLAVAVDRYLAICVPLRYKSLVTGT RARGVIAVLWVLAFGIGLTPFLGWNSKDSATNNCTEPWDGTTNESCCLVKCLFENVVPMS YMVYFNFFGCVLPPLLIMLVIYIKIFLVACRQLQRTELMDHSRTTLQREIHAAKSLAMIV GIFALCWLPVHAVNCVTLFQPAQGKNKPKWAMNMAILLSHANSVVNPIVYAYRNRDFRYT FHKIISRYLLCQADVKSGNGQAGVQPALGVGL Click to Show/Hide
|
|||||
3D Structure | Click to Show 3D Structure of This Target | AlphaFold |
Drugs and Modes of Action | Top | |||||
---|---|---|---|---|---|---|
Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
1 | Adenosine | Drug Info | Approved | Paroxysmal supraventricular tachycardia | [2], [3] | |
2 | Vidarabine | Drug Info | Approved | Herpes simplex virus infection | [4], [5] | |
Clinical Trial Drug(s) | [+] 8 Clinical Trial Drugs | + | ||||
1 | A295 | Drug Info | IND submitted | Aggressive cancer | [6] | |
2 | Tonapofylline | Drug Info | Phase 2 | Acute and chronic heart failure | [7] | |
3 | YT-146 | Drug Info | Phase 2 | Hypertension | [8] | |
4 | AB928 | Drug Info | Phase 1/2 | Metastatic colorectal cancer | [9] | |
5 | CVT-6883 | Drug Info | Phase 1 | Asthma | [10], [11] | |
6 | KF-17837 | Drug Info | Phase 1 | Parkinson disease | [12] | |
7 | PBF-1129 | Drug Info | Phase 1 | Non-small-cell lung cancer | [13] | |
8 | Xanthine | Drug Info | Phase 1 | Apnea | [14], [15] | |
Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
1 | PF-1913539 | Drug Info | Discontinued in Phase 3 | Alzheimer disease | [16] | |
2 | METHYLTHIOADENOSINE | Drug Info | Terminated | Multiple sclerosis | [20] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | BAY 60-6583 | Drug Info | Preclinical | Myocardial ischemia | [17] | |
2 | LAS-101057 | Drug Info | Preclinical | Asthma | [18], [19] | |
Mode of Action | [+] 4 Modes of Action | + | ||||
Modulator | [+] 3 Modulator drugs | + | ||||
1 | Adenosine | Drug Info | [1] | |||
2 | Vidarabine | Drug Info | [1] | |||
3 | CVT-6883 | Drug Info | [11] | |||
Inhibitor | [+] 71 Inhibitor drugs | + | ||||
1 | A295 | Drug Info | [6] | |||
2 | Tonapofylline | Drug Info | [21] | |||
3 | KF-17837 | Drug Info | [23] | |||
4 | METHYLTHIOADENOSINE | Drug Info | [28] | |||
5 | ZM-241385 | Drug Info | [29] | |||
6 | (1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl | Drug Info | [30] | |||
7 | 1,3-Diallyl-3,7-dihydro-purine-2,6-dione | Drug Info | [34] | |||
8 | 1,3-Diethyl-3,7-dihydro-purine-2,6-dione | Drug Info | [34] | |||
9 | 1,3-Dipropyl-3,7-dihydro-purine-2,6-dione | Drug Info | [34] | |||
10 | 1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione | Drug Info | [35] | |||
11 | 1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione | Drug Info | [36] | |||
12 | 1-METHYLXANTHINE | Drug Info | [34] | |||
13 | 1-Propyl-3,7-dihydro-purine-2,6-dione | Drug Info | [35] | |||
14 | 1H-Imidazo[4,5-c]quinolin-4-ylamine HCl | Drug Info | [30] | |||
15 | 2'-Me-tecadenoson | Drug Info | [37] | |||
16 | 2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine | Drug Info | [38] | |||
17 | 2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine | Drug Info | [39] | |||
18 | 2-(6-amino-8-bromo-9H-purin-9-yl)ethanol | Drug Info | [40] | |||
19 | 2-Amino-4,6-di-furan-2-yl-nicotinonitrile | Drug Info | [41] | |||
20 | 2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile | Drug Info | [41] | |||
21 | 2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile | Drug Info | [41] | |||
22 | 2-chloro-2'-C-methyl-tecadenoson | Drug Info | [37] | |||
23 | 2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine | Drug Info | [30] | |||
24 | 2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine | Drug Info | [43] | |||
25 | 2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine | Drug Info | [30] | |||
26 | 3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione | Drug Info | [35] | |||
27 | 3-noradamantyl-1,3-dipropylxanthine | Drug Info | [45] | |||
28 | 8-(3-Fluoro-phenyl)-9-methyl-9H-purin-6-ylamine | Drug Info | [47] | |||
29 | 8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine | Drug Info | [48] | |||
30 | 8-Bromo-9-(2-butyl)-9H-adenine | Drug Info | [48] | |||
31 | 8-Bromo-9-(2-hydroxypropyl)-9H-adenine | Drug Info | [48] | |||
32 | 8-Bromo-9-(3-hydroxypropyl)-9H-adenine | Drug Info | [48] | |||
33 | 8-Bromo-9-(sec-butyl)-9H-adenine | Drug Info | [48] | |||
34 | 8-Bromo-9-cyclobutyl-9H-adenine | Drug Info | [48] | |||
35 | 8-Bromo-9-cyclopentyl-9H-adenine | Drug Info | [48] | |||
36 | 8-Bromo-9-ethyl-9H-adenine | Drug Info | [48] | |||
37 | 8-bromo-9-isobutyl-9H-purin-6-amine | Drug Info | [40] | |||
38 | 8-Bromo-9-isopropyl-9H-adenine | Drug Info | [48] | |||
39 | 8-Bromo-9-methyl-9H-adenine | Drug Info | [48] | |||
40 | 8-Bromo-9-propyl-9H-adenine | Drug Info | [48] | |||
41 | 8-PHENYL THEOPHYLLINE | Drug Info | [47] | |||
42 | 8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione | Drug Info | [36] | |||
43 | 9-(sec-Butyl)-9H-adenine | Drug Info | [48] | |||
44 | 9-Allyl-8-bromo-9H-adenine | Drug Info | [48] | |||
45 | 9-Cyclobutyl-9H-adenine | Drug Info | [48] | |||
46 | 9-Isopropyl-9H-adenine | Drug Info | [48] | |||
47 | 9-Propyl-9H-adenine | Drug Info | [48] | |||
48 | Alloxazine | Drug Info | [50] | |||
49 | BETA-HYDROXYETHYL THEOPHYLLINE | Drug Info | [40] | |||
50 | CVT-6694 | Drug Info | [40] | |||
51 | CVT-7124 | Drug Info | [40] | |||
52 | Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate | Drug Info | [21] | |||
53 | GNF-PF-2224 | Drug Info | [58] | |||
54 | GNF-PF-2700 | Drug Info | [40] | |||
55 | isobutylmethylxanthine | Drug Info | [59] | |||
56 | Isoguanosine | Drug Info | [60] | |||
57 | LUF-5816 | Drug Info | [39] | |||
58 | LUF-5978 | Drug Info | [39] | |||
59 | LUF-5980 | Drug Info | [39] | |||
60 | LUF-5981 | Drug Info | [39] | |||
61 | N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide | Drug Info | [65] | |||
62 | N6-((+/-)-endo-norborn-2-yl)adenosine | Drug Info | [38] | |||
63 | N6-CYCLOPENTYLADENOSINE | Drug Info | [66] | |||
64 | PD-115199 | Drug Info | [67] | |||
65 | PSB-0788 | Drug Info | [68] | |||
66 | PSB-09120 | Drug Info | [68] | |||
67 | PSB-1115 | Drug Info | [68] | |||
68 | PSB-601 | Drug Info | [40] | |||
69 | SB-298 | Drug Info | [68] | |||
70 | ST-1535 | Drug Info | [50] | |||
71 | [3H]CCPA | Drug Info | [37] | |||
Agonist | [+] 19 Agonist drugs | + | ||||
1 | YT-146 | Drug Info | [22] | |||
2 | BAY 60-6583 | Drug Info | [26] | |||
3 | (R,S)-PHPNECA | Drug Info | [32] | |||
4 | (S)-PIA | Drug Info | [33] | |||
5 | 2-chloroadenosine | Drug Info | [42] | |||
6 | AB-MECA | Drug Info | [49] | |||
7 | AB-NECA | Drug Info | [33] | |||
8 | APNEA | Drug Info | [25] | |||
9 | CGS 21680 | Drug Info | [54] | |||
10 | CGS 24012 | Drug Info | [55] | |||
11 | CV-1674 | Drug Info | [25] | |||
12 | CV-1808 | Drug Info | [57] | |||
13 | MRS5151 | Drug Info | [64] | |||
14 | N(6)-cyclohexyladenosine | Drug Info | [42] | |||
15 | PENECA | Drug Info | [32] | |||
16 | R-N6-(phenylisopropyl)adenosine | Drug Info | [42] | |||
17 | TCPA | Drug Info | [71] | |||
18 | [3H]HEMADO | Drug Info | [76] | |||
19 | [3H]NECA | Drug Info | [49], [66] | |||
Antagonist | [+] 54 Antagonist drugs | + | ||||
1 | AB928 | Drug Info | [13] | |||
2 | PBF-1129 | Drug Info | [13] | |||
3 | Xanthine | Drug Info | [24] | |||
4 | PF-1913539 | Drug Info | [25] | |||
5 | LAS-101057 | Drug Info | [27] | |||
6 | (E)-8-(3-chlorostyryl)-caffeine | Drug Info | [31] | |||
7 | 3-isobutyl-8-pyrrolidinoxanthine | Drug Info | [44] | |||
8 | 4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one | Drug Info | [46] | |||
9 | AS100 | Drug Info | [51] | |||
10 | AS16 | Drug Info | [51] | |||
11 | AS70 | Drug Info | [51] | |||
12 | AS74 | Drug Info | [51] | |||
13 | AS94 | Drug Info | [51] | |||
14 | AS95 | Drug Info | [51] | |||
15 | AS96 | Drug Info | [51] | |||
16 | AS99 | Drug Info | [51] | |||
17 | ATL-801 | Drug Info | [31] | |||
18 | ATL-844 | Drug Info | [31], [52] | |||
19 | ATL802 | Drug Info | [53] | |||
20 | CPFPX | Drug Info | [56] | |||
21 | DEPX | Drug Info | [33] | |||
22 | flavone | Drug Info | [46] | |||
23 | I-ABOPX | Drug Info | [33] | |||
24 | KF 17837S | Drug Info | [57] | |||
25 | KF26777 | Drug Info | [61] | |||
26 | MRE 2029F20 | Drug Info | [62] | |||
27 | MRE 3008F20 | Drug Info | [63] | |||
28 | MRS1041 | Drug Info | [46] | |||
29 | MRS1042 | Drug Info | [46] | |||
30 | MRS1065 | Drug Info | [46] | |||
31 | MRS1084 | Drug Info | [46] | |||
32 | MRS1086 | Drug Info | [46] | |||
33 | MRS1088 | Drug Info | [46] | |||
34 | MRS1093 | Drug Info | [46] | |||
35 | MRS1132 | Drug Info | [46] | |||
36 | MRS1191 | Drug Info | [31] | |||
37 | MRS1523 | Drug Info | [31] | |||
38 | MRS1706 | Drug Info | [53] | |||
39 | MRS923 | Drug Info | [46] | |||
40 | MRS928 | Drug Info | [46] | |||
41 | PSB-10 | Drug Info | [69] | |||
42 | PSB-11 | Drug Info | [69] | |||
43 | PSB36 | Drug Info | [70] | |||
44 | PSB603 | Drug Info | [68] | |||
45 | sakuranetin | Drug Info | [46] | |||
46 | visnagin | Drug Info | [46] | |||
47 | VUF5574 | Drug Info | [72] | |||
48 | xanthine amine congener | Drug Info | [55], [73] | |||
49 | XCC | Drug Info | [52] | |||
50 | [125I]ABOPX | Drug Info | [33] | |||
51 | [125I]ZM-241385 | Drug Info | [74] | |||
52 | [3H]DPCPX | Drug Info | [75] | |||
53 | [3H]OSIP339391 | Drug Info | [40], [75] | |||
54 | [3H]ZM 241385 | Drug Info | [73] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
Different Human System Profiles of Target | Top |
---|---|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
|
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
---|---|---|---|
Rap1 signaling pathway | hsa04015 | Affiliated Target |
|
Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
Calcium signaling pathway | hsa04020 | Affiliated Target |
|
Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
Vascular smooth muscle contraction | hsa04270 | Affiliated Target |
|
Class: Organismal Systems => Circulatory system | Pathway Hierarchy |
Degree | 1 | Degree centrality | 1.07E-04 | Betweenness centrality | 0.00E+00 |
---|---|---|---|---|---|
Closeness centrality | 1.78E-01 | Radiality | 1.29E+01 | Clustering coefficient | 0.00E+00 |
Neighborhood connectivity | 1.40E+01 | Topological coefficient | 1.00E+00 | Eccentricity | 13 |
Download | Click to Download the Full PPI Network of This Target | ||||
Chemical Structure based Activity Landscape of Target | Top |
---|---|
Drug Property Profile of Target | Top | |
---|---|---|
(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
||
(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
||
(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
||
"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
---|---|---|---|---|---|---|
Co-Targets |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Regulators | Top | |||||
---|---|---|---|---|---|---|
Target-regulating microRNAs |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
1 | Rap1 signaling pathway | |||||
2 | Calcium signaling pathway | |||||
3 | Neuroactive ligand-receptor interaction | |||||
4 | Vascular smooth muscle contraction | |||||
5 | Alcoholism | |||||
NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
1 | TGF_beta_Receptor Signaling Pathway | |||||
2 | TCR Signaling Pathway | |||||
Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
1 | Intracellular Signalling Through Adenosine Receptor A2b and Adenosine | |||||
PID Pathway | [+] 1 PID Pathways | + | ||||
1 | C-MYB transcription factor network | |||||
Reactome | [+] 3 Reactome Pathways | + | ||||
1 | Adenosine P1 receptors | |||||
2 | G alpha (s) signalling events | |||||
3 | Surfactant metabolism | |||||
WikiPathways | [+] 4 WikiPathways | + | ||||
1 | Nucleotide GPCRs | |||||
2 | GPCRs, Class A Rhodopsin-like | |||||
3 | GPCR ligand binding | |||||
4 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 2 | 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. (Ligand id: 2844). | |||||
REF 3 | Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22. | |||||
REF 4 | 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. (Ligand id: 4806). | |||||
REF 5 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050486. | |||||
REF 6 | Clinical pipeline report, company report or official report of Klus Pharma | |||||
REF 7 | Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. | |||||
REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001363) | |||||
REF 9 | ClinicalTrials.gov (NCT04660812) An Open Label Study Evaluating the Efficacy and Safety of AB928 Based Treatment Combinations in Patients With Metastatic Colorectal Cancer.. U.S. National Institutes of Health. | |||||
REF 10 | 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. (Ligand id: 5615). | |||||
REF 11 | GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J Pharmacol Exp Ther. 2012 Dec;343(3):587-95. | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005980) | |||||
REF 13 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 14 | 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. (Ligand id: 4557). | |||||
REF 15 | Febuxostat (TMX-67), a novel, non-purine, selective inhibitor of xanthine oxidase, is safe and decreases serum urate in healthy volunteers. Nucleosides Nucleotides Nucleic Acids. 2004 Oct;23(8-9):1111-6. | |||||
REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021875) | |||||
REF 17 | Circadian rhythm as a therapeutic target. Nat Rev Drug Discov. 2021 Apr;20(4):287-307. | |||||
REF 18 | 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. (Ligand id: 5617). | |||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027811) | |||||
REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000987) | |||||
REF 21 | 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 22 | Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells. Biochem Biophys Res Commun. 1994 Mar 15;199(2):905-10. | |||||
REF 23 | Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine. J Med Chem. 1993 Nov 12;36(23):3731-3. | |||||
REF 24 | Role of adenosine in asthma. Drug Dev Res. 1996;39:333-6. | |||||
REF 25 | Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors. Biochem Pharmacol. 1999 Jan 1;57(1):65-75. | |||||
REF 26 | Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors. Circulation. 2007 Mar 27;115(12):1581-90. | |||||
REF 27 | Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist. ACS Med Chem Lett. 2010 Dec 20;2(3):213-8. | |||||
REF 28 | 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. | |||||
REF 29 | Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. Bioorg Med Chem. 2010 Mar 15;18(6):2081-2088. | |||||
REF 30 | 1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. J Med Chem. 1991 Mar;34(3):1202-6. | |||||
REF 31 | 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: 20). | |||||
REF 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. | |||||
REF 33 | Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells. Mol Pharmacol. 1999 Oct;56(4):705-13. | |||||
REF 34 | Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. J Med Chem. 1988 Oct;31(10):2034-9. | |||||
REF 35 | 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. | |||||
REF 36 | 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. | |||||
REF 37 | 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. | |||||
REF 38 | 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. | |||||
REF 39 | 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34. | |||||
REF 40 | 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. | |||||
REF 41 | 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem. 2008 Aug 14;51(15):4449-55. | |||||
REF 42 | Adenosine receptor activation in human fibroblasts: nucleoside agonists and antagonists. Can J Physiol Pharmacol. 1980 Jun;58(6):673-91. | |||||
REF 43 | 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. | |||||
REF 44 | 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. | |||||
REF 45 | 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 46 | Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301. | |||||
REF 47 | 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 48 | 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. | |||||
REF 49 | 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. | |||||
REF 50 | 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. | |||||
REF 51 | Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors. Biochem Pharmacol. 2005 Nov 25;70(11):1601-12. | |||||
REF 52 | [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochem Pharmacol. 2001 Mar 15;61(6):657-63. | |||||
REF 53 | 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. | |||||
REF 54 | [3H]CGS 21680, a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain. J Pharmacol Exp Ther. 1989 Dec;251(3):888-93. | |||||
REF 55 | Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem. 1995 Jun 9;270(23):13987-97. | |||||
REF 56 | 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. | |||||
REF 57 | Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261. Br J Pharmacol. 1997 Jun;121(3):353-60. | |||||
REF 58 | Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist, Bioorg. Med. Chem. Lett. 6(17):2059-2062 (1996). | |||||
REF 59 | Adenosine receptors: targets for future drugs. J Med Chem. 1982 Mar;25(3):197-207. | |||||
REF 60 | High selectivity of novel isoguanosine analogues for the adenosine A1 receptor. Bioorg. Med. Chem. Lett. 1(9):481-486 (1991). | |||||
REF 61 | 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. | |||||
REF 62 | 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. | |||||
REF 63 | Adenosine receptors as therapeutic targets. Nat Rev Drug Discov. 2006 Mar;5(3):247-64. | |||||
REF 64 | 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. | |||||
REF 65 | 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. | |||||
REF 66 | Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. J Med Chem. 1988 Jun;31(6):1179-83. | |||||
REF 67 | (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. | |||||
REF 68 | 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. | |||||
REF 69 | 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. | |||||
REF 70 | Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists. Bioorg Med Chem. 2006 Jun 1;14(11):3654-61. | |||||
REF 71 | Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells. Br J Pharmacol. 1997 Nov;122(5):867-74. | |||||
REF 72 | A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. J Med Chem. 1998 Oct 8;41(21):3987-93. | |||||
REF 73 | Use of the triazolotriazine [3H]ZM 241385 as a radioligand at recombinant human A2B adenosine receptors. Drug Des Discov. 1999 Nov;16(3):217-26. | |||||
REF 74 | 125I-4-(2-[7-amino-2-[2-furyl][1,2,4]triazolo[2,3-a][1,3,5] triazin-5-yl-amino]ethyl)phenol, a high affinity antagonist radioligand selective for the A2a adenosine receptor. Mol Pharmacol. 1995 Dec;48(6):970-4. | |||||
REF 75 | [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors. Biochem Pharmacol. 2004 Jul 15;68(2):305-12. | |||||
REF 76 | [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor. Eur J Pharmacol. 2007 Feb 5;556(1-3):14-8. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.