Target Information
Target General Information | Top | |||||
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Target ID |
T86679
(Former ID: TTDS00188)
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Target Name |
Adenosine A2b receptor (ADORA2B)
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Synonyms |
Adenosine receptor A2b; A2b Adenosine receptor
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Gene Name |
ADORA2B
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Target Type |
Successful target
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[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
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MLLETQDALYVALELVIAALSVAGNVLVCAAVGTANTLQTPTNYFLVSLAAADVAVGLFA
IPFAITISLGFCTDFYGCLFLACFVLVLTQSSIFSLLAVAVDRYLAICVPLRYKSLVTGT RARGVIAVLWVLAFGIGLTPFLGWNSKDSATNNCTEPWDGTTNESCCLVKCLFENVVPMS YMVYFNFFGCVLPPLLIMLVIYIKIFLVACRQLQRTELMDHSRTTLQREIHAAKSLAMIV GIFALCWLPVHAVNCVTLFQPAQGKNKPKWAMNMAILLSHANSVVNPIVYAYRNRDFRYT FHKIISRYLLCQADVKSGNGQAGVQPALGVGL Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold |
Drugs and Modes of Action | Top | |||||
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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) | [+] 7 Clinical Trial Drugs | + | ||||
1 | Tonapofylline | Drug Info | Phase 2 | Acute and chronic heart failure | [6] | |
2 | YT-146 | Drug Info | Phase 2 | Hypertension | [7] | |
3 | AB928 | Drug Info | Phase 1/2 | Metastatic colorectal cancer | [8] | |
4 | CVT-6883 | Drug Info | Phase 1 | Asthma | [9], [10] | |
5 | KF-17837 | Drug Info | Phase 1 | Parkinson disease | [11] | |
6 | PBF-1129 | Drug Info | Phase 1 | Non-small-cell lung cancer | [12] | |
7 | Xanthine | Drug Info | Phase 1 | Apnea | [13], [14] | |
Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
1 | PF-1913539 | Drug Info | Discontinued in Phase 3 | Alzheimer disease | [15] | |
2 | METHYLTHIOADENOSINE | Drug Info | Terminated | Multiple sclerosis | [19] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | BAY 60-6583 | Drug Info | Preclinical | Myocardial ischemia | [16] | |
2 | LAS-101057 | Drug Info | Preclinical | Asthma | [17], [18] | |
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 | [10] | |||
Inhibitor | [+] 70 Inhibitor drugs | + | ||||
1 | Tonapofylline | Drug Info | [20] | |||
2 | KF-17837 | Drug Info | [22] | |||
3 | METHYLTHIOADENOSINE | Drug Info | [27] | |||
4 | ZM-241385 | Drug Info | [28] | |||
5 | (1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl | Drug Info | [29] | |||
6 | 1,3-Diallyl-3,7-dihydro-purine-2,6-dione | Drug Info | [33] | |||
7 | 1,3-Diethyl-3,7-dihydro-purine-2,6-dione | Drug Info | [33] | |||
8 | 1,3-Dipropyl-3,7-dihydro-purine-2,6-dione | Drug Info | [33] | |||
9 | 1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione | Drug Info | [34] | |||
10 | 1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione | Drug Info | [35] | |||
11 | 1-METHYLXANTHINE | Drug Info | [33] | |||
12 | 1-Propyl-3,7-dihydro-purine-2,6-dione | Drug Info | [34] | |||
13 | 1H-Imidazo[4,5-c]quinolin-4-ylamine HCl | Drug Info | [29] | |||
14 | 2'-Me-tecadenoson | Drug Info | [36] | |||
15 | 2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine | Drug Info | [37] | |||
16 | 2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine | Drug Info | [38] | |||
17 | 2-(6-amino-8-bromo-9H-purin-9-yl)ethanol | Drug Info | [39] | |||
18 | 2-Amino-4,6-di-furan-2-yl-nicotinonitrile | Drug Info | [40] | |||
19 | 2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile | Drug Info | [40] | |||
20 | 2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile | Drug Info | [40] | |||
21 | 2-chloro-2'-C-methyl-tecadenoson | Drug Info | [36] | |||
22 | 2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine | Drug Info | [29] | |||
23 | 2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine | Drug Info | [42] | |||
24 | 2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine | Drug Info | [29] | |||
25 | 3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione | Drug Info | [34] | |||
26 | 3-noradamantyl-1,3-dipropylxanthine | Drug Info | [44] | |||
27 | 8-(3-Fluoro-phenyl)-9-methyl-9H-purin-6-ylamine | Drug Info | [46] | |||
28 | 8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine | Drug Info | [47] | |||
29 | 8-Bromo-9-(2-butyl)-9H-adenine | Drug Info | [47] | |||
30 | 8-Bromo-9-(2-hydroxypropyl)-9H-adenine | Drug Info | [47] | |||
31 | 8-Bromo-9-(3-hydroxypropyl)-9H-adenine | Drug Info | [47] | |||
32 | 8-Bromo-9-(sec-butyl)-9H-adenine | Drug Info | [47] | |||
33 | 8-Bromo-9-cyclobutyl-9H-adenine | Drug Info | [47] | |||
34 | 8-Bromo-9-cyclopentyl-9H-adenine | Drug Info | [47] | |||
35 | 8-Bromo-9-ethyl-9H-adenine | Drug Info | [47] | |||
36 | 8-bromo-9-isobutyl-9H-purin-6-amine | Drug Info | [39] | |||
37 | 8-Bromo-9-isopropyl-9H-adenine | Drug Info | [47] | |||
38 | 8-Bromo-9-methyl-9H-adenine | Drug Info | [47] | |||
39 | 8-Bromo-9-propyl-9H-adenine | Drug Info | [47] | |||
40 | 8-PHENYL THEOPHYLLINE | Drug Info | [46] | |||
41 | 8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione | Drug Info | [35] | |||
42 | 9-(sec-Butyl)-9H-adenine | Drug Info | [47] | |||
43 | 9-Allyl-8-bromo-9H-adenine | Drug Info | [47] | |||
44 | 9-Cyclobutyl-9H-adenine | Drug Info | [47] | |||
45 | 9-Isopropyl-9H-adenine | Drug Info | [47] | |||
46 | 9-Propyl-9H-adenine | Drug Info | [47] | |||
47 | Alloxazine | Drug Info | [49] | |||
48 | BETA-HYDROXYETHYL THEOPHYLLINE | Drug Info | [39] | |||
49 | CVT-6694 | Drug Info | [39] | |||
50 | CVT-7124 | Drug Info | [39] | |||
51 | Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate | Drug Info | [20] | |||
52 | GNF-PF-2224 | Drug Info | [57] | |||
53 | GNF-PF-2700 | Drug Info | [39] | |||
54 | isobutylmethylxanthine | Drug Info | [58] | |||
55 | Isoguanosine | Drug Info | [59] | |||
56 | LUF-5816 | Drug Info | [38] | |||
57 | LUF-5978 | Drug Info | [38] | |||
58 | LUF-5980 | Drug Info | [38] | |||
59 | LUF-5981 | Drug Info | [38] | |||
60 | N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide | Drug Info | [64] | |||
61 | N6-((+/-)-endo-norborn-2-yl)adenosine | Drug Info | [37] | |||
62 | N6-CYCLOPENTYLADENOSINE | Drug Info | [65] | |||
63 | PD-115199 | Drug Info | [66] | |||
64 | PSB-0788 | Drug Info | [67] | |||
65 | PSB-09120 | Drug Info | [67] | |||
66 | PSB-1115 | Drug Info | [67] | |||
67 | PSB-601 | Drug Info | [39] | |||
68 | SB-298 | Drug Info | [67] | |||
69 | ST-1535 | Drug Info | [49] | |||
70 | [3H]CCPA | Drug Info | [36] | |||
Agonist | [+] 19 Agonist drugs | + | ||||
1 | YT-146 | Drug Info | [21] | |||
2 | BAY 60-6583 | Drug Info | [25] | |||
3 | (R,S)-PHPNECA | Drug Info | [31] | |||
4 | (S)-PIA | Drug Info | [32] | |||
5 | 2-chloroadenosine | Drug Info | [41] | |||
6 | AB-MECA | Drug Info | [48] | |||
7 | AB-NECA | Drug Info | [32] | |||
8 | APNEA | Drug Info | [24] | |||
9 | CGS 21680 | Drug Info | [53] | |||
10 | CGS 24012 | Drug Info | [54] | |||
11 | CV-1674 | Drug Info | [24] | |||
12 | CV-1808 | Drug Info | [56] | |||
13 | MRS5151 | Drug Info | [63] | |||
14 | N(6)-cyclohexyladenosine | Drug Info | [41] | |||
15 | PENECA | Drug Info | [31] | |||
16 | R-N6-(phenylisopropyl)adenosine | Drug Info | [41] | |||
17 | TCPA | Drug Info | [70] | |||
18 | [3H]HEMADO | Drug Info | [75] | |||
19 | [3H]NECA | Drug Info | [48], [65] | |||
Antagonist | [+] 54 Antagonist drugs | + | ||||
1 | AB928 | Drug Info | [12] | |||
2 | PBF-1129 | Drug Info | [12] | |||
3 | Xanthine | Drug Info | [23] | |||
4 | PF-1913539 | Drug Info | [24] | |||
5 | LAS-101057 | Drug Info | [26] | |||
6 | (E)-8-(3-chlorostyryl)-caffeine | Drug Info | [30] | |||
7 | 3-isobutyl-8-pyrrolidinoxanthine | Drug Info | [43] | |||
8 | 4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one | Drug Info | [45] | |||
9 | AS100 | Drug Info | [50] | |||
10 | AS16 | Drug Info | [50] | |||
11 | AS70 | Drug Info | [50] | |||
12 | AS74 | Drug Info | [50] | |||
13 | AS94 | Drug Info | [50] | |||
14 | AS95 | Drug Info | [50] | |||
15 | AS96 | Drug Info | [50] | |||
16 | AS99 | Drug Info | [50] | |||
17 | ATL-801 | Drug Info | [30] | |||
18 | ATL-844 | Drug Info | [30], [51] | |||
19 | ATL802 | Drug Info | [52] | |||
20 | CPFPX | Drug Info | [55] | |||
21 | DEPX | Drug Info | [32] | |||
22 | flavone | Drug Info | [45] | |||
23 | I-ABOPX | Drug Info | [32] | |||
24 | KF 17837S | Drug Info | [56] | |||
25 | KF26777 | Drug Info | [60] | |||
26 | MRE 2029F20 | Drug Info | [61] | |||
27 | MRE 3008F20 | Drug Info | [62] | |||
28 | MRS1041 | Drug Info | [45] | |||
29 | MRS1042 | Drug Info | [45] | |||
30 | MRS1065 | Drug Info | [45] | |||
31 | MRS1084 | Drug Info | [45] | |||
32 | MRS1086 | Drug Info | [45] | |||
33 | MRS1088 | Drug Info | [45] | |||
34 | MRS1093 | Drug Info | [45] | |||
35 | MRS1132 | Drug Info | [45] | |||
36 | MRS1191 | Drug Info | [30] | |||
37 | MRS1523 | Drug Info | [30] | |||
38 | MRS1706 | Drug Info | [52] | |||
39 | MRS923 | Drug Info | [45] | |||
40 | MRS928 | Drug Info | [45] | |||
41 | PSB-10 | Drug Info | [68] | |||
42 | PSB-11 | Drug Info | [68] | |||
43 | PSB36 | Drug Info | [69] | |||
44 | PSB603 | Drug Info | [67] | |||
45 | sakuranetin | Drug Info | [45] | |||
46 | visnagin | Drug Info | [45] | |||
47 | VUF5574 | Drug Info | [71] | |||
48 | xanthine amine congener | Drug Info | [54], [72] | |||
49 | XCC | Drug Info | [51] | |||
50 | [125I]ABOPX | Drug Info | [32] | |||
51 | [125I]ZM-241385 | Drug Info | [73] | |||
52 | [3H]DPCPX | Drug Info | [74] | |||
53 | [3H]OSIP339391 | Drug Info | [39], [74] | |||
54 | [3H]ZM 241385 | Drug Info | [72] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"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 | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-regulating microRNAs |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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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 | |||||
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Target Validation |
References | Top | |||||
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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 | Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. | |||||
REF 7 | 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 8 | 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 9 | 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 10 | 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 11 | 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 12 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 13 | 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 14 | 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 15 | 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 16 | Circadian rhythm as a therapeutic target. Nat Rev Drug Discov. 2021 Apr;20(4):287-307. | |||||
REF 17 | 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 18 | 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 19 | 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 20 | 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 21 | Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells. Biochem Biophys Res Commun. 1994 Mar 15;199(2):905-10. | |||||
REF 22 | 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 23 | Role of adenosine in asthma. Drug Dev Res. 1996;39:333-6. | |||||
REF 24 | 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 25 | Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors. Circulation. 2007 Mar 27;115(12):1581-90. | |||||
REF 26 | 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 27 | 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 28 | 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 29 | 1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. J Med Chem. 1991 Mar;34(3):1202-6. | |||||
REF 30 | 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 31 | 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 32 | 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 33 | Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. J Med Chem. 1988 Oct;31(10):2034-9. | |||||
REF 34 | 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 35 | 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 36 | 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 37 | 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 38 | 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34. | |||||
REF 39 | 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 40 | 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 41 | Adenosine receptor activation in human fibroblasts: nucleoside agonists and antagonists. Can J Physiol Pharmacol. 1980 Jun;58(6):673-91. | |||||
REF 42 | 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 43 | 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 44 | 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 45 | Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301. | |||||
REF 46 | 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 47 | 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 48 | 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 49 | 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. | |||||
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