Target Information
| Target General Information | Top | |||||
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| Target ID |
T25663
(Former ID: TTDS00185)
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| Target Name |
Adenosine receptor (ADOR)
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| Synonyms |
P1 receptor
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Chronic obstructive pulmonary disease [ICD-11: CA22] | |||||
| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Theophylline | Drug Info | Approved | Chronic obstructive pulmonary disease | [2], [3] | |
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | DIADENOSINE TETRAPHOSPHATE | Drug Info | Phase 2 | Cardiac arrhythmias | [4] | |
| 2 | NIR178 | Drug Info | Phase 2 | Non-hodgkin lymphoma | [5] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | M-216765 | Drug Info | Terminated | Hypertension | [6] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Antagonist | [+] 5 Antagonist drugs | + | ||||
| 1 | Theophylline | Drug Info | [1], [7] | |||
| 2 | NIR178 | Drug Info | [5] | |||
| 3 | 8-sulfophenyl theophylline | Drug Info | [11] | |||
| 4 | GNF-PF-2224 | Drug Info | [11], [12], [13], [14] | |||
| 5 | SPT | Drug Info | [15] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | DIADENOSINE TETRAPHOSPHATE | Drug Info | [8], [9] | |||
| 2 | M-216765 | Drug Info | [10] | |||
| 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 | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Emerging adenosine receptor agonists. Expert Opin Emerg Drugs. 2007 Sep;12(3):479-92. | |||||
| 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: 413). | |||||
| REF 3 | Non-corticosteroid therapy for the long-term control of asthma. Expert Opin Pharmacother. 2007 Sep;8(13):2077-87. | |||||
| 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: 1732). | |||||
| REF 5 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001629) | |||||
| REF 7 | Role of adenosine in airway inflammation in an allergic mouse model of asthma. Int Immunopharmacol. 2006 Jan;6(1):36-45. | |||||
| REF 8 | Negative chronotropic and inotropic effects exerted by diadenosine hexaphosphate (AP6A) via A1-adenosine receptors. Br J Pharmacol. 1996 Nov;119(5):835-44. | |||||
| REF 9 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 10 | US patent application no. 2010,0009,934, Beta adrenergic receptor agonists for the treatment of b-cell proliferative disorders. | |||||
| REF 11 | Minoxidil-induced hair growth is mediated by adenosine in cultured dermal papilla cells: possible involvement of sulfonylurea receptor 2B as a target of minoxidil. J Invest Dermatol. 2001 Dec;117(6):1594-600. | |||||
| REF 12 | Influence of the antagonist of adenosine A1 receptors, 8-cyclopentyl-1 ,3-dipropylxanthine, upon the anticonvulsant activity of antiepileptic drugs in mice. Przegl Lek. 2008;65(11):759-63. | |||||
| REF 13 | Potent adenosine receptor antagonists that are selective for the A1 receptor subtype. Mol Pharmacol. 1987 Mar;31(3):247-52. | |||||
| REF 14 | Adenosine receptor ligands: differences with acute versus chronic treatment. Trends Pharmacol Sci. 1996 Mar;17(3):108-13. | |||||
| REF 15 | Pretreatment with angiotensin II activates protein kinase C and limits myocardial infarction in isolated rabbit hearts. J Mol Cell Cardiol. 1995 Mar;27(3):883-92. | |||||
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