Target Information
| Target General Information | Top | |||||
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| Target ID |
T15117
(Former ID: TTDNS00566)
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| Target Name |
Adrenergic receptor (ADR)
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| Synonyms |
Adrenoceptor
Click to Show/Hide
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 5 Target-related Diseases | + | ||||
| 1 | Cushing syndrome [ICD-11: 5A70] | |||||
| 2 | Diagnostic imaging [ICD-11: N.A.] | |||||
| 3 | Glaucoma [ICD-11: 9C61] | |||||
| 4 | Hypertension [ICD-11: BA00-BA04] | |||||
| 5 | Orthostatic hypotension [ICD-11: BA21] | |||||
| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 5 Approved Drugs | + | ||||
| 1 | Befunolol hci | Drug Info | Approved | Glaucoma/ocular hypertension | [1] | |
| 2 | Celiprolol hcl | Drug Info | Approved | Hypertension | [1] | |
| 3 | Ovine corticotropin-releasing hormone | Drug Info | Approved | Cushing disease | [1] | |
| 4 | Oxilofrine | Drug Info | Approved | Orthostatic hypotension | [1] | |
| 5 | Terbutyline | Drug Info | Approved | Hypertension | [1] | |
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | Dabelotine | Drug Info | Phase 3 | Cognitive impairment | [3] | |
| 2 | AR08 | Drug Info | Phase 2 | Attention deficit hyperactivity disorder | [4] | |
| Patented Agent(s) | [+] 1 Patented Agents | + | ||||
| 1 | PMID30124346-Compound-60TABLE5 | Drug Info | Patented | Parkinson disease | [5], [6], [7] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | Etilefrine | Drug Info | Withdrawn from market | Cardiovascular disease | [1] | |
| 2 | AIR-Epinephrine | Drug Info | Discontinued in Phase 1 | Allergy | [8] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Modulator | [+] 8 Modulator drugs | + | ||||
| 1 | Befunolol hci | Drug Info | [9], [10] | |||
| 2 | Celiprolol hcl | Drug Info | [9], [11] | |||
| 3 | Ovine corticotropin-releasing hormone | Drug Info | [1] | |||
| 4 | Oxilofrine | Drug Info | [1] | |||
| 5 | Terbutyline | Drug Info | [1] | |||
| 6 | Dabelotine | Drug Info | [12] | |||
| 7 | AR08 | Drug Info | [13] | |||
| 8 | Etilefrine | Drug Info | [1] | |||
| Ligand | [+] 1 Ligand drugs | + | ||||
| 1 | PMID30124346-Compound-60TABLE5 | Drug Info | [7] | |||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | AIR-Epinephrine | Drug Info | [14] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (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 | ||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 2 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018104. | |||||
| REF 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002175) | |||||
| REF 4 | ClinicalTrials.gov (NCT01876719) AR08 for Treatment of ADHD in Children. U.S. National Institutes of Health. | |||||
| REF 5 | mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706. | |||||
| REF 6 | Caspase inhibitors: a review of recently patented compounds (2013-2015).Expert Opin Ther Pat. 2018 Jan;28(1):47-59. | |||||
| REF 7 | 5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689. | |||||
| 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 800019414) | |||||
| REF 9 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 10 | Enzyme immunoassays for beta-adrenoreceptor blocking agent, befunolol and its main metabolite, M1. J Immunoassay. 1983;4(4):351-71. | |||||
| REF 11 | Celiprolol: a new beta adrenoceptor antagonist with novel ancillary properties. J Cardiovasc Pharmacol. 1986;8 Suppl 4:S29-32. | |||||
| REF 12 | US patent application no. 2007,0049,576, Neurogenesis by muscarinic receptor modulation. | |||||
| REF 13 | Optimizing treatments for nicotine dependence by increasing cognitive performance during withdrawal. Expert Opin Drug Discov. 2014 June; 9(6): 579-594. | |||||
| REF 14 | Prostaglandin synthesis inhibitors reverse alpha-adrenergic inhibition of acute insulin response to glucose. Am J Physiol. 1980 Dec;239(6):E490-500. | |||||
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