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Beta-2 adrenergic receptor
A beta-2 adrenergic receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P07550]
Synonyms
Beta-2 adrenoreceptor;
Beta-2 adrenoceptor
Research
Bioassay Publications (118)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 8 (6.78) | 18.7374 |
| 1990's | 11 (9.32) | 18.2507 |
| 2000's | 38 (32.20) | 29.6817 |
| 2010's | 55 (46.61) | 24.3611 |
| 2020's | 6 (5.08) | 2.80 |
Compounds (109)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| albuterol | Homo sapiens (human) | IC50 | 1.2618 | 3 | 2 |
| albuterol | Homo sapiens (human) | Ki | 0.8512 | 4 | 3 |
| alprenolol | Homo sapiens (human) | IC50 | 0.0031 | 4 | 4 |
| alprenolol | Homo sapiens (human) | Ki | 0.0010 | 3 | 4 |
| atenolol | Homo sapiens (human) | IC50 | 14.6340 | 1 | 0 |
| atenolol | Homo sapiens (human) | Ki | 9.8055 | 2 | 1 |
| bisoprolol | Homo sapiens (human) | Ki | 0.2500 | 1 | 1 |
| carvedilol | Homo sapiens (human) | IC50 | 0.0002 | 1 | 0 |
| carvedilol | Homo sapiens (human) | Ki | 0.0002 | 1 | 0 |
| cgp 20712a | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| cisapride | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| clenbuterol | Homo sapiens (human) | IC50 | 0.6705 | 2 | 1 |
| clenbuterol | Homo sapiens (human) | Ki | 0.3893 | 3 | 2 |
| clorprenaline | Homo sapiens (human) | IC50 | 1.9930 | 1 | 0 |
| clorprenaline | Homo sapiens (human) | Ki | 1.3700 | 1 | 0 |
| doxazosin | Homo sapiens (human) | IC50 | 2.7480 | 1 | 0 |
| doxazosin | Homo sapiens (human) | Ki | 1.8890 | 1 | 0 |
| berotek | Homo sapiens (human) | Ki | 0.1260 | 1 | 1 |
| formoterol fumarate | Homo sapiens (human) | Ki | 0.0191 | 8 | 8 |
| ici 118551 | Homo sapiens (human) | IC50 | 0.0017 | 6 | 6 |
| ici 118551 | Homo sapiens (human) | Ki | 0.0004 | 4 | 4 |
| isoproterenol | Homo sapiens (human) | IC50 | 0.2460 | 1 | 0 |
| isoproterenol | Homo sapiens (human) | Ki | 0.2036 | 6 | 5 |
| labetalol | Homo sapiens (human) | IC50 | 0.0160 | 1 | 0 |
| labetalol | Homo sapiens (human) | Ki | 0.0110 | 1 | 0 |
| loperamide | Homo sapiens (human) | IC50 | 3.0050 | 1 | 0 |
| loperamide | Homo sapiens (human) | Ki | 2.0660 | 1 | 0 |
| metoprolol | Homo sapiens (human) | IC50 | 2.5730 | 1 | 0 |
| metoprolol | Homo sapiens (human) | Ki | 0.9945 | 2 | 1 |
| pindolol | Homo sapiens (human) | IC50 | 0.0005 | 1 | 0 |
| pindolol | Homo sapiens (human) | Ki | 0.0004 | 2 | 1 |
| procaterol | Homo sapiens (human) | Ki | 0.0330 | 1 | 1 |
| propafenone | Homo sapiens (human) | IC50 | 0.0520 | 1 | 0 |
| propafenone | Homo sapiens (human) | Ki | 0.0360 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 0.0114 | 6 | 5 |
| propranolol | Homo sapiens (human) | Ki | 0.0014 | 5 | 4 |
| salmeterol xinafoate | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| salmeterol xinafoate | Homo sapiens (human) | Ki | 0.0183 | 11 | 11 |
| dpi 201-106 | Homo sapiens (human) | Ki | 0.0573 | 1 | 1 |
| sotalol | Homo sapiens (human) | IC50 | 3.8170 | 2 | 1 |
| sotalol | Homo sapiens (human) | Ki | 0.2983 | 1 | 0 |
| lysergic acid diethylamide | Homo sapiens (human) | Ki | 0.7400 | 1 | 1 |
| isoproterenol hydrochloride | Homo sapiens (human) | Ki | 0.5011 | 1 | 2 |
| ergotamine | Homo sapiens (human) | IC50 | 2.7610 | 1 | 0 |
| ergotamine | Homo sapiens (human) | Ki | 1.8980 | 1 | 0 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n-methyllaurotetanine | Homo sapiens (human) | Ki | 0.9500 | 1 | 1 |
| dexpropranolol | Homo sapiens (human) | IC50 | 0.0760 | 1 | 0 |
| dexpropranolol | Homo sapiens (human) | Ki | 0.0520 | 1 | 0 |
| lisuride | Homo sapiens (human) | IC50 | 0.0410 | 1 | 0 |
| lisuride | Homo sapiens (human) | Ki | 0.0290 | 1 | 0 |
| 1-(3-chloro-5-benzo[b][1]benzoxepinyl)-4-methylpiperazine | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
| timolol | Homo sapiens (human) | IC50 | 0.0003 | 1 | 0 |
| timolol | Homo sapiens (human) | Ki | 0.0002 | 2 | 1 |
| dobutamine | Homo sapiens (human) | IC50 | 1.5170 | 1 | 0 |
| dobutamine | Homo sapiens (human) | Ki | 1.0430 | 1 | 0 |
| levobunolol | Homo sapiens (human) | IC50 | 0.0008 | 1 | 0 |
| levobunolol | Homo sapiens (human) | Ki | 0.0005 | 1 | 0 |
| bopindolol | Homo sapiens (human) | IC50 | 0.0200 | 1 | 0 |
| bopindolol | Homo sapiens (human) | Ki | 0.0140 | 1 | 0 |
| quinpirole | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| ractopamine | Homo sapiens (human) | IC50 | 0.3300 | 1 | 1 |
| ractopamine | Homo sapiens (human) | Ki | 0.1800 | 2 | 2 |
| sematilide | Homo sapiens (human) | IC50 | 7,000.0000 | 1 | 1 |
| carmoterol | Homo sapiens (human) | Ki | 0.0032 | 1 | 1 |
| sotalol hydrochloride | Homo sapiens (human) | IC50 | 7.2000 | 1 | 1 |
| talinolol | Homo sapiens (human) | Ki | 0.9000 | 1 | 1 |
| carazolol | Homo sapiens (human) | Ki | 0.0001 | 2 | 2 |
| u 74006f | Homo sapiens (human) | IC50 | 22.6590 | 1 | 0 |
| u 74006f | Homo sapiens (human) | Ki | 15.5780 | 1 | 0 |
| pramipexole | Homo sapiens (human) | Ki | 55.0000 | 2 | 2 |
| sb 204070a | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| levalbuterol | Homo sapiens (human) | Ki | 4.7008 | 3 | 6 |
| sc 53116 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sc 53116 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sibenadet | Homo sapiens (human) | Ki | 0.0040 | 1 | 1 |
| L-isoprenaline | Homo sapiens (human) | Ki | 0.0460 | 1 | 1 |
| darifenacin | Homo sapiens (human) | Ki | 0.0384 | 2 | 2 |
| (S)-(-)-pindolol | Homo sapiens (human) | IC50 | 0.0016 | 1 | 0 |
| (S)-(-)-pindolol | Homo sapiens (human) | Ki | 0.0011 | 1 | 0 |
| ru 42173 | Homo sapiens (human) | IC50 | 0.6200 | 1 | 1 |
| ru 42173 | Homo sapiens (human) | Ki | 0.3200 | 2 | 2 |
| sb-224289 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 3-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| montelukast | Homo sapiens (human) | IC50 | 3.4880 | 1 | 0 |
| montelukast | Homo sapiens (human) | Ki | 2.3980 | 1 | 0 |
| cl 316243 | Homo sapiens (human) | Ki | 79.2000 | 1 | 1 |
| ici 118551 | Homo sapiens (human) | IC50 | 0.0007 | 1 | 1 |
| ici 118551 | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| cgp 12177a | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| dihydrexidine | Homo sapiens (human) | Ki | 1.2000 | 1 | 1 |
| 7-hydroxy-2-n,n-dipropylaminotetralin, (r)-isomer | Homo sapiens (human) | Ki | 86.0000 | 1 | 1 |
| nps2143 | Homo sapiens (human) | IC50 | 0.0043 | 1 | 1 |
| indacaterol | Homo sapiens (human) | Ki | 0.0391 | 3 | 3 |
| l 755507 | Homo sapiens (human) | IC50 | 1.5950 | 2 | 2 |
| l 755507 | Homo sapiens (human) | Ki | 0.1600 | 1 | 1 |
| brl 37344 | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| brl 37344 | Homo sapiens (human) | Ki | 2.8500 | 1 | 1 |
| solabegron | Homo sapiens (human) | Ki | 1.5849 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 77-lh-28-1 | Homo sapiens (human) | Ki | 43.6516 | 1 | 1 |
| sb-649915 | Homo sapiens (human) | Ki | 0.5012 | 1 | 1 |
| l 764646 | Homo sapiens (human) | IC50 | 12.0000 | 2 | 2 |
| 5-hydroxy-2-n,n-dipropylaminotetralin, (s)-isomer | Homo sapiens (human) | Ki | 40.0000 | 1 | 1 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| bix 02565 | Homo sapiens (human) | IC50 | 1.8200 | 1 | 0 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| isoproterenol | Homo sapiens (human) | Km | 0.0500 | 1 | 1 |
[no title available]Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Recent Advances in βJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.Journal of medicinal chemistry, , May-13, Volume: 53, Issue:9, 2010
Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[no title available],
Controlling cellular distribution of drugs with permeability modifying moieties.MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
[no title available]Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.ACS medicinal chemistry letters, , Oct-10, Volume: 4, Issue:10, 2013
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[no title available],
[no title available]Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[no title available]Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[no title available],
[no title available]Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Similarity- and Substructure-Based Development of βACS medicinal chemistry letters, , May-11, Volume: 8, Issue:5, 2017
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 14, Issue:22, 2004
β2-Adrenoceptor agonists in the regulation of mitochondrial biogenesis.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
[no title available],
Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.ACS medicinal chemistry letters, , Oct-10, Volume: 4, Issue:10, 2013
β2-Adrenoceptor agonists in the regulation of mitochondrial biogenesis.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
β2-Adrenoceptor agonists in the regulation of mitochondrial biogenesis.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.Journal of medicinal chemistry, , May-13, Volume: 53, Issue:9, 2010
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Studies towards topical selective beta2-adrenoceptor agonists with a long duration of action.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Use of 5-hydroxy-4H-benzo[1,4]oxazin-3-ones as beta2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 14, Issue:18, 2004
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a beta2 adrenoceptor agonist.European journal of medicinal chemistry, , Volume: 44, Issue:7, 2009
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
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 pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
[no title available]Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
8-Hydroxyquinolin-2(1H)-one analogues as potential βEuropean journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
[no title available]Journal of natural products, , 11-22, Volume: 82, Issue:11, 2019
[no title available]Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019
Synthesis and biological evaluation of βEuropean journal of medicinal chemistry, , May-25, Volume: 152, 2018
[no title available]Journal of natural products, , 04-27, Volume: 81, Issue:4, 2018
[no title available]Journal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
Comparative molecular field analysis of fenoterol derivatives interacting with an agonist-stabilized form of the β₂-adrenergic receptor.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
β2-Adrenoceptor agonists in the regulation of mitochondrial biogenesis.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and molecular modeling based on the solved X-ray structure of the beta2-adrenergic receptor: part 6.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a beta2 adrenoceptor agonist.European journal of medicinal chemistry, , Volume: 44, Issue:7, 2009
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists.Bioorganic & medicinal chemistry, , May-01, Volume: 17, Issue:9, 2009
Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and evaluation of physical properties as potential overactive bladder therapies: part 5.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 17, Issue:15, 2009
Synthesis of bivalent beta2-adrenergic and adenosine A1 receptor ligands.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Discovery of a novel series of benzoic acid derivatives as potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Discovery of a novel series of biphenyl benzoic acid derivatives as highly potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. Part II.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.Journal of medicinal chemistry, , May-04, Volume: 49, Issue:9, 2006
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.Bioorganic & medicinal chemistry letters, , Jan-17, Volume: 15, Issue:2, 2005
Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.Journal of medicinal chemistry, , Jan-31, Volume: 45, Issue:3, 2002
2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: novel selective beta3-adrenoceptor agonists.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
3,4-O-diacetylisoproterenol. Preparation, structure proof, and beta-receptor effect.Journal of medicinal chemistry, , Volume: 28, Issue:12, 1985
Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols.Journal of medicinal chemistry, , Volume: 25, Issue:6, 1982
[no title available],
β2-Adrenoceptor agonists in the regulation of mitochondrial biogenesis.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a beta2 adrenoceptor agonist.European journal of medicinal chemistry, , Volume: 44, Issue:7, 2009
[no title available]Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[no title available],
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 17, Issue:20, 2007
[no title available],
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.Journal of medicinal chemistry, , Volume: 27, Issue:8, 1984
Conformational effects on the activity of drugs. 10. Synthesis, conformation, and pharmacological properties of 1-(2,5-dimethoxyphenyl)-2-aminoethanols and their morpholine analogues.Journal of medicinal chemistry, , Volume: 26, Issue:2, 1983
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
β2-Adrenoceptor agonists in the regulation of mitochondrial biogenesis.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
Photoswitchable Antagonists for a Precise Spatiotemporal Control of βJournal of medicinal chemistry, , 08-13, Volume: 63, Issue:15, 2020
[no title available]Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Comparative molecular field analysis of fenoterol derivatives interacting with an agonist-stabilized form of the β₂-adrenergic receptor.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a beta2 adrenoceptor agonist.European journal of medicinal chemistry, , Volume: 44, Issue:7, 2009
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[omega-[4-[(alkylsulfonyl)amino]phenyl]-omega- hydroxyalkyl]-1H-imidazolium salts and related compounds.Journal of medicinal chemistry, , Volume: 30, Issue:4, 1987
[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.Journal of medicinal chemistry, , Volume: 27, Issue:8, 1984
Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds.Journal of medicinal chemistry, , Volume: 27, Issue:9, 1984
[no title available],
8-Hydroxyquinolin-2(1H)-one analogues as potential βEuropean journal of medicinal chemistry, , Nov-15, Volume: 224, 2021
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent βBioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Recent Advances in βJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
[no title available]Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
Multivalent design of long-acting β(2)-adrenoceptor agonists incorporating biarylamines.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 24, Issue:13, 2014
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
Comparative molecular field analysis of fenoterol derivatives: A platform towards highly selective and effective beta(2)-adrenergic receptor agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.Journal of medicinal chemistry, , May-13, Volume: 53, Issue:9, 2010
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
The discovery of long acting beta2-adrenoreceptor agonists.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 17, Issue:14, 2007
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 14, Issue:18, 2004
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
[no title available],
β2-Adrenoceptor agonists in the regulation of mitochondrial biogenesis.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 21, Issue:13, 2011
Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a beta2 adrenoceptor agonist.European journal of medicinal chemistry, , Volume: 44, Issue:7, 2009
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.British journal of pharmacology, , Volume: 144, Issue:3, 2005
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent βBioorganic & medicinal chemistry, , 01-01, Volume: 28, Issue:1, 2020
Cell-based and in-silico studies on the high intrinsic activity of two boron-containing salbutamol derivatives at the human β₂-adrenoceptor.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DJournal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.Bioorganic & medicinal chemistry, , 06-15, Volume: 24, Issue:12, 2016
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.Journal of medicinal chemistry, , Feb-09, Volume: 49, Issue:3, 2006
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 22, Issue:19, 2012
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014
Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacJournal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 22, Issue:19, 2012
Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
Recent Advances in βJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function bJournal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.Journal of medicinal chemistry, , Apr-26, Volume: 44, Issue:9, 2001
2,4-Thiazolidinediones as potent and selective human beta3 agonists.Bioorganic & medicinal chemistry letters, , Mar-26, Volume: 11, Issue:6, 2001
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Similarity- and Substructure-Based Development of βACS medicinal chemistry letters, , May-11, Volume: 8, Issue:5, 2017
Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacJournal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Recent Advances in βJournal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 24, Issue:17, 2014
From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.Journal of medicinal chemistry, , May-13, Volume: 53, Issue:9, 2010
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.Journal of medicinal chemistry, , Apr-26, Volume: 44, Issue:9, 2001
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 8, Issue:21, 1998
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.Bioorganic & medicinal chemistry letters, , May-05, Volume: 8, Issue:9, 1998
Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 19, Issue:9, 2010
Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes.Bioorganic & medicinal chemistry, , Apr-01, Volume: 15, Issue:7, 2007
Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 8, Issue:21, 1998
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 9, Issue:5, 1999
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 9, Issue:5, 1999
Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).Journal of medicinal chemistry, , 07-11, Volume: 62, Issue:13, 2019
Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacJournal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Enables
This protein enables 9 target(s):
| Target | Category | Definition |
|---|
| amyloid-beta binding | molecular function | Binding to an amyloid-beta peptide/protein. [GOC:hjd] |
| beta2-adrenergic receptor activity | molecular function | Combining with epinephrine or norepinephrine to initiate a change in cell activity via activation of a G protein, with pharmacological characteristics of beta2-adrenergic receptors. [GOC:mah, IUPHAR_GPCR:1274] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| adenylate cyclase binding | molecular function | Binding to an adenylate cyclase. [GOC:jl] |
| potassium channel regulator activity | molecular function | Binds to and modulates the activity of a potassium channel. [GOC:dos, GOC:mah] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
| norepinephrine binding | molecular function | Binding to norepinephrine, (3,4-dihydroxyphenyl-2-aminoethanol), a hormone secreted by the adrenal medulla and a neurotransmitter in the sympathetic peripheral nervous system and in some tracts of the CNS. It is also the biosynthetic precursor of epinephrine. [GOC:ai] |
Located In
This protein is located in 11 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| lysosome | cellular component | A small lytic vacuole that has cell cycle-independent morphology found in most animal cells and that contains a variety of hydrolases, most of which have their maximal activities in the pH range 5-6. The contained enzymes display latency if properly isolated. About 40 different lysosomal hydrolases are known and lysosomes have a great variety of morphologies and functions. [GOC:mah, ISBN:0198506732] |
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| early endosome | cellular component | A membrane-bounded organelle that receives incoming material from primary endocytic vesicles that have been generated by clathrin-dependent and clathrin-independent endocytosis; vesicles fuse with the early endosome to deliver cargo for sorting into recycling or degradation pathways. [GOC:mah, NIF_Subcellular:nlx_subcell_20090701, PMID:19696797] |
| Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| endosome membrane | cellular component | The lipid bilayer surrounding an endosome. [GOC:mah] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| clathrin-coated endocytic vesicle membrane | cellular component | The lipid bilayer surrounding a clathrin-coated endocytic vesicle. [GOC:mah] |
| neuronal dense core vesicle | cellular component | A dense core vesicle (granule) that is part of a neuron. These vesicles typically contain neuropeptides. They can be found in all parts of neurons, including the soma, dendrites, axonal swellings (varicosities) and synaptic terminals. [GOC:dos, ISBN:978-0-07-181001-2, Wikipedia:Neuropeptide&oldid=713905176] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 32 target(s):
| Target | Category | Definition |
|---|
| diet induced thermogenesis | biological process | The process that results in increased metabolic rate in tissues of an organism. It is triggered by the detection of dietary excess. This process is achieved via signaling in the sympathetic nervous system. [PMID:12161655] |
| regulation of sodium ion transport | biological process | Any process that modulates the frequency, rate or extent of the directed movement of sodium ions (Na+) into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:dph] |
| transcription by RNA polymerase II | biological process | The synthesis of RNA from a DNA template by RNA polymerase II (RNAP II), originating at an RNA polymerase II promoter. Includes transcription of messenger RNA (mRNA) and certain small nuclear RNAs (snRNAs). [GOC:jl, GOC:txnOH, ISBN:0321000382] |
| receptor-mediated endocytosis | biological process | An endocytosis process in which cell surface receptors ensure specificity of transport. A specific receptor on the cell surface binds tightly to the extracellular macromolecule (the ligand) that it recognizes; the plasma-membrane region containing the receptor-ligand complex then undergoes endocytosis, forming a transport vesicle containing the receptor-ligand complex and excluding most other plasma-membrane proteins. Receptor-mediated endocytosis generally occurs via clathrin-coated pits and vesicles. [GOC:mah, ISBN:0716731363] |
| smooth muscle contraction | biological process | A process in which force is generated within smooth muscle tissue, resulting in a change in muscle geometry. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. Smooth muscle differs from striated muscle in the much higher actin/myosin ratio, the absence of conspicuous sarcomeres and the ability to contract to a much smaller fraction of its resting length. [GOC:ef, GOC:jl, GOC:mtg_muscle, ISBN:0198506732] |
| cell surface receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling] |
| activation of transmembrane receptor protein tyrosine kinase activity | biological process | Any process that initiates the activity of the inactive transmembrane receptor protein tyrosine kinase activity. [GOC:dph, GOC:tb] |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194] |
| endosome to lysosome transport | biological process | The directed movement of substances from endosomes to lysosomes. [GOC:ai, ISBN:0716731363] |
| response to cold | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cold stimulus, a temperature stimulus below the optimal temperature for that organism. [GOC:lr] |
| positive regulation of protein kinase A signaling | biological process | Any process that increases the rate, frequency, or extent of protein kinase A signaling. PKA signaling is the series of reactions, mediated by the intracellular serine/threonine kinase protein kinase A, which occurs as a result of a single trigger reaction or compound. [GOC:BHF, GOC:dph, GOC:tb] |
| positive regulation of bone mineralization | biological process | Any process that activates or increases the frequency, rate or extent of bone mineralization. [GOC:go_curators] |
| heat generation | biological process | Any homeostatic process in which an organism produces heat, thereby raising its internal temperature. [GOC:mah] |
| negative regulation of multicellular organism growth | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of growth of an organism to reach its usual body size. [GOC:dph, GOC:ems, GOC:tb] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| bone resorption | biological process | The process in which specialized cells known as osteoclasts degrade the organic and inorganic portions of bone, and endocytose and transport the degradation products. [GOC:mah, PMID:10968780] |
| negative regulation of G protein-coupled receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of G protein-coupled receptor signaling pathway. [GOC:go_curators] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| negative regulation of smooth muscle contraction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
| brown fat cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a brown adipocyte, an animal connective tissue cell involved in adaptive thermogenesis. Brown adipocytes contain multiple small droplets of triglycerides and a high number of mitochondria. [PMID:12588810] |
| positive regulation of mini excitatory postsynaptic potential | biological process | Any process that increases the frequency, rate or extent of mini excitatory postsynaptic potential. Mini excitatory postsynaptic potential is a process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell, induced by the spontaneous release of a single vesicle of an excitatory neurotransmitter into the synapse. [GOC:aruk, GOC:bc, PMID:20395454] |
| adrenergic receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:BHF] |
| adenylate cyclase-activating adrenergic receptor signaling pathway | biological process | An adenylate cyclase-activating G protein-coupled receptor signaling pathway initiated by a ligand binding to an adrenergic receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process. [GOC:BHF, GOC:mah, GOC:signaling] |
| positive regulation of protein serine/threonine kinase activity | biological process | Any process that increases the rate, frequency, or extent of protein serine/threonine kinase activity. [GOC:mah] |
| positive regulation of cold-induced thermogenesis | biological process | Any process that activates or increases the frequency, rate or extent of cold-induced thermogenesis. [PMID:27876809] |
| positive regulation of autophagosome maturation | biological process | Any process that activates or increases the frequency, rate or extent of autophagosome maturation. [GOC:autophagy, GOC:TermGenie, PMID:10436019, PMID:21383079] |
| positive regulation of lipophagy | biological process | Any process that activates or increases the frequency, rate or extent of lipophagy. [GO_REF:0000058, GOC:autophagy, GOC:dph, GOC:TermGenie, PMID:25383539] |
| cellular response to amyloid-beta | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a amyloid-beta stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:23555824] |
| response to psychosocial stress | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of exposure to aversive or demanding psychological and social conditions that tax or exceed the behavioral resources of the organism. [PMID:22922217, PMID:26458179] |
| positive regulation of cAMP-dependent protein kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of cAMP-dependent protein kinase activity. [GOC:obol] |
| positive regulation of AMPA receptor activity | biological process | Any process that activates or increases the frequency, rate or extent of AMPA selective glutamate receptor activity. [PMID:21423165] |
| norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure | biological process | A process that results in an increase in the diameter of an artery during the norepinephrine-epinephrine response to blood pressure change. [GOC:mtg_cardio, PMID:10358008] |