Proteins > Muscarinic acetylcholine receptor
Page last updated: 2024-08-07 17:19:48
Muscarinic acetylcholine receptor
[no definition available]
Synonyms
Research
Bioassay Publications (24)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 2 (8.33) | 18.7374 |
| 1990's | 7 (29.17) | 18.2507 |
| 2000's | 10 (41.67) | 29.6817 |
| 2010's | 5 (20.83) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (35)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| arecoline | Cavia porcellus (domestic guinea pig) | IC50 | 65.0000 | 1 | 1 |
| omeprazole | Cavia porcellus (domestic guinea pig) | IC50 | 3.8000 | 1 | 1 |
| oxotremorine | Cavia porcellus (domestic guinea pig) | Ki | 2,505,935,000,000.0800 | 2 | 2 |
| pirenzepine | Cavia porcellus (domestic guinea pig) | Ki | 0.0657 | 2 | 2 |
| carbachol | Cavia porcellus (domestic guinea pig) | IC50 | 150.0000 | 1 | 1 |
| carbachol | Cavia porcellus (domestic guinea pig) | Ki | 67.5911 | 4 | 4 |
| (4-(m-chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride | Cavia porcellus (domestic guinea pig) | Ki | 3.8019 | 1 | 1 |
| neostigmine bromide | Cavia porcellus (domestic guinea pig) | IC50 | 0.0450 | 1 | 2 |
| dihydrotestosterone | Cavia porcellus (domestic guinea pig) | Ki | 0.0002 | 1 | 1 |
| quinuclidinyl benzilate | Cavia porcellus (domestic guinea pig) | Ki | 0.0002 | 1 | 1 |
| nitrogenase stabilizing-protective protein, bacteria | Cavia porcellus (domestic guinea pig) | Ki | 0.1510 | 1 | 1 |
| xanomeline | Cavia porcellus (domestic guinea pig) | Ki | 0.1585 | 1 | 1 |
| n-methylscopolamine | Cavia porcellus (domestic guinea pig) | Ki | 3,154,785,000,000,000.0000 | 2 | 2 |
| atropine | Cavia porcellus (domestic guinea pig) | Ki | 158,489,000,000,000.0000 | 1 | 1 |
| br 100 | Cavia porcellus (domestic guinea pig) | Ki | 1.6000 | 1 | 1 |
| ipratropium bromide anhydrous | Cavia porcellus (domestic guinea pig) | Ki | 0.0013 | 1 | 1 |
| sabcomeline | Cavia porcellus (domestic guinea pig) | IC50 | 0.1700 | 1 | 1 |
| pitolisant | Cavia porcellus (domestic guinea pig) | Ki | 0.0117 | 1 | 1 |
| tiotropium bromide | Cavia porcellus (domestic guinea pig) | IC50 | 0.0004 | 1 | 1 |
| tiotropium bromide | Cavia porcellus (domestic guinea pig) | Ki | 0.0003 | 1 | 1 |
| lgd 2226 | Cavia porcellus (domestic guinea pig) | Ki | 0.0015 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| caffeine | Cavia porcellus (domestic guinea pig) | Kb | 25.0000 | 1 | 1 |
| psb 11 | Cavia porcellus (domestic guinea pig) | Kb | 2.1000 | 1 | 1 |
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.Journal of medicinal chemistry, , Nov-12, Volume: 36, Issue:23, 1993
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.Bioorganic & medicinal chemistry, , Dec-15, Volume: 15, Issue:24, 2007
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.Bioorganic & medicinal chemistry, , Dec-15, Volume: 17, Issue:24, 2009
Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.Journal of medicinal chemistry, , Sep-25, Volume: 46, Issue:20, 2003
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.Journal of medicinal chemistry, , Nov-12, Volume: 36, Issue:23, 1993
Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.Journal of medicinal chemistry, , Sep-25, Volume: 46, Issue:20, 2003
Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
[no title available]Bioorganic & medicinal chemistry, , 05-15, Volume: 26, Issue:9, 2018
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
Structure-activity relationships among methoctramine-related polymethylene tetraamines. Chain-length and substituent effects on M-2 muscarinic receptor blocking activity.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Enantioselectivity of muscarinic antagonists. 2,2-Dicyclohexyl-5-[(dimethylamino)methyl]-1,3-oxathiolane methiodides and related 3-oxides.Journal of medicinal chemistry, , Volume: 31, Issue:9, 1988
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008