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Adenosine receptor A1
An adenosine receptor A1 that is encoded in the genome of cow. [OMA:P28190, PRO:DNx]
Synonyms
Research
Bioassay Publications (21)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 3 (14.29) | 18.7374 |
| 1990's | 2 (9.52) | 18.2507 |
| 2000's | 16 (76.19) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (34)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 1,3-diethyl-8-phenylxanthine | Bos taurus (cattle) | IC50 | 1,509,975.0015 | 2 | 2 |
| 1,3-dipropyl-8-cyclopentylxanthine | Bos taurus (cattle) | Ki | 0.0005 | 8 | 8 |
| 1,3-dipropyl-8-(4-sulfophenyl)xanthine | Bos taurus (cattle) | IC50 | 0.0034 | 1 | 1 |
| 8-(4-sulfophenyl)theophylline | Bos taurus (cattle) | IC50 | 0.0219 | 1 | 1 |
| 8-cyclopentyl-1,3-dimethylxanthine | Bos taurus (cattle) | Ki | 0.0005 | 1 | 1 |
| 8-phenyltheophylline | Bos taurus (cattle) | IC50 | 1,509,975.0015 | 2 | 2 |
| 8-phenyltheophylline | Bos taurus (cattle) | Ki | 0.0031 | 1 | 1 |
| theophylline | Bos taurus (cattle) | IC50 | 1,006,650,005.0433 | 3 | 3 |
| theophylline | Bos taurus (cattle) | Ki | 4.1143 | 7 | 7 |
| 8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine | Bos taurus (cattle) | Ki | 0.0013 | 1 | 1 |
| 9,10-phenanthrenequinone | Bos taurus (cattle) | IC50 | 0.7000 | 1 | 1 |
| 2-chloroadenosine | Bos taurus (cattle) | Ki | 0.0202 | 1 | 1 |
| 1,2-naphthoquinone | Bos taurus (cattle) | IC50 | 3.0000 | 1 | 1 |
| rolofylline | Bos taurus (cattle) | Ki | 0.0002 | 1 | 1 |
| 1,3-dipropyl-8-(2-amino-4-chlorophenyl)xanthine | Bos taurus (cattle) | IC50 | 548,240.0000 | 2 | 2 |
| 1,3-dipropyl-8-(2-amino-4-chlorophenyl)xanthine | Bos taurus (cattle) | Ki | 0.0000 | 1 | 1 |
| phenylisopropyladenosine | Bos taurus (cattle) | Ki | 0.0082 | 3 | 3 |
| n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Bos taurus (cattle) | Ki | 0.0226 | 2 | 2 |
| 2-chloro-n(6)cyclopentyladenosine | Bos taurus (cattle) | Ki | 0.0003 | 2 | 2 |
| 1,3-dipropyl-8-phenylxanthine | Bos taurus (cattle) | IC50 | 706,270.0004 | 2 | 2 |
| kfm 19 | Bos taurus (cattle) | Ki | 0.0150 | 1 | 1 |
| tecadenoson | Bos taurus (cattle) | Ki | 0.0031 | 1 | 1 |
| sch 58261 | Bos taurus (cattle) | Ki | 0.3570 | 1 | 1 |
| trichostatin a | Bos taurus (cattle) | IC50 | 0.1900 | 1 | 1 |
| adenosine-5'-(n-ethylcarboxamide) | Bos taurus (cattle) | Ki | 0.0140 | 3 | 3 |
| 3'-c-methyladenosine | Bos taurus (cattle) | Ki | 49.5000 | 1 | 1 |
| 2'-c-methyladenosine | Bos taurus (cattle) | Ki | 0.9300 | 2 | 2 |
| n(6)-cyclopentyladenosine | Bos taurus (cattle) | Ki | 0.0004 | 2 | 2 |
| fk 838 | Bos taurus (cattle) | Ki | 0.0066 | 1 | 1 |
| 2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Bos taurus (cattle) | Ki | 0.8900 | 1 | 1 |
| endomorphin 1 | Bos taurus (cattle) | Ki | 0.0011 | 1 | 1 |
| n-(1-methyl-2-phenylethyl)adenosine, (s)-isomer | Bos taurus (cattle) | Ki | 0.0117 | 1 | 1 |
| 7-chloro-4-hydroxy-2-phenyl-1,8-naphthyridine | Bos taurus (cattle) | Ki | 0.0011 | 2 | 3 |
| xanthostigmine | Bos taurus (cattle) | IC50 | 0.0003 | 1 | 1 |
| a 803467 | Bos taurus (cattle) | IC50 | 6.7400 | 1 | 1 |
Drugs with Activation Measurements
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists.Journal of medicinal chemistry, , Oct-24, Volume: 45, Issue:22, 2002
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.Journal of medicinal chemistry, , Volume: 28, Issue:8, 1985
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.Journal of medicinal chemistry, , Volume: 28, Issue:8, 1985
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998