Page last updated: 2024-11-04

enprofylline

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

enprofylline : Xanthine bearing a propyl substituent at position 3. A bronchodilator, it is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID1676
CHEMBL ID279898
CHEBI ID126237
SCHEMBL ID156402
SCHEMBL ID18029491
MeSH IDM0105916

Synonyms (86)

Synonym
smr000058496
d-4028
enprofylline
EU-0100910
enprofylline (usan/inn)
D04006
41078-02-8
enprofyllinum [inn-latin]
einecs 255-201-8
enprofylline [usan:inn]
enprofilina [inn-spanish]
1h-purine-2,6-dione, 3,7-dihydro-3-propyl-
nilyph
NCGC00015824-01
lopac-p-5679
PDSP2_001186
PDSP1_001202
LOPAC0_000910
3,7-dihydro-3-propyl-1h-purine-2,6-dione
3-propyl-3,7-dihydro-purine-2,6-dione
3-n-propylxanthine
DB00824
PDSP2_001003
NCGC00022716-05
MLS000069700
3-propylxanthine
PDSP1_001019
NCGC00022716-03
NCGC00015824-02
NCGC00022716-04
NCGC00015824-05
CHEBI:126237 ,
enprofilina
3-propyl-3,7-dihydro-1h-purine-2,6-dione
enprofyllinum
P 5679 ,
NCGC00015824-08
CHEMBL279898 ,
d 4028
L000242
3-propylxanthine (enprofylline)
3-propyl-3,7-dihydro-purine-2,6-dione(enprofylline)
bdbm50001493
3-propyl-7h-purine-2,6-dione
NCGC00015824-07
HMS3262F22
AKOS006271777
cas-41078-02-8
dtxsid9045186 ,
dtxcid7025186
tox21_110232
CCG-204992
HMS2234D09
NCGC00015824-03
NCGC00015824-04
NCGC00015824-06
NCGC00015824-09
AKOS013464325
unii-dt7dt5e518
dt7dt5e518 ,
FT-0630617
LP00910
HMS3369J09
SIQPXVQCUCHWDI-UHFFFAOYSA-N
SCHEMBL156402
enprofylline [who-dd]
enprofylline [usan]
enprofylline [mart.]
enprofylline [inn]
NCGC00261595-01
tox21_500910
SCHEMBL18029491
3-propyl-1h-purine-2,6(3h,7h)-dione
3-propyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione
sr-01000000173
SR-01000000173-2
Q5379482
Z1198148417
BCP14343
EN300-132307
SDCCGSBI-0050885.P002
3-propylxanthfine
A914216
MS-23050
HY-14117
CS-0003206

Research Excerpts

Overview

Enprofylline is a novel xanthine derivative with negligible adenosine antagonizing ability. It is a more potent smooth muscle relaxant and antiasthmatic drug than theophylline but does not produce diuretic or CNS-stimulant effects.

ExcerptReferenceRelevance
"Enprofylline is a potent bronchodilating xanthine derivative that has been shown to have little or no ability to antagonize adenosine in a variety of cell types. "( A novel bronchodilator xanthine apparently without adenosine receptor antagonism and tremorogenic effect.
Andersson, KE; Lunell, E; Persson, CG; Svedmyr, N, 1983
)
1.71
"Enprofylline is a novel xanthine derivative with negligible adenosine antagonizing ability. "( Intravenous enprofylline in asthma patients.
Andersson, KE; Lunell, E; Persson, CG; Svedmyr, N, 1984
)
2.09
"Enprofylline is a new xanthine derivative that shares theophylline's bronchodilator properties but is free of theophylline's adenosine receptor antagonist activity. "( Long-term xanthine therapy of asthma. Enprofylline and theophylline compared. International Enprofylline Study Group.
Chapman, KR; Kallen, A; Ljungholm, K, 1994
)
2
"Enprofylline is a novel xanthine with a low adenosine antagonistic potency, but with a good bronchodilator activity. "( Actions of enprofylline in the rat hippocampus.
Bergman, B; Fredholm, BB; Lindström, K, 1985
)
2.1
"Enprofylline is a more potent smooth muscle relaxant and antiasthmatic drug than theophylline but does not produce, e.g., theophylline-like diuretic effects, CNS-stimulant behavioural effects (restlessness - seizures), gastric secretory effects and release of free fatty acids."( Effects of enprofylline and theophylline may show the role of adenosine.
Andersson, KE; Kjellin, G; Persson, CG, 1986
)
1.38
"Enprofylline was shown to be a rather potent smooth muscle relaxant [inhibitory concentration that decreases response by 50% (IC50) = 3 X 10(-5) mol/L] and an almost equally potent cyclic adenosine monophosphate-dependent phosphodiesterase inhibitor (IC50 = 10(-4) mol/L), whereas it was a less potent cyclic guanosine monophosphate-dependent phosphodiesterase inhibitor."( Effects of enprofylline, a new xanthine derivate, on human pregnant myometrium.
Andersson, RG; Berg, G; Rydén, G, 1987
)
1.38
"Enprofylline is a xanthine derivative with anti-asthmatic effect but, in contrast to aminophylline, enprofylline has very weak adenosine antagonistic properties."( Adenosine in the inhibition of diazepam sedation by aminophylline.
Arvidsson, S; Ekström-Jodal, B; Martinell, S; Niemand, D; Svedmyr, N, 1986
)
0.99
"Enprofylline is a novel xanthine derivative with negligible adenosine antagonizing ability. "( Additive bronchodilator effects of terbutaline and enprofylline in asthma.
Lunell, E; Rasmussen, JB, 1987
)
1.97
"Enprofylline (E) is a xanthine drug that has poor ability to antagonize physiological actions of adenosine."( Effects of theophylline and enprofylline on diaphragmatic contractility.
Aubier, M; Mal, H; Murciano, D; Pariente, R; Viirès, N, 1987
)
1.29

Effects

Enprofylline has a short half-life in children, but the sustained-release formulation provides stable serum concentrations and satisfactory relief of asthma throughout the 12-hour dosing interval.

ExcerptReferenceRelevance
"Enprofylline has a short half-life in children, but the sustained-release formulation provides stable serum concentrations and satisfactory relief of asthma throughout the 12-hour dosing interval."( Pharmacokinetics of enprofylline administered intravenously and as a sustained-release tablet at steady state in children with asthma.
Simons, FE; Simons, KJ; Watson, WT, 1988
)
1.32
"Enprofylline has been reported (Persson et al., Life Sci."( Dissociation of effects of xanthine analogs on renal prostaglandins and renal excretory function in the awake rat.
Armstrong, EL; Baer, PG; Cagen, LM, 1983
)
0.99
"Enprofylline which has been shown to exhibit some actions like caffeine but with a low adenosine antagonistic potency did not affect the normal synaptic transmission or the effect of forskolin at a lower concentration (10 microM)."( Promotion of forskolin-induced long-term potentiation of synaptic transmission by caffeine in area CA1 of the rat hippocampus.
Gean, PW; Lu, KT; Wu, SP, 1999
)
1.02
"Enprofylline has a short half-life in children, but the sustained-release formulation provides stable serum concentrations and satisfactory relief of asthma throughout the 12-hour dosing interval."( Pharmacokinetics of enprofylline administered intravenously and as a sustained-release tablet at steady state in children with asthma.
Simons, FE; Simons, KJ; Watson, WT, 1988
)
1.32

Toxicity

ExcerptReferenceRelevance
" We conclude that the emetic side effect of xanthine bronchodilators results from the inhibition of one or more forms of PDE rather than from adenosine antagonism."( Mechanism for the emetic side effect of xanthine bronchodilators.
Howell, RE; Kinnier, WJ; Muehsam, WT, 1990
)
0.28
" In addition, we assessed the risk of adverse events by normalising data on safety as a function of person-weeks."( Efficacy and safety profile of xanthines in COPD: a network meta-analysis.
Barnes, PJ; Calzetta, L; Cazzola, M; Criner, GJ; Gabriella Matera, M; Martinez, FJ; Papi, A, 2018
)
0.48

Pharmacokinetics

The pharmacokinetic characteristics, peritoneal permeability and hydrophobicity of three xanthine derivatives, theophylline, enprofylline and 1-methyl-3-propylxanthine (MPX) were investigated in rats. Significant differences were observed between nonpregnant rats and pregnant rats on the 20th day of gestation.

ExcerptReferenceRelevance
" The possibility of an interspecies pharmacokinetic scale was also evaluated."( Interspecies differences and scaling for the pharmacokinetics of xanthine derivatives.
Hasegawa, T; Nabeshima, T; Nadai, M; Takagi, K; Tsunekawa, Y, 1992
)
0.28
" Significant differences in the pharmacokinetic parameters of enprofylline were observed between nonpregnant rats and pregnant rats on the 20th day of gestation: volume of distribution was higher, and systemic clearance was lower in pregnant rats."( Pharmacokinetics and renal handling of enprofylline in pregnant rats.
Hasegawa, T; Kato, K; Muraoka, I; Nabeshima, T; Nadai, M,
)
0.64
" The pharmacokinetic parameters were estimated by model-independent methods."( Dose-dependent pharmacokinetics of enprofylline and its renal handling in rats.
Hasegawa, T; Muraoka, I; Nabeshima, T; Nadai, M; Takagi, K, 1991
)
0.56
" The mean plasma half-life of enprofylline (1."( Enprofylline pharmacokinetics in children with asthma.
Borgå, O; Hultqvist, C, 1987
)
2
" In the patients the plasma half-life was prolonged and the total and renal clearances were reduced in direct proportion to the degree of renal insufficiency as determined by scanning clearance."( Pharmacokinetics of enprofylline in patients with impaired renal function after a single intravenous dose.
Borgå, O; Larsson, R; Lunell, E, 1984
)
0.59
" Pharmacokinetic parameters for both total and unbound enprofylline were estimated by model-independent methods."( Alterations in the pharmacokinetics and protein binding of enprofylline in Eisai hyperbilirubinemic rats.
Hasegawa, T; Nabeshima, T; Nadai, M; Tagaya, O; Wang, L,
)
0.62
" The pharmacokinetic parameters of enprofylline were determined by a model-independent method."( Time-dependent changes in the pharmacokinetics and renal excretion of xanthine derivative enprofylline induced by bacterial endotoxin in rats.
Haghgoo, S; Hasegawa, T; Kato, N; Nabeshima, T; Nadai, M; Wang, L, 1995
)
0.79
"The pharmacokinetic characteristics, peritoneal permeability and hydrophobicity of three xanthine derivatives, theophylline, enprofylline and 1-methyl-3-propylxanthine (MPX), were investigated in rats."( Structure-related pharmacokinetics of xanthines after direct administration into the peritoneal cavity of rats.
Hasegawa, T; Kuzuya, T; Nabeshima, T; Shiraki, R, 1997
)
0.5
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Compound-Compound Interactions

The haemodynamic response to two xanthines, enprofylline and theophylline, was studied in 6 healthy male volunteers at rest, during exercise and in combination with the beta 2-agonist terbutaline.

ExcerptReferenceRelevance
"Long-term ambulatory Holter-monitoring was used to evaluate the arrhythmogenic effects of beta 2-agonist therapy, alone and in combination with a xanthine derivative, theophylline or enprofylline."( Cardiac arrhythmias in patients with mild-to-moderate obstructive lung disease. Comparison of beta-agonist therapy alone and in combination with a xanthine derivative, enprofylline or theophylline.
Conradson, TB; Eklundh, G; Olofsson, B; Pahlm, O; Persson, G, 1985
)
0.66
"The haemodynamic response to two xanthines, enprofylline and theophylline, was studied in 6 healthy male volunteers at rest, during exercise and in combination with the beta 2-agonist, terbutaline."( Cardiovascular effects of two different xanthines in healthy subjects. Studies at rest, during exercise and in combination with a beta-agonist, terbutaline.
Conradson, TB, 1984
)
0.53

Bioavailability

ExcerptReferenceRelevance
" An oral dose (5 mg/kg) of enprofylline to rats was almost completely recovered in the urine as unchanged drug, showing that this xanthine is well absorbed and negligibly metabolised."( Tracheal relaxant and cardiostimulant actions of xanthines can be differentiated from diuretic and CNS-stimulant effects. Role of adenosine antagonism?
Edholm, LE; Erjefält, I; Karlsson, JA; Lamm, CJ; Persson, CG, 1982
)
0.56
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

A double-blind crossover study has been performed in 14 patients with moderately severe chronic asthma to compare the bronchodilator efficacy. The dosage of enprofylline in children would be more accurate if calculated in proportion to surface area rather than to body weight.

ExcerptRelevanceReference
" A beta 1-pattern was seen in both regions when lipolysis dose-response curves were arranged in order of potency."( Mechanisms for differences in lipolysis between human subcutaneous and omental fat cells.
Arner, P; Hellmér, J; Marcus, C; Sonnenfeld, T, 1992
)
0.28
" Dose-response measurements with tissues from intact or sympathectomized (6-OHDA) animals indicate that the thermogenic effects of low concentrations of ephedrine and also of caffeine are entirely dependent upon the presence of intact sympathetic nerve endings, and thus depend on presynaptic mechanisms."( Peripheral mechanisms of thermogenesis induced by ephedrine and caffeine in brown adipose tissue.
Dulloo, AG; Girardier, L; Seydoux, J, 1991
)
0.28
"The effect of dosage on the pharmacokinetics of the potent bronchodilator enprofylline (3-propylxanthine; PX) and its renal handling were investigated in rats."( Dose-dependent pharmacokinetics of enprofylline and its renal handling in rats.
Hasegawa, T; Muraoka, I; Nabeshima, T; Nadai, M; Takagi, K, 1991
)
0.79
" Theophylline was administered in identical doses, except that the final dosage increase was not made if plasma theophylline was 12 mg/ml or higher."( A comparison of enprofylline and theophylline in the maintenance therapy of chronic reversible obstructive airway disease.
Abboud, RT; Boucher, S; Chapman, KR; Day, A; Hodder, RV; Hyland, RH; Kreisman, H; Peters, S; Rivington, R; York, EL, 1990
)
0.63
" Neither xanthine shifted the calcium dose-response when PMNs were activated with calcium ionophore."( Therapeutic concentrations of theophylline and enprofylline potentiate catecholamine effects and inhibit leukocyte activation.
Crowley, JJ; Cusack, BJ; Nielson, CP; Vestal, RE, 1986
)
0.53
" The mean increase in morning PEFR 12 h after dosing was: for 450 mg, 14(17)%; for 300 mg, 8(23)%; for 150 mg, 2(11)%, for placebo 0(10)%."( A placebo-controlled dose-response study of enprofylline in the maintenance therapy of asthma.
Bryant, D; Chapman, KR; Inouye, T; Koskinen, S; Marlin, GE; Mitchell, C; Osen, SS; Pedersen, B; Ringdal, N; Ruffin, R, 1989
)
0.54
"A double-blind crossover study has been performed in 14 patients with moderately severe chronic asthma to compare the bronchodilator efficacy of two dosage regimens of intravenous enprofylline (high dose = 2 mg/kg bolus and 1 mg/kg/hour infusion; low dose = 1 mg/kg bolus and 500 micrograms/kg/hour infusion) with aminophylline (5 mg/kg/bolus and 500 micrograms/kg/hour infusion) and placebo."( Enprofylline in chronic asthma.
Capewell, S; Chapman, BJ; Crompton, GK; Frame, MH; McDonald, C, 1988
)
1.91
" Apart from clinical situations where effective dosages of drugs must be administered rapidly, the method showed be useful in pharmacological dose-response studies."( Creation of four consecutive instantaneous steady-state plasma concentration plateaus of theophylline and enprofylline by repeated infusions with exponentially decreasing delivery rates.
Borgström, L; de Noord, OE; Jonkman, JH; Koëter, GH; Kraan, J; Laseur, M, 1988
)
0.49
"3 mg/kg given as a sustained-release tablet after 8 days of oral dosing twice daily."( Pharmacokinetics of enprofylline administered intravenously and as a sustained-release tablet at steady state in children with asthma.
Simons, FE; Simons, KJ; Watson, WT, 1988
)
0.6
" The dosage of enprofylline in children would be more accurate if calculated in proportion to surface area rather than to body weight."( Enprofylline pharmacokinetics in children with asthma.
Borgå, O; Hultqvist, C, 1987
)
2.07
" The dose-response relationships of theophylline and enprofylline were studied on these preparations."( Potent bronchodilating effects of enprofylline and theophylline on contractions induced by egg albumin or by slow reacting substance (SRS).
Andersson, RG; Hedman, SE, 1984
)
0.8
" The dosage of each xanthine was incremented from 150 mg twice daily at initiation to 300 and later 450 mg twice daily depending on the patient's tolerance and, in the case of theophylline, the rapidly assayed serum theophylline level."( Long-term xanthine therapy of asthma. Enprofylline and theophylline compared. International Enprofylline Study Group.
Chapman, KR; Kallen, A; Ljungholm, K, 1994
)
0.56
" When compounds were intraduodenally administered to the guinea pig, 1-(2'-ethoxyethyl)-, 1-(3'-methoxypropyl)-, 1-(3'-butenyl)-, and 1-[(dimethylamino)-ethyl]-3-propylxanthines, 1-methyl-7-(2'-oxopropyl)-3-propylxanthine, and denbufylline (1,3-di-n-butyl-7-(2'-oxopropyl)xanthine) effectively inhibited the acetylcholine-induced bronchospasm without heart stimulation or central nervous system-stimulation at the effective dosage range."( Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
Hasegawa, T; Iwasaki, N; Konno, K; Kurita, M; Miyamoto, K; Ohshima, T; Sakai, R; Sanae, F; Takagi, K; Yamamoto, Y, 1993
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
bronchodilator agentAn agent that causes an increase in the expansion of a bronchus or bronchial tubes.
anti-asthmatic drugA drug used to treat asthma.
anti-arrhythmia drugA drug used for the treatment or prevention of cardiac arrhythmias. Anti-arrhythmia drugs may affect the polarisation-repolarisation phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibres.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
oxopurine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (25)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency6.30960.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency6.30960.025120.237639.8107AID886
thioredoxin reductaseRattus norvegicus (Norway rat)Potency3.76860.100020.879379.4328AID488772; AID588456
GLS proteinHomo sapiens (human)Potency31.62280.35487.935539.8107AID624146
regulator of G-protein signaling 4Homo sapiens (human)Potency13.93560.531815.435837.6858AID504845
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency26.83250.000214.376460.0339AID720692
arylsulfatase AHomo sapiens (human)Potency0.15101.069113.955137.9330AID720538
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.19950.540617.639296.1227AID2364; AID2528
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency3.54810.001815.663839.8107AID894
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency23.77810.168316.404067.0158AID720504
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency2.05960.004611.374133.4983AID624297
Cellular tumor antigen p53Homo sapiens (human)Potency1.18830.002319.595674.0614AID651631
TAR DNA-binding protein 43Homo sapiens (human)Potency35.48131.778316.208135.4813AID652104
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency8.49210.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
Adenosine receptor A3Homo sapiens (human)Ki125.30000.00000.930610.0000AID266274; AID372140
Adenosine receptor A1Rattus norvegicus (Norway rat)Ki97.33330.00011.20929.9700AID31860; AID32491; AID372141
Adenosine receptor A3Rattus norvegicus (Norway rat)Ki65.00000.00030.91969.0000AID372144
Adenosine receptor A2aHomo sapiens (human)Ki67.72600.00001.06099.7920AID1871328; AID266273; AID30624; AID30797; AID372138
Adenosine receptor A2bHomo sapiens (human)Ki35.12710.00021.635210.0000AID1289958; AID1428099; AID266271; AID30624; AID30797; AID33176; AID372139
Adenosine receptor A2bRattus norvegicus (Norway rat)Ki124.60000.00061.353610.0000AID30797; AID33434; AID33897
Adenosine receptor A1Homo sapiens (human)Ki43.00000.00020.931610.0000AID266272; AID372137
Adenosine receptor A2aRattus norvegicus (Norway rat)Ki109.16670.00021.494010.0000AID30797; AID33434; AID33897; AID372142
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A2aHomo sapiens (human)EC50 (µMol)7.20000.00030.708110.0000AID74022
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A1Rattus norvegicus (Norway rat)Kb32.00000.00021.73678.7000AID31695
Adenosine receptor A2aRattus norvegicus (Norway rat)Kb120.00000.00071.84855.4000AID7690
Adenosine receptor A2bMus musculus (house mouse)Kb18.00000.00201.05102.1000AID7695
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (263)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo sapiens (human)
synaptic transmission, dopaminergicAdenosine receptor A2aHomo sapiens (human)
response to amphetamineAdenosine receptor A2aHomo sapiens (human)
regulation of DNA-templated transcriptionAdenosine receptor A2aHomo sapiens (human)
phagocytosisAdenosine receptor A2aHomo sapiens (human)
apoptotic processAdenosine receptor A2aHomo sapiens (human)
inflammatory responseAdenosine receptor A2aHomo sapiens (human)
cellular defense responseAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
cell-cell signalingAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, cholinergicAdenosine receptor A2aHomo sapiens (human)
central nervous system developmentAdenosine receptor A2aHomo sapiens (human)
blood coagulationAdenosine receptor A2aHomo sapiens (human)
sensory perceptionAdenosine receptor A2aHomo sapiens (human)
locomotory behaviorAdenosine receptor A2aHomo sapiens (human)
blood circulationAdenosine receptor A2aHomo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A2aHomo sapiens (human)
response to xenobiotic stimulusAdenosine receptor A2aHomo sapiens (human)
response to inorganic substanceAdenosine receptor A2aHomo sapiens (human)
positive regulation of glutamate secretionAdenosine receptor A2aHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionAdenosine receptor A2aHomo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A2aHomo sapiens (human)
response to purine-containing compoundAdenosine receptor A2aHomo sapiens (human)
response to caffeineAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
positive regulation of urine volumeAdenosine receptor A2aHomo sapiens (human)
vasodilationAdenosine receptor A2aHomo sapiens (human)
eating behaviorAdenosine receptor A2aHomo sapiens (human)
negative regulation of vascular permeabilityAdenosine receptor A2aHomo sapiens (human)
negative regulation of neuron apoptotic processAdenosine receptor A2aHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, sleepAdenosine receptor A2aHomo sapiens (human)
negative regulation of alpha-beta T cell activationAdenosine receptor A2aHomo sapiens (human)
astrocyte activationAdenosine receptor A2aHomo sapiens (human)
neuron projection morphogenesisAdenosine receptor A2aHomo sapiens (human)
positive regulation of protein secretionAdenosine receptor A2aHomo sapiens (human)
negative regulation of inflammatory responseAdenosine receptor A2aHomo sapiens (human)
regulation of mitochondrial membrane potentialAdenosine receptor A2aHomo sapiens (human)
membrane depolarizationAdenosine receptor A2aHomo sapiens (human)
regulation of calcium ion transportAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
inhibitory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
prepulse inhibitionAdenosine receptor A2aHomo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2aHomo sapiens (human)
positive regulation of long-term synaptic potentiationAdenosine receptor A2aHomo sapiens (human)
positive regulation of apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
positive regulation of chronic inflammatory response to non-antigenic stimulusAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A2bHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionAdenosine receptor A2bHomo sapiens (human)
positive regulation of cGMP-mediated signalingAdenosine receptor A2bHomo sapiens (human)
cGMP-mediated signalingAdenosine receptor A2bHomo sapiens (human)
positive regulation of chemokine productionAdenosine receptor A2bHomo sapiens (human)
positive regulation of interleukin-6 productionAdenosine receptor A2bHomo sapiens (human)
mast cell degranulationAdenosine receptor A2bHomo sapiens (human)
positive regulation of mast cell degranulationAdenosine receptor A2bHomo sapiens (human)
relaxation of vascular associated smooth muscleAdenosine receptor A2bHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2bHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
vasodilationAdenosine receptor A2bHomo sapiens (human)
temperature homeostasisAdenosine receptor A1Homo sapiens (human)
response to hypoxiaAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system processAdenosine receptor A1Homo sapiens (human)
negative regulation of acute inflammatory responseAdenosine receptor A1Homo sapiens (human)
negative regulation of leukocyte migrationAdenosine receptor A1Homo sapiens (human)
positive regulation of peptide secretionAdenosine receptor A1Homo sapiens (human)
positive regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
negative regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
regulation of glomerular filtrationAdenosine receptor A1Homo sapiens (human)
protein targeting to membraneAdenosine receptor A1Homo sapiens (human)
phagocytosisAdenosine receptor A1Homo sapiens (human)
inflammatory responseAdenosine receptor A1Homo sapiens (human)
signal transductionAdenosine receptor A1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
cell-cell signalingAdenosine receptor A1Homo sapiens (human)
nervous system developmentAdenosine receptor A1Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A1Homo sapiens (human)
response to inorganic substanceAdenosine receptor A1Homo sapiens (human)
negative regulation of glutamate secretionAdenosine receptor A1Homo sapiens (human)
response to purine-containing compoundAdenosine receptor A1Homo sapiens (human)
lipid catabolic processAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicAdenosine receptor A1Homo sapiens (human)
positive regulation of nucleoside transportAdenosine receptor A1Homo sapiens (human)
negative regulation of neurotrophin productionAdenosine receptor A1Homo sapiens (human)
positive regulation of protein dephosphorylationAdenosine receptor A1Homo sapiens (human)
vasodilationAdenosine receptor A1Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, non-REM sleepAdenosine receptor A1Homo sapiens (human)
negative regulation of apoptotic processAdenosine receptor A1Homo sapiens (human)
positive regulation of potassium ion transportAdenosine receptor A1Homo sapiens (human)
positive regulation of MAPK cascadeAdenosine receptor A1Homo sapiens (human)
negative regulation of hormone secretionAdenosine receptor A1Homo sapiens (human)
cognitionAdenosine receptor A1Homo sapiens (human)
leukocyte migrationAdenosine receptor A1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
positive regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
regulation of sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergicAdenosine receptor A1Homo sapiens (human)
fatty acid homeostasisAdenosine receptor A1Homo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A1Homo sapiens (human)
long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
mucus secretionAdenosine receptor A1Homo sapiens (human)
negative regulation of mucus secretionAdenosine receptor A1Homo sapiens (human)
triglyceride homeostasisAdenosine receptor A1Homo sapiens (human)
regulation of cardiac muscle cell contractionAdenosine receptor A1Homo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic potentiationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (57)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aHomo sapiens (human)
protein bindingAdenosine receptor A2aHomo sapiens (human)
calmodulin bindingAdenosine receptor A2aHomo sapiens (human)
lipid bindingAdenosine receptor A2aHomo sapiens (human)
enzyme bindingAdenosine receptor A2aHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingAdenosine receptor A2aHomo sapiens (human)
identical protein bindingAdenosine receptor A2aHomo sapiens (human)
protein-containing complex bindingAdenosine receptor A2aHomo sapiens (human)
alpha-actinin bindingAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2bHomo sapiens (human)
protein bindingAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor activityAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor bindingAdenosine receptor A1Homo sapiens (human)
purine nucleoside bindingAdenosine receptor A1Homo sapiens (human)
protein bindingAdenosine receptor A1Homo sapiens (human)
heat shock protein bindingAdenosine receptor A1Homo sapiens (human)
G-protein beta/gamma-subunit complex bindingAdenosine receptor A1Homo sapiens (human)
heterotrimeric G-protein bindingAdenosine receptor A1Homo sapiens (human)
protein heterodimerization activityAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (51)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
intermediate filamentAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
membraneAdenosine receptor A2aHomo sapiens (human)
dendriteAdenosine receptor A2aHomo sapiens (human)
axolemmaAdenosine receptor A2aHomo sapiens (human)
asymmetric synapseAdenosine receptor A2aHomo sapiens (human)
presynaptic membraneAdenosine receptor A2aHomo sapiens (human)
neuronal cell bodyAdenosine receptor A2aHomo sapiens (human)
postsynaptic membraneAdenosine receptor A2aHomo sapiens (human)
presynaptic active zoneAdenosine receptor A2aHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2bHomo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A2bHomo sapiens (human)
presynapseAdenosine receptor A2bHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2bHomo sapiens (human)
plasma membraneAdenosine receptor A2bHomo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
basolateral plasma membraneAdenosine receptor A1Homo sapiens (human)
axolemmaAdenosine receptor A1Homo sapiens (human)
asymmetric synapseAdenosine receptor A1Homo sapiens (human)
presynaptic membraneAdenosine receptor A1Homo sapiens (human)
neuronal cell bodyAdenosine receptor A1Homo sapiens (human)
terminal boutonAdenosine receptor A1Homo sapiens (human)
dendritic spineAdenosine receptor A1Homo sapiens (human)
calyx of HeldAdenosine receptor A1Homo sapiens (human)
postsynaptic membraneAdenosine receptor A1Homo sapiens (human)
presynaptic active zoneAdenosine receptor A1Homo sapiens (human)
synapseAdenosine receptor A1Homo sapiens (human)
dendriteAdenosine receptor A1Homo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (87)

Assay IDTitleYearJournalArticle
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID33176Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID266272Displacement of [3H]CPX from human adenosine A3 receptor expressed in CHO cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID219846Inhibition of c-AMP phosphodiesterase activity in guinea pig tracheal muscle1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
AID220054Inhibition of cyclic AMP-phosphodiesterase ( PDE) in the supernatant of tracheal muscle homogenate1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID32155Affinity against adenosine A1 receptor in the brain membranes by the displacement of [3H]CPX.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
AID372144Binding affinity to rat adenosine A3 receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID372139Binding affinity to human adenosine A2B receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID32491Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
AID75916Effective concentration required in vitro for heart stimulation (right atrium) in guinea pig1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
AID372138Binding affinity to human adenosine A2A receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID30807Binding affinity against Adenosine A2 receptor in rat striatal membranes using [3H]5'-(N-ethylcarboxamido)-adenosine (NECA) as the ligand1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors.
AID266274Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.
AID227877Ratio of stimulatory activity in right atrium to relaxant activity in tracheal muscle1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
AID223359In vivo positive chronotropic effect on isolated guinea pig right atrium1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID31860Binding affinity for Adenosine A1 receptor from rat brain using [3H]-PIA as radioligand1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Imidazodiazepinediones: a new class of adenosine receptor antagonists.
AID31695Inhibition against Adenosine A1 receptor of rat fat cell membranes2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
AID223360In vivo reduction of acetylcholine-induced bronchospasm in guinea pigs by intraduodenal dose1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
AID266271Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.
AID75917Positive chronotropic effect on isolated guinea pig right atrium (heart stimulation).1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
AID31881Binding affinity at Adenosine A1 receptor in rat brain cortical membrane using [3H]N6-R-phenylisopropyladenosine (R-PIA) as radioligand1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors.
AID1428099Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay2017European journal of medicinal chemistry, Feb-15, Volume: 127A
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID372141Binding affinity to rat adenosine A1 receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID30500Affinity against adenosine A2 receptor in the brain membranes measured by the displacement of [3H]-CPX1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
AID30797Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via adenosine A2 receptor in human platelet membranes.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID233055Bronchoselectivity expressed as ratio of stimulatory activity in the right atrium (EC15) to relaxant activity in the tracheal muscle (EC50)1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
AID32159Binding affinity against adenosine A1 receptor of cerebral cortex using [3H]CPX as a radioligand1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
AID7695Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
AID372137Binding affinity to human adenosine A1 receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID33434Binding affinity for Adenosine A2 receptor from rat striatum using [3H]NECA as radioligand1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Imidazodiazepinediones: a new class of adenosine receptor antagonists.
AID453203Lipophilicity, log D of the compound2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID74022Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
AID33897Antagonism of N-ethylcarboxamido adenosine-stimulated adenylate cyclase associated with stimulation of Adenosine A2 receptor of rat PC12 membranes1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Imidazodiazepinediones: a new class of adenosine receptor antagonists.
AID30624Binding affinity against adenosine A2 receptor of striatal membrane using [3H]CGS-21680 as a radioligand1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
AID233052Bronchoselectivity, ratio of positive chronotropic action (ED15) to bronchodilator action (ED50)1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
AID73739Effective concentration required in vitro for tracheal muscle (from male Hartley guinea pigs) relaxation1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
AID221857Positive chronotropic effect, 15% increase in heart rate of male Hartley guinea pigs on intraduodenal administration (mean of 3-5 animals)1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
AID1289958Displacement of [3H]DPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID372142Binding affinity to rat adenosine A2A receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID372140Binding affinity to human adenosine A3 receptor2009Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
AID453204Permeability in human skin after 48 hrs by Franz cell permeability assay2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay.
AID1871328Antagonist activity at adenosine A2A receptor (unknown origin)2022European journal of medicinal chemistry, Jan-05, Volume: 227Adenosine receptor antagonists: Recent advances and therapeutic perspective.
AID221859Bronchodilatory effect, 50% inhibition of spasmogen-induced response in male Hartley guinea pigs on intraduodenal administration1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
AID7690Inhibition against A2A-Adenosine Receptor of rat PC12 cell membranes2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
AID266273Displacement of [3H]ZM-241385 from human adenosine A2a receptor expressed in HEK cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (212)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990114 (53.77)18.7374
1990's56 (26.42)18.2507
2000's21 (9.91)29.6817
2010's14 (6.60)24.3611
2020's7 (3.30)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.34

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index23.34 (24.57)
Research Supply Index5.57 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.34)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials41 (18.64%)5.53%
Reviews11 (5.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other168 (76.36%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]