Page last updated: 2024-11-07

xamoterol

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Description

Xamoterol: A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID155774
CHEMBL ID75753
CHEBI ID10055
SCHEMBL ID64461
MeSH IDM0026277

Synonyms (69)

Synonym
chebi:10055 ,
ici-118,587
CHEMBL75753
gtpl538
BSPBIO_000826
ici-118587
LOPAC0_001259
BPBIO1_000910
PRESTWICK2_000923
xamoterol (usan)
D06328
PRESTWICK3_000923
AB00514723
81801-12-9
xamoterol
NCGC00024897-03
xamoterolum [latin]
(+-)-n-(2-((2-hydroxy-3-(p-hydroxyphenoxy)propyl)amino)ethyl)-4-morpholinecarboxamide
4-morpholinecarboxamide, n-(2-((2-hydroxy-3-(4-hydroxyphenoxy)propyl)amino)ethyl)-, (+-)-
SPBIO_003005
PRESTWICK0_000923
PRESTWICK1_000923
NCGC00024897-02
HMS2089I13
L000630
n-[2-[[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]morpholine-4-carboxamide
NCGC00016099-04 ,
7he0jql703 ,
unii-7he0jql703
xamoterolum
xamoterol [usan:inn:ban]
dtxcid6025222
dtxsid8045222 ,
cas-81801-12-9
tox21_110304
CCG-205333
n-(2-((2-hydroxy-3-(4-hydroxyphenoxy)propyl)amino)ethyl)morpholine-4-carboxamide
AM806653
NCGC00016099-03
NCGC00016099-05
xamoterol [usan]
(+/-)-n-(2-((2-hydroxy-3-(p-hydroxyphenoxy)propyl)amino)ethyl)-4-morpholinecarboxamide
xamoterol [mi]
4-morpholinecarboxamide, n-(2-((2-hydroxy-3-(4-hydroxyphenoxy)propyl)amino)ethyl)-, (+/-)-
xamoterol [who-dd]
xamoterol [inn]
SCHEMBL64461
n-(2-((2-hydroxy-3-(4-hydroxyphenoxy)propyl)amino)ethyl)-4-morpholinecarboxamide
DXPOSRCHIDYWHW-UHFFFAOYSA-N
AB00514723-05
xamoterolhemifumarate
(+/-)-n-[2-[[hydroxy-3-(4-hydroxy)propyl]amino]ethyl-4-morpholinecarboxamide hemifumarate salt
AKOS027420460
sr-01000075155
SR-01000075155-1
n-(2-(2-hydroxy-3-(4-hydroxyphenoxy)propylamino)ethyl)morpholine-4-carboxamide
SR-01000075155-3
DB13781
bdbm50248358
FT-0717367
Q4021708
69630-08-6
ici 118587; ici-118587; ici118587; xamoterol hemifumarate; xamtol
xamoterol (fumarate)
SB50140
EN300-18457256
n-(2-{[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino}ethyl)morpholine-4-carboxamide
HY-101327
CS-0021161

Research Excerpts

Overview

Xamoterol acts as a beta 1-adrenoceptor agonist at low sympathetic activity and as an antagonist at high activity. It reduces myocardial ischaemia and improves ventricular function in patients with mild to moderate heart failure.

ExcerptReferenceRelevance
"Xamoterol is a new orally active partial beta-adrenoceptor agonist. "( Cardioselectivity, kinetics, hemodynamics, and metabolic effects of xamoterol.
Bobik, A; Jennings, G; Oddie, C; Restall, R, 1984
)
1.95
"Xamoterol is a partial beta-1 adrenergic agonist capable of stabilising the beta-1 receptor to 43% of their maximal activity. "( [The value of xamoterol in moderate ischemic cardiac insufficiency].
Cheron, P; Lavenne, F; Pouleur, H; Rousseau, MF; Vincent, MF,
)
1.93
"Xamoterol showed to be a beta-adrenergic receptors agonist in long-term chagasic patients with sinus node dysfunction at rest, when the simpatic tone was low, with evident action on the electrophysiologic parameters."( [Acute electrophysiologic and echocardiographic changes induced by xamoterol in chronic chagasic patients with sinus node dysfunction].
Ladeira, R; Pimenta, J; Tosta, C, 1993
)
1.96
"Xamoterol acts as a beta 1-adrenoceptor agonist at low sympathetic activity and as an antagonist at high activity. "( Predominant beta-adrenoceptor blocking effect of xamoterol averaged over the day in patients with mild to moderate heart failure: insight into the mechanism of its long-term clinical efficacy.
Hori, M; Imai, K; Inoue, M; Kamada, T; Kitabatake, A; Matsuyama, T; Ozaki, H; Sato, H; Yokoyama, H, 1992
)
1.98
"Xamoterol is a novel partial agonist of beta 1 adrenoceptors that reduces myocardial ischaemia and improves ventricular function in patients with mild to moderate heart failure. "( Effects of xamoterol in acute myocardial infarction: blood pressure, heart rate, arrhythmias and early clinical course.
Lang, CC; MacLean, D; McDevitt, DG; McMurray, J; Struthers, AD, 1991
)
2.11
"Xamoterol is a partial beta 1-adrenergic agonist that has combined beta 1-stimulating and beta 1-blocking actions. "( Effects of the partial beta 1-adrenergic agonist, xamoterol, on hemodynamics and regional myocardial function during acute coronary occlusion in dogs.
Katayama, K; Kohno, M; Kumada, T; Kusukawa, R; Matsuzaki, M; Miura, T; Ozaki, M; Toma, Y; Yonezawa, F, 1990
)
1.97
"Xamoterol would appear to be a suitable and safe drug in the therapy of mild to moderate heart failure."( Exercise capacity, arrhythmias, humoral and chemical parameters during long-term therapy with xamoterol.
Bleifeld, W; Erlemeier, HH; Kupper, W, 1990
)
1.22
"Xamoterol is a beta-1 selective partial adrenoceptor agonist. "( [Hemodynamic and humoral changes following intravenous administration of xamoterol in patients with heart failure and coronary heart disease].
Bleifeld, W; Erlemeier, HH; Kupper, W, 1990
)
1.95
"Xamoterol is a beta 1-selective adrenoceptor partial agonist. "( Sympathetic modulation in practice: the German clinical experience.
Bleifeld, W; Erlemeier, HH; Kupper, W, 1990
)
1.72
"Xamoterol is a selective partial beta-adrenoceptor agonist. "( Lack of tolerance development after long-term administration of the partial beta-adrenoceptor agonist xamoterol.
Bleifeld, W; Erlemeier, HH; Kupper, W, 1990
)
1.94
"Xamoterol is a beta-adrenoceptor partial agonist which selectively acts at the beta 1-receptors of the heart. "( Selective beta-1-adrenoceptor partial agonist treatment for congestive heart failure.
Shabetai, R, 1990
)
1.72
"6. Xamoterol is a promising, well-tolerated addition to established therapies for chronic mild or moderate heart failure."( Long-term studies with xamoterol in heart failure.
Waller, DG, 1989
)
1.1
"Xamoterol is a partial beta 1 adrenoceptor agonist with positive inotropic properties. "( Digoxin and xamoterol in patients with moderate chronic heart failure. A double-blind, randomized, controlled study.
Andersen, MF; Faergeman, O; Sorensen, EV; Sterndorff, B, 1989
)
2.1
"Xamoterol seems to be a useful alternative in the treatment of postural hypotension."( Xamoterol, a new selective beta-1-adrenoceptor partial agonist, in the treatment of postural hypotension.
Mehlsen, J; Trap-Jensen, J, 1986
)
2.44
"1. Xamoterol is a cardioselective beta-adrenoceptor partial agonist which may have a role in the management of cardiac failure. "( The effect of age and cardiac failure on xamoterol pharmacokinetics.
Bastain, W; Petrie, JC; Scott, AK; Webster, J, 1988
)
1.16
"Xamoterol is a partial agonist at the beta 1-adrenoceptor. "( Xamoterol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use.
Brogden, RN; Furlong, R, 1988
)
3.16

Effects

Xamoterol has been shown to reduce the frequency of oedema and lung crepitations in heart failure. It has been administered both intravenously and orally over a 100-fold dose range to male beagle dogs.

ExcerptReferenceRelevance
"Xamoterol has a phenolic hydroxyl group at which both sulphation and glucuronidation may occur. "( Pharmacokinetics of xamoterol glucuronidation in the rat in vivo and in liver perfusion.
Groen, K; Meijer, DK; Mulder, GJ; Tijdens, RB, 1987
)
2.04
"Xamoterol has been shown in large, double-blind studies to produce benefit in patients with heart failure. "( Xamoterol in mild to moderate heart failure: a subgroup analysis of patients with cardiomegaly but no concomitant angina pectoris.
, 1989
)
3.16
"Xamoterol has been shown to reduce the frequency of oedema and lung crepitations in heart failure. "( Effects of xamoterol on sodium excretion in volunteers.
Day, MA; Hadj-Aissa, A; Madonna, O; Pozet, N; Snow, HM; Zech, PY, 1989
)
2.11
"Xamoterol has a phenolic hydroxyl group at which both sulphation and glucuronidation may occur. "( Pharmacokinetics of xamoterol glucuronidation in the rat in vivo and in liver perfusion.
Groen, K; Meijer, DK; Mulder, GJ; Tijdens, RB, 1987
)
2.04
"1. Xamoterol has been administered both intravenously and orally over a 100-fold dose range to male beagle dogs. "( Sulphation and glucuronidation of xamoterol in the dog: dose dependence and site of sulphation.
Booth, BS; Groen, K; Miles, GS; Mulder, GJ; Warrander, A, 1988
)
1.18

Actions

Xamoterol did not enhance arrhythmias during 24-hour ambulatory Holter monitoring. The drug did not produce a noteworthy decrease in heart rate or positive dp/dtmax during exercise, even at a dosage of 1 mg/kg.

ExcerptReferenceRelevance
"Xamoterol did not enhance arrhythmias during 24-hour ambulatory Holter monitoring."( Exercise capacity, arrhythmias, humoral and chemical parameters during long-term therapy with xamoterol.
Bleifeld, W; Erlemeier, HH; Kupper, W, 1990
)
1.22
"Xamoterol did not cause any detectable agonist effect but was well tolerated under basal conditions."( [Noninvasive evaluation of partial beta adrenergic agonist properties of xamoterol in cardiac insufficiency].
Fournier, P; Fraysse, JB; Grosgogeat, Y; Komajda, M; Landault, C; Lechat, P; Richaud, M, 1990
)
1.23
"Xamoterol did not produce a noteworthy decrease in heart rate or positive dp/dtmax during exercise, even at a dosage of 1 mg/kg."( Haemodynamic and metabolic effects of xamoterol in exercising dogs.
Ehrendorfer, S; Fischer, G; Grohs, JG; Raberger, G; Schneider, W, 1990
)
1.27
"Xamoterol may increase sodium excretion by an action on renal haemodynamics."( Effects of xamoterol on sodium excretion in volunteers.
Day, MA; Hadj-Aissa, A; Madonna, O; Pozet, N; Snow, HM; Zech, PY, 1989
)
1.39

Treatment

Treatment with xamoterol and digoxin was compared in 19 patients with cardiac failure (NYHA class II-III) Treatment with x amoterol did not affect this noradrenaline response to myocardial infarction. Both xamotersol and combined treatment reduced the increase in CO (-4.6 l.min-1 after xamotorol and -3.4 l. min-1 following combined treatment)

ExcerptReferenceRelevance
"Both xamoterol and combined treatment reduced the increase in CO (-4.6 l.min-1 after xamoterol and -3.4 l.min-1 after combined treatment vs."( Lack of pharmacodynamic interactions between acute dose flosequinan and xamoterol. A pilot study in healthy subjects.
Breckenridge, AM; Ng, HW; Tsao, Y; Walley, TJ, 1994
)
0.98
"Treatment with xamoterol raised supine systolic blood pressure by 11 mmHg but a reduced standing systolic blood pressure by 11 mmHg with an increase in the standing-supine systolic blood pressure difference."( A double-blind crossover study of oral xamoterol in postural hypotension due to diabetic autonomic neuropathy.
Clarke, BF; Ewing, DJ; Leslie, PJ; Thompson, C, 1991
)
0.89
"Treatment with xamoterol did not affect this noradrenaline response to myocardial infarction."( Neuroendocrine changes post myocardial infarction: effects of xamoterol.
Lang, CC; MacLean, D; McDevitt, DG; McMurray, JJ; Struthers, AD, 1990
)
0.86
"Treatment with xamoterol and digoxin was compared in 19 patients with cardiac failure (NYHA class II-III)."( Digoxin and xamoterol in patients with moderate chronic heart failure. A double-blind, randomized, controlled study.
Andersen, MF; Faergeman, O; Sorensen, EV; Sterndorff, B, 1989
)
1

Toxicity

ExcerptReferenceRelevance
" There were no adverse effects."( The efficacy and safety of chronic oral administration of xamoterol to patients with severe heart failure treated with ACE inhibitors.
Hanet, C; Pouleur, H; Rousseau, MF, 1989
)
0.52

Pharmacokinetics

ExcerptReferenceRelevance
" A small increase in the terminal plasma elimination half-life (t1/2) was observed in patients when compared with controls (15."( The pharmacokinetics of xamoterol in liver disease.
Bastain, W; McCann, JP; Nicholls, DP; Shanks, RG; Taggart, AJ, 1989
)
0.58
"The possible cardiovascular pharmacodynamic interactions at rest and during exercise of combining oral flosequinan (100 mg) with xamoterol (200 mg) was investigated in a four-way randomised double-blind placebo-controlled crossover trial in eight healthy male volunteers."( Lack of pharmacodynamic interactions between acute dose flosequinan and xamoterol. A pilot study in healthy subjects.
Breckenridge, AM; Ng, HW; Tsao, Y; Walley, TJ, 1994
)
0.73
" 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

Bioavailability

After oral doses, the absolute bioavailability of xamoterol was shown to be 5% irrespective of whether the dose was administered as a tablet or solution.

ExcerptReferenceRelevance
" The low bioavailability of xamoterol was confirmed (6."( The pharmacokinetics of xamoterol in liver disease.
Bastain, W; McCann, JP; Nicholls, DP; Shanks, RG; Taggart, AJ, 1989
)
0.88
" After oral doses, the absolute bioavailability of xamoterol was shown to be 5% irrespective of whether the dose was administered as a tablet or solution."( Pharmacokinetics of xamoterol after intravenous and oral administration to volunteers.
Bastain, W; Boyce, MJ; Clarke, DA; Marlow, HF; Morton, PB; Stafford, LE, 1988
)
0.85
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"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

Xamoterol did not produce a noteworthy decrease in heart rate or positive dp/dtmax during exercise, even at a dosage of 1 mg/kg. The magnitude of the inotropic response was reduced during beta 1-stimulation in patients with an ejection fraction less than or equal to 35%.

ExcerptRelevanceReference
" Examination of the dosing regimen used, however, suggests that insufficient daily dosage of captopril or the inadequate schedule of administration, or both, might be responsible for different degrees of angiotensin-converting enzyme inhibition between the enalapril and captopril groups and hence for the difference in mortality."( Difference in mortality between patients treated with captopril or enalapril in the Xamoterol in Severe Heart Failure Study.
Oakley, C; Pouleur, H; Rousseau, MF; Rydén, L, 1991
)
0.51
" To determine if these hemodynamic changes were maintained after prolonged administration, the dose-response relation to cumulative doses of xamoterol was determined in a group of 14 patients with mild (n = 6)-to-serve (n = 8) ischemic left ventricular dysfunction."( Effects of the beta 1-adrenergic receptor partial agonist xamoterol on left ventricular diastolic function. An evaluation after 1-6 years of oral therapy.
Etienne, J; Gurné, O; Pouleur, H; Rousseau, MF; Van Mechelen, H, 1990
)
0.72
" Maximum decreases in QS2I were noted 1 to 2 h after dosing and were achieved with a dose of 100 mg."( The effect of oral dosing of xamoterol on systolic time intervals in man and xamoterol plasma concentrations in heart failure patients.
Barker, NP; Bastain, W; Channer, KS; Harry, JD; James, MA; Jones, JV; Marlow, HF; Papouchado, M; Wardleworth, AG, 1990
)
0.57
" Xamoterol did not produce a noteworthy decrease in heart rate or positive dp/dtmax during exercise, even at a dosage of 1 mg/kg."( Haemodynamic and metabolic effects of xamoterol in exercising dogs.
Ehrendorfer, S; Fischer, G; Grohs, JG; Raberger, G; Schneider, W, 1990
)
1.46
" These results contrast with those obtained with other beta-adrenoceptor drugs, prenalterol and pirbuterol which were unsuccessful on chronic dosing (Currie et al."( The pharmacology of xamoterol: a basis for modulation of the autonomic control of the heart.
Snow, HM, 1989
)
0.6
" The dose-response curves to cumulative doses of xamoterol, a beta 1-adrenoceptor partial agonist, confirmed that the magnitude of the inotropic response was reduced during beta 1-stimulation in patients with an ejection fraction less than or equal to 35% when compared with patients with a greater ejection fraction."( Left ventricular sensitivity to beta-adrenoceptor-stimulating drugs in patients with ischemic heart disease and varying degrees of ventricular dysfunction.
Charlier, AA; Hanet, C; Marlow, HF; Pouleur, H; Rousseau, MF, 1987
)
0.53
" In order to mimic the intrinsic effects of the partial agonist drugs, control dose-response curves for isoproterenol were determined in pithed rats in which the base-line heart rate was elevated by thoracic spinal cord stimulation."( Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol.
Cavero, I; Hicks, PE; Langer, SZ; Lefevre-Borg, F; Manoury, P, 1987
)
0.49
" The relationship of the profile of hormonal suppression seen with enalapril and drug dosage to observed beneficial effects on morbidity or mortality is unclear."( Role of the circulating and tissue-based renin-angiotensin system in the development of heart failure: implications for therapy.
MacFadyen, RJ, 1993
)
0.29
" We have evaluated the effect of subacute dosing with xamoterol, a beta-1 adrenoreceptor partial agonist with inotropic properties, on right ventricular function in patients with PHD."( Xamoterol improves right ventricular systolic and diastolic function in pulmonary heart disease.
Fleming, JS; Oliver, RM; Waller, DG, 1996
)
1.99
" Dose-response curves for the effects of isoprenaline (non selective beta-agonist), salbutamol (beta2-agonist), dobutamine (beta1-agonist) on ICa were obtained in the absence and presence of various concentrations of ICI 118551 (beta2-antagonist), metoprolol (beta1-antagonist) and xamoterol (partial beta1-agonist) to derive EC50 (i."( Pharmacological characterization of the receptors involved in the beta-adrenoceptor-mediated stimulation of the L-type Ca2+ current in frog ventricular myocytes.
Fischmeister, R; Jurevicius, J; Skeberdis, VA, 1997
)
0.47
" These effects were well maintained after chronic dosing with no signs of beta1-adrenoceptor desensitization."( Ketotifen and cardiovascular effects of xamoterol following single and chronic dosing in healthy volunteers.
Brodde, OE; Daul, AE; Karl, I; Mennicke, K; Philipp, T; Schäfers, RF, 1999
)
0.57
") and shifted the dose-response curve for isoprenaline to higher agonist concentrations without altering HVC responses."( Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses.
Baker, JG; Fretwell, L; Gardiner, SM; Hill, SJ; Kemp, P; March, J, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
morpholinesAny compound containing morpholine as part of its structure.
[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 (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GLS proteinHomo sapiens (human)Potency31.62280.35487.935539.8107AID624170
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[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)
Beta-2 adrenergic receptorHomo sapiens (human)EC50 (µMol)0.70790.00000.311110.0000AID739706
Beta-2 adrenergic receptorHomo sapiens (human)Kd1.19920.00000.62888.9130AID739710; AID739713
Beta-1 adrenergic receptorHomo sapiens (human)EC50 (µMol)0.01100.00010.49146.0000AID739708
Beta-1 adrenergic receptorHomo sapiens (human)Kd0.04950.00010.803910.0000AID739711; AID739714
Beta-3 adrenergic receptorHomo sapiens (human)EC50 (µMol)100.00000.00010.455310.0000AID739704
Beta-3 adrenergic receptorHomo sapiens (human)Kd19.95260.00010.76318.9130AID739709
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (83)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
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)
diet induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
regulation of sodium ion transportBeta-2 adrenergic receptorHomo sapiens (human)
transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorHomo sapiens (human)
smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
cell surface receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
endosome to lysosome transportBeta-2 adrenergic receptorHomo sapiens (human)
response to coldBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase A signalingBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of bone mineralizationBeta-2 adrenergic receptorHomo sapiens (human)
heat generationBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorHomo sapiens (human)
bone resorptionBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of mini excitatory postsynaptic potentialBeta-2 adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of lipophagyBeta-2 adrenergic receptorHomo sapiens (human)
cellular response to amyloid-betaBeta-2 adrenergic receptorHomo sapiens (human)
response to psychosocial stressBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of AMPA receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
carbohydrate metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
generation of precursor metabolites and energyBeta-3 adrenergic receptorHomo sapiens (human)
energy reserve metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
response to coldBeta-3 adrenergic receptorHomo sapiens (human)
heat generationBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-3 adrenergic receptorHomo sapiens (human)
eating behaviorBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-3 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-3 adrenergic receptorHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (41)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
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)
amyloid-beta bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase bindingBeta-2 adrenergic receptorHomo sapiens (human)
potassium channel regulator activityBeta-2 adrenergic receptorHomo sapiens (human)
identical protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-2 adrenergic receptorHomo sapiens (human)
protein-containing complex bindingBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta3-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
beta-3 adrenergic receptor bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-3 adrenergic receptorHomo sapiens (human)
epinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
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)
nucleusBeta-2 adrenergic receptorHomo sapiens (human)
lysosomeBeta-2 adrenergic receptorHomo sapiens (human)
endosomeBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorHomo sapiens (human)
Golgi apparatusBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
endosome membraneBeta-2 adrenergic receptorHomo sapiens (human)
membraneBeta-2 adrenergic receptorHomo sapiens (human)
apical plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneBeta-2 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-2 adrenergic receptorHomo sapiens (human)
receptor complexBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
receptor complexBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (53)

Assay IDTitleYearJournalArticle
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.
AID771315Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID739701Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation at 100 uM after 5 hrs relative to isoprenaline2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID739708Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
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.
AID739714Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID40531Positive inotropic effects by direct or indirect beta-1 adrenergic receptor activation.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
In search of the digitalis replacement.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID771317Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID739713Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID739700Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of 3H]cAMP accumulation after 5 hrs relative to isoprenaline2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
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.
AID739706Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
AID739709Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID59375Intrinsic sympathomimetic activity (ISA), calculated as the percent of maximum change in hind limb perfusion pressure (HLPP)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Beta-adrenoceptor stimulant properties of amidoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID739704Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID59674Effective dose required for the maximum hind limb perfusion pressure(HLPP) in anesthetized dogs.1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Beta-adrenoceptor stimulant properties of amidoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols.
AID771314Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID59673Effective dose required for the maximum heart rate in anesthetized dogs.1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Beta-adrenoceptor stimulant properties of amidoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID739710Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
AID739711Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
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.
AID739712Selectivity ratio of Kd for human beta1 adrenoceptor expressed in CHOK1 cells by radioligand displacement assay to Kd for human beta2 adrenoceptor expressed in CHOK1 cells by radioligand displacement assay2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
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.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID234276Selectivity is expressed as the ratio of ED50 on hind limb perfusion pressure to the ED50 on heart rate1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Beta-adrenoceptor stimulant properties of amidoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID59374Intrinsic sympathomimetic activity (ISA, calculated as the percent of maximum change in heart rate (HR)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Beta-adrenoceptor stimulant properties of amidoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols.
AID739696Selectivity ratio of Kd for human beta1 adrenoceptor expressed in CHOK1 cells by c-AMP accumulation assay to Kd for human beta2 adrenoceptor expressed in CHOK1 cells by c-AMP accumulation assay2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
AID739707Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation measured after 5 hrs relative to isoprenaline2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID771316Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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.
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.
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.
AID1346260Human beta1-adrenoceptor (Adrenoceptors)1999Molecular pharmacology, Nov, Volume: 56, Issue:5
Binding pockets of the beta(1)- and beta(2)-adrenergic receptors for subtype-selective agonists.
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 (261)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990110 (42.15)18.7374
1990's107 (41.00)18.2507
2000's26 (9.96)29.6817
2010's14 (5.36)24.3611
2020's4 (1.53)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.13

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 Index28.13 (24.57)
Research Supply Index5.86 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index39.34 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials80 (29.74%)5.53%
Reviews31 (11.52%)6.00%
Case Studies4 (1.49%)4.05%
Observational0 (0.00%)0.25%
Other154 (57.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]