Page last updated: 2024-12-05

synephrine

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

Synephrine is a naturally occurring phenethylamine alkaloid found in plants such as bitter orange, citrus aurantium, and the fruit of the Osage orange. It is structurally similar to epinephrine (adrenaline) and norepinephrine, and it acts as a stimulant by activating adrenergic receptors, particularly α1 and β3 receptors. Synephrine has been studied for its potential effects on weight loss, blood pressure, and athletic performance. It is thought to work by increasing thermogenesis (heat production) and fat metabolism, as well as by increasing blood pressure and heart rate. However, the evidence for these effects is mixed, and more research is needed to determine the safety and efficacy of synephrine. Synephrine is often used as an ingredient in dietary supplements, particularly those marketed for weight loss. However, it is important to note that synephrine supplements are not regulated by the FDA, and there is a risk of adverse effects, such as headache, anxiety, insomnia, and high blood pressure. Synephrine is also found in some prescription medications, such as nasal decongestants. Synephrine is a complex compound that has been the subject of much research. It is studied because of its potential effects on human health, particularly its ability to stimulate the sympathetic nervous system. However, more research is needed to determine its safety and efficacy for various applications.'

Cross-References

ID SourceID
PubMed CID7172
CHEMBL ID33720
CHEBI ID29081
SCHEMBL ID146500
MeSH IDM0020958

Synonyms (187)

Synonym
BSPBIO_001136
BPBIO1_001250
HMS3394G09
nsc-170956
nsc170956
beta-methylamino-alpha-(4-hydroxyphenyl)ethyl alcohol
4-hydroxy-alpha-[(methylamino)methyl]benzenemethanol
p-hydroxy-alpha-[(methylamino)methyl]benzyl alcohol
CHEBI:29081 ,
1-(4-hydroxyphenyl)-2-methylaminoethanol
smr000059111
MLS000069435
EU-0101085
(+/-)-synephrine, >=98%
synefrin [czech]
benzenemethanol, 4-hydroxy-alpha-((methylamino)methyl)-
4-(1-hydroxy-2-(methylamino)ethyl)phenol
p-hydroxyphenylmethylaminoethanol
nsc 166285
einecs 202-300-9
benzyl alcohol, p-hydroxy-alpha-((methylamino)methyl)-
pentedrin [german]
p-methylaminoethanolphenol
parakorper [german]
methylaminomethyl(4-hydroxyphenyl)carbinol
(rs)-1-(4-hydroxyphenyl)-2-(methylamino)ethanol
4-hydroxy-alpha-((methylamino)methyl)benzenemethanol
alpha-(4-oxyphenyl)alpha-oxy-beta-methylaminoaethan [german]
p-hydroxy-alpha-((methylamino)methyl)benzyl alcohol
ethaphene
cas-94-07-5
NCGC00016351-01
oxedrine (ban)
D07148
PDSP1_000167
LOPAC0_001085
PRESTWICK2_001088
PRESTWICK3_001088
NCGC00089788-02
MLS001424216
AB00514040
synephrine ,
1-(4-hydroxyphenyl)-2-(methylamino)ethanol
(+/-)-synephrine
94-07-5
C04548
p-[(methylamino)ethanol]phenol
p-hydroxyphenyl(methylamino)ethanol
sympatol
nsc-166285
parasympatol
1-(4-hydroxyphenyl)-(n-methylethanol)amine
p-hydroxy-.alpha.-[(methylamino)methyl]benzylalcohol
simpalon
sympaethamin
sympaethamine
oxedrine
s 38537-9
p-hydroxy-.alpha.-[(methylamino)methyl]benzyl alcohol
sympathol
simpatol
nsc166285 ,
synthenate
1-(4-hydroxyphenyl)-(2-methylamino)ethanol
wln: qr dyq1m1
p-oxedrine
analeptin
.beta.-methylamino-.alpha.-(4-hydroxyphenyl)ethyl alcohol
benzyl alcohol, p-hydroxy-.alpha.-[(methylamino)methyl]-
benzenemethanol, 4-hydroxy-.alpha.-[(methylamino)methyl]-
synephrin
[(methylamino)methyl][(4-hydroxyphenyl)carbinol]
p-synephrine
1-(4-hydroxyphenyl)-n-methylethanolamine
PDSP2_000166
PRESTWICK1_001088
SPBIO_003028
PRESTWICK0_001088
4-[1-hydroxy-2-(methylamino)ethyl]phenol
NCGC00089788-04
(?)-synephrine
NCGC00089788-03
NCGC00015924-05
7336264B-EDC9-42C5-939B-FF800AB5BB4A
S 0752
4-hydroxy-alpha-(methylaminomethyl)benzyl alcohol
HMS2052G09
( inverted question mark)-synephrine
NCGC00015924-08
advantra z
s-38537-9
CHEMBL33720
dl-synephrine
FT-0653012
S0232
HMS1571I18
(+,-)-synephrine
STK803113
BBL015111
AKOS004119915
HMS3263I12
HMS3264E11
HMS2098I18
tox21_200962
NCGC00258515-01
nsc-759316
pharmakon1600-01506085
nsc759316
dtxcid8010588
tox21_110390
dtxsid0030588 ,
CCG-205162
SYNEPHRINE - OXEDRINE
HMS2233F20
CCG-101098
NCGC00015924-04
NCGC00015924-03
NCGC00015924-09
NCGC00015924-06
oxedrine [inn:ban]
alpha-(4-oxyphenyl)alpha-oxy-beta-methylaminoaethan
parakorper
peg5dp7434 ,
nsc 170956
unii-peg5dp7434
synefrin
(+-)-n-methyloctopamine
BP-12742
FT-0618685
NCGC00015924-13
LP01085
S2362
HMS3369C13
SCHEMBL146500
NC00348
AKOS016038542
NCGC00015924-12
tox21_110390_1
KS-5152
benzenemethanol, 4-hydroxy-.alpha.-((methylamino)methyl)-
oxedrine [who-dd]
synephrine [usp-rs]
synephrine [mi]
synephrine [inci]
oxedrine [mart.]
oxedrine [usp impurity]
(+/-)-oxedrine
(y)-synephrine
NCGC00261770-01
tox21_501085
4-hydroxy-a-(methylaminomethyl)benzyl alcohol
W-100214
(.+/-.)-n-methyloctopamine
p-((methylamino)ethanol)phenol
4-hydroxy-.alpha.-((methylamino)methyl)benzenemethanol
4-[1-hydroxy-2-(methylamino)ethyl]phenol #
(.+/-.)-synephrine
((methylamino)methyl)((4-hydroxyphenyl)carbinol)
Q-100668
AB00384265_11
mfcd00002370
DB09203
synephrine, analytical standard
HMS3656O09
(+)-[(methylamino)methyl]-benzenemethano
bdbm50102660
SR-01000002983-7
sr-01000002983
SR-01000002983-3
SR-01000002983-8
SBI-0051055.P002
HMS3715I18
SW197214-5
CS-0007857
HY-N0132
synephrine (oxedrine)
synephrine,(s)
Q421351
SDCCGSBI-0051055.P003
NCGC00015924-25
HMS3884D15
benzenemethanol, 4-hydroxy-a-[(methylamino)methyl]-, (ar)-
rac-synephrine
4-(1-hydroxy-2-methylamino-ethyl)phenol
oxedrine, sympatol
synepherine
EN300-267997

Research Excerpts

Overview

P-Synephrine is a natural compound, frequently added to ephedra-free dietary supplements for weight-loss. It is an adrenergic amine found in Citrus aurantium L.

ExcerptReferenceRelevance
"P-Synephrine is a protoalkaloid widely used as an ergogenic aid in sports. "( Acute consumption of p-synephrine does not enhance performance in sprint athletes.
Abían-Vicen, J; Areces, F; Del Coso, J; Gallo, C; Gutiérrez-Hellín, J; Lara, B; Puente, C; Salinero, JJ, 2016
)
1.47
"p-Synephrine is a protoalkaloid widely used in dietary supplements for weight management because of its purported thermogenic effects. "( Acute p-synephrine ingestion increases fat oxidation rate during exercise.
Del Coso, J; Gutiérrez-Hellín, J, 2016
)
1.59
"Synephrine is a natural compound, frequently added to ephedra-free dietary supplements for weight-loss, due to its effects as a nonspecific adrenergic agonist. "( Structural isomerization of synephrine influences its uptake and ensuing glutathione depletion in rat-isolated cardiomyocytes.
Carvalho, F; Costa, VM; de Lourdes Bastos, M; de Pinho, PG; Remião, F; Rossato, LG, 2011
)
2.11
"p-Synephrine is an adrenergic amine found in Citrus aurantium L. "( Toxicological effects of a mixture used in weight loss products: p-synephrine associated with ephedrine, salicin, and caffeine.
Arbo, MD; Dallegrave, E; Krahn, CL; Leal, MB; Limberger, RP; Lorensi, AL; Maciel, ES; Mariotti, KC; Schmitt, GC, 2012
)
1.34
"Synephrine is a natural phenylethylamine derivative present in some food supplements containing Citrus aurantium, permitted in sport regulations."( Study of the photocatalytic transformation of synephrine: a biogenic amine relevant in anti-doping analysis.
Aragno, M; Baiocchi, C; Calza, P; Dal Bello, F; Giancotti, V; Medana, C, 2013
)
1.37

Effects

Synephrine has lipolytic effects in human fat cells only at high doses, and octopamine does not have lipolytics effects in humans. The synephrine concentration has been determined in the juices of Citrus unshiu mandarins.

ExcerptReferenceRelevance
"Synephrine has been used to promote weight loss; however, its safety and efficacy have not been fully established. "( The Safety and Efficacy of
Bahar, MA; Csupor, D; Koncz, D; Roza, O; Tóth, B, 2022
)
2.16
"The synephrine concentration has been determined in the juices of Citrus unshiu mandarins harvested from 10 different groves located in a major growing region in California."( Synephrine content of juice from Satsuma mandarins (Citrus unshiu Marcovitch).
Breksa, AP; Cain, B; Dragull, K, 2008
)
2.27
"Synephrine has lipolytic effects in human fat cells only at high doses, and octopamine does not have lipolytic effects in human adipocytes."( Citrus aurantium, an ingredient of dietary supplements marketed for weight loss: current status of clinical and basic research.
Fugh-Berman, A; Myers, A, 2004
)
1.04

Treatment

ExcerptReferenceRelevance
"p-Synephrine treatment markedly activated the protein kinase B (PKB/Akt) pathway and sequentially inhibited glycogen synthase kinase 3β (GSK3β) activity."( p-Synephrine exhibits anti-adipogenic activity by activating the Akt/GSK3β signaling pathway in 3T3-L1 adipocytes.
Chen, G; Guo, LX; Yin, ZY; Zhang, YH; Zheng, XX, 2019
)
1.79

Toxicity

At doses up to 100 mg synephrine/kg body weight, there were no adverse effects on embryolethality, fetal weight, or incidences of gross, visceral, or skeletal abnormalities. The toxic effects observed seem to be related with adrenergic stimulation and should alert for possible side effects.

ExcerptReferenceRelevance
" Altogether, the examples presented illustrate that natural does not equal safe and that in modern society adverse health effects, upon either acute or chronic exposure to phytochemicals, can occur as a result of use of plant- or herb-based foods, teas, or other extracts."( Molecular mechanisms of toxicity of important food-borne phytotoxins.
Alink, GM; Boersma, MG; Martena, MJ; Rietjens, IM; Spiegelenberg, W, 2005
)
0.33
"Dissociating glucocorticoid receptor (GR) ligands hold great promise for treating inflammatory disorders since it is assumed that they exert beneficial activities mediated by transrepression but avoid adverse effects of GR action requiring transactivation."( Therapeutic and adverse effects of a non-steroidal glucocorticoid receptor ligand in a mouse model of multiple sclerosis.
Hanisch, UK; John, M; Lühder, F; Menzfeld, C; Reichardt, HM; Tischner, D; Tuckermann, JP; van den Brandt, J; Wüst, S, 2009
)
0.35
"CpdA has significant therapeutic potential although adverse effects severely compromise its application in vivo."( Therapeutic and adverse effects of a non-steroidal glucocorticoid receptor ligand in a mouse model of multiple sclerosis.
Hanisch, UK; John, M; Lühder, F; Menzfeld, C; Reichardt, HM; Tischner, D; Tuckermann, JP; van den Brandt, J; Wüst, S, 2009
)
0.35
" The data indicate that based on current knowledge, the use of bitter orange extract and p-synephrine appears to be exceedingly safe with no serious adverse effects being directly attributable to these ingredients."( The safety of Citrus aurantium (bitter orange) and its primary protoalkaloid p-synephrine.
Preuss, HG; Shara, M; Stohs, SJ, 2011
)
0.82
" Animals were sacrificed on GD 21, and fetuses were examined for the presence of various developmental toxic endpoints."( Developmental toxicity of Citrus aurantium in rats.
Hansen, DK; Juliar, BE; Pellicore, LS; White, GE, 2011
)
0.37
"At doses up to 100 mg synephrine/kg body weight, there were no adverse effects on embryolethality, fetal weight, or incidences of gross, visceral, or skeletal abnormalities."( Developmental toxicity of Citrus aurantium in rats.
Hansen, DK; Juliar, BE; Pellicore, LS; White, GE, 2011
)
0.68
" Because ephedrine has cardiovascular effects that may be exacerbated during physical exercise, the purpose of this study was to determine whether extracts containing synephrine produced adverse effects on the cardiovascular system in exercising rats."( Cardiovascular toxicity of Citrus aurantium in exercised rats.
Abdel-Rahman, A; Fabricant, D; George, NI; Hansen, DK; Pellicore, LS; White, GE, 2013
)
0.58
" No adverse effects were reported."( Cardiovascular Safety of Oral p-Synephrine (Bitter Orange) in Healthy Subjects: A Randomized Placebo-Controlled Cross-over Clinical Trial.
Mukattash, TL; Shara, M; Stohs, SJ, 2016
)
0.72
" This review, as well as several other assessments published in recent years, has concluded that bitter orange extract and p-synephrine are safe for use in dietary supplements and foods at the commonly used doses."( Safety, Efficacy, and Mechanistic Studies Regarding Citrus aurantium (Bitter Orange) Extract and p-Synephrine.
Stohs, SJ, 2017
)
0.88
" No adverse effects were reported in response to the bitter orange (p-synephrine)."( Safety evaluation of p-synephrine following 15 days of oral administration to healthy subjects: A clinical study.
Shara, M; Smadi, MM; Stohs, SJ, 2018
)
1.03
" However, with its increasing popularity, numerous cases of adverse events related to synephrine use have been reported."( Review of Case Reports on Adverse Events Related to Pre-workout Supplements Containing Synephrine.
de Jonge, MLL; Egberink, LB; Kieviet, LC; Sierts, M; van der Heyden, MAG, 2023
)
1.36

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic parameters are quite comparable to the sympathomimetics similar in structure."( [Pharmacokinetics and metabolism of 3H-synephrine (author's transl)].
Aulepp, H; Hengstmann, JH, 1978
)
0.53

Compound-Compound Interactions

The purpose of this study was to examine the metabolic, lipolytic, and cardiovascular responses to supplementation with p-synephrine alone and in combination with caffeine during resistance exercise (RE)

ExcerptReferenceRelevance
" Therefore, the purpose of the present study was to examine the effects of supplementation with p-synephrine alone and in combination with caffeine on free-weight resistance exercise performance."( The effects of supplementation with P-Synephrine alone and in combination with caffeine on resistance exercise performance.
Bush, JA; Diamond, KB; Faigenbaum, AD; Kang, J; Kraemer, WJ; Leise, MD; Nocera, VG; Ratamess, NA; Stohs, SJ, 2015
)
0.91
"The purpose of this study was to examine the metabolic, lipolytic, and cardiovascular responses to supplementation with p-synephrine alone and in combination with caffeine during resistance exercise (RE)."( The Effects of Supplementation with p-Synephrine Alone and in Combination with Caffeine on Metabolic, Lipolytic, and Cardiovascular Responses during Resistance Exercise.
Bush, JA; Campbell, SC; Diamond, KB; Faigenbaum, AD; Kang, J; Kraemer, WJ; Leise, MD; Miller, HB; Nocera, VG; Ratamess, NA; Stohs, SJ,
)
0.61
"The purpose was to examine cardiovascular responses to supplementation with p-synephrine alone and in combination with caffeine during quiet sitting."( Acute cardiovascular effects of bitter orange extract (p-synephrine) consumed alone and in combination with caffeine in human subjects: A placebo-controlled, double-blind study.
Bush, JA; Ellis, NL; Faigenbaum, AD; Hasan, SB; Kang, J; Kuper, JD; O'Grady, EA; Ratamess, NA; Stohs, SJ; Vought, IT, 2018
)
0.95
"The purpose of this study was to examine acute hematological and mood perception responses to supplementation with p-synephrine alone and in combination with caffeine during quiet sitting."( Acute hematological and mood perception effects of bitter orange extract (p-synephrine) consumed alone and in combination with caffeine: A placebo-controlled, double-blind study.
Bush, JA; Ellis, NL; Faigenbaum, AD; Kang, J; Kuper, JD; O'Grady, EA; Ratamess, NA; Stohs, SJ; Vought, IT, 2018
)
0.92

Bioavailability

ExcerptReferenceRelevance
" The resulting bioavailability has to be calculated to 22% only."( [Pharmacokinetics and metabolism of 3H-synephrine (author's transl)].
Aulepp, H; Hengstmann, JH, 1978
)
0.53
" Juice from the orange (Seville orange juice [SOJ]) is used to "knock out" intestinal cytochrome P450 (CYP) 3A4 in bioavailability studies."( Seville (sour) orange juice: synephrine content and cardiovascular effects in normotensive adults.
Cold, JA; Desai, HD; Gurley, BJ; Hon, YY; Jann, MW; Penzak, SR, 2001
)
0.6
"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

This study developed and validated a positive-ion mode liquid chromatography/tandem mass spectrometry (LC/MS/MS) method for the quantitative determination of the major (synephrine) and minor adrenergic protoalkaloids in bitter orange. Female Sprague-Dawley rats were dosed daily for 28 days with synephrine from two different extracts.

ExcerptRelevanceReference
" The main object of this study was to determine if est rogene could cause the alpha-receptors to be more sensitive to the alpha -receptor stimulating drugs, so that by using an equal dosage of alpha-r eceptor stimulating drugs in a preliminary estrogenic treatment, a stronger tonic effect would be achieved in the urethra musculature than by using the alpha-receptor stimulating drugs alone."( Estrogenic sensitivity of alpha-receptors in the urethra musculature.
Fuchs, P; Schreiter, F; Stockamp, K, 1976
)
0.26
" When m-synephrine hydrochloride was administered orally to humans in normal dosage regimens four main metabolites were excreted in urine: (i) unconjugated m-hydroxymandelic acid (MHMA, 30%), (ii) m-hydroxyphenylglycol (MHPG) sulphate (6%), (iii) m-synephrine sulphate (47%) and (iv) m-synephrine glucuronide (12%)."( The mammalian metabolism of R-(-)-m-synephrine.
Crowley, JR; Ibrahim, KE; Midgley, JM; Williams, CM, 1983
)
0.98
" This study developed and validated a positive-ion mode liquid chromatography/tandem mass spectrometry (LC/MS/MS) method for the quantitative determination of the major (synephrine) and minor (tyramine, N-methyltyramine, octopamine, and hordenine) adrenergic protoalkaloids in a suite of National Institute of Standards and Technology (NIST) bitter orange Standard Reference Materials (SRMs): SRM 3258 Bitter Orange Fruit, SRM 3259 Bitter Orange Extract, and SRM 3260 Bitter Orange Solid Oral Dosage Form."( Mass spectrometric determination of the predominant adrenergic protoalkaloids in bitter orange (Citrus aurantium).
Nelson, BC; Putzbach, K; Sander, LC; Sharpless, KE, 2007
)
0.53
"Sprague-Dawley rats were dosed daily by gavage with one of several different doses of synephrine from one of two different extracts."( Developmental toxicity of Citrus aurantium in rats.
Hansen, DK; Juliar, BE; Pellicore, LS; White, GE, 2011
)
0.59
"Female Sprague-Dawley rats were dosed daily by gavage for 28 days with synephrine from two different extracts."( Physiological effects following administration of Citrus aurantium for 28 days in rats.
Abdel-Rahman, A; Fabricant, D; George, NI; Hansen, DK; Pellicore, LS; White, GE, 2012
)
0.61
" Sprague-Dawley rats were dosed daily by gavage for 28 days with 10 or 50 mg of synephrine/kg body weight from one of two different extracts; caffeine was added to some doses."( Cardiovascular toxicity of Citrus aurantium in exercised rats.
Abdel-Rahman, A; Fabricant, D; George, NI; Hansen, DK; Pellicore, LS; White, GE, 2013
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
plant metaboliteAny eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms.
alpha-adrenergic agonistAn agent that selectively binds to and activates alpha-adrenergic receptors.
[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 (3)

ClassDescription
ethanolamines
phenethylamine alkaloid
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
[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 (28)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency3.54810.004023.8416100.0000AID485290
Chain A, Beta-lactamaseEscherichia coli K-12Potency17.78280.044717.8581100.0000AID485294
interleukin 8Homo sapiens (human)Potency42.16320.047349.480674.9780AID651758
glp-1 receptor, partialHomo sapiens (human)Potency3.45680.01846.806014.1254AID624148; AID624172; AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency34.02390.100020.879379.4328AID488773; AID588453
RAR-related orphan receptor gammaMus musculus (house mouse)Potency33.49150.006038.004119,952.5996AID1159521
SMAD family member 2Homo sapiens (human)Potency0.09520.173734.304761.8120AID1346924
GLS proteinHomo sapiens (human)Potency11.90470.35487.935539.8107AID624146; AID624170
SMAD family member 3Homo sapiens (human)Potency0.09520.173734.304761.8120AID1346924
ThrombopoietinHomo sapiens (human)Potency10.00000.02517.304831.6228AID917; AID918
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency22.38720.011212.4002100.0000AID1030
EWS/FLI fusion proteinHomo sapiens (human)Potency0.00130.001310.157742.8575AID1259253
farnesoid X nuclear receptorHomo sapiens (human)Potency61.56190.375827.485161.6524AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency48.45900.005428.02631,258.9301AID1346982
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency1.09470.001024.504861.6448AID743215
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency25.54520.001019.414170.9645AID588536; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency15.46360.023723.228263.5986AID743223
arylsulfatase AHomo sapiens (human)Potency2.68551.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency35.40850.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency68.45010.000723.06741,258.9301AID743085; AID743122
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00280.540617.639296.1227AID2364; AID2528
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency22.38720.01789.637444.6684AID588834
survival motor neuron protein isoform dHomo sapiens (human)Potency0.70790.125912.234435.4813AID1458
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency100.00000.00419.962528.1838AID2675
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency1.41250.00106.000935.4813AID943
Nuclear receptor ROR-gammaHomo sapiens (human)Potency2.66030.026622.448266.8242AID651802
[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
[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)
Neuromedin-U receptor 2Homo sapiens (human)EC50 (µMol)6.60000.00041.31046.6000AID1166579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (46)

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 transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-gammaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-gammaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-gammaHomo sapiens (human)
regulation of fat cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-gammaHomo sapiens (human)
adipose tissue developmentNuclear receptor ROR-gammaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
reduction of food intake in response to dietary excessNeuromedin-U receptor 2Homo sapiens (human)
regulation of smooth muscle contractionNeuromedin-U receptor 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayNeuromedin-U receptor 2Homo sapiens (human)
neuropeptide signaling pathwayNeuromedin-U receptor 2Homo sapiens (human)
cell-cell signalingNeuromedin-U receptor 2Homo sapiens (human)
central nervous system developmentNeuromedin-U receptor 2Homo sapiens (human)
grooming behaviorNeuromedin-U receptor 2Homo sapiens (human)
feeding behaviorNeuromedin-U receptor 2Homo sapiens (human)
response to painNeuromedin-U receptor 2Homo sapiens (human)
arachidonic acid secretionNeuromedin-U receptor 2Homo sapiens (human)
positive regulation of calcium-mediated signalingNeuromedin-U receptor 2Homo sapiens (human)
chloride transmembrane transportNeuromedin-U receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

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)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
protein bindingNuclear receptor ROR-gammaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-gammaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-gammaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-gammaHomo sapiens (human)
neuromedin U receptor activityNeuromedin-U receptor 2Homo sapiens (human)
G protein-coupled receptor activityNeuromedin-U receptor 2Homo sapiens (human)
intracellularly calcium-gated chloride channel activityNeuromedin-U receptor 2Homo sapiens (human)
protein bindingNeuromedin-U receptor 2Homo sapiens (human)
GTP bindingNeuromedin-U receptor 2Homo sapiens (human)
neuromedin U bindingNeuromedin-U receptor 2Homo sapiens (human)
neuropeptide receptor activityNeuromedin-U receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

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)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaHomo sapiens (human)
nuclear bodyNuclear receptor ROR-gammaHomo sapiens (human)
chromatinNuclear receptor ROR-gammaHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
plasma membraneNeuromedin-U receptor 2Homo sapiens (human)
membraneNeuromedin-U receptor 2Homo sapiens (human)
plasma membraneNeuromedin-U receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (70)

Assay IDTitleYearJournalArticle
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID215613Dissociation constant against a series of agonists of membranes of the turkey erythrocyte containing mainly Beta adrenergic receptor was determined1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Correlation between affinity toward adrenergic receptors and approximate electrostatic potentials of phenylethylamine derivatives. 1. Effects of the side chain.
AID781325pKa (acid-base dissociation constant) as determined by Liao ref: J Chem Info Model 20092014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
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.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1166579Agonist activity at human NMU2R transfected in HEK293 cells after 7 hrs by luciferase reporter gene assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and biological activity of flavonoid derivatives as selective agonists for neuromedin U 2 receptor.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (395)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990174 (44.05)18.7374
1990's17 (4.30)18.2507
2000's71 (17.97)29.6817
2010's102 (25.82)24.3611
2020's31 (7.85)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 50.90

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index50.90 (24.57)
Research Supply Index6.08 (2.92)
Research Growth Index4.96 (4.65)
Search Engine Demand Index141.76 (26.88)
Search Engine Supply Index3.42 (0.95)

This Compound (50.90)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials20 (4.83%)5.53%
Reviews21 (5.07%)6.00%
Case Studies15 (3.62%)4.05%
Observational0 (0.00%)0.25%
Other358 (86.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (7)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Sex Differences in Sympathetic Vascular Reactivity at High Altitude [NCT05525416]17 participants (Actual)Interventional2022-07-28Completed
A Randomized Double Blind Trial of Vasoactive Drugs for the Management of Shock in the ICU [NCT02118467]Phase 4836 participants (Anticipated)Interventional2014-05-31Recruiting
A Comparative Effectiveness Study Evaluating the Effects of Two Thermogenic Supplements on Body Composition Using a Double-Blinded Placebo-Controlled Protocol [NCT01423019]75 participants (Anticipated)Interventional2011-10-31Completed
Sex Differences in Sympathetic Activity and Vascular Reactivity During Acute and Chronic Hypoxia. [NCT05001048]14 participants (Actual)Interventional2019-08-04Completed
Goal-Directed Intraoperative Fluid Management Using FloTrac© Monitoring in High-Risk Neurosurgical Patients [NCT02701582]66 participants (Actual)Interventional2014-03-31Completed
Comparison of Two Different Doses of Intramuscular Phenylephrine HCL for Prevention of Spinal Anesthesia Induced Hypotension During Cesarean Section: A Prospective Randomized Double-blinded Parallel Study [NCT05348980]Phase 460 participants (Actual)Interventional2020-01-01Completed
A Single Center, Pilot Study of Induced Hypertension for Minimizing Infarct Progression in Patients With Acute Large-vessel Occlusion Ischemic Stroke Undergoing Endovascular Therapy [NCT04218773]Early Phase 140 participants (Anticipated)Interventional2020-09-11Enrolling by invitation
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02701582 (9) [back to overview]Area Under Curve of MAP Below 65
NCT02701582 (9) [back to overview]Creatinine Change
NCT02701582 (9) [back to overview]Fluid Balance Measured by Inputs and Outputs (I/Os) of All Measurable Fluid in Peri-operative Period
NCT02701582 (9) [back to overview]Number of ICU Stays Greater Than 1.5 Days
NCT02701582 (9) [back to overview]Number of Patients Treated for Hypotension With Phenylephrine Drip
NCT02701582 (9) [back to overview]Organ Oxygenation as Measured by Arterial Blood Gas Values
NCT02701582 (9) [back to overview]Organ Oxygenation as Measured by Serum Lactate
NCT02701582 (9) [back to overview]Patients Requiring Fluid Bolus for Management
NCT02701582 (9) [back to overview]Pulmonary Status as Measured by the Number of Participants Who Require Supplemental Oxygen

Area Under Curve of MAP Below 65

Hypotension as measured by area under the curve of MAP less than 65. (NCT02701582)
Timeframe: 1 Day

InterventionmmHG x minutes (Mean)
Goal Directed Therapy-65.06
Control Group-61.88

[back to top]

Creatinine Change

Change in creatinine in the 72 hour post-op period (mg/dL) (NCT02701582)
Timeframe: Baseline and 72 hours

Interventionmg/dL (Mean)
Goal Directed Therapy-0.04
Control Group-0.13

[back to top]

Fluid Balance Measured by Inputs and Outputs (I/Os) of All Measurable Fluid in Peri-operative Period

Fluid balance measured by I/Os of all fluid in the peri-op period during the first 12 hours after the subject's surgery. (NCT02701582)
Timeframe: Baseline and 12 Hours

Interventionml/kg (Mean)
Goal Directed TherapyNA
Control GroupNA

[back to top]

Number of ICU Stays Greater Than 1.5 Days

the sum of ICU stays greater than the 1.5 Days eligibility for discharge from hospital according to the surgeon, over the course of 20 Days (NCT02701582)
Timeframe: 20 Days

InterventionNumber of ICU Stays greater that 1.5 Day (Number)
Goal Directed Therapy13
Control Group20

[back to top]

Number of Patients Treated for Hypotension With Phenylephrine Drip

The number of patients on a phenylephrine drip within 24 hours post-op. (NCT02701582)
Timeframe: 1 day

InterventionParticipants (Count of Participants)
Goal Directed Therapy0
Control Group4

[back to top]

Organ Oxygenation as Measured by Arterial Blood Gas Values

Patient's organ oxygenation as measured by base deficit mEq/L, during the first 24 hours after surgery. (NCT02701582)
Timeframe: Baseline and 1 day

InterventionmEq/L (Mean)
Goal Directed Therapy3.55
Control Group4.75

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Organ Oxygenation as Measured by Serum Lactate

Serum lactate levels, as measured in mmol/L, in patients during the first 24 hours after surgery. (NCT02701582)
Timeframe: Baseline and 24 Hours

Interventionmmol/L (Mean)
Goal Directed Therapy2.0
Control Group1.75

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Patients Requiring Fluid Bolus for Management

Number of patients who received fluid boluses in the first 24 hours post-op (NCT02701582)
Timeframe: 1 day

InterventionParticipants (Count of Participants)
Goal Directed Therapy7
Control Group6

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Pulmonary Status as Measured by the Number of Participants Who Require Supplemental Oxygen

We looked at the number of patients who required supplemental oxygen within the first 24 hours after surgery. (NCT02701582)
Timeframe: 1 day

InterventionParticipants (Count of Participants)
Goal Directed Therapy17
Control Group25

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