Page last updated: 2024-11-04

fenclonine

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

Description

Fenclonine is a serotonin synthesis inhibitor. It acts by inhibiting the enzyme tryptophan hydroxylase, which is responsible for the rate-limiting step in serotonin synthesis. Fenclonine has been studied as a potential treatment for a variety of conditions, including depression, anxiety, and obsessive-compulsive disorder. It is also being investigated as a potential therapeutic agent for migraine headaches and other pain conditions. Fenclonine has been shown to have both antidepressant and anxiolytic effects in animal models. However, it has not been widely studied in humans, and its safety and efficacy are not yet fully established.'

Fenclonine: A selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine acts pharmacologically to deplete endogenous levels of serotonin. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4652
CHEMBL ID1256351
CHEBI ID110187
SCHEMBL ID26382
MeSH IDM0015725

Synonyms (144)

Synonym
4-chlorophenylalanine
ai3-62057
fenclonina [inn-spanish]
alanine, 3-(p-chlorophenyl)-
alanine, 3-(4-chlorophenyl)-, dl-
c-pal
einecs 231-051-9
fencloninum [inn-latin]
brn 2805758
para-chlorophenylalanine
alanine, 3-(p-chlorophenyl)-, dl-
phenylalanine, 4-chloro-
nsc 77370
BRD-A81615860-001-02-9
KBIO1_000873
DIVK1C_000873
EU-0100286
SPECTRUM_001188
p-chlorophenylalanine ,
SPECTRUM5_001312
dl-4-chlorophenylalanine
fenclonine
cp-10,188
cp-10188
4-chloro-dl-phenylalanine
nsc77370
dl-p-chlorophenylalanine
cp 10188
p-chloro-dl-phenylalanine
dl-pcpa
nsc-77370
(.+-.)-p-chlorophenylalanine
fenchlonine
dl-3-(p-chlorophenyl)alanine
parachlorophenylalanine
dl-phenylalanine, 4-chloro-
cp 10,188
fenclonin
7424-00-2
D04143
LOPAC0_000286
BSPBIO_003231
NCGC00024889-03
KBIO2_004236
KBIO2_006804
KBIO2_001668
KBIO3_002731
KBIOGR_001525
KBIOSS_001668
SPECTRUM2_001479
SPBIO_001437
NINDS_000873
SPECTRUM4_000863
SPECTRUM3_001766
SPECTRUM1502162
IDI1_000873
NCGC00024889-04
NCGC00024889-02
(?)-p-chlorophenylalanine
NCGC00024889-05
1991-78-2
NCGC00015255-03
CHEBI:110187
p-cpa
( inverted question mark)-p-chlorophenylalanine
C 6506
h-dl-phe(4-cl)-oh
2-amino-3-(4-chlorophenyl)propionic acid
NCGC00015255-07
AKOS000183864
HMS502L15
2-amino-3-(4-chlorophenyl)propanoic acid
STK735561
NCGC00015255-04
HMS3260J14
p-chlorophenylalanine, dl-
CHEMBL1256351
cas-7424-00-2
dtxcid2025139
tox21_110114
dtxsid4045139 ,
cas_7424-00-2
bdbm82270
S4586
CCG-39197
NCGC00015255-05
NCGC00015255-06
r5j7e3l9sp ,
hsdb 7747
unii-r5j7e3l9sp
FT-0625406
FT-0618218
FT-0618213
AM20060839
LP00286
(+/-)-p-chlorophenylalanine
AB02502
AB03058
AB00241
fenclonine [inn]
fenclonine [usan]
fenclonine [mart.]
fenclonine [hsdb]
gtpl5240
AB00052283-03
BBL027391
AKOS016050371
SCHEMBL26382
NCGC00015255-08
tox21_110114_1
NCGC00260971-01
CS-4900
(y)-p-chlorophenylalanine
tox21_500286
4-chlorophenylalanine #
(.+/-.)-p-chlorophenylalanine
(.+/-.)-p-chlorphenylalanine
4-chloro-dl-.beta.-phenylalanine
W-204245
J-300388
dl-phe(4-cl)-oh
HY-B1368
(a+/-)-p-chlorophenylalanine
F2147-6563
AB00052283_04
mfcd00063065
mfcd00002601
AC-9879
SR-01000075543-1
sr-01000075543
SR-01000075543-3
h-p-chloro-dl-phe-oh
(rs)-2-amino-3-(4-chloro-phenyl)-propionic acid;h-4-chloro-dl-phe-oh;fenclonine;pcpa
SY035278
SY032852
NCGC00015255-09
Q5443204
AS-49808
fenclonine ; 2-amino-3-(4-chlorophenyl)propanoic acid
SDCCGSBI-0050274.P003
NCGC00015255-13
N10776
EN300-112373
Z317024982

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"4 mg/kg - dose 1/4th of LD50 given ip), produced several autonomic, neurological and behavioral effects in mice with peak effects being at 15 min."( Acute neurobehavioural toxicity of phosphamindon and its drug-induced alteration.
Agarwal, AK; Sankaranarayanan, A; Sharma, PL, 1990
)
0.28
" These findings suggest that reduction of 5HT during early zebrafish development may have an adverse effect on body length, notochordal morphology, locomotor behavior, and serotonin message-related expression."( Adverse effects of serotonin depletion in developing zebrafish.
Airhart, MJ; Lee, DH; Miller, BE; Miller, MN; Monaco, PJ; Skalko, RG; Wilson, TD,
)
0.13

Pharmacokinetics

ExcerptReferenceRelevance
" The purpose of this study is to compare the pharmacokinetic properties of five protoberberine-type alkaloids (i."( Integrated pharmacokinetics of five protoberberine-type alkaloids in normal and insomnic rats after single and multiple oral administration of Jiao-Tai-Wan.
Cai, H; He, W; Hou, W; Liao, Q; Liu, G; Sun, X; Xie, Z; Zhang, P, 2014
)
0.4
" Plasma samples were collected at different time points to construct pharmacokinetic profiles by plotting drug concentration versus time and estimate pharmacokinetic parameters."( Integrated pharmacokinetics of five protoberberine-type alkaloids in normal and insomnic rats after single and multiple oral administration of Jiao-Tai-Wan.
Cai, H; He, W; Hou, W; Liao, Q; Liu, G; Sun, X; Xie, Z; Zhang, P, 2014
)
0.4
" In the single-dose oral administration, the Cmax and Tmax of five ingredients in insomnic rats had significant differences compared with those of normal rats."( Integrated pharmacokinetics of five protoberberine-type alkaloids in normal and insomnic rats after single and multiple oral administration of Jiao-Tai-Wan.
Cai, H; He, W; Hou, W; Liao, Q; Liu, G; Sun, X; Xie, Z; Zhang, P, 2014
)
0.4
"The pharmacokinetic behavior of five protoberberine-type alkaloids was described in this paper."( Integrated pharmacokinetics of five protoberberine-type alkaloids in normal and insomnic rats after single and multiple oral administration of Jiao-Tai-Wan.
Cai, H; He, W; Hou, W; Liao, Q; Liu, G; Sun, X; Xie, Z; Zhang, P, 2014
)
0.4

Compound-Compound Interactions

ExcerptReferenceRelevance
"A series of agents were tested for their ability to interact with the analgetic actions of either d-amphetamine (d-AMP) or l-amphetamine (l-AMP), or morphine in rats using the hot plate procedure."( Differential analgetic actions of amphetamine enantiomers in the mouse: a drug-drug interaction study.
Maickel, RP; Spratto, GR; Tocco, DR, 1985
)
0.27

Bioavailability

ExcerptReferenceRelevance
" Multiple dosing may improve the absorption of JTW in insomnic rats, which will increase the bioavailability and bring into active role in therapeutical effect."( Integrated pharmacokinetics of five protoberberine-type alkaloids in normal and insomnic rats after single and multiple oral administration of Jiao-Tai-Wan.
Cai, H; He, W; Hou, W; Liao, Q; Liu, G; Sun, X; Xie, Z; Zhang, P, 2014
)
0.4
"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

ExcerptRelevanceReference
" Chronic administration of p-chlorophenylalanine (p-CPA) in a dosage regimen which produced and maintained approximately 95% depletion of brain serotonin (5-HT) did not alter motor impairment after initial acute administration of ethanol or pentobarbital."( Effect of p-chlorophenylalanine on the acquisition of tolerance to ethanol and pentobarbital.
Frankel, D; Kalant, H; Khanna, JM; LeBlanc, AE, 1975
)
0.25
"Effects of electrical stimulation of the hippocampus (HPC), lateral amygdala (1-AMYG) and midbrain central gray matter (CG) on the release of ovulatory gonadotropin were examined using proestrous Wistar rats with or without pretreatment with reserpine, atropine or p-chlorophenylalanine (PCPA) at such dosage that had been confirmed not to block ovulation."( Cholinergic and serotonergic neural links and the inhibitory effects of hippocampus, lateral amygdala and central gray matter on gonadotropin release.
Kawagoe, S; Kawakami, M; Kimura, F, 1976
)
0.26
" Chronic administration of p-chlorophenylalanine (p-CPA), in a dosage regimen previously demonstrated to maintain extensive brain serotonin (5-HT) depletion, slowed down cross-tolerance development."( Effect of p-chlorophenylalanine on development of cross-tolerance between pentobarbital and ethanol.
Frankel, D; Kalant, H; Khanna, JM; LeBlanc, AE, 1977
)
0.26
" In two separate studies it was demonstrated that p-CPA, in a dosage regimen that produces extensive depletion of brain serotonin (5-HT), accelerated tolerance loss."( Effect of p-chlorophenylalnine on the loss and maintenance of tolerance to ethanol.
Frankel, D; Kalant, H; Khanna, JM; Leblanc, AE, 1978
)
0.26
" In addition, 5-HT markedly shifted to the left the cumulative dose-response curve of glutamate-induced excitation of motoneurons."( Serotonergic facilitation of facial motoneuron excitation.
Aghajanian, GK; McCall, RB, 1979
)
0.26
" The derivative [1,3'-DCM2]TRH was still potent enough to block PB-induced PRL secretion at an intraventricular dosage of 50 ng."( Antagonism of pentobarbital-induced hormonal changes by TRH in rats.
Collu, R; Ducharme, JR; Ruisseau, PD; Taché, Y, 1977
)
0.26
" Two populations of units were observed in the latter group: two-thirds of cells showed a dose-response curve similar to that of the non-pretreated group whereas the remaining one-third were unaffected either by morphine or naloxone."( The depressive effects of morphine on the C fibre response of dorsal horn neurones in the spinal rat pretreated or not by pCPA.
Besson, JM; Guilbaud, G; Le Bars, D; Menetrey, D; Rivot, JP, 1979
)
0.26
" These results suggest that endogenous serotonin causes a biphasic dose-response effect on T-cell activity with serotonin being required for optimal T-cell function, low doses being immune stimulatory and higher doses being suppressive."( Regulation of murine T-lymphocyte function by spleen cell-derived and exogenous serotonin.
Crayton, JW; Kut, JL; Wright, MA; Young, ME; Young, MR, 1992
)
0.28
" PCPA pretreatment shifted the cocaine dose-response curve to the right and blocked the ability of zacopride to reverse cocaine-induced activity."( 5-HT3 receptor antagonists block cocaine-induced locomotion via a PCPA-sensitive mechanism.
Hitzemann, R; Svingos, AL, 1992
)
0.28
" Para-chlorophenylalanine (p-CPA), a competitive inhibitor of the serotonin (5-HT) synthesis enzyme tryptophan hydroxylase, was administered to rats at a dosage (100 mg/kg daily for 3 days) that depletes 5-HT."( Effect of serotonin depletion by p-chlorophenylalanine upon discriminative behaviours.
Schechter, MD, 1991
)
0.28
" The dose-response curve of the 5HT1A-mediated, 8-hydroxy-2-(di-n-propylamino)tetralin (0."( Depletion of brain serotonin differently affects behaviors induced by 5HT1A, 5HT1C, and 5HT2 receptor activation in rats.
Berendsen, HH; Broekkamp, CL; van Delft, AM, 1991
)
0.28
" Dose-response studies revealed that the gastric acid secretion induced by submaximal but not high doses of RX 77368 was elevated significantly by p-CPA pretreatment."( Serotonin depletion potentiates gastric secretory and motor responses to vagal but not peripheral gastric stimulants.
Garrick, T; Stephens, RL; Taché, Y; Weiner, H, 1989
)
0.28
" Our results show that TRM induced both the depression and excitation in the behavior of mice depending on the dosage and TRM-induced excitatory behaviors may be attributed to both its direct stimulation of 5-HT receptors and facilitation of 5-HT release."( Effect of tryptamine on the behavior of mice.
Horisaka, K; Sugimoto, Y; Yamada, J, 1986
)
0.27
" The dose-response curves were bell-shaped."( Relation between yawning behavior and central serotonergic neuronal system in rats.
Aihara, H; Hashimoto, S; Okuyama, S; Shimamura, H, 1987
)
0.27
"The serotonin-depleting drug, parachlorophenylalanine (PCPA), in a dosage of 300 mg/kg, was administered to rats in an effort to test the hypothesis that altered distribution of PGO waves following drug treatment may be responsible for the sleep disruption and consequent sleep loss that accompany decreased serotonin levels."( PGO waves and insomnia in PCPA-treated rats.
Marks, GA; Roffwarg, HP, 1988
)
0.27
" The dose-response relationship for hyperactivity in grouped mice following the injection of morphine sulphate has been established."( Monoamine mediation of the morphine-induced activation of mice.
Carroll, BJ; Sharp, PT, 1972
)
0.25
"3 A second cannabis extract (II) with a different ratio of cannabinoids (also administered in dosage equivalent to 10 mg Delta(9)-THC/kg) failed to affect pentobarbitone anaesthesia in mice."( Interaction of cannabis and general anaesthetic agents in mice.
Chesher, GB; Jackson, DM; Starmer, GA, 1974
)
0.25
" The dose-response relationship of LVP was non-linear."( Facilitatory effects of monoamine synthesis inhibitors on lysine-vasopressin induced changes in the exploratory behaviour pattern of male rats.
Höglund, AU; Meyerson, BJ, 1984
)
0.27
"00 h the same dosage of 5-HTP failed to elicit any increase in plasma ACTH."( [Effect of the time of administration of 5-hydroxytryptophan on the restoration of circadian stimulation of ACTH secretion in rats treated with p-chlorophenylalanine].
Assenmacher, I; Ixart, G; Malaval, F; Nouguier-Soulé, J; Szafarczyk, A, 1980
)
0.26
" A dose-response relationship (5-100 mg/kg) for the hypothermic effect of delta 9-THC was seen."( The mechanism of action of delta 9-tetrahydrocannabinol on body temperature in mice.
Davies, JA; Graham, JD, 1980
)
0.26
" 5-HTP alone (200 mg/kg) increased wet dog shakes epissodes, whereas TP alone in the same dosage practically did not have any influence on the wet dog shakes in morphine-dependent rats."( The role of central serotoninergic neurotransmission in the morphine abstinence syndrome in rats.
Kruszewska, A; Langwiński, R, 1983
)
0.27
" Depletion of serotonin with p-chlorophenylalanine, p-chloroamphetamine and 5,7-dihydroxytryptamine did not affect the initial dose-response curve to the centrally injected barbiturate, but all treatments resulted in significant delays in tolerance development."( The role of cerebral serotonin in the development of tolerance to centrally administered phenobarbital.
Lyness, WH; Mycek, MJ, 1980
)
0.26
" To determine if para-chlorophenylalanine (PCPA), which alters the pattern of the behavioral response to amphetamine, also changes the pattern of the neuronal response to the drug, a dose-response analysis was performed on amphetamine-induced changes in unit activity in the anterior neostriatum of rats pretreated 48 h previously with 300 mg/kg PCPA or vehicle."( Apparent serotonergic modulation of the dose-dependent biphasic response of neostriatal neurons produced by D-amphetamine.
Alloway, KD; Curtis, SD; Rebec, GV, 1981
)
0.26
" A muscarinic agonist, carbachol, produced a dose-related rightward shift of the dose-response curve to IMI."( Suppression of the rat micturition reflex by imipramine.
Kim, CY; Sohn, UD, 1997
)
0.3
" The purpose of the study was to investigate the role of Trp or its metabolite, given in different dosing regimens in induction of tissue damage."( Tryptophan toxicity--time and dose response in rats.
Gross, B; Honigman, S; Livne, E; Ronen, N, 1999
)
0.3
" Dose-response studies showed that the potency of cyanopindolol to inhibit clearance of 5-HT was equivalent to that of the selective 5-HT reuptake inhibitor fluvoxamine."( 5-HT(1B) receptor-mediated regulation of serotonin clearance in rat hippocampus in vivo.
Daws, LC; Frazer, A; Gerhardt, GA; Gould, GG; Teicher, SD, 2000
)
0.31
") at three different dosing times, or (iv) both pCPA and l-OHP."( Pharmacological blockage of serotonin biosynthesis and circadian changes in oxaliplatin toxicity in rats.
Ben Attia, M; Boughattas, NA; Ixart, G; Lemaigre, G; Mechkouri, M; Reinberg, A, 2002
)
0.31
" The basal firing rate was not modified by either a single dose or repeated doses of MDMA, although the latter produced a shift to the right in the dose-response curve for clonidine-induced inhibition of the firing rate (ED(50) increased by 59%) and a reduction in tyrosine hydroxylase activity (20%) in the hippocampus."( Short-term effects of 3,4-methylenedioximethamphetamine on noradrenergic activity in locus coeruleus and hippocampus of the rat.
Arrue, A; Giralt, MT; Ruiz-Ortega, JA; Ugedo, L, 2003
)
0.32
" Finally, a dose-response study showed that progressive doses of corticosterone (0-40 mg/kg/day) in ADX rats resulted in diminished suppression of proliferation in 5-HT-depleted compared with 5-HT-intact rats."( Serotonin modulates the suppressive effects of corticosterone on proliferating progenitor cells in the dentate gyrus of the hippocampus in the adult rat.
Herbert, J; Huang, GJ, 2005
)
0.33
" For this purpose, neuronal activity was measured in rats with rivastigmine-induced elevated ACh levels after a 95% 5-HT depletion obtained by dosing p-chlorophenylalanine followed by D,L-fenfluramine."( Serotonin depletion results in a decrease of the neuronal activation caused by rivastigmine in the rat hippocampus.
Aznar, S; Knudsen, GM; Kornum, BR; Moller, A; Ronn, LC; Weikop, P, 2006
)
0.33
" Blood samples for analysis of glucose and lactate were taken at 30-45 min intervals before and after drug dosing and body temperature was monitored by telemetry."( Serotonin mediates rapid changes of striatal glucose and lactate metabolism after systemic 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") administration in awake rats.
Cumming, P; Gramsbergen, JB, 2007
)
0.34
" Multiple dosing may improve the absorption of JTW in insomnic rats, which will increase the bioavailability and bring into active role in therapeutical effect."( Integrated pharmacokinetics of five protoberberine-type alkaloids in normal and insomnic rats after single and multiple oral administration of Jiao-Tai-Wan.
Cai, H; He, W; Hou, W; Liao, Q; Liu, G; Sun, X; Xie, Z; Zhang, P, 2014
)
0.4
" Non-targeted metabolic profiling and a targeted pCPA dose-response study identified 21 biomarkers in the pCPA-treated mice while 17 metabolites in the Tph2-/- mice were found to be significantly altered compared with the control mice."( Metabolomics Approach Reveals Integrated Metabolic Network Associated with Serotonin Deficiency.
Bai, Y; Burton, C; Chang, C; Liu, H; Liu, Y; Shen, S; Tian, Y; Weng, R; Xu, X, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
phenylalanine derivativeAn amino acid derivative resulting from reaction of alanine at the amino group or the carboxy group, or from the replacement of any hydrogen of phenylalanine by a heteroatom. The definition normally excludes peptides containing phenylalanine residues.
[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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
endonuclease IVEscherichia coliPotency3.16230.707912.432431.6228AID1708
thioredoxin reductaseRattus norvegicus (Norway rat)Potency39.81070.100020.879379.4328AID588453
GLS proteinHomo sapiens (human)Potency5.62340.35487.935539.8107AID624146
arylsulfatase AHomo sapiens (human)Potency5.35821.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.74430.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00400.540617.639296.1227AID2364; AID2528
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency33.807823.934123.934123.9341AID1967
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID488953
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency3.54810.01789.637444.6684AID588834
flap endonuclease 1Homo sapiens (human)Potency0.02990.133725.412989.1251AID588795
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (53)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
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.
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.
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.
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.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
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).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,478)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901719 (69.37)18.7374
1990's375 (15.13)18.2507
2000's209 (8.43)29.6817
2010's144 (5.81)24.3611
2020's31 (1.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.38

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 Index27.38 (24.57)
Research Supply Index7.88 (2.92)
Research Growth Index4.22 (4.65)
Search Engine Demand Index42.09 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials15 (0.57%)5.53%
Reviews55 (2.09%)6.00%
Case Studies8 (0.30%)4.05%
Observational0 (0.00%)0.25%
Other2,555 (97.04%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]