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perphenazine

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Description

Perphenazine is a typical antipsychotic medication used to treat schizophrenia and other mental health conditions. It is a phenothiazine derivative and acts as a dopamine antagonist, blocking dopamine receptors in the brain. Perphenazine is synthesized through a multi-step process involving the reaction of a phenothiazine derivative with a substituted piperazine. The primary effects of perphenazine include reducing positive symptoms of psychosis such as hallucinations and delusions. It is also effective in treating agitation and anxiety. Perphenazine is studied extensively for its potential therapeutic applications in treating schizophrenia, bipolar disorder, and other mental health disorders. Research focuses on its efficacy, safety, and long-term effects, as well as exploring its mechanisms of action and potential for drug interactions.'

Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID4748
CHEMBL ID567
CHEBI ID8028
SCHEMBL ID42125
MeSH IDM0016378

Synonyms (221)

Synonym
BIDD:GT0150
AC-12196
MLS001146929
BRD-K10995081-001-05-5
gtpl209
EU-0072164
DIVK1C_000880
KBIO1_000880
sch-3940
EU-0100930
SPECTRUM_001610
PRESTWICK_536
lopac-p-6402
NCGC00015826-02
cas-58-39-9
NCGC00015826-01
chlorpiprazine
perphenazinum
CHEBI:8028 ,
2-{4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]piperazin-1-yl}ethanol
perfenazina
gamma-(4-(beta-hydroxyethyl)piperazin-1-yl)propyl-2-chlorophenothiazine
2-chloro-10-(3-(4-(2-hydroxyethyl)piperazin-1-yl)propyl)phenothiazine
2-(4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-1-piperazinyl)ethanol
LOPAC0_000930
PRESTWICK2_000125
BSPBIO_002376
SPECTRUM5_001493
OPREA1_603835
BSPBIO_000170
hsdb 3379
1-(2-hydroxyethyl)-4-(3-(2-chloro-10-phenothiazinyl)propyl)piperazine
piperazineethanol, 4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)-
einecs 200-381-5
ai3-50151
nsc 150866
perfenazina [inn-spanish]
1-piperazineethanol, 4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)-
1-piperazineethanol, 4-(3-(2-chlorophenothiazin-10-yl)propyl)-
2-chloro-10-(3-(1-(2-hydroxyethyl)-4-piperazinyl)propyl)phenothiazine
1',1-(2-idrossietil)-4,3-(2-cloro-10-fenotiazil)propilpiperazina [italian]
perphenazinum [inn-latin]
2-chloro-10-3-(1-(2-hydroxyethyl)-4-piperazinyl)propyl phenothiazine
perfenazina [italian]
4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-1-piperazineethanol
2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol
AB00052390
58-39-9
C07427
4-(3-(2-chlorophenothiazin-10-yl)propyl)-1-piperazineethanol
perphenazine
nsc150866
tranquisan
1-piperazineethanol, 4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-
1-(2-hydroxyethyl)-4-[3-(2-chloro-10-phenothiazinyl)propyl]piperazine
4-[3-(2-chlorophenothiazin-10-yl)propyl]-1-piperazineethanol
.gamma.-[4-(.beta.-hydroxyethyl)piperazin-1-yl]propyl-2-chlorophenothiazine
trilifan
1-piperazineethanol, 4-[3-(2-chlorophenothiazin-10-yl)propyl]-
etaperazin
emesinal
pzc ,
2-chloro-10-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl]phenothiazine
etaperazine
chlorperphenazine
perphenan
trilafon
perphenazin
fentazin
wln: t c666 bn isj eg b3- at6n dntj d2q
trifaron
1-piperazineethanol, trihydrochloride
decentan
nsc-150866
thilatazin
2-chloro-10-3-[1-(2-hydroxyethyl)-4-piperazinyl]propyl phenothiazine
perfenazine
sch 3940
f-mon
ethaperazine
triphenot
DB00850
D00503
perphenazine (jp17/usp/inn)
NCGC00024092-04
NCGC00024092-05
MLS000069637 ,
smr000058180
KBIO2_007226
KBIO2_002090
KBIO2_004658
KBIO3_001596
KBIOSS_002090
KBIOGR_001445
SPECTRUM3_000758
SPECTRUM2_001602
PRESTWICK1_000125
NINDS_000880
SPBIO_002109
SPECTRUM4_000843
SPBIO_001603
PRESTWICK0_000125
SPECTRUM1503934
IDI1_000880
BPBIO1_000188
PRESTWICK3_000125
NCGC00024092-03
NCGC00015826-03
NCGC00024092-06
SR-01000000137-4
STK019818
NCGC00015826-06
P 6402 ,
HMS2093M15
NCGC00015826-10
bdbm50130273
L000919
CHEMBL567 ,
HMS502L22
perfenil
AKOS000664046
HMS1922M14
HMS1568I12
A831863
HMS2095I12
HMS3259C09
HMS3262J22
perphenazine maleate [jan]
MLS002548897
pharmakon1600-01503934
nsc758649
nsc-758649
tox21_110233
dtxsid1023441 ,
dtxcid703441
HMS2232D21
S4731
2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]-piperazin-1-yl]ethanol
CCG-39060
NCGC00015826-05
NCGC00015826-09
NCGC00015826-08
NCGC00015826-04
NCGC00015826-07
fta7xxy4ez ,
1',1-(2-idrossietil)-4,3-(2-cloro-10-fenotiazil)propilpiperazina
unii-fta7xxy4ez
perphenazine [usp:inn:ban:jan]
FT-0603244
LP00930
perphenazine [jan]
perphenazine [mart.]
fluphenazine dihydrochloride impurity e [ep impurity]
etrafon-a component perphenazine
perphenazine [usp monograph]
perphenazine [usp-rs]
perphenazine [who-dd]
perphenazine [mi]
perphenazine [ep monograph]
perphenazine [orange book]
perphenazine [vandf]
perphenazine component of etrafon-a
perphenazine [inn]
perphenazine [hsdb]
HMS3370O14
NC00472
SCHEMBL42125
2-{4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]piperazin-1-yl}ethan-1-ol
NCGC00015826-13
tox21_110233_1
KS-5105
CS-5137
HY-A0077
tox21_500930
NCGC00261615-01
REGID_FOR_CID_4748
2-(4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)piperazin-1-yl)ethanol
W-105390
.gamma.-(4-(.beta.-hydroxyethyl)piperazin-1-yl)propyl-2-chlorophenothiazine
2-(4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-1-piperazinyl)ethanol #
etrafon (salt/mix)
component of triavil (salt/mix)
piperazineethanol, 4-[3-(2-chloro-10h-phenothiazin-10-yl)propyl]-
perphenazine, british pharmacopoeia (bp) reference standard
P1970
OPERA_ID_1161
AB00052390_17
mfcd00056798
sr-01000000137
SR-01000000137-2
perphenazine, united states pharmacopeia (usp) reference standard
perphenazine for system suitability, european pharmacopoeia (ep) reference standard
perphenazine, european pharmacopoeia (ep) reference standard
perphenazine 1.0 mg/ml in methanol
SR-01000000137-8
SR-01000000137-5
MRF-0000509
SBI-0050904.P003
HMS3712I12
2-(4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)piperazin-1-yl)ethan-1-ol
Q423520
5,7-eicosadiynoicacid
BRD-K10995081-001-15-4
EN300-120640
SDCCGSBI-0050904.P004
HMS3885H20
NCGC00015826-20
D82041
Z1530532754
ps16 - perphenazine
perphenazine (usp-rs)
perphenazine (ep monograph)
2-(4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)-1-piperazinyl)ethanol
1-piperazineethanol, 4(3-(2-chloro-10h-phenothiazin-10-yl)propyl)-
perphenazinum (inn-latin)
perphenazine (mart.)
4-(3-(2-chloro-10h-phenothiazin-10-yl)propyl)-1-piperazineethanol
perphenazine (usp monograph)
perfenazina (inn-spanish)
n05ab03
perphenazine (usp:inn:ban:jan)

Research Excerpts

Overview

Perphenazine (PPZ) is a typical antipsychotic that is mainly administrated for the treatment of schizophrenia. Perphenazine is a treatment option in postoperative nausea and vomiting (PONV) prophylaxis.

ExcerptReferenceRelevance
"Perphenazine is a classical antipsychotic drug that can reportedly induce extrapyramidal and sympatholytic side effects."( Lysosomal membrane permeabilization mediated apoptosis involve in perphenazine-induced hepatotoxicity in vitro and in vivo.
Cao, Y; Chen, L; Cui, Y; Dai, Z; Ge, X; Liu, W; Qing, Y; Shi, D; Tao, L; Zhang, L, 2022
)
1.68
"Perphenazine is an old, generic, cheap, phenothiazine antipsychotic drug that has been in continuous clinical use worldwide since the 1950's."( Adding perphenazine to increase effectiveness of standard glioblastoma chemoirradiation.
Kast, RE,
)
1.31
"Perphenazine (PPZ) is a typical antipsychotic that is mainly administrated for the treatment of schizophrenia. "( Pharmacokinetics and brain distribution studies of perphenazine-loaded solid lipid nanoparticles.
Derakhshandeh, K; Ghaleiha, A; Mahboobian, MM; Mahjub, R; Mohammadi, M; Mohammadi, P, 2021
)
2.32
"Perphenazine is a treatment option in postoperative nausea and vomiting (PONV) prophylaxis. "( Extrapyramidal symptoms following administration of oral perphenazine 4 or 8 mg: an 11-year retrospective analysis.
Henao, JP; Lichvar, AB; Orebaugh, SL; Peperzak, KA; Pippi, MA; Skledar, SJ; Williams, BA, 2014
)
2.09
"Perphenazine is an old phenothiazine antipsychotic with a potency similar to haloperidol. "( Perphenazine for schizophrenia.
Hartung, B; Leucht, S; Sampson, S, 2015
)
3.3
"Perphenazine is a phenothiazine-type antipsychotic that is a potential candidate for sublingual administration due to its extensive first-pass metabolism. "( Development and validation of a gas chromatographic-mass spectrometric method for quantitative determination of perphenazine in rabbit plasma after sublingual administration.
Jarho, P; Järvinen, T; Lehtonen, M; Turunen, E, 2008
)
2
"Perphenazine is an old phenothiazine antipsychotic with a potency similar to haloperidol. "( Perphenazine for schizophrenia.
Hartung, B; Laux, G; Leucht, S; Wada, M, 2005
)
3.21

Effects

ExcerptReferenceRelevance
"Perphenazine enanthate has been used in wild animals as a tranquilizer during the period of adaptation to new environments to reduce stress, mortalities and injuries. "( Quantification of perphenazine in eurasian otter (Lutra lutra lutra) urine samples by gas chromatography-mass spectrometry.
Bergés, R; Casasampere, M; Fernández-Morán, J; Segura, J; Ventura, R, 2002
)
2.09

Treatment

Perphenazine is a treatment option in postoperative nausea and vomiting (PONV) prophylaxis. Perphenazine-treated patients had a higher incidence of extrapyramidal symptom-related adverse events. Treatment with perphenazine was less costly than treatment with second-generation antipsychotics.

ExcerptReferenceRelevance
"Perphenazine is a treatment option in postoperative nausea and vomiting (PONV) prophylaxis. "( Extrapyramidal symptoms following administration of oral perphenazine 4 or 8 mg: an 11-year retrospective analysis.
Henao, JP; Lichvar, AB; Orebaugh, SL; Peperzak, KA; Pippi, MA; Skledar, SJ; Williams, BA, 2014
)
2.09
"Perphenazine-treated patients had a higher incidence of extrapyramidal symptom-related adverse events, mean increases (i.e., worsening) in extrapyramidal symptom rating scale scores, and a higher rate of elevated prolactin levels than aripiprazole (57.7% vs."( Aripiprazole for treatment-resistant schizophrenia: results of a multicenter, randomized, double-blind, comparison study versus perphenazine.
Carson, WH; Kane, JM; Marcus, RN; McQuade, RD; Meltzer, HY; Sanchez, R, 2007
)
1.27
"The perphenazine treated patients required fewer rescue antiemetics than the control group, P < 0.05."( Perphenazine decreases vomiting by children after tonsillectomy.
Roberts, DJ; Splinter, WM, 1997
)
2.22
"Perphenazine treatment advanced the spring transitional period and subsequent ovulation by approximately 30 d."( The effects of perphenazine and bromocriptine on follicular dynamics and endocrine profiles in anestrous pony mares.
Bennett-Wimbush, K; Evans, T; Loch, WE; Plata-Madrid, H, 1998
)
1.37
"Treatment with perphenazine was less costly than treatment with second-generation antipsychotics with no significant differences in measures of effectiveness. "( Cost-effectiveness of second-generation antipsychotics and perphenazine in a randomized trial of treatment for chronic schizophrenia.
Davis, SM; Hsiao, JK; Keefe, RS; Leslie, DL; Lieberman, J; Lin, H; McEvoy, J; Miller, EA; Perkins, DO; Rosenheck, RA; Sindelar, J; Stroup, TS; Swartz, M, 2006
)
0.93
"Treatment with perphenazine was more effective than treatment with quetiapine (p = .010) or ziprasidone (p = .002) in individuals of inferred African ancestry and homozygous for the rs951439 C allele."( Ethnic stratification of the association of RGS4 variants with antipsychotic treatment response in schizophrenia.
Campbell, DB; Ebert, PJ; Levitt, P; Lieberman, J; Skelly, T; Stroup, TS; Sullivan, PF, 2008
)
0.69

Toxicity

ExcerptReferenceRelevance
" This study demonstrates that PD is a safe and effective remedy for maintenance therapy in psychotic patients."( Long-term depot neuroleptic treatment with perphenazine decanoate. I. Efficacy and side effects in a 12 month study of 42 drug monitored psychotic patients.
Hansen, LB; Højholdt, K; Knudsen, P; Larsen, NE, 1985
)
0.53
" Statistically significant differences of mean change of BAS total score from baseline to endpoint were noted between treatment groups Treatment--emergent adverse events occurred more frequently in patients receiving perphenazine (46%), than in patients receiving olanzapine (17%)."( [Safety and efficacy of olanzapine versus perphenazine in patients with schizophrenia: results of multicenter, 18-week, double-blind clinical trial].
Araszkiewicz, A; Bilikiewicz, A; Bomba, J; Chrzanowski, W; Debowska, G; Jarema, M; Landowski, J; Olajossy, M; Rybakowski, J,
)
0.58
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Dopaminergic and serotonergic pathways are involved in the therapeutic and adverse effects of the drug."( Serotonin and dopamine receptor gene polymorphisms and the risk of extrapyramidal side effects in perphenazine-treated schizophrenic patients.
Dahl, ML; Gunes, A; Jaanson, P; Scordo, MG, 2007
)
0.56
" In the present study, PPZ-containing solid lipid nanoparticles (PPZ-SLNs) were prepared and optimized based on different factors, including lipid and surfactant amount, to develop appropriate and safe novel oral dosage forms of PPZ."( Development of Perphenazine-Loaded Solid Lipid Nanoparticles: Statistical Optimization and Cytotoxicity Studies.
Farsani, PA; Mahboobian, MM; Mahjub, R; Mohammadi, M; Oliaei, SS, 2021
)
0.97

Pharmacokinetics

CYP2D6 contributes to pharmacodynamic tissue sensitivity to perphenazine as measured by the areas under the curve (AUCs) expressed as a ratio (prolactin-A UC0-6/perphenazine-AUC0- 6) in Chinese Canadians.

ExcerptReferenceRelevance
" They allowed to make the pharmacokinetic profile of Perphenazine Enanthate, a long-acting neuroleptic, and to draw some information concerning its therapeutic use."( [Pharmacokinetic profile of perphenazine enanthate].
Viala, A, 1976
)
0.8
" Moreover pharmacokinetic data increasingly have been clinically applied."( Chemotherapy with neuroleptics. Clinical and pharmacokinetic aspects with a particular view to depot preparations.
Knudsen, P, 1985
)
0.27
"The purpose of the study was to investigate clinical and pharmacokinetic parameters concerning perphenazine decanoate (PD) and haloperidol decanoate (HD) with an interval of 3 weeks during a study period of 51 weeks."( A long-term cross-over pharmacokinetic study comparing perphenazine decanoate and haloperidol decanoate in schizophrenic patients.
Dencker, SJ; Giös, I; Mårtensson, E; Nordén, T; Nyberg, G; Persson, R; Roman, G; Stockman, O; Svärd, KO, 1994
)
0.75
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" Notably, volunteers homozygous for CYP2D6*10 exhibited a significant reduction (66%) in mean pharmacodynamic tissue sensitivity as measured by the (prolactin-AUC0-6/perphenazine-AUC0-6) ratio (P=0."( CYP2D6 genotype in relation to perphenazine concentration and pituitary pharmacodynamic tissue sensitivity in Asians: CYP2D6-serotonin-dopamine crosstalk revisited.
Albers, LJ; Bertilsson, L; Carpenter, E; Endrenyi, L; Harper, P; Kalow, W; Kennedy, JL; Miura, J; Ozdemir, V; Reist, C; Svensson, JO; Widén, J, 2007
)
0.82
" We suggest that CYP2D6 genetic variation may potentially influence pharmacodynamic tissue sensitivity in the pituitary, presumably through disposition of an endogenous substrate (e."( CYP2D6 genotype in relation to perphenazine concentration and pituitary pharmacodynamic tissue sensitivity in Asians: CYP2D6-serotonin-dopamine crosstalk revisited.
Albers, LJ; Bertilsson, L; Carpenter, E; Endrenyi, L; Harper, P; Kalow, W; Kennedy, JL; Miura, J; Ozdemir, V; Reist, C; Svensson, JO; Widén, J, 2007
)
0.63
" This method was used to perform a pilot pharmacokinetic study of PPZ after subcutaneous administration to one ewe."( HPLC quantification of perphenazine in sheep plasma: application to a pharmacokinetic study.
Castells, G; Cristòfol, C; Manteca, X; Pedernera, C; Ruiz, JL, 2007
)
0.65
"We observed that CYP2D6 contributes to pharmacodynamic tissue sensitivity to perphenazine as measured by the areas under the curve (AUCs) expressed as a ratio (prolactin-AUC0-6/perphenazine-AUC0-6) in Chinese Canadians [Pharmacogenetics and Genomics 2007; 17:339-347]."( CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine.
Aklillu, E; Endrenyi, L; Harper, P; Kalow, W; Miura, J; Ozdemir, V, 2007
)
0.78
"After controlling for DRD2 polymorphisms, CYP2D6 was a significant predictor of pituitary pharmacodynamic tissue sensitivity to perphenazine (P=0."( CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine.
Aklillu, E; Endrenyi, L; Harper, P; Kalow, W; Miura, J; Ozdemir, V, 2007
)
0.76
"CYP2D6 seems to be an independent contributor to pituitary pharmacodynamic tissue sensitivity to perphenazine after accounting for DRD2 functional polymorphisms."( CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine.
Aklillu, E; Endrenyi, L; Harper, P; Kalow, W; Miura, J; Ozdemir, V, 2007
)
0.77
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"We investigated the pharmacokinetic behavior of orally disintegrating tablets (ODTs) containing perphenazine/hydroxypropyl-beta-cyclodextrin inclusion complex (PPZ/HP-beta-CD) in rabbits and evaluated their bioequivalence with conventional tablets."( Pharmacokinetics of orally disintegrating tablets of perphenazine/hydroxypropyl-beta-cyclodextrin inclusion complex in rabbits.
Chen, ML; Wang, L; Xiao, YY; Zeng, F; Zong, L, 2013
)
0.86
"The significant improvement in the pharmacokinetic properties of PPZ following one oral dose indicates that SLN is a promising drug delivery system for PPZ and shows a high potential for successful brain delivery of this antipsychotic."( Pharmacokinetics and brain distribution studies of perphenazine-loaded solid lipid nanoparticles.
Derakhshandeh, K; Ghaleiha, A; Mahboobian, MM; Mahjub, R; Mohammadi, M; Mohammadi, P, 2021
)
0.87

Compound-Compound Interactions

ExcerptReferenceRelevance
"A detector for liquid chromatography, based on anodic electrochemical oxidation at a glassy carbon electrode, is used in combination with reversed-phase liquid chromatography for the determination of the long-acting tricyclic psychotropic drugs fluphenazine and perphenazine in blood."( Anodic coulometric detection with a glassy carbon electrode in combination with reversed-phase high-performance liquid chromatography. Determination of blood levels of perphenazine and fluphenazine.
Lankelma, J; Poppe, H; Tjaden, UR, 1976
)
0.63

Bioavailability

The aim of this study was to evaluate the solid-state stability of a fast-dissolving perphenazine/β-cyclodextrin (β-CD) complex. The main scope of the present investigation was to improve the bioavailability of perphenazines by incorporating it into the nanostructured lipid carriers.

ExcerptReferenceRelevance
" The bioavailability of cefmetazole, determined by area under the blood concentration curve method, increased 20 to 30% by the coadministration of calmodulin inhibitors."( Effects of phenothiazines and N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide on rat colonic absorption of cefmetazole.
Furuya, A; Kamada, A; Nishihata, T; Suzuka, T, 1986
)
0.27
" The possible utility of this response in bioavailability testing is discussed."( Serum prolactin level increase in normal subjects following administration of perphenazine oral dosage forms: possible application to bioavailability testing.
Erb, RJ; Stoltman, WP, 1982
)
0.49
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" The developed tablet formulation could be a promising drug delivery system with improvements in PPZ bioavailability and patient compliance."( Development of orally disintegrating tablets of Perphenazine/hydroxypropyl-β-cyclodextrin inclusion complex.
Wang, L; Zeng, F; Zong, L,
)
0.39
" The aim of this study was to evaluate the solid-state stability of a fast-dissolving perphenazine/β-cyclodextrin (β-CD) complex, which has been found to be well absorbed after sublingual administration to rabbits."( Effect of storage on the dissolution rate of a fast-dissolving perphenazine/β-cyclodextrin complex.
Ahtiainen, H; Jarho, P; Järvinen, K; Kauppinen, A; Korhonen, O; Lehto, VP; Turunen, E, 2014
)
0.87
"Solubility represents an important challenge for formulation of drugs, because the therapeutic efficacy of a drug depends on the bioavailability and ultimately on its solubility."( Electrospun fibers as potential carrier systems for enhanced drug release of perphenazine.
Berbenni, V; Bruni, G; D Aniello, S; Friuli, V; Girella, A; Lorenzo, RD; Maggi, L; Maietta, M; Marini, A; Milanese, C; Tammaro, L, 2016
)
0.66
"Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule."( Highly predictive and interpretable models for PAMPA permeability.
Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017
)
0.46
"Poor bioavailability of PPZ necessitated the development of fast-dissolving PPZ formulations regardless of delivery routes."( Amorphous nanoparticle complex of perphenazine and dextran sulfate as a new solubility enhancement strategy of antipsychotic perphenazine.
Dong, B; Hadinoto, K, 2017
)
0.73
"The simple yet efficient preparation, excellent physical characteristics, fast dissolution, and high apparent solubility exhibited by the PPZ-DXT nanoplex established its potential as a new bioavailability enhancement strategy of PPZ."( Amorphous nanoparticle complex of perphenazine and dextran sulfate as a new solubility enhancement strategy of antipsychotic perphenazine.
Dong, B; Hadinoto, K, 2017
)
0.73
"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
" Due to its highly lipophilic nature and extensive hepatic first-pass metabolism, its oral bioavailability is low (40%)."( Pharmacokinetics and brain distribution studies of perphenazine-loaded solid lipid nanoparticles.
Derakhshandeh, K; Ghaleiha, A; Mahboobian, MM; Mahjub, R; Mohammadi, M; Mohammadi, P, 2021
)
0.87
" Compared to PPZ suspension, the relative bioavailability and the brain distribution of PPZ-SLN were increased up to 2-fold and 16-fold, respectively."( Pharmacokinetics and brain distribution studies of perphenazine-loaded solid lipid nanoparticles.
Derakhshandeh, K; Ghaleiha, A; Mahboobian, MM; Mahjub, R; Mohammadi, M; Mohammadi, P, 2021
)
0.87
"The main scope of the present investigation was to improve the bioavailability of perphenazine (PPZ) by incorporating it into the nanostructured lipid carriers (NLCs)."( Preparation, characterization, and
Derakhshandeh, K; Mahboobian, MM; Mohammadi, M; Saghafi, Z, 2021
)
0.85
"As a result of lipophilic nature and poor aqueous solubility, as well as extensive hepatic metabolism, PPZ has low systemic bioavailability via the oral route."( Preparation, characterization, and
Derakhshandeh, K; Mahboobian, MM; Mohammadi, M; Saghafi, Z, 2021
)
0.62
" Despite the lipophilic essence, PPZ encounters limited bioavailability caused by the first-pass metabolism following oral administration."( Development of Perphenazine-Loaded Solid Lipid Nanoparticles: Statistical Optimization and Cytotoxicity Studies.
Farsani, PA; Mahboobian, MM; Mahjub, R; Mohammadi, M; Oliaei, SS, 2021
)
0.97
" Our findings were corroborated by rat studies, where co-dosing of a bile acid sequestrant substantially reduced the bioavailability of Perphenazine but not Metoprolol."( Bile Is a Selective Elevator for Mucosal Mechanics and Transport.
Bellstedt, P; Choudhury, S; Endres, S; Guck, J; Hanio, S; Heinze, KG; Höpfel, AI; Keßler, C; Meinel, L; Möckel, C; Möllmert, S; Pöppler, AC; Scheller, L; Scherf-Clavel, O; Schlauersbach, J; Schubert, US; Zorn, T, 2023
)
1.11

Dosage Studied

Perphenazine is routinely administered in a divided dosage regimen because of its relatively short plasma half-life. Patients with schizophrenia (DSM-IV) randomly allocated to treatment with perphenazine were also randomly assigned to once-daily or twice-daily dosing and followed over 18 months.

ExcerptRelevanceReference
" Therefore, monitoring treatment by dosage adjustment alone is of little value."( Plasma level monitoring of antipsychotic drugs.
Cooper, TB,
)
0.13
" Their plasma levels are not correlated with their dosage in a man to another, but, for some of them, there is lineary relation for one person."( [Relations between the levels of neuroleptics and the doses, the therapeutic effects and the side effects].
Andersson, JC; Davy, JP; Halbecq, JJ; Morel, P; Moulin, M; Poilpre, E, 1978
)
0.26
" Improvement was recorded in a double blind study of 18 patients treated with maximum tolerated dosage (mean 18."( Tardive dyskinesia treated with pimozide.
Calne, DB; Claveria, LE; Haskayne, L; Lodge-Patch, IC; Pallis, CA; Petrie, A; Teychenne, PF, 1975
)
0.25
" Patients were treated up to 30 days and the dosage of bromperidol was increased depending on effects and side-effects up to 5 mg per day."( Effects and side-effects of bromperidol in comparison with other antipsychotic drugs.
Woggon, B,
)
0.13
" The employed dosage caused no strong sedation."( Double-blind comparison of bromperidol and perphenazine.
Angst, J; Woggon, B, 1978
)
0.52
" The average daily dosage was 81."( Loxapine versus perphenazine in psychotic patients. A double-blind, randomized, multicentre trial.
Fensbo, C; Fruensgaard, K; Hansen, KM; Sihm, F; Wollenberg, J, 1978
)
0.6
" The daily dosage varied from 300 to 1,200 mg Sulpiride orally and 12 to 48 mg Perphenazine."( [Study of the clinical effects of sulpiride and perphenazine in 82 schizophrenic patients by the double blind method].
Asada, S; Ishimaru, T; Kodama, H; Kubo, S; Masuda, K, 1976
)
0.74
" Twenty normal subjects were tested four times in a double blind study in order to control the short- and long-term effects of a low dosage of perphenacine."( [Psychometric effects of perphenacine below the "neuroleptic threshold" (author's transl)].
Jacobi, P; Maxion, HH, 1975
)
0.25
" The dosage was progressively increased until the optimal clinical effect was attained."( [Experience with using etaperazine (perphenazine) in the treatment of patients with schizophrenia in a preschool psychiatric department].
Proselkova, ME; Uzhanov, NV, 1991
)
0.56
" In the majority of cases, the team of physicians in the department succeeded in finding the dosage most appropriate on the basis of the serum concentration level."( [Therapy control of perphenazine in paranoid conditions. 1. Organizational aspects].
Andersen, E; Brøsen, K; Gerholt, F; Glue, P; Hørder, M; Kjeldsen, CS; Klitgaard, NA; Kragh-Sørensen, P; Krarup, G; Rask, PH, 1991
)
0.6
" Dose-response studies of catalepsy and ptosis were conducted in male Sprague-Dawley rats aged 30, 56, or 100 days."( Decreasing sensitivity to neuroleptic agents in developing rats; evidence for a pharmacodynamic factor.
Baldessarini, RJ; Campbell, A; Teicher, MH, 1988
)
0.27
" The dosage and intervals between injections were on an individual basis."( Perphenazine decanoate in sesame oil vs. perphenazine enanthate in sesame oil: a comparative study of pharmacokinetic properties and some clinical implications.
Hansen, LB; Knudsen, P; Larsen, NE, 1985
)
1.71
" In the patients treated with PD there were signs of accumulation indicating the possibility of prolonging dosage intervals."( Perphenazine decanoate vs. perphenazine enanthate: efficacy and side effects in a 6 week double-blind, comparative study of 50 drug monitored psychotic patients.
Auken, G; Hansen, LB; Højholdt, K; Knudsen, P; Larsen, NE; Waehrens, J, 1985
)
1.71
"A liquid chromatographic method is described for determination of perphenazine and perphenazine sulfoxide in representative dosage forms."( Liquid chromatographic method for perphenazine and its sulfoxide in pharmaceutical dosage forms for determination of stability.
Beaulieu, N; Lovering, EG,
)
0.65
" In addition to evaluating the PRL secretory pattern and lactotroph response, the PCOS individuals were given dopamine agonist therapy in a graduated dosage schedule, increasing each month, over a 3-month interval."( The value of prolactin dynamics as a predictor of ovulation with bromocriptine in patients with polycystic ovary syndrome.
Buckman, MT; Mattox, JH; Peake, GT, 1984
)
0.27
" In the second study, the subjects were dosed with two 10-mg amitriptyline tablets, one 10-mg amitriptyline tablet with one combination tablet containing 10 mg of amitriptyline and 4 mg of perphenazine, and two combination tablets, each containing 10 mg of amitriptyline and 4 mg of perphenazine."( Serum prolactin level increase in normal subjects following administration of perphenazine oral dosage forms: possible application to bioavailability testing.
Erb, RJ; Stoltman, WP, 1982
)
0.68
" The dosage was changed in most of these patients (80-90%) in order to bring the concentration within the therapeutic level."( [The effect of serum monitoring on concentration of perphenazine and zuclopenthixole].
Olesen, OV; Poulsen, JH; Thomsen, K, 1993
)
0.54
" If this finding can be confirmed in a larger population, genotyping may become an important tool for the dosing of these two neuroleptic agents."( The CYP2D6 genotype predicts the oral clearance of the neuroleptic agents perphenazine and zuclopenthixol.
Aberg-Wistedt, A; Bertilsson, L; Dahl, ML; Jerling, M; Landell, NE; Liljenberg, B; Sjöqvist, F, 1996
)
0.52
" We describe a case of acute dystonia with atypical onset without relation to changes in dosage and with laryngeal involvement with aphonia, but without dyspnoea."( [Atypical acute dystonia].
Mors, NP; Nielsen, AS, 1998
)
0.3
"025 mg/ml, resulting in a dosage of 4 mg/kg of body weight and 2 mg/kg, respectively, to the dams."( Use of perphenazine to control cannibalism in DBA/1 mice.
Carter, DB; Franklin, CL; Kennett, MJ, 2002
)
0.77
" This dosage should be varied depending on health, age, and temperament of the individual cheetah."( Evaluation of long-term sedation in cheetah (Acinonyx jubatus) with perphenazine enanthate and zuclopenthixol acetate.
Huber, C; Slotta-Bachmayr, L; Walzer, C, 2001
)
0.55
" In treated patients, no correlation was found between NSS and daily dosage or duration of exposure of neuroleptic treatment, extrapyramidal symptoms and level of CGI-improvement."( [Neuroleptic treatment and neurological soft signs in schizophrenic patients].
Chebel, S; Gaha, L; Mandhouj, O; Mechri, A; Slama, H,
)
0.13
" The 32 mg dose of BL-1020 resulted in an average D(2) RO of 44% at 4-6 h post dosing (pd), which declined to 33% at 24 h pd."( BL-1020, a novel antipsychotic candidate with GABA-enhancing effects: D2 receptor occupancy study in humans.
Antoni, G; Appel, L; Eriksson, C; Geffen, Y; Heurling, K; Kapur, S, 2009
)
0.35
" Dosing started at 20 mg/d and increased over 7 days to 40 mg/d."( An open-label tolerability study of BL-1020 antipsychotic: a novel gamma aminobutyric acid ester of perphenazine.
Anand, R; Dan, I; Geffen, Y; Vasile, D,
)
0.35
"The objective of this study was to evaluate the impact of once- versus twice-daily dosing of perphenazine, which has a plasma half-life of 8-12 hours, on clinical outcomes in patients with schizophrenia."( Impact of once- versus twice-daily perphenazine dosing on clinical outcomes: an analysis of the CATIE data.
Bies, RR; Fervaha, G; Grönte, D; Remington, G; Suzuki, T; Takeuchi, H; Uchida, H, 2014
)
0.9
" Patients with schizophrenia (DSM-IV) randomly allocated to treatment with perphenazine were also randomly assigned to once-daily (N = 133) or twice-daily (N = 124) dosing and followed over 18 months."( Impact of once- versus twice-daily perphenazine dosing on clinical outcomes: an analysis of the CATIE data.
Bies, RR; Fervaha, G; Grönte, D; Remington, G; Suzuki, T; Takeuchi, H; Uchida, H, 2014
)
0.91
"No significant differences were found in any outcome measures between the once-daily and twice-daily dosing groups, which remained the same when using the mean dose of perphenazine as a covariate."( Impact of once- versus twice-daily perphenazine dosing on clinical outcomes: an analysis of the CATIE data.
Bies, RR; Fervaha, G; Grönte, D; Remington, G; Suzuki, T; Takeuchi, H; Uchida, H, 2014
)
0.87
"Perphenazine is routinely administered in a divided dosage regimen because of its relatively short plasma half-life."( Impact of once- versus twice-daily perphenazine dosing on clinical outcomes: an analysis of the CATIE data.
Bies, RR; Fervaha, G; Grönte, D; Remington, G; Suzuki, T; Takeuchi, H; Uchida, H, 2014
)
2.12
" However, dissolution testing of thin films is challenging since the commonly used dissolution tests for conventional dosage forms correspond rather poorly to the physiological conditions at the site of administration."( Reflectometric monitoring of the dissolution process of thin polymeric films.
Ketolainen, J; Korhonen, K; Laitinen, R; Peiponen, KE; Räty, J, 2017
)
0.46
" In the present study, PPZ-containing solid lipid nanoparticles (PPZ-SLNs) were prepared and optimized based on different factors, including lipid and surfactant amount, to develop appropriate and safe novel oral dosage forms of PPZ."( Development of Perphenazine-Loaded Solid Lipid Nanoparticles: Statistical Optimization and Cytotoxicity Studies.
Farsani, PA; Mahboobian, MM; Mahjub, R; Mohammadi, M; Oliaei, SS, 2021
)
0.97
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
phenothiazine antipsychotic drugnull
dopaminergic antagonistA drug that binds to but does not activate dopamine receptors, thereby blocking the actions of dopamine or exogenous agonists.
antiemeticA drug used to prevent nausea or vomiting. An antiemetic may act by a wide range of mechanisms: it might affect the medullary control centres (the vomiting centre and the chemoreceptive trigger zone) or affect the peripheral 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 (4)

ClassDescription
phenothiazines
N-alkylpiperazine
N-(2-hydroxyethyl)piperazine
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
[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 (124)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency31.62280.003245.467312,589.2998AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency11.38070.004023.8416100.0000AID485290
Chain A, Beta-lactamaseEscherichia coli K-12Potency22.38720.044717.8581100.0000AID485341
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.23410.631035.7641100.0000AID504339
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency35.48130.125919.1169125.8920AID2549
endonuclease IVEscherichia coliPotency6.30960.707912.432431.6228AID1708
acetylcholinesteraseHomo sapiens (human)Potency27.54040.002541.796015,848.9004AID1347398
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
phosphopantetheinyl transferaseBacillus subtilisPotency50.11870.141337.9142100.0000AID1490
RAR-related orphan receptor gammaMus musculus (house mouse)Potency15.55670.006038.004119,952.5996AID1159521; AID1159523
Fumarate hydrataseHomo sapiens (human)Potency35.48130.00308.794948.0869AID1347053
NFKB1 protein, partialHomo sapiens (human)Potency15.84890.02827.055915.8489AID895; AID928
GLS proteinHomo sapiens (human)Potency25.11890.35487.935539.8107AID624146
TDP1 proteinHomo sapiens (human)Potency17.61410.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency9.28280.000714.592883.7951AID1259369; AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency12.64500.180013.557439.8107AID1460
ThrombopoietinHomo sapiens (human)Potency15.84890.02517.304831.6228AID917; AID918
AR proteinHomo sapiens (human)Potency33.49150.000221.22318,912.5098AID1259243; AID1259247
Smad3Homo sapiens (human)Potency25.11890.00527.809829.0929AID588855
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency31.62280.707912.194339.8107AID720542
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.49150.013326.981070.7614AID1346978
thyroid stimulating hormone receptorHomo sapiens (human)Potency15.84890.001318.074339.8107AID926; AID938
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency19.96820.000657.913322,387.1992AID1259377; AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency33.49150.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency33.49150.000417.946075.1148AID1346784; AID1346795
regulator of G-protein signaling 4Homo sapiens (human)Potency23.77810.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency7.79960.01237.983543.2770AID1346984; AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.84930.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency5.74790.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency31.67040.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency33.48890.375827.485161.6524AID743217
pregnane X nuclear receptorHomo sapiens (human)Potency10.59090.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency1.02100.000229.305416,493.5996AID743075
cytochrome P450 2D6Homo sapiens (human)Potency0.02750.00108.379861.1304AID1645840
polyproteinZika virusPotency35.48130.00308.794948.0869AID1347053
67.9K proteinVaccinia virusPotency11.67660.00018.4406100.0000AID720579; AID720580
glucocerebrosidaseHomo sapiens (human)Potency23.94010.01268.156944.6684AID2101
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency25.11890.707936.904389.1251AID504333
caspase-3Homo sapiens (human)Potency33.49150.013326.981070.7614AID1346978
IDH1Homo sapiens (human)Potency20.59620.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency23.44550.035520.977089.1251AID504332
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency58.47890.016525.307841.3999AID602332
aryl hydrocarbon receptorHomo sapiens (human)Potency12.05180.000723.06741,258.9301AID743085; AID743122
thyroid stimulating hormone receptorHomo sapiens (human)Potency30.82810.001628.015177.1139AID1224895; AID1259385; AID1259395
activating transcription factor 6Homo sapiens (human)Potency21.31380.143427.612159.8106AID1159516
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency23.24560.057821.109761.2679AID1159526; AID1159528
Caspase-7Cricetulus griseus (Chinese hamster)Potency33.49150.006723.496068.5896AID1346980
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.11550.00207.533739.8107AID891
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.04790.01262.451825.0177AID485313
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency47.754823.934123.934123.9341AID1967
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.92440.316212.443531.6228AID902; AID924
cytochrome P450 2C19 precursorHomo sapiens (human)Potency3.16230.00255.840031.6228AID899
D(1A) dopamine receptorHomo sapiens (human)Potency6.28930.02245.944922.3872AID488981; AID488982; AID488983
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency70.79460.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency31.62280.006026.168889.1251AID488953
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency3.57170.01789.637444.6684AID588834
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency25.11890.794321.275750.1187AID624246
caspase-3Cricetulus griseus (Chinese hamster)Potency33.49150.006723.496068.5896AID1346980
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency5.38330.000323.4451159.6830AID743065; AID743067
mitogen-activated protein kinase 1Homo sapiens (human)Potency24.92910.039816.784239.8107AID1454; AID995
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency16.48160.00669.809418.4927AID1347050
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency12.58930.65619.452025.1189AID927
ras-related protein Rab-9AHomo sapiens (human)Potency73.07800.00022.621531.4954AID485297
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency19.86840.00378.618923.2809AID2660; AID2667; AID2668
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency33.48890.000627.21521,122.0200AID743202
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency15.84890.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency21.04610.004611.374133.4983AID463097; AID504364; AID624296; AID624297
VprHuman immunodeficiency virus 1Potency12.58931.584919.626463.0957AID651644
survival motor neuron protein isoform dHomo sapiens (human)Potency1.60820.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency2.51190.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency25.98090.177824.735279.4328AID488949
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency19.95260.09120.09120.0912AID488979
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency15.58640.00106.000935.4813AID943; AID944
lethal factor (plasmid)Bacillus anthracis str. A2012Potency25.11890.020010.786931.6228AID912
lamin isoform A-delta10Homo sapiens (human)Potency16.31850.891312.067628.1838AID1459; AID1487
neuropeptide S receptor isoform AHomo sapiens (human)Potency17.55950.015812.3113615.5000AID1461
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency10.86310.316212.765731.6228AID881
Integrin beta-3Homo sapiens (human)Potency15.84890.316211.415731.6228AID924
Integrin alpha-IIbHomo sapiens (human)Potency15.84890.316211.415731.6228AID924
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency10.86310.00638.235039.8107AID881
D(1A) dopamine receptorSus scrofa (pig)Potency26.12160.00378.108123.2809AID2667
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency14.12540.009610.525035.4813AID1479145
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency12.58931.584913.004325.1189AID927
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency35.48133.981146.7448112.2020AID720708
GABA theta subunitRattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
Ataxin-2Homo sapiens (human)Potency14.12540.011912.222168.7989AID588378
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency2.51191.000012.224831.6228AID885
[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)
NADPH oxidase 1Homo sapiens (human)IC50 (µMol)17.00000.04401.26095.5000AID2808
ubiquitin-conjugating enzyme E2 NHomo sapiens (human)IC50 (µMol)14.79000.873010.721978.4000AID493155; AID493182
bcl-2-related protein A1Mus musculus (house mouse)IC50 (µMol)20.00000.41907.756335.1000AID504689
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Aldehyde oxidase 1Mus musculus (house mouse)IC50 (µMol)6.10000.15002.25006.1000AID547839
Bile salt export pumpHomo sapiens (human)IC50 (µMol)100.94670.11007.190310.0000AID1443980; AID1449628; AID1473738
Retinal dehydrogenase 1Homo sapiens (human)IC50 (µMol)0.52420.02001.04766.7900AID1809349
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)10.60000.00002.800510.0000AID1210069
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC50 (µMol)4.21600.00001.612910.0000AID625171
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki3.45410.00042.03378.6606AID625171
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)0.00030.00000.74728.0000AID750642
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC50 (µMol)1.40001.30003.37279.6000AID581672
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki0.02300.00030.380610.0000AID6677
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)10.60000.01202.53129.4700AID1210069
Aldehyde oxidaseHomo sapiens (human)IC50 (µMol)0.03300.00230.63203.3000AID547838
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)4.21600.00091.901410.0000AID625171
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki3.45410.00211.840710.0000AID625171
Aldehyde oxidase 1Macaca fascicularis (crab-eating macaque)IC50 (µMol)3.60000.11001.40333.6000AID547843
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC50 (µMol)4.21600.10482.83988.3173AID625171
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki3.45410.08582.95428.6606AID625171
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Aldehyde oxidase 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.74000.19001.90606.4000AID547840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Snq2pSaccharomyces cerevisiae EC1118INH13.10003.20006.26008.8000AID581808
protein AF-9 isoform aHomo sapiens (human)AC5012.41000.08008.380217.9800AID720495
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC5013.94000.150012.066235.2100AID652116
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH6.40004.20006.18338.3000AID581806
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (326)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
retinoid metabolic processRetinal dehydrogenase 1Homo sapiens (human)
cellular aldehyde metabolic processRetinal dehydrogenase 1Homo sapiens (human)
gamma-aminobutyric acid biosynthetic processRetinal dehydrogenase 1Homo sapiens (human)
fructosamine catabolic processRetinal dehydrogenase 1Homo sapiens (human)
maintenance of lens transparencyRetinal dehydrogenase 1Homo sapiens (human)
retinol metabolic processRetinal dehydrogenase 1Homo sapiens (human)
cellular detoxification of aldehydeRetinal dehydrogenase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisRetinal dehydrogenase 1Homo sapiens (human)
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
smooth muscle contraction5-hydroxytryptamine receptor 7Homo sapiens (human)
circadian rhythm5-hydroxytryptamine receptor 7Homo sapiens (human)
blood circulation5-hydroxytryptamine receptor 7Homo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 7Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 7Homo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
lipid metabolic processAldehyde oxidaseHomo sapiens (human)
xenobiotic metabolic processAldehyde oxidaseHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (119)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
retinal dehydrogenase activityRetinal dehydrogenase 1Homo sapiens (human)
aldehyde dehydrogenase (NAD+) activityRetinal dehydrogenase 1Homo sapiens (human)
GTPase activator activityRetinal dehydrogenase 1Homo sapiens (human)
androgen bindingRetinal dehydrogenase 1Homo sapiens (human)
protein bindingRetinal dehydrogenase 1Homo sapiens (human)
aminobutyraldehyde dehydrogenase activityRetinal dehydrogenase 1Homo sapiens (human)
glyceraldehyde-3-phosphate dehydrogenase (NAD+) (non-phosphorylating) activityRetinal dehydrogenase 1Homo sapiens (human)
NAD bindingRetinal dehydrogenase 1Homo sapiens (human)
3-deoxyglucosone dehydrogenase activityRetinal dehydrogenase 1Homo sapiens (human)
benzaldehyde dehydrogenase (NAD+) activityRetinal dehydrogenase 1Homo sapiens (human)
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
aldehyde oxidase activityAldehyde oxidaseHomo sapiens (human)
iron ion bindingAldehyde oxidaseHomo sapiens (human)
identical protein bindingAldehyde oxidaseHomo sapiens (human)
protein homodimerization activityAldehyde oxidaseHomo sapiens (human)
molybdopterin cofactor bindingAldehyde oxidaseHomo sapiens (human)
flavin adenine dinucleotide bindingAldehyde oxidaseHomo sapiens (human)
NAD bindingAldehyde oxidaseHomo sapiens (human)
2 iron, 2 sulfur cluster bindingAldehyde oxidaseHomo sapiens (human)
FAD bindingAldehyde oxidaseHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (78)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
cytoplasmRetinal dehydrogenase 1Homo sapiens (human)
cytosolRetinal dehydrogenase 1Homo sapiens (human)
axonRetinal dehydrogenase 1Homo sapiens (human)
synapseRetinal dehydrogenase 1Homo sapiens (human)
extracellular exosomeRetinal dehydrogenase 1Homo sapiens (human)
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
trans-Golgi network membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
synapse5-hydroxytryptamine receptor 7Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolAldehyde oxidaseHomo sapiens (human)
extracellular exosomeAldehyde oxidaseHomo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (288)

Assay IDTitleYearJournalArticle
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
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.
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.
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.
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.
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.
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.
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.
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.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
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.
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.
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.
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.
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.
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.
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.
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
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1508612NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Highly predictive and interpretable models for PAMPA permeability.
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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
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.
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.
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.
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).
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID395327Dissociation constant, pKa by capillary electrophoresis2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID547843Inhibition of monkey aldehyde oxidase2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID103232Anti MDR activity was expressed as MDR ratio or MDR fold reversal in doxorubicin resistant human breast carcinoma tumor cell line MCF-7/DOX1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
Molecular modeling of phenothiazines and related drugs as multidrug resistance modifiers: a comparative molecular field analysis study.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1553362Inhibition of protein phosphatase 2A in mouse FL5.12 cells assessed as induction of surface nutrient transporter loss by measuring downregulation of CD98 expression level at 10 uM preincubated with PP2A inhibitor calyculin A for 60 mins followed by compou2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Design, synthesis and anticancer activity of constrained sphingolipid-phenoxazine/phenothiazine hybrid constructs targeting protein phosphatase 2A.
AID23961logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1364923Cytotoxicity against BHK cells assessed as reduction in cell viability after 48 hrs in presence of ATP by Celltiter-Glo luminescent assay2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
The medicinal chemistry of Chikungunya virus.
AID475504Binding affinity to amyloid beta (1 to 42) fibrils by change in fluorescence at 100 uM after 10 mins2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta.
AID581806Inhibition of Saccharomyces cerevisiae MKPDR5h multidrug transporter Pdr5p assessed as concentration required to threefold increase in rate of fluorescence signal relative to absence of inhibitor by fluorescein diacetate based high-throughput screening sp2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
New high-throughput screening assay to reveal similarities and differences in inhibitory sensitivities of multidrug ATP-binding cassette transporters.
AID1210070Inhibition of CYP2D6 in human liver microsomes using bufuralol substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1663685Induction of apoptosis in progesterone-sensitive human Ishikawa cells assessed as late apoptotic cells at 10 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 3.56%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID383685Inhibition of D-amphetamine-induced hyperactivity in Wistar rat at 2.5 mg/kg, po2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1809332Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1663675Potency index, ratio of medroxyprogesterone acetate IC50 to test compound IC50 for antiproliferative activity against human KLE cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1663674Potency index, ratio of medroxyprogesterone acetate IC50 to test compound IC50 for antiproliferative activity against human Ishikawa cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
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.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1148005Octanol-water partition coefficient, log P of the compound1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Quantitative correlations between albumin binding constants and chromatographic Rm values of phenothiazine derivatives.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID547840Inhibition of rat aldehyde oxidase2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.
AID1148003Dissociation constant, pKa of the compound by UV-visible spectrophotometer analysis1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Quantitative correlations between albumin binding constants and chromatographic Rm values of phenothiazine derivatives.
AID1210074Inhibition of CYP1A2 in human liver microsomes using phenacetin substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1663671Antiproliferative activity against human Hec1A cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID25603Dissociation constant was reported1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Side-chain effects on phenothiazine cation radical reactions.
AID1148004Oleyl alcohol-water partition coefficient, Rm of the compound measured at 0% methanol by reverse-phase thin layer chromatography1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Quantitative correlations between albumin binding constants and chromatographic Rm values of phenothiazine derivatives.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1663676Potency index, ratio of medroxyprogesterone acetate IC50 to test compound IC50 for antiproliferative activity against human Hec1A cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID310931Partition coefficient, log P of the compound2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities.
AID1663680Inhibition of colony formation in progesterone resistant human KLE cells2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1663697Induction of apoptosis in progesterone-resistant human KLE cells after 48 hrs by Annexin-V/PI staining based flow cytometry2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1663688Induction of apoptosis in progesterone-sensitive human Ishikawa cells assessed as late apoptotic cells at 20 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 3.56%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID383674Increase in prolactin level in Wistar rat plasma at 5 mg/kg, ip after 2 hrs relative to control2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects.
AID310933Permeability across PAMPA membrane after 7 hrs2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities.
AID1663689Induction of apoptosis in progesterone-sensitive human Ishikawa cells assessed as necrotic cells at 20 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 1.21%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1553360Inhibition of protein phosphatase 2A in mouse FL5.12 cells assessed as reduction in cell viability incubated for 48 hrs by propidium iodide staining based flow cytometric analysis2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Design, synthesis and anticancer activity of constrained sphingolipid-phenoxazine/phenothiazine hybrid constructs targeting protein phosphatase 2A.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID322958Inhibition of synthetic amyloid beta-42 fibrillation by light scattering analysis relative to control2007The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14
Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID547838Inhibition of human aldehyde oxidase2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.
AID1663693Induction of apoptosis in progesterone-resistant human KLE cells assessed as early apoptotic cells at 20 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 2.85%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID581672Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
New high-throughput screening assay to reveal similarities and differences in inhibitory sensitivities of multidrug ATP-binding cassette transporters.
AID26518Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1663673Antiproliferative activity against human AN3CA cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID322955Inhibition of synthetic amyloid beta-42 oligomerization by ELISA2007The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14
Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1210072Inhibition of CYP2C9 in human liver microsomes using tolbutamide substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID395329Dissociation constant, pKa by mass spectrometry2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1663698Inhibition of AKT phosphorylation at ser 473 residue in human Ishikawa cells at 20 uM after 48 hrs by Western blot analysis2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1809336Resistant factor, ratio of IC50 for antiproliferative activity against drug-tolerant human MDA-MB-231 cells to IC50 for human MDA-MB-231 cells
AID1663703Toxicity in mouse xenografted with human Ishikawa cells assessed as effect on body weight at 3 to 15 mg/kg after 28 days2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID186205Log (1/ED50) was measured as histamine releasing activity in rat mast cells; log(1/ED50*10e-3).1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1663678Potency index, ratio of medroxyprogesterone acetate IC50 to test compound IC50 for antiproliferative activity against human AN3CA cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1663669Antiproliferative activity against human Ishikawa cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1553364Induction of vacuolation in mouse FL5.12 cells assessed as vacuolation score at 2.5 uM preincubated with PP2A inhibitor calyculin A for 60 mins followed by compound addition and measured after 2 hrs by fluorescence microscopic method2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Design, synthesis and anticancer activity of constrained sphingolipid-phenoxazine/phenothiazine hybrid constructs targeting protein phosphatase 2A.
AID1663677Potency index, ratio of medroxyprogesterone acetate IC50 to test compound IC50 for antiproliferative activity against human HEC1B cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID521210Ratio of EC50 for mouse astrocytes to EC50 for 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.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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.
AID1663679Inhibition of colony formation in progesterone sensitive human Ishikawa cells2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID135326BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID1210073Inhibition of CYP2C19 in human liver microsomes using omeprazole substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID322957Inhibition of synthetic amyloid beta-42 fibrillation by ThT fluorescence analysis relative to control2007The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14
Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
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.
AID120997Compound was tested at subtoxic dose of 25 mg/kg in mice; Symptoms are hyperactivity, irritability, stereotypy.2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization.
AID194149Apparent partition coefficient was measured as histamine releasing activity in rat mast cells.1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID19262Aqueous solubility2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Prediction of drug solubility from Monte Carlo simulations.
AID1809331Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
AID26396Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1148006Binding affinity to bovine serum albumin by circular dichroic probe technique1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Quantitative correlations between albumin binding constants and chromatographic Rm values of phenothiazine derivatives.
AID581808Inhibition of Saccharomyces cerevisiae MKSNQ2h multidrug transporter Snq2p assessed as concentration required to threefold increase in rate of fluorescence signal relative to absence of inhibitor by fluorescein diacetate based high-throughput screening sp2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
New high-throughput screening assay to reveal similarities and differences in inhibitory sensitivities of multidrug ATP-binding cassette transporters.
AID521209Antiproliferative activity against mouse astrocyte cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID750643Antagonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response at 10 uM incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR ass2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID1663682Antimigratory activity against progesterone sensitive human Ishikawa cells assessed as inhibition of cell migration at 10 uM after 48 hrs by transwell assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
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.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID547621Cytotoxicity against BESM cells after 88 hrs by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1663699Inhibition of AKT phosphorylation at ser 473 residue in human KLE cells at 20 uM after 48 hrs by Western blot analysis2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1663690Induction of apoptosis in progesterone-resistant human KLE cells assessed as early apoptotic cells at 10 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 2.85%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID547622Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID475505Binding affinity to amyloid beta (1 to 42) oligomers by change in fluorescence at 100 uM after 10 mins2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta.
AID1663692Induction of apoptosis in progesterone-resistant human KLE cells assessed as necrotic cells at 10 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 1.30%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1765968Inhibition of Leishmania Trypanothione reductase
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1809349Inhibition of ALDH1A1 in human drug-tolerant MDA-MB-231/lapatinib cells assessed as after 24 hrs
AID23971logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID383672Increase in prolactin level in Wistar rat plasma at 5 mg/kg, ip after 1 hr relative to control2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects.
AID146870The compound was tested for its ability to inhibit Na+/K+ ATPase in rat brain.1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID416533Acute toxicity in NMRI mouse assessed as behavioral changes at 5 mg/kg, ip by CNS activity test2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.
AID1663696Induction of apoptosis in progesterone-sensitive human Ishikawa cells after 48 hrs by Annexin-V/PI staining based flow cytometry2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1210071Inhibition of CYP3A4 in human liver microsomes using testosterone substrate by LC-MS/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID42111BSA binding (log K)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1553361Inhibition of protein phosphatase 2A in mouse FL5.12 cells assessed as induction of surface nutrient transporter loss by measuring downregulation of CD98 expression level at 2.5 uM preincubated with PP2A inhibitor calyculin A for 60 mins followed by compo2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Design, synthesis and anticancer activity of constrained sphingolipid-phenoxazine/phenothiazine hybrid constructs targeting protein phosphatase 2A.
AID1663683Antimigratory activity against progesterone-resistant human KLE cells assessed as reduction in cell migration at 10 uM after 48 hrs by transwell assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1809334Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay
AID395326Fraction unbound in rat brain2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID750642Antagonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics.
AID383681Toxicity assessed as induction of cataleptic extrapyramidal symptoms in orally dosed Wistar rat by wall descending test2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID6677Binding affinity towards human 5-hydroxytryptamine 7 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID1663691Induction of apoptosis in progesterone-resistant human KLE cells assessed as late apoptotic cells at 10 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 3.56%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1663670Antiproliferative activity against human KLE cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1663686Induction of apoptosis in progesterone-sensitive human Ishikawa cells assessed as necrotic cells at 10 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 1.21%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID26297Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1663694Induction of apoptosis in progesterone-resistant human KLE cells assessed as late apoptotic cells at 20 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 3.56%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1663702Antitumor activity against human Ishikawa cells xenografted in mouse assessed as tumor growth inhibition at 15 mg/kg measured after 28 days relative to control2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID547804Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID26520Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1663701Antitumor activity against human Ishikawa cells xenografted in mouse assessed as tumor growth inhibition at 3 mg/kg measured after 28 days relative to control2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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.
AID524793Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1663684Induction of apoptosis in progesterone-sensitive human Ishikawa cells assessed as early apoptotic cells at 10 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 1.92%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1553365Induction of vacuolation in mouse FL5.12 cells assessed as vacuolation score at 10 uM preincubated with PP2A inhibitor calyculin A for 60 mins followed by compound addition and measured after 2 hrs by fluorescence microscopic method2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Design, synthesis and anticancer activity of constrained sphingolipid-phenoxazine/phenothiazine hybrid constructs targeting protein phosphatase 2A.
AID1283268Inhibition of delta 8-7 isomerase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID1809333Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay
AID547839Inhibition of mouse aldehyde oxidase2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.
AID1283269Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1364913Antiviral activity against Chikungunya virus LR2006 OPY1 infected in BHK cells measured at 14 hrs post infection by luciferase reporter gene assay2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
The medicinal chemistry of Chikungunya virus.
AID521208Antiproliferative activity against 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.
AID383676Toxicity assessed as induction of cataleptic extrapyramidal symptoms in Wistar rat at 5 mg/kg, ip after 2 hrs by wall descending test2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID581807Inhibition of Saccharomyces cerevisiae MKCDR1h multidrug transporter Cdr1p assessed as concentration required to threefold increase in rate of fluorescence signal relative to absence of inhibitor by fluorescein diacetate based high-throughput screening sp2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
New high-throughput screening assay to reveal similarities and differences in inhibitory sensitivities of multidrug ATP-binding cassette transporters.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1663695Induction of apoptosis in progesterone-resistant human KLE cells assessed as necrotic cells at 20 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 1.30%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1663687Induction of apoptosis in progesterone-sensitive human Ishikawa cells assessed as early apoptotic cells at 20 uM after 48 hrs by Annexin-V/PI staining based flow cytometry (Rvb = 1.92%)2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID1663672Antiproliferative activity against human HEC1B cells assessed as inhibition of cell viability by CCK8 assay2020Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14
Repurposing of antipsychotics perphenazine for the treatment of endometrial cancer.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1364924Selectivity index, ratio of CC50 for BHK cells to IC50 for Chikungunya virus LR2006 OPY12017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
The medicinal chemistry of Chikungunya virus.
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.
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.
AID1345788Human D2 receptor (Dopamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID624223Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1994The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)2005Psychopharmacology, May, Volume: 179, Issue:2
Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)2005Psychopharmacology, May, Volume: 179, Issue:2
Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1994The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors.
AID1346037Human H1 receptor (Histamine receptors)2003Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3
H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.
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.
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,546)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901114 (72.06)18.7374
1990's142 (9.18)18.2507
2000's140 (9.06)29.6817
2010's118 (7.63)24.3611
2020's32 (2.07)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 72.16

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 Index72.16 (24.57)
Research Supply Index7.55 (2.92)
Research Growth Index4.34 (4.65)
Search Engine Demand Index129.42 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (72.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials243 (14.59%)5.53%
Reviews46 (2.76%)6.00%
Case Studies130 (7.80%)4.05%
Observational1 (0.06%)0.25%
Other1,246 (74.79%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (22)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Networked Drug REpurposing for Mechanism-based neuroPrOtection in Ischaemic STROKE (REPO-STROKE IIa) [NCT05762146]Phase 228 participants (Anticipated)Interventional2022-09-05Recruiting
A Twelve-Month, Prospective, Randomized, Active-Controlled, Open-Label, Flexible-Dose Study of Paliperidone Palmitate Compared With Oral Antipsychotic Treatment in Adults With Schizophrenia Who Have Been Recently Discharged From an Inpatient Psychiatric H [NCT01193166]Phase 40 participants (Actual)Interventional2010-08-31Withdrawn(stopped due to This study was stopped due to an internal reconsideration of priorities of the product portfolio.)
Clinical Evaluation in Healthy Volunteers of Potential syneRgistic Vascular Effects of PrOpylthiouracil, Riociguat, and Perphenazine a Possible STROKE Medication [NCT04776499]Phase 18 participants (Actual)Interventional2021-03-18Completed
Randomized, Embedded, Multifactorial Adaptive Platform for Perioperative Medicine at UPMC (UPMC REMAP): Core Protocol - Enhanced Recovery Protocols (ERP) [NCT04606264]Phase 32,500 participants (Anticipated)Interventional2023-05-15Recruiting
Evaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics for the Prevention of Relapse in Long-term Stabilized Schizophrenic Patients: a Randomized, Single-blind, Longitudinal Trial [NCT02307396]Phase 421 participants (Actual)Interventional2015-02-01Completed
A Prospective, Matched-Control, Randomized, Open-Label, Flexible-Dose, Study in Subjects With Recent-Onset Schizophrenia or Schizophreniform Disorder to Compare Disease Progression and Disease Modification Following Treatment With Paliperidone Palmitate L [NCT02431702]Phase 3337 participants (Actual)Interventional2015-07-08Completed
Atypical Antipsychotics and Hyperglycemic Emergencies: Multicentre, Retrospective Cohort Study of Administrative Data [NCT02582736]725,489 participants (Actual)Observational2012-04-30Completed
A Double-Blind, Controlled Study of Aripiprazole in Co-Morbid Schizophrenia and Cocaine Dependence [NCT00737256]Phase 244 participants (Anticipated)Interventional2008-08-31Recruiting
A 12-Month Randomized, Open-Label Study of Caregiver Psycho-education and Skills Training in Patients Recently Diagnosed With Schizophrenia, Schizoaffective Disorder, or Schizophreniform Disorder and Receiving Paliperidone Palmitate or Oral Antipsychotic [NCT02600741]296 participants (Actual)Observational2015-07-24Completed
Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies [NCT02893371]1,037,352 participants (Actual)Observational2016-09-30Completed
A Fifteen-month, Prospective, Randomized, Active-controlled, Open-label, Flexible Dose Study of Paliperidone Palmitate Compared With Oral Antipsychotic Treatment in Delaying Time to Treatment Failure in Adults With Schizophrenia Who Have Been Incarcerated [NCT01157351]Phase 4450 participants (Actual)Interventional2010-05-31Completed
Serotonergic Pharmacotherapy for Agitation of Dementia [NCT00009204]Phase 30 participants Interventional1995-09-30Completed
Antipsychotic Polypharmacy in Schizophrenia [NCT00493233]100 participants (Anticipated)Interventional2006-11-30Completed
An Open-label, Multi-center, 6-week, Sequential Cohort Study Designed to Determine the Safety and Tolerability of Two Dose Ranges of BL-1020 in Hospitalized Subjects With Chronic Schizophrenia or Schizo-affective Disorder [NCT00480571]Phase 290 participants (Anticipated)Interventional2007-06-30Completed
[NCT00480246]Phase 10 participants Interventional2007-05-31Completed
Comparative Effectiveness of Antipsychotic Medications in Patients With Schizophrenia (CATIE Schizophrenia Trial) [NCT00014001]Phase 41,600 participants Interventional2000-12-31Completed
Randomized Multicentric Open-label Phase III Clinical Trial to Evaluate the Efficacy of Continual Treatment Versus Discontinuation Based in the Presence of Prodromes in a First Episode of Non-affective Psychosis. [NCT01765829]Phase 3104 participants (Anticipated)Interventional2012-11-30Recruiting
Correlation Between Cognitive Function and Relapse of Schizophrenia Regarding Dose Reduction in Patients Undergoing High-dose Antipsychotic Therapy [NCT03019887]139 participants (Actual)Interventional2011-04-30Completed
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
Lurasidone Effects on Tissue Glutamate in Schizophrenia [NCT02199743]Phase 435 participants (Actual)Interventional2013-02-28Completed
Comparison of Optimal Antipsychotic Treatments for Schizophrenia Pilot Study [NCT00802100]Phase 421 participants (Actual)Interventional2008-12-31Completed
Improving Metabolic Parameters of Antipsychotic Child Treatment (IMPACT) [NCT00806234]Phase 4127 participants (Actual)Interventional2009-01-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00802100 (2) [back to overview]Feasibility of Randomizing a Cohort of Participants Meeting the Inclusion and Exclusion Criteria of the Study
NCT00802100 (2) [back to overview]Antipsychotic Efficacy, Defined as Completion of the Trial Without Psychiatric Hospitalization, Clinician Decision to Discontinue Treatment, or Patient Decision to Discontinue Treatment
NCT00806234 (4) [back to overview]Triglyceride Levels
NCT00806234 (4) [back to overview]Body Mass Index (BMI) Z-score Change
NCT00806234 (4) [back to overview]Change in Low Density Lipoprotein (LDL) Cholesterol Level
NCT00806234 (4) [back to overview]Change in Whole Body Insulin Sensitivity Index
NCT01157351 (6) [back to overview]Change From Baseline in Clinical Global Impression - Severity (CGI-S) Score During Overall Treatment Duration
NCT01157351 (6) [back to overview]Change From Baseline in Personal and Social Performance (PSP) Total Score During Overall Treatment Duration
NCT01157351 (6) [back to overview]Time to First Psychiatric Hospitalization
NCT01157351 (6) [back to overview]Time to First Psychiatric Hospitalization or Arrest/Incarceration
NCT01157351 (6) [back to overview]Percentage of Participants in Each Event Category of First Treatment Failure
NCT01157351 (6) [back to overview]Time to First Treatment Failure
NCT02199743 (2) [back to overview]Brief Assessments of Cognition in Schizophrenia Scores (BACS)
NCT02199743 (2) [back to overview]Cerebral Glutamate Levels
NCT02431702 (31) [back to overview]Part 3 (Disease Modification): Personal and Social Performance (PSP) Total Observed Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Attention/Vigilance Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Reasoning and Problem Solving: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Social Cognition Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Speed of Processing Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Total Score
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Visual Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Working Memory Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Time to First Treatment Failure
NCT02431702 (31) [back to overview]Part 3 (Extended Disease Progression [EDP]): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score
NCT02431702 (31) [back to overview]Part-2 (Disease Progression): Time to First Treatment Failure
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by Clinician-Rated Dimensions of Psychosis Symptom Severity Scale (CRDPSS)
NCT02431702 (31) [back to overview]Part 3 (EDP): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by CRDPSS
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Adjusted Intracortical Myelin (ICM) Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Attention/Vigilance Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Reasoning and Problem Solving: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Social Cognition Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Speed of Processing Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (EDP): Change From Baseline in Verbal Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Verbal Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Visual Learning Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 2 (Disease Progression): Change From Baseline in Working Memory Score: MCCB Domain
NCT02431702 (31) [back to overview]Part 3 (Disease Modification): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (SE MRI)
NCT02431702 (31) [back to overview]Part 3 (Disease Modification): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score
NCT03019887 (1) [back to overview]Number of Participants With Relapse

Feasibility of Randomizing a Cohort of Participants Meeting the Inclusion and Exclusion Criteria of the Study

Goal was to randomize 60 participants who met eligibility criteria. (NCT00802100)
Timeframe: Baseline

Interventionparticipants (Number)
Overall Study21

[back to top]

Antipsychotic Efficacy, Defined as Completion of the Trial Without Psychiatric Hospitalization, Clinician Decision to Discontinue Treatment, or Patient Decision to Discontinue Treatment

(NCT00802100)
Timeframe: Measured over 28 weeks of study visits

,,
Interventionparticipants (Number)
InefficacyUnacceptable side effectsPatient refusalDrop-out, no information availableAdministrativeCompleted trial without discontinuing
Aripiprazole100032
Olanzapine003210
Perphenazine100152

[back to top]

Triglyceride Levels

(NCT00806234)
Timeframe: Change from baseline to 24 weeks

Interventionmg/dL (Least Squares Mean)
Healthy Lifestyle Information0.2
Switch Treatment + Healthy Lifestyle Instruction16.6
Metformin Treatment + Healthy Lifestyle Instruction14.7

[back to top]

Body Mass Index (BMI) Z-score Change

(NCT00806234)
Timeframe: Change from baseline to 24 weeks

InterventionZ Score (Least Squares Mean)
Healthy Lifestyle Information0.040
Switch Treatment + Healthy Lifestyle Instruction-0.112
Metformin Treatment + Healthy Lifestyle Instruction-0.088

[back to top]

Change in Low Density Lipoprotein (LDL) Cholesterol Level

(NCT00806234)
Timeframe: From Baseline to Week 24

Interventionmg/dL (Least Squares Mean)
Healthy Lifestyle Information3.6
Switch Treatment + Healthy Lifestyle Instruction-8.1
Metformin Treatment + Healthy Lifestyle Instruction-4.1

[back to top]

Change in Whole Body Insulin Sensitivity Index

(NCT00806234)
Timeframe: Change from baseline to 24 weeks

InterventionmU/L (Least Squares Mean)
Healthy Lifestyle Information0.74
Switch Treatment + Healthy Lifestyle Instruction0.42
Metformin Treatment + Healthy Lifestyle Instruction-0.34

[back to top]

Change From Baseline in Clinical Global Impression - Severity (CGI-S) Score During Overall Treatment Duration

The CGI-S rating scale was a 7-point global assessment of symptom severity with scores determined by clinician as follows: 1=Not ill, 2=Very Mild, 3= Mild, 4= Moderate, 5= Marked, 6= Severe, and 7= Extremely Severe. The higher the score the worse the illness. (NCT01157351)
Timeframe: Baseline up to Month 15

InterventionUnits on a scale (Least Squares Mean)
Paliperidone Palmitate-0.48
Oral Antipsychotics-0.43

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Change From Baseline in Personal and Social Performance (PSP) Total Score During Overall Treatment Duration

The PSP score assesses the degree of difficulty a participant exhibit over a 1 month period within 4 domains of behavior: a) socially useful activities, b) personal and social relationships, c) self-care, and d) disturbing and aggressive behavior. The investigators rate participants' degree of difficulty in each of the 4 domains using a 6-point Likert scale (from 0=absent to 5=very severe). The domain ratings were then transformed to PSP total score ranging from 1 to 100. Higher PSP total scores denote better functioning. A score between 71 and 100 represents normal to mild degree of dysfunction; a score between 31 and 70 represents varying degree of difficulty; and a score <=30 represents poor function that requires intensive supervision. (NCT01157351)
Timeframe: Baseline up to Month 15

InterventionUnits on a scale (Least Squares Mean)
Paliperidone Palmitate5.75
Oral Antipsychotics5.36

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Time to First Psychiatric Hospitalization

"A time-to parameter looking only at 1 component event of treatment failure: psychiatric hospitalization. Time to first psychiatric hospitalization was admission date of the psychiatric hospitalization recorded in the Assessment of Treatment Failure - Psychiatric Hospitalization." (NCT01157351)
Timeframe: From date of randomization up to Month 15

InterventionDays (Median)
Paliperidone PalmitateNA
Oral AntipsychoticsNA

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Time to First Psychiatric Hospitalization or Arrest/Incarceration

A time to parameter looking only at 2 component events of treatment failure: arrest or incarceration, and psychiatric hospitalization. An arrest was defined as the taking of a participant into custody by legal authority, for any reason. Incarceration was defined as involuntary confinement by an officer of the law. Psychiatric hospitalization was an inpatient psychiatric hospitalization that occurred due to the participant's clinically significant worsening of symptoms of schizophrenia. (NCT01157351)
Timeframe: From date of randomization up to Month 15

InterventionDays (Median)
Paliperidone PalmitateNA
Oral Antipsychotics274

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Percentage of Participants in Each Event Category of First Treatment Failure

First treatment failure was a composite endpoint consisting of any of the following events: arrest/incarceration, psychiatric hospitalization, discontinuation (D/C) of antipsychotic treatment due to safety or tolerability, treatment supplementation with another antipsychotic due to inadequate efficacy, discontinuation of antipsychotic treatment due to inadequate efficacy, increase in level of psychiatric services to prevent imminent psychiatric hospitalization, suicide. A Treatment Failure Event Monitoring Board (EMB), blinded to individual participant treatment assignment, determined the occurrence and date of the first treatment failure event. Percentage of participants who experienced treatment failure due to any event and for each specific category of event were assessed. (NCT01157351)
Timeframe: From date of randomization up to Month 15

,
Interventionpercentage of participants (Number)
Treatment Failure Due to Any EventArrest/incarcerationPsychiatric hospitalizationD/C due to safety/tolerabilityTreatment supplementationD/C due to inadequate efficacyIncrease in level of psychiatric servicesSuicide
Oral Antipsychotics53.729.411.93.72.84.11.80
Paliperidone Palmitate39.821.28.06.62.20.41.30

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Time to First Treatment Failure

Time to first treatment failure was the time from participant randomization to the first treatment failure, which was a composite endpoint consisting of any of the following events: arrest/incarceration, psychiatric hospitalization, discontinuation of antipsychotic treatment due to safety or tolerability, treatment supplementation with another antipsychotic due to inadequate efficacy, discontinuation of antipsychotic treatment due to inadequate efficacy, increase in level of psychiatric services to prevent imminent psychiatric hospitalization, suicide. A Treatment Failure Event Monitoring Board (EMB), blinded to individual participant treatment assignment, determined the occurrence and date of the first treatment failure event. (NCT01157351)
Timeframe: From date of randomization up to Month 15

InterventionDays (Median)
Paliperidone Palmitate416
Oral Antipsychotics226

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Brief Assessments of Cognition in Schizophrenia Scores (BACS)

"Mean of cognition was assessed by BACS, which measures neurocognitive function in schizophrenia. BACs is a validated, composite measure of cognition which is used in schizophrenia. It is composed of Verbal memory (range: 0-75), Working memory (range: 0-28), Motor speed (range: 0-100), Verbal Fluency (number of words generated), Information processing (range: 0-110) and Executive functions (range: 0-22).~Higher z-scores indicate a better performance and outcome. BACS composite score are represented as z-scores which can be positive or negative. There is no minimum or maximum as this is a continuous measure." (NCT02199743)
Timeframe: Baseline and 4 weeks

,
InterventionBACS composite score (z score) (Mean)
Baseline (week 0)week 4
Lurasidone-1.596573107-2.002433521
Non-Lurasidone-1.933853656-1.500292967

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Cerebral Glutamate Levels

"Mean values of cerebral glutamate levels was measured by high resolution 3T magnetic resonance spectroscopy (MRS) in the anterior cingulate cortex (ACC). Data were acquired from the dorsal anterior cingulate cortex (ACC) using single voxel localized PRESS (TE1, TE2) = (32, 65) ms with an 8-channel head coil in a 3T whole-body scanner (Philips Medical Systems). Voxel size was 30x20x15 mm3 (9 mL) and were placed over the bilateral anterior cingulate cortex (ACC). All values are normalized to water.~More negative values represent less cerebral glutamate levels." (NCT02199743)
Timeframe: Baseline and 4 weeks

,
Interventionrelative unit (RU as compared to water) (Mean)
Baseline (week 0)week 4
Lurasidone-1.434662171-1.412294235
Non-Lurasidone-1.933853656-1.838991525

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Part 3 (Disease Modification): Personal and Social Performance (PSP) Total Observed Score

The Personal and Social Performance (PSP) scale assesses degree of a participant's dysfunction within 4 domains of behavior: 1) socially useful activities, 2) personal and social relationships, 3) self-care, and 4) disturbing and aggressive behavior. Score ranges from 1 to 100, divided into 10 equal intervals to rate degree of difficulty (1 = absent, 2 = mild, 3 = manifest, 4 = marked, 5 = severe, and 6 = very severe) in each of the 4 domains. Based on 4 domains there will be 1 transformed total score. Participants with score of 71 to 100 have mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. (NCT02431702)
Timeframe: Month 9 of Part 3

Interventionunits on a scale (Least Squares Mean)
Part 3-PP to PP67.6
Part 3- OAP to PP (or Delayed-Start PP)66.1
Part 3-OAP to OAP66.6

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Part 3 (EDP): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)

"The adjusted ICM fraction score is quantified as: 1. The volume of myelinated brain tissue is measured separately on co-localized IR and proton density (PD) MRI images, by outlining the boundary between gray matter and white matter on each image. 2. ICM is calculated from the difference of IR volume minus PD volume. 3. ICM is then expressed as a fraction of the total intracranial volume (ICM divided by intracranial volume). 4. The ICM fraction is then adjusted for effects of age, gender, and race/ethnicity in the sample of treated participants and healthy controls. A decrease in the adjusted ICM fraction score may be a sign of disease progression." (NCT02431702)
Timeframe: Baseline and 18 Months

Interventionratio (Mean)
Part 3-PP to PP-0.001
Part 3-OAP to OAP-0.003

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Part 3 (EDP): Change From Baseline in Attention/Vigilance Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess attention/vigilance score of participants. The range of attention/vigilance score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP2.4
Part 3-OAP to OAP0.7

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Part 3 (EDP): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score

"The Clinical Global Impression Severity (CGI-S) rating scale is used to rate the severity of a participant's overall clinical condition on a 7 point scale. The total score ranges from 1 to 7, where 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Higher scores indicate worsening." (NCT02431702)
Timeframe: Baseline, up to 18 Months

Interventionunits on a scale (Mean)
Part 3-PP to PP-0.7
Part 3-OAP to OAP-0.7

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Part 3 (EDP): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score

The Personal and Social Performance (PSP) scale assesses degree of a participant's dysfunction within 4 domains of behavior: 1) socially useful activities, 2) personal and social relationships, 3) self-care, and 4) disturbing and aggressive behavior. Each domain was assessed on a 6-point scale, from 1 (absent) to 6 (very severe) (1 = absent, 2 = mild, 3 = manifest, 4 = marked, 5 = severe, and 6 = very severe). PSP total score was calculated as sum of all the domain scores and ranges from 1 to 100. Participants with score of 71 to 100 have mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. Higher score indicate better performance. (NCT02431702)
Timeframe: Baseline and 18 Months

Interventionunits on a scale (Mean)
Part 3-PP to PP7.5
Part 3-OAP to OAP7.0

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Part 3 (EDP): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Score

The Medication Satisfaction Questionnaire (MSQ) is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). Total score ranges from 1 to 7. Higher score indicate improvement. (NCT02431702)
Timeframe: Baseline, up to 18 Months

Interventionunits on a scale (Mean)
Part 3-PP to PP0.3
Part 3-OAP to OAP0.4

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Part 3 (EDP): Change From Baseline in Reasoning and Problem Solving: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess reasoning and problem solving score of participants. The range of reasoning and problem solving T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP3.4
Part 3-OAP to OAP4.7

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Part 3 (EDP): Change From Baseline in Social Cognition Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess social cognition score of participants. The range of social cognition score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP-0.2
Part 3-OAP to OAP1.4

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Part 3 (EDP): Change From Baseline in Speed of Processing Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess speed of processing score of participants. The range of speed of processing score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP2.5
Part 3-OAP to OAP4.9

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Part 2 (Disease Progression): Change From Baseline in Medication Satisfaction Questionnaire (MSQ) Total Score

The Medication Satisfaction Questionnaire (MSQ) is a 7-point, verbally administered, Likert-type scale rated as follows: 1=Extremely Dissatisfied, 2=Very Dissatisfied, 3=Somewhat Dissatisfied, 4=Neither Satisfied Nor Dissatisfied, 5=Somewhat Satisfied, 6=Very Satisfied, 7=Extremely Satisfied. Worst value is 1 (Extremely Dissatisfied) and best value is 7 (Extremely Satisfied). Total score ranges from 1 to 7. Higher score indicate improvement. (NCT02431702)
Timeframe: Baseline and endpoint Part 2 (up to 9 Months)

Interventionunits on a scale (Mean)
Part-2: Paliperidone Palmitate (PP)-0.2
Part-2: OAP0.1

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Part 3 (EDP): Change From Baseline in Visual Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess visual learning score of participants. The range of visual learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP0.2
Part 3-OAP to OAP-0.2

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Part 3 (EDP): Change From Baseline in Working Memory Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess working memory of participants. The range of working memory score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP-1.7
Part 3-OAP to OAP0.7

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Part 3 (EDP): Time to First Treatment Failure

Treatment failure is defined as the time from participant's randomization to first treatment failure, which was a composite endpoint consisting of any of the following: 1) Psychiatric hospitalization due to worsening symptoms; 2) Any deliberate self-injury, suicidal ideation or behavior, homicidal ideation or violent behavior that is clinically significant and needs immediate intervention as determined by the study physician; 3) New arrest/incarceration; 4) Discontinuation of antipsychotic treatment due to inadequate efficacy as determined by the study physician; 5) Discontinuation of antipsychotic treatment due to safety or tolerability as determined by the study physician; 6) Treatment supplementation with another antipsychotic due to inadequate efficacy as determined by the study physician; 7) Increase in the level of psychiatric services in order to prevent imminent psychiatric hospitalization as determined by the study physician. (NCT02431702)
Timeframe: From Day 1 Up to 18 Months

Interventiondays (Median)
Part 3-PP to PPNA
Part 3-OAP to OAPNA

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Part 3 (Extended Disease Progression [EDP]): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score

The MATRICS Consensus Cognitive Battery is an instrument that contains 10 tests to measure cognitive performance in 7 cognitive domains: speed processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition. The composite score combines the individual scores of the 10 tests and scores them on a normative scale to derive a T-score and composites scores. The range of T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP1.6
Part 3-OAP to OAP3.2

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Part-2 (Disease Progression): Time to First Treatment Failure

Treatment failure is defined as the time from participant's randomization to first treatment failure, which was a composite endpoint consisting of any of the following: 1) Psychiatric hospitalization due to worsening symptoms; 2) Any deliberate self-injury, suicidal ideation or behavior, homicidal ideation or violent behavior that is clinically significant and needs immediate intervention as determined by the study physician; 3) New arrest/incarceration; 4) Discontinuation of antipsychotic treatment due to inadequate efficacy as determined by the study physician; 5) Discontinuation of antipsychotic treatment due to safety or tolerability as determined by the study physician; 6) Treatment supplementation with another antipsychotic due to inadequate efficacy as determined by the study physician; 7) Increase in the level of psychiatric services in order to prevent imminent psychiatric hospitalization as determined by the study physician. (NCT02431702)
Timeframe: From Day 1 up to 9 Months

Interventiondays (Median)
Part-2: Paliperidone Palmitate (PP)NA
Part-2: OAPNA

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Part 2 (Disease Progression): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by Clinician-Rated Dimensions of Psychosis Symptom Severity Scale (CRDPSS)

The CRDPSS is an 8-item measure that assesses the severity of mental health symptoms that are important across psychotic disorders, including delusions, hallucinations, disorganized speech, abnormal psychomotor behavior, negative symptoms. Each item on the measure is rated on a 5-point scale (0=none; 1=equivocal; 2=present, but mild; 3=present and moderate; and 4=present and severe). Total Score is taken as summation. A higher score indicates a more severe condition. Worsened or improved is defined as increase or decrease compared to baseline. (NCT02431702)
Timeframe: Baseline, up to 9 Months

InterventionParticipants (Count of Participants)
Hallucinations72513608Hallucinations72513614Delusions72513614Delusions72513608Disorganized Speech72513614Disorganized Speech72513608Abnormal Psychomotor Behavior72513614Abnormal Psychomotor Behavior72513608Negative Symptoms72513608Negative Symptoms72513614Impaired Cognition72513614Impaired Cognition72513608Mania72513608Mania72513614Depression72513608Depression72513614
UnchangedImprovedWorsened
Part-2: OAP19
Part-2: Paliperidone Palmitate (PP)29
Part-2: OAP73
Part-2: Paliperidone Palmitate (PP)14
Part-2: OAP33
Part-2: Paliperidone Palmitate (PP)10
Part-2: OAP20
Part-2: Paliperidone Palmitate (PP)23
Part-2: OAP70
Part-2: OAP35
Part-2: OAP13
Part-2: Paliperidone Palmitate (PP)36
Part-2: OAP85
Part-2: Paliperidone Palmitate (PP)12
Part-2: OAP27
Part-2: Paliperidone Palmitate (PP)9
Part-2: OAP14
Part-2: Paliperidone Palmitate (PP)37
Part-2: OAP86
Part-2: Paliperidone Palmitate (PP)4
Part-2: OAP25
Part-2: Paliperidone Palmitate (PP)16
Part-2: OAP61
Part-2: Paliperidone Palmitate (PP)17
Part-2: OAP39
Part-2: Paliperidone Palmitate (PP)13
Part-2: OAP29
Part-2: Paliperidone Palmitate (PP)22
Part-2: OAP52
Part-2: Paliperidone Palmitate (PP)15
Part-2: OAP44
Part-2: Paliperidone Palmitate (PP)1
Part-2: OAP7
Part-2: Paliperidone Palmitate (PP)47
Part-2: OAP107
Part-2: Paliperidone Palmitate (PP)2
Part-2: OAP11
Part-2: Paliperidone Palmitate (PP)7
Part-2: OAP28
Part-2: Paliperidone Palmitate (PP)33
Part-2: OAP74
Part-2: OAP23

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Part 3 (EDP): Number of Participants With Change From Baseline in Severity of Psychotic Symptoms, as Measured by CRDPSS

The CRDPSS is an 8-item measure that assesses the severity of mental health symptoms that are important across psychotic disorders, including delusions, hallucinations, disorganized speech, abnormal psychomotor behavior, negative symptoms. Each item on the measure is rated on a 5-point scale (0=none; 1=equivocal; 2=present, but mild; 3=present and moderate; and 4=present and severe). Total Score is taken as summation. A higher score indicates a more severe condition. Worsened or improved is defined as increase or decrease compared to baseline. (NCT02431702)
Timeframe: Baseline, up to 18 Months

InterventionParticipants (Count of Participants)
Hallucinations72513609Hallucinations72513610Delusions72513609Delusions72513610Disorganized Speech72513609Disorganized Speech72513610Abnormal Psychomotor Behavior72513609Abnormal Psychomotor Behavior72513610Negative Symptoms72513609Negative Symptoms72513610Impaired Cognition72513609Impaired Cognition72513610Mania72513609Mania72513610Depression72513609Depression72513610
WorsenedUnchangedImproved
Part 3-PP to PP3
Part 3-OAP to OAP8
Part 3-PP to PP27
Part 3-OAP to OAP29
Part 3-PP to PP11
Part 3-OAP to OAP10
Part 3-PP to PP6
Part 3-PP to PP21
Part 3-OAP to OAP20
Part 3-PP to PP14
Part 3-OAP to OAP17
Part 3-PP to PP2
Part 3-OAP to OAP36
Part 3-PP to PP12
Part 3-PP to PP4
Part 3-OAP to OAP2
Part 3-PP to PP32
Part 3-OAP to OAP37
Part 3-PP to PP5
Part 3-OAP to OAP4
Part 3-OAP to OAP22
Part 3-PP to PP19
Part 3-OAP to OAP21
Part 3-PP to PP10
Part 3-OAP to OAP9
Part 3-OAP to OAP23
Part 3-PP to PP17
Part 3-OAP to OAP15
Part 3-PP to PP0
Part 3-OAP to OAP3
Part 3-PP to PP40
Part 3-OAP to OAP39
Part 3-PP to PP1
Part 3-OAP to OAP5
Part 3-PP to PP7
Part 3-OAP to OAP6
Part 3-PP to PP26
Part 3-PP to PP8
Part 3-OAP to OAP12

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Part 2 (Disease Progression): Change From Baseline in Adjusted Intracortical Myelin (ICM) Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (MRI)

"The adjusted ICM fraction score is quantified as: 1. The volume of myelinated brain tissue is measured separately on co-localized IR and proton density (PD) MRI images, by outlining the boundary between gray matter and white matter on each image. 2. ICM is calculated from the difference of IR volume minus PD volume. 3. ICM is then expressed as a fraction of the total intracranial volume (ICM divided by intracranial volume). 4. The ICM fraction is then adjusted for effects of age, gender, and race/ethnicity in the sample of treated participants and healthy controls. A decrease in the adjusted ICM fraction score may be a sign of disease progression." (NCT02431702)
Timeframe: Baseline and Day 260

Interventionratio (Mean)
Part-2: Paliperidone Palmitate (PP)-0.001
Part-2: OAP-0.004

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Part 2 (Disease Progression): Change From Baseline in Attention/Vigilance Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess attention/vigilance score of participants. The range of attention/vigilance score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)3.2
Part-2: OAP0.7

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Part 2 (Disease Progression): Change From Baseline in Clinical Global Impression Severity (CGI-S) Score

"The Clinical Global Impression Severity (CGI-S) rating scale is used to rate the severity of a participant's overall clinical condition on a 7 point scale. The score ranges from 1 to 7, where 1 is equivalent to Normal, not at all ill and a rating of 7 is equivalent to Among the most extremely ill participants. Higher scores indicate worsening." (NCT02431702)
Timeframe: Baseline, up to 9 Months of Part 2

Interventionunits on a scale (Mean)
Part-2: Paliperidone Palmitate (PP)-0.2
Part-2: OAP-0.3

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Part 2 (Disease Progression): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score

The MATRICS Consensus Cognitive Battery is an instrument that contains 10 tests to measure cognitive performance in 7 cognitive domains: speed processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition. The composite score combines the individual scores of the 10 tests and scores them on a normative scale to derive a T-score and composites scores. The range of T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Month 9

InterventionT-score (Least Squares Mean)
Part-2: Paliperidone Palmitate (PP)2.0
Part-2: OAP2.8

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Part 2 (Disease Progression): Change From Baseline in Functioning as Measured by the Personal and Social Performance (PSP) Total Score

The Personal and Social Performance (PSP) scale assesses degree of a participant's dysfunction within 4 domains of behavior: 1) socially useful activities, 2) personal and social relationships, 3) self-care, and 4) disturbing and aggressive behavior. Each domain was assessed on a 6-point scale, from 1 (absent) to 6 (very severe) (1 = absent, 2 = mild, 3 = manifest, 4 = marked, 5 = severe, and 6 = very severe). PSP total score was calculated as sum of all the domain scores and ranges from 1 to 100. Participants with score of 71 to 100 have mild degree of difficulty; from 31 to 70, varying degrees of disability; less than or equal to 30, functioning so poorly as to require intensive supervision. Higher score indicate better performance. (NCT02431702)
Timeframe: Baseline and Month 9

Interventionunits on a scale (Mean)
Part-2: Paliperidone Palmitate (PP)2.5
Part-2: OAP2.9

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Part 2 (Disease Progression): Change From Baseline in Reasoning and Problem Solving: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess reasoning and problem solving of participants. The range of reasoning and problem solving T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)0.2
Part-2: OAP2.8

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Part 2 (Disease Progression): Change From Baseline in Social Cognition Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess social cognition score of participants. The range of social cognition score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)0.3
Part-2: OAP1.6

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Part 2 (Disease Progression): Change From Baseline in Speed of Processing Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess speed of processing score of participants. The range of speed of processing T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)1.8
Part-2: OAP3.5

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Part 3 (EDP): Change From Baseline in Verbal Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess verbal learning score of participants. The range of verbal learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and 18 Months

InterventionT-score (Mean)
Part 3-PP to PP0.3
Part 3-OAP to OAP0.8

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Part 2 (Disease Progression): Change From Baseline in Verbal Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess verbal learning score of participants. The range of verbal learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)1.3
Part-2: OAP1.0

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Part 2 (Disease Progression): Change From Baseline in Visual Learning Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess visual learning score of participants. The range of visual learning score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)1.3
Part-2: OAP1.4

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Part 2 (Disease Progression): Change From Baseline in Working Memory Score: MCCB Domain

MCCB measures cognitive function across cognitive domains and is comprised of 10 independent tests assessing 7 cognitive domains (speed of processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition). A subset of the MCCB cognitive domain was used to assess working memory of participants. The range of working memory score T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part-2: Paliperidone Palmitate (PP)-0.2
Part-2: OAP-0.8

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Part 3 (Disease Modification): Change From Baseline in Adjusted Intracortical Myelin Fraction Score as Measured by Inversion Recovery (IR) and Spin Echo Magnetic Resonance Imaging (SE MRI)

"The adjusted ICM fraction score is quantified as: 1. The volume of myelinated brain tissue is measured separately on co-localized IR and proton density (PD) MRI images, by outlining the boundary between gray matter and white matter on each image. 2. ICM is calculated from the difference of IR volume minus PD volume. 3. ICM is then expressed as a fraction of the total intracranial volume (ICM divided by intracranial volume). 4. The ICM fraction is then adjusted for effects of age, gender, and race/ethnicity in the sample of treated participants and healthy controls. A decrease in the adjusted ICM fraction score may be a sign of disease progression." (NCT02431702)
Timeframe: Baseline and Month 9 of Part 3

Interventionratio (Least Squares Mean)
Part 3-PP to PP-0.7
Part 3- OAP to PP (or Delayed-Start PP)-0.2
Part 3-OAP to OAP0.5

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Part 3 (Disease Modification): Change From Baseline in Cognition as Measured by the MATRICS Consensus Cognitive Battery (MCCB) Composite Score

The MATRICS Consensus Cognitive Battery is an instrument that contains 10 tests to measure cognitive performance in 7 cognitive domains: speed processing, attention/vigilance, working memory, verbal learning, visual learning, reasoning and problem solving, and social cognition. The composite score combines the individual scores of the 10 tests and scores them on a normative scale to derive a T-score and composites scores. The range of T-scores for a normal control population is between 0 to 100 with a mean of 50 and standard deviation of 10. Higher scores indicate better cognitive functioning. (NCT02431702)
Timeframe: Baseline and Day 260

InterventionT-score (Mean)
Part 3- PP to PP-0.7
Part 3- OAP to PP (or Delayed-Start PP)-0.2
Part 3-OAP to OAP0.5

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Number of Participants With Relapse

The definition of relapse is as follows 1.50% or greater increase in total DIEPSS score, 2. an increase in the total PANSS score of 25% or more from baseline, 3. deliberate self-injury, 4. emergence of clinically significant suicidal ideation, 5. violent behavior resulting in clinically significant injury to another person or property damage. (NCT03019887)
Timeframe: One year after the baseline cognitive function test or three months after the end of dose reduction, whichever came first.

InterventionParticipants (Count of Participants)
Dose Reduction130

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