Page last updated: 2024-11-04

phenelzine

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

Description

Phenelzine is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) used as an antidepressant. It was synthesized in the 1950s and is marketed under the brand name Nardil. Phenelzine inhibits the activity of monoamine oxidase enzymes, which are responsible for breaking down neurotransmitters like norepinephrine, dopamine, and serotonin. By inhibiting these enzymes, phenelzine increases the levels of these neurotransmitters in the brain, leading to its antidepressant effects. Phenelzine is effective in treating major depressive disorder, especially in cases that are resistant to other treatments. However, it is associated with several side effects, including dietary restrictions and potential interactions with other medications. Due to its potency and potential for adverse reactions, phenelzine is generally reserved for patients who have not responded to other antidepressants. Research continues to investigate the mechanisms of action and potential uses of phenelzine in treating other conditions, including anxiety disorders and chronic pain.'

Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3675
CHEMBL ID1089
CHEBI ID8060
SCHEMBL ID34335
MeSH IDM0016502

Synonyms (120)

Synonym
chebi:8060 ,
CHEMBL1089 ,
BRD-K87024524-065-05-2
phenalzine
nardil
fenelzin
hydrazine, phenethyl-
hydrazine, (2-phenylethyl)-
KBIO1_000062
DIVK1C_000062
SPECTRUM_000851
BSPBIO_000039
phenelzinum [inn-latin]
w 1544-a
einecs 200-117-9
w1544 ,
fenelzina [inn-spanish]
2-phenylethylhydrazine
beta-phenylethylhydrazine
fenelzyne [polish]
phenethylhydrazine
brn 0742354
phenelzine [inn:ban]
fenelzyna [polish]
1-hydrazino-2-phenylethane
2-phenethylhydrazine
NCGC00015830-01
lopac-p-6777
SPECTRUM5_000990
LOPAC0_000971
PRESTWICK3_000170
beta phenylethylhydrazine
2 phenethylhydrazine
PRESTWICK2_000170
CMAP_000003
BPBIO1_000043
CBCHROMO1_000176
BSPBIO_002373
AB00053520
phenelzine
C07430
51-71-8
DB00780
IDI1_000062
KBIO2_001331
KBIOSS_002266
KBIO2_007401
KBIO2_003899
KBIO2_006467
KBIOSS_001331
KBIO3_002745
KBIOGR_002265
KBIOGR_000950
KBIO3_001593
KBIO2_002265
KBIO2_004833
SPECTRUM2_001009
PRESTWICK1_000170
SPECTRUM4_000475
NINDS_000062
SPBIO_001960
PRESTWICK0_000170
SPBIO_001137
SPECTRUM3_000677
NCGC00162301-01
NCGC00015830-04
phenelzine (ban)
D08349
bdbm50105417
phenethyl-hydrazine
AKOS000131105
HMS3259L04
fenelzyne
hsdb 8127
fenelzina
4-15-00-01269 (beilstein handbook reference)
unii-o408n561gf
phenelzinum
o408n561gf ,
fenelzyna
A828737
CCG-205051
NCGC00015830-03
NCGC00015830-05
phenylethylhydrazine
FT-0631225
NCGC00015830-07
(2-phenylethyl)hydrazine
gtpl7266
phenelzine [mi]
phenelzine [inn]
phenelzine [who-dd]
phenelzine [vandf]
W-1544 ,
NC00692
SCHEMBL34335
CS-4532
phenethyl hydrazine
1-(2-phenylethyl)hydrazine
1-(2-phenethyl)hydrazine
1-(2-phenylethyl)hydrazine #
nardil (salt/mix)
.beta.-phenylethylhydrazine
HY-B1018
AB00053520_12
DTXSID2041094 ,
mfcd00047825
SBI-0050944.P004
(2-phenyl-ethyl)-hydrazine
14847-47-3
Q1747559
SDCCGSBI-0050944.P005
NCGC00015830-13
EN300-58071
AS-77074
F74244
fenelzina (inn-spanish)
phenelzinum (inn-latin)
phenelzinum (latin)
dtxcid0021094

Research Excerpts

Overview

Phenelzine (PLZ) is a monoamine oxidase (MAO)-inhibiting antidepressant with anxiolytic properties. It is a scavenger of the lipid peroxidation (LP)-derived reactive aldehyde 4-hydroxynonenal (4-HNE) due to its hydrazine functional group.

ExcerptReferenceRelevance
"Phenelzine (PLZ) is a monoamine oxidase (MAO)-inhibiting antidepressant with anxiolytic properties. "( Overview of the Neuroprotective Effects of the MAO-Inhibiting Antidepressant Phenelzine.
Baker, GB; Holt, A; Kar, S; Kumpula, D; MacKenzie, EM; Matveychuk, D; Song, MS; Todd, KG; Wood, PL, 2022
)
2.39
"Phenelzine is an antidepressant drug known to increase the risk of hypertensive crisis when dietary tyramine is not restricted. "( Body fat reduction without cardiovascular changes in mice after oral treatment with the MAO inhibitor phenelzine.
Carpéné, C; Galitzky, J; Le Gonidec, S; Mercader, J; Mialet-Perez, J; Schaak, S; Zakaroff-Girard, A, 2018
)
2.14
"Phenelzine is a worldwide prescribed MAO-I, studied in a variety of mood and anxiety disorders."( [Phenelzine: legacy or current psychiatric practice?].
Brugnoli, R; Marini, S; Serata, D,
)
1.76
"Phenelzine (PZ) is a U.S."( Phenelzine Protects Brain Mitochondrial Function In Vitro and In Vivo following Traumatic Brain Injury by Scavenging the Reactive Carbonyls 4-Hydroxynonenal and Acrolein Leading to Cortical Histological Neuroprotection.
Cebak, JE; Hall, ED; Hill, RL; Singh, IN; Wang, JA, 2017
)
2.62
"Phenelzine is an irreversible monoamine oxidase inhibitor (MAOI). "( Phenelzine-induced myocardial injury: a case report.
Ho, RY; Ngo, AS; Olson, KR, 2010
)
3.25
"Phenelzine is a potent monoamine oxidase inhibitor that is used in patients with depression. "( Phenelzine (monoamine oxidase inhibitor) increases production of nitric oxide and proinflammatory cytokines via the NF-κB pathway in lipopolysaccharide-activated microglia cells.
Bae, H; Chung, HS; Kim, H, 2012
)
3.26
"Phenelzine (PZ) is a scavenger of the lipid peroxidation (LP)-derived reactive aldehyde 4-hydroxynonenal (4-HNE) due to its hydrazine functional group, which can covalently react with 4-HNE. "( Phenelzine mitochondrial functional preservation and neuroprotection after traumatic brain injury related to scavenging of the lipid peroxidation-derived aldehyde 4-hydroxy-2-nonenal.
Cebak, JE; Gilmer, LK; Hall, ED; Miller, DM; Singh, IN; Wang, JA, 2013
)
3.28
"Phenelzine appears to be a suitable alternative to tranylcypromine."( Efficacy and tolerability of tranylcypromine versus phenelzine: a double-blind study in antidepressant-refractory depressed inpatients.
Birkenhäger, TK; Bruijn, JA; Moleman, P; Mulder, PG; van den Broek, WW, 2004
)
1.3
"Phenelzine is a drug commonly used in the treatment of depression. "( Two fatalities involving phenelzine.
Cohn, RD; Lichtenwalner, MR; Pinder, RD; Tully, RG,
)
1.88
"Phenelzine (PLZ) is a non-selective monoamine oxidase (MAO) inhibitor commonly used to treat depression and panic disorder. "( Task-dependent effects of the antidepressant/antipanic drug phenelzine on memory.
Baker, GB; Habib, MK; Parent, MB, 1999
)
1.99
"Phenelzine (PLZ) is a non-selective monoamine oxidase (MAO) inhibitor commonly used to treat depression and panic disorder. "( Time-dependent changes in brain monoamine oxidase activity and in brain levels of monoamines and amino acids following acute administration of the antidepressant/antipanic drug phenelzine.
Baker, GB; Habib, MK; Parent, MB, 2000
)
1.94
"Phenelzine (PLZ) is a non-selective monoamine oxidase inhibitor (MAOI) commonly used to treat depression and panic disorder. "( Effects of the antidepressant/antipanic drug phenelzine and its putative metabolite phenylethylidenehydrazine on extracellular gamma-aminobutyric acid levels in the striatum.
Baker, GB; Kashlub, S; Master, S; Parent, MB, 2002
)
2.02
"1. Phenelzine (PLZ) is an antidepressant with anxiolytic properties. "( Effects of the antidepressant/antipanic drug phenelzine on alanine and alanine transaminase in rat brain.
Baker, GB; Martin, IL; Parent, MB; Paslawski, T; Tanay, VA; Wong, JT, 2001
)
1.19
"Phenelzine is an excellent agent for treating ambulatory patients with neurotic depression and those with agoraphobia and social phobias."( Use of MAOI antidepressants.
Bartlett, D; Ives, JO; Nies, A; Ravaris, CL; Robinson, DS, 1978
)
0.98
"Phenelzine is a more potent monoamine oxidase inhibitor than is N2-acetylphenelzine."( N2-acetylphenelzine: effects on rat brain GABA, alanine and biogenic amines.
Baker, GB; Coutts, RT; McKenna, KF, 1991
)
1.42
"Phenelzine appeared to be a particularly effective treatment for the generalized form of social phobia."( Phenelzine and atenolol in social phobia.
Campeas, R; Fyer, A; Gorman, J; Hatterer, J; Hollander, E; Liebowitz, MR; Papp, L; Schneier, F, 1990
)
2.44
"Phenelzine is a monoamine oxidase inhibitor with antidepressant properties. "( Effects of acute and chronic phenelzine on regional monoamine metabolism in rats and its potentiation by deuterium substitution.
Boulton, AA; Greenshaw, AJ; Juorio, AV, 1986
)
2
"Phenelzine is a suicide monoamine oxidase (MAO) inhibitor with antidepressant properties. "( Deuterium isotope effect of phenelzine on the inhibition of rat liver mitochondrial monoamine oxidase activity.
Tipton, KF; Yu, PH, 1989
)
2.01

Effects

Phenelzine has no interest to be combined with low doses of resveratrol for treating/preventing obesity, when considering the VHFD mouse model.

ExcerptReferenceRelevance
"Phenelzine has been suggested to have an antiobesity effect by inhibiting de novo lipogenesis, which led us to investigate the metabolic effects of oral chronic phenelzine treatment in high-sucrose-drinking mice. "( Metabolic Effects of Oral Phenelzine Treatment on High-Sucrose-Drinking Mice.
Carpéné, C; Chaplin, A; Gómez-Zorita, S; Mercader, J, 2018
)
2.22
"Phenelzine has no interest to be combined with low doses of resveratrol for treating/preventing obesity, when considering the VHFD mouse model."( Combination of low dose of the anti-adipogenic agents resveratrol and phenelzine in drinking water is not sufficient to prevent obesity in very-high-fat diet-fed mice.
Bertrand, C; Cadoudal, T; Carpéné, C; Gomez, A; Gomez-Zorita, S; Grès, S; Gupta, R; Iffiu-Soltész, Z; Mercader, J; Rancoule, C, 2014
)
2.08
"1. Phenelzine has been found to be methylated by enzymes obtained from bovine adrenal and some rat tissues in the presence of S-adenosylmethionine (SAM) as methyl group donor. "( Enzymatic N-methylation of phenelzine catalyzed by phenylethanolamine N-methyltransferase.
Davis, BA; Durden, DA; Yu, PH, 1991
)
1.2

Actions

Phenelzine can inhibit Jeko-1 cell proliferation and induce apoptosis by regulating methylation and acetylation of histone. It also suppresses Wnt/β-catenin signal pathway, suggesting its therapeutic benefit for mantle cell lymophma.

ExcerptReferenceRelevance
"Phenelzine can inhibit Jeko-1 cell proliferation and induce apoptosis by regulating methylation and acetylation of histone and suppressing Wnt/β-catenin signal pathway, suggesting its therapeutic benefit for mantle cell lymophma."( [Effect of Monoamine Oxidase Inhibitor Phenelzine on Proliferation of Mantle Cell Lymphoma and Its Mechanism].
Chen, Q; Huang, YQ; Ma, XD; Zhan, LF, 2017
)
2.17
"Phenelzine predicted to cause an increase in the AUC of efavirenz and bupropion by 9.4- and 2.4-fold respectively considering unbound hepatic inlet concentrations of phenelzine."( Evaluation of metabolism dependent inhibition of CYP2B6 mediated bupropion hydroxylation in human liver microsomes by monoamine oxidase inhibitors and prediction of potential as perpetrators of drug interaction.
Bhyrapuneni, G; Manoharan, A; Mohammed, AR; Nirogi, R; Palacharla, RC; Ponnamaneni, RK, 2015
)
1.14
"Phenelzine did not increase paraventricular hypothalamus CRH or vasopressin mRNA in ADX mice lacking corticosterone replacement."( Chronic treatment with the monoamine oxidase inhibitor phenelzine increases hypothalamic-pituitary-adrenocortical activity in male C57BL/6 mice: relevance to atypical depression.
Han, J; Jacobson, L; Kier, A, 2005
)
1.3
"Phenelzine was chosen because cocaine is contraindicated in patients taking the medication and also because it reduces the craving for cocaine."( Cocaine abuse treated with phenelzine.
Golwyn, DH, 1988
)
1.29

Treatment

Phenelzine-treated mice showed decreased levels of pro-inflammatory cytokines, such as interleukin-1β, interleokin-6, and tumor necrosis factor-α in the injured spinal cord during the acute phase of inflammation. Phenelzined mice presented higher rectal temperature, which was associated to reduced mRNA levels of uncoupling protein 1 in brown adipose tissue.

ExcerptReferenceRelevance
"Phenelzine-treated mice exhibited lower body fat content, subcutaneous WAT mass and lipid content in skeletal muscles than control, without decreased body weight gain or food consumption. "( Body fat reduction without cardiovascular changes in mice after oral treatment with the MAO inhibitor phenelzine.
Carpéné, C; Galitzky, J; Le Gonidec, S; Mercader, J; Mialet-Perez, J; Schaak, S; Zakaroff-Girard, A, 2018
)
2.14
"Phenelzine treatment up-regulated the expression and proteolysis of L1.1 (a homolog of the mammalian recognition molecule L1) and phosphorylation of Erk in the spinal cord caudal to lesion site."( Phenelzine, a cell adhesion molecule L1 mimetic small organic compound, promotes functional recovery and axonal regrowth in spinal cord-injured zebrafish.
Li, R; Sahu, S; Schachner, M, 2018
)
2.64
"Phenelzine-treated mice showed decreased levels of pro-inflammatory cytokines, such as interleukin-1β, interleukin-6, and tumor necrosis factor-α in the injured spinal cord during the acute phase of inflammation."( Phenelzine, a small organic compound mimicking the functions of cell adhesion molecule L1, promotes functional recovery after mouse spinal cord injury.
Li, R; Sahu, S; Schachner, M, 2018
)
2.64
"Phenelzine-treated mice presented higher rectal temperature, which was associated to reduced mRNA levels of uncoupling protein 1 in brown adipose tissue."( Metabolic Effects of Oral Phenelzine Treatment on High-Sucrose-Drinking Mice.
Carpéné, C; Chaplin, A; Gómez-Zorita, S; Mercader, J, 2018
)
1.5
"Phenelzine treatment reduced nuclear demethylase activity and increased transcription and expression of M1-like signatures both"( Lysine-Specific Histone Demethylase 1A Regulates Macrophage Polarization and Checkpoint Molecules in the Tumor Microenvironment of Triple-Negative Breast Cancer.
Donovan, T; Forwood, JK; Hardy, K; McCuaig, R; Rao, S; Tan, AHY; Tsimbalyuk, S; Tu, W, 2019
)
1.24
"The phenelzine treatments each resulted in an equivalent inhibition of brain monoamine oxidase activity."( Induction of functional down-regulation of beta-adrenoceptors in rats by 2-phenylethylamine.
Baker, GB; Greenshaw, AJ; Paetsch, PR, 1993
)
0.77
"Phenelzine treatment concurrent with mild chronic stress prevented habituation and maintained the anxiogenic effect of CRF in spite of the downregulation of CRF receptors in the amygdala."( Corticotropin-releasing factor and defensive withdrawal: inhibition of monoamine oxidase prevents habituation to chronic stress.
Azzaro, AJ; Birkle, DL; Cottrell, DJ; Goodman, IJ; Johnson, EA; Ward, HE, 1998
)
1.02
"For phenelzine-treated patients, development of hypomania during follow-up was associated with a better outcome at 6 months and absence of life events prior to the onset of the episode was associated with a worse outcome at 6 months."( Predictors of antidepressant treatment outcome in melancholia: psychosocial, clinical and biological indicators.
Bulbena, A; Catalan, R; Gasto, C; Menchon, JM; Vallejo, J, 1991
)
0.76
"Phenelzine treatment blocked panic attacks in 100% of the patients with panic disorder and in 94.7% of the agoraphobics."( Therapeutic response to phenelzine in patients with panic disorder and agoraphobia with panic attacks.
Buigues, J; Vallejo, J, 1987
)
1.3
"4. Treatment with phenelzine did not enhance the rate of elimination of nicotine."( Phenelzine produces subsensitivity to nicotine.
Davidson, RK; Dilsaver, SC; Hariharan, M, 1993
)
2.05
"Treatment with phenelzine should be reviewed if myoclonus occurs."( Myoclonus and episodic delirium associated with phenelzine: a case report.
White, PD, 1987
)
0.87

Toxicity

We report the safe use of remifentanil as part of the anaesthetic technique in a patient undergoing major head and neck surgery. The patient was being treated for depressive illness with the non-specific monoamine oxidase inhibitor (MAOI) phenelzine.

ExcerptReferenceRelevance
"There have been numerous case reports of adverse reactions involving monoamine oxidase inhibitors (MAOIs), including reactions that developed when one MAOI was substituted for another."( Central nervous system toxicity after abrupt monoamine oxidase inhibitor switch: a case report.
Masiar, SJ; Safferman, AZ, 1992
)
0.28
" No adverse reactions were reported, including hypertensive and hyperpyrexic crises."( The safety of switching rapidly from tricyclic antidepressants to monoamine oxidase inhibitors.
Kahn, D; Opler, LA; Silver, JM, 1989
)
0.28
"84 per patients) and a total of 125 side effect reports were noted in 39 of 42 phenelzine patients (2."( Common side effects associated with monoamine oxidase inhibitors.
Froese, C; Keller, FD; Remick, RA, 1989
)
0.5
"All 10 patients tolerated the addition of an MAOI well, and mean self-rated side effect scores did not change significantly."( Addition of monoamine oxidase inhibitors to carbamazepine: preliminary evidence of safety and antidepressant efficacy in treatment-resistant depression.
Ketter, TA; Parekh, PI; Post, RM; Worthington, K, 1995
)
0.29
"We report the safe use of remifentanil as part of the anaesthetic technique in a patient undergoing major head and neck surgery who was being treated for depressive illness with the non-specific monoamine oxidase inhibitor (MAOI) phenelzine."( Safe use of remifentanil in a patient treated with the monoamine oxidase inhibitor phenelzine.
Gillies, MA; James, KS; Ure, DS, 2000
)
0.72
"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
" Antidepressant monotherapy was found to be a safe and effective treatment for bipolar-II depression."( Efficacy and safety of antidepressant monotherapy in the treatment of bipolar-II depression.
Agosti, V; Stewart, JW, 2007
)
0.34
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36

Pharmacokinetics

ExcerptReferenceRelevance
" Site-specific, stable isotope-labeled phenelzine analogs were synthesized and used in metabolic and pharmacokinetic studies in humans."( Metabolism and pharmacokinetics of phenelzine: lack of evidence for acetylation pathway in humans.
Cooper, TB; Corcella, J; Jindal, SP; Lutz, T; Robinson, DS, 1985
)
0.82

Compound-Compound Interactions

ExcerptReferenceRelevance
" Ice packs combined with a cooling blanket and dantrolene 80 mg iv were administered to control fever and rigidity, respectively."( Sertraline-phenelzine drug interaction: a serotonin syndrome reaction.
Graber, MA; Hoehns, TB; Perry, PJ, 1994
)
0.68
"Selective serotonin reuptake inhibitor antidepressants should not be combined with monoamine oxidase inhibitor antidepressants because of the risk of serotonin syndrome."( Sertraline-phenelzine drug interaction: a serotonin syndrome reaction.
Graber, MA; Hoehns, TB; Perry, PJ, 1994
)
0.68
"The objective of the study was to evaluate the metabolism dependent inhibition of CYP2B6 catalyzed bupropion hydroxylation in human liver microsomes by monoamine oxidase (MAO) inhibitors and to predict the drug-drug interaction potential of monoamine oxidase inhibitors as perpetrators of drug interaction."( Evaluation of metabolism dependent inhibition of CYP2B6 mediated bupropion hydroxylation in human liver microsomes by monoamine oxidase inhibitors and prediction of potential as perpetrators of drug interaction.
Bhyrapuneni, G; Manoharan, A; Mohammed, AR; Nirogi, R; Palacharla, RC; Ponnamaneni, RK, 2015
)
0.42

Bioavailability

ExcerptReferenceRelevance
" Relative bioavailability of conjugated tyramine was elevated sixfold by brofaromine and 11."( Monoamine oxidase inhibition by phenelzine and brofaromine in healthy volunteers.
Antonin, KH; Bieck, PR; Firkusny, L; Nilsson, E; Schick, C; Schulz, R; Schwenk, M; Wollmann, H, 1989
)
0.56
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Phenelzine is a monoamine oxidase-inhibiting antidepressant and antipanic drug. Administering high dosage led to complete alleviation of depression in 10 weeks. 3 weeks afterwards the OCN was markedly improved.

ExcerptRelevanceReference
" In determination of the optimal individual dosage must continue to be an empirical process based on clinical observations and experience."( [Correlation between plasma concentration and clinical effect of neuroleptics and antidepressants].
Modestin, J; Petrin, A, 1976
)
0.26
" Clinical response to phenelzine is related to platelet MAO inhibition and dosage per unit body weight."( Clinical pharmacology of phenelzine.
Bartlett, D; Ives, JO; Nies, A; Ravaris, CL; Robinson, DS, 1978
)
0.88
" Drug dosage is an important variable influencing clinical outcome in this patient group."( A multiple-dose, controlled study of phenelzine in depression-anxiety states.
Ives, JO; Korson, L; Lamborn, KR; Nies, A; Ravaris, CL; Robinson, DS, 1976
)
0.53
"Time- and dose-response studies were carried out on the effects of the monoamine oxidase-inhibiting antidepressant and antipanic drug phenelzine on GABA levels in rat whole brain."( Effects of the antidepressant phenelzine on brain levels of gamma-aminobutyric acid (GABA).
Baker, GB; Coutts, RT; Wong, JT; Yeung, JM, 1991
)
0.77
"Patients who failed to respond to sustained, adequate treatment with the tricyclic imipramine (mean maximum dosage = 260 mg/day) and interpersonal psychotherapy were withdrawn from imipramine and treated in a standardized, but open-label 6-week trial with either phenelzine (N = 4; 60 mg/day) or tranylcypromine (N = 36; mean = 38."( Treatment of imipramine-resistant recurrent depression, III: Efficacy of monoamine oxidase inhibitors.
Frank, E; Hamer, T; Kupfer, DJ; Mallinger, AG; Thase, ME, 1992
)
0.46
"Time- and dose-response studies were conducted to determine the effects of the antidepressant and antipanic drug phenelzine (a monoamine oxidase inhibitor) on whole brain levels of the aliphatic amino acid alanine."( Long-lasting elevation of alanine in brain produced by the antidepressant phenelzine.
Baker, GB; Coutts, RT; Dewhurst, WG; Wong, JT, 1990
)
0.72
" Administering the monoamine oxidase inhibitor phenelzine in high dosage led to complete alleviation of his depression in 10 weeks, and 3 weeks afterwards the OCN was markedly improved."( A remarkable response of chronic severe obsessive-compulsive neurosis to phenelzine.
Mahgoub, OM, 1987
)
0.76
" During a control period, the dogs received bolus injections of epinephrine, norepinephrine, and levonordefrin sufficient to construct log-linear dose-response curves for each agent."( Drug interactions and vasoconstrictors used in local anesthetic solutions.
Duffin, SR; Hunt, LM; Yagiela, JA, 1985
)
0.27
"Monitoring platelet monoamine oxidase activity in plasma of depressed patients receiving monoamine oxidase inhibitors is used as an indicator of therapeutic dosage and efficacy."( Liquid chromatographic determination of inhibition of monoamine oxidase activity in platelet rich plasma of depressed patients treated with phenelzine.
Gupta, RN; Steiner, M, 1985
)
0.47
" Effects of TCP on concentrations of DA and NA varied, depending on the brain area investigated and the dosage used."( Regional concentrations of cerebral amines: effects of tranylcypromine and phenelzine.
Baker, GB; Calverly, DG; Dewhurst, WG; McKim, RH, 1983
)
0.5
" In a clinical trial of the efficacy of two dosage regimes of phenelzine in 60 patients the presence of personality disorder significantly impaired clinical outcome."( Relationship between neurosis and personality disorder.
Casey, P; Gall, J; Tyrer, P, 1983
)
0.51
" Dosage ranged from 15-75 mg daily."( Resistant geriatric depressions and therapeutic response to monoamine oxidase inhibitors.
Ferris, S; Friedman, E; Georgotas, A; Krakowski, M; Mann, J; McCarthy, M; Siegel, R, 1983
)
0.27
"Sixty patients, 30 with depressive neurosis, 15 with anxiety neurosis and 15 with phobic anxiety states, were treated with the monoamine oxidase inhibitor, phenelzine, in two different dosage schedules for four weeks."( Clinical and pharmacokinetic factors affecting response to phenelzine.
Gardner, M; Lambourn, J; Tyrer, P; Whitford, M, 1980
)
0.7
" 2 Antipyrine elimination was slightly but significantly slowed by 28 days treatment with phenelzine but the degree of slowing was uninfluenced by acetylator phenotype or dosage of phenelzine administered."( Antipyrine elimination by patients under treatment with monoamine oxidase inhibitors.
Lambourn, J; Smith, SE; Tyrer, PJ, 1980
)
0.48
" It was found that intramitochondrial and cytoplasmatic redox ratios were not influenced at a hypoglycemic effective dosage (145 mumol/kg body weight) of these substances in fasted guinea pigs."( Hydrazonopropionic acid, a new class of hypoglycemic substances. 2. Influence of 2-(phenylethylhydrazono)- and 2-(2-cyclohexyl-ethylhydrazono)-propionic acid on redox systems, acid base status and monoamino oxidase activity.
Haeckel, R; Oellerich, M, 1980
)
0.26
" There was no correlation of pyridoxal phosphate level with phenelzine daily dosage over the range of 30 mg to 90 mg."( Phenelzine reduces plasma vitamin B6.
Bowen, RC; Hawkes, J; Hussein, M; Malcolm, DE; O'Donovan, C; Yu, PH, 1994
)
1.97
" By study phase, Eight of 27 (30%) patients remitted with initial dosing of tranylcypromine up to 60 mg/d, 6/18 (33%) remitted with above PDR dosing of tranylcypromine up to 120 mg/d, and 1/6 (17%) to adding dextroamphetamine."( How treatable is refractory depression?
Deliyannides, DA; McGrath, PJ; Stewart, JW, 2014
)
0.4
" We found PZ treatment preserves both synaptic and non-synaptic mitochondrial bioenergetics at 24 h and that this protection is partially maintained out to 72 h post-injury using various dosing regimens."( Protective effects of phenelzine administration on synaptic and non-synaptic cortical mitochondrial function and lipid peroxidation-mediated oxidative damage following TBI in young adult male rats.
Hall, ED; Hill, RL; Kulbe, JR; Singh, IN; Wang, JA, 2020
)
0.87
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
primary amineA compound formally derived from ammonia by replacing one hydrogen atom by a hydrocarbyl group.
[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]

Pathways (2)

PathwayProteinsCompounds
phenylethylamine degradation I220
superpathway of phenylethylamine degradation939

Protein Targets (52)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency12.28980.007215.758889.3584AID624030
dopamine D1 receptorHomo sapiens (human)Potency0.05170.00521.30228.1995AID624455
ATAD5 protein, partialHomo sapiens (human)Potency12.28370.004110.890331.5287AID493106; AID493107
NFKB1 protein, partialHomo sapiens (human)Potency0.01000.02827.055915.8489AID895; AID928
GLS proteinHomo sapiens (human)Potency35.48130.35487.935539.8107AID624146
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency15.84890.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.12590.001318.074339.8107AID926
regulator of G-protein signaling 4Homo sapiens (human)Potency23.77810.531815.435837.6858AID504845
EWS/FLI fusion proteinHomo sapiens (human)Potency12.59590.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency18.88760.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency4.41070.00207.533739.8107AID891
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency10.32250.01262.451825.0177AID485313
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.55530.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency5.07930.00636.904339.8107AID883
ras-related protein Rab-9AHomo sapiens (human)Potency14.12540.00022.621531.4954AID485297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency15.47190.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency12.58930.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency5.55280.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency18.88760.177824.735279.4328AID488949
lamin isoform A-delta10Homo sapiens (human)Potency0.50120.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency5.07930.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Ataxin-2Homo sapiens (human)Potency14.12540.011912.222168.7989AID588378
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency5.55281.000012.224831.6228AID885
Single-stranded DNA cytosine deaminaseHomo sapiens (human)Potency45.494728.183860.145389.1251AID1347427; AID1347430
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency33.80780.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Lysine-specific histone demethylase 1AHomo sapiens (human)Ki11.70000.00962.54425.6000AID1459719; AID1800332; AID604075; AID639764
Bile salt export pumpHomo sapiens (human)IC50 (µMol)897.20000.11007.190310.0000AID1449628
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)2.00000.00011.753610.0000AID625251
Cytochrome P450 2C8Homo sapiens (human)Ki1.20000.00180.38733.3000AID589253
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)1.00000.00002.015110.0000AID625249
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)4.00000.00002.800510.0000AID625248
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)IC50 (µMol)14.00000.05373.075710.0000AID1184068
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki0.09400.00081.09276.0000AID1192622
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)0.19200.00002.37899.7700AID1459578; AID625150
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki1.62770.00192.379710.0000AID1459586; AID1800333
Amine oxidase [flavin-containing] BHomo sapiens (human)IC50 (µMol)0.14300.00001.89149.5700AID1459579
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki1.23450.00061.777110.0000AID1192622; AID1459588; AID1800333
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)0.80000.00002.398310.0000AID625247
Membrane primary amine oxidaseHomo sapiens (human)IC50 (µMol)0.02000.02001.04004.1000AID512126
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (143)

Processvia Protein(s)Taxonomy
regulation of double-strand break repair via homologous recombinationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of protein ubiquitinationLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of protein localizationLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to UVLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to gamma radiationLysine-specific histone demethylase 1AHomo sapiens (human)
DNA repair-dependent chromatin remodelingLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neuroblast proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
protein demethylationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of epithelial to mesenchymal transitionLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neuron projection developmentLysine-specific histone demethylase 1AHomo sapiens (human)
cerebral cortex developmentLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
neuron maturationLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediatorLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cell sizeLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA-templated transcriptionLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
guanine metabolic processLysine-specific histone demethylase 1AHomo sapiens (human)
muscle cell developmentLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of androgen receptor signaling pathwayLysine-specific histone demethylase 1AHomo sapiens (human)
response to fungicideLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to cAMPLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of DNA methylation-dependent heterochromatin formationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cold-induced thermogenesisLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neural precursor cell proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of stem cell proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
chromatin remodelingLysine-specific histone demethylase 1AHomo 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)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
lipid hydroxylationCytochrome P450 2C8Homo sapiens (human)
organic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C8Homo sapiens (human)
steroid metabolic processCytochrome P450 2C8Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C8Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C8Homo sapiens (human)
retinol metabolic processCytochrome P450 2C8Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
oxidative demethylationCytochrome P450 2C8Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo 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)
regulation of activated T cell proliferationIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of T cell tolerance inductionIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of chronic inflammatory responseIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of type 2 immune responseIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
tryptophan catabolic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
inflammatory responseIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
female pregnancyIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
tryptophan catabolic process to kynurenineIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
response to lipopolysaccharideIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
negative regulation of interleukin-10 productionIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of interleukin-12 productionIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
multicellular organismal response to stressIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
kynurenic acid biosynthetic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
swimming behaviorIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
T cell proliferationIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
negative regulation of T cell proliferationIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
negative regulation of T cell apoptotic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of T cell apoptotic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
'de novo' NAD biosynthetic process from tryptophanIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
response to xenobiotic stimulusAmine oxidase [flavin-containing] BHomo sapiens (human)
response to toxic substanceAmine oxidase [flavin-containing] BHomo sapiens (human)
response to aluminum ionAmine oxidase [flavin-containing] BHomo sapiens (human)
response to selenium ionAmine oxidase [flavin-containing] BHomo sapiens (human)
negative regulation of serotonin secretionAmine oxidase [flavin-containing] BHomo sapiens (human)
phenylethylamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
substantia nigra developmentAmine oxidase [flavin-containing] BHomo sapiens (human)
response to lipopolysaccharideAmine oxidase [flavin-containing] BHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to ethanolAmine oxidase [flavin-containing] BHomo sapiens (human)
positive regulation of dopamine metabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
hydrogen peroxide biosynthetic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to corticosteroneAmine oxidase [flavin-containing] BHomo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
inflammatory responseMembrane primary amine oxidaseHomo sapiens (human)
cell adhesionMembrane primary amine oxidaseHomo sapiens (human)
amine metabolic processMembrane primary amine oxidaseHomo sapiens (human)
response to antibioticMembrane primary amine oxidaseHomo sapiens (human)
negative regulation of primary amine oxidase activityMembrane primary amine oxidaseHomo 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)
mRNA processingSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
cytidine deaminationSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
somatic diversification of immunoglobulinsSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
somatic hypermutation of immunoglobulin genesSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
B cell differentiationSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
regulation of nuclear cell cycle DNA replicationSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
defense response to bacteriumSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
positive regulation of gene expression via chromosomal CpG island demethylationSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
isotype switchingSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
cellular response to lipopolysaccharideSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
DNA cytosine deaminationSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
DNA demethylationSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
cytidine to uridine editingSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
negative regulation of single stranded viral RNA replication via double stranded DNA intermediateSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
defense response to virusSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (74)

Processvia Protein(s)Taxonomy
telomeric DNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
p53 bindingLysine-specific histone demethylase 1AHomo sapiens (human)
chromatin bindingLysine-specific histone demethylase 1AHomo sapiens (human)
transcription coactivator activityLysine-specific histone demethylase 1AHomo sapiens (human)
protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
oxidoreductase activityLysine-specific histone demethylase 1AHomo sapiens (human)
enzyme bindingLysine-specific histone demethylase 1AHomo sapiens (human)
nuclear receptor coactivator activityLysine-specific histone demethylase 1AHomo sapiens (human)
demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone H3K4 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone H3K9 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
identical protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
MRF bindingLysine-specific histone demethylase 1AHomo sapiens (human)
flavin adenine dinucleotide bindingLysine-specific histone demethylase 1AHomo sapiens (human)
nuclear androgen receptor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
telomeric repeat-containing RNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
DNA-binding transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
FAD-dependent H3K4me/H3K4me3 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
promoter-specific chromatin bindingLysine-specific histone demethylase 1AHomo sapiens (human)
transcription factor bindingLysine-specific histone demethylase 1AHomo 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)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2C8Homo sapiens (human)
iron ion bindingCytochrome P450 2C8Homo sapiens (human)
protein bindingCytochrome P450 2C8Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C8Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C8Homo sapiens (human)
aromatase activityCytochrome P450 2C8Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
heme bindingCytochrome P450 2C8Homo 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 2C8Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo 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 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo 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)
electron transfer activityIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
heme bindingIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
indoleamine 2,3-dioxygenase activityIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
metal ion bindingIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
tryptophan 2,3-dioxygenase activityIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
electron transfer activityAmine oxidase [flavin-containing] BHomo sapiens (human)
identical protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo 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 2C19Homo sapiens (human)
copper ion bindingMembrane primary amine oxidaseHomo sapiens (human)
calcium ion bindingMembrane primary amine oxidaseHomo sapiens (human)
protein bindingMembrane primary amine oxidaseHomo sapiens (human)
primary amine oxidase activityMembrane primary amine oxidaseHomo sapiens (human)
identical protein bindingMembrane primary amine oxidaseHomo sapiens (human)
protein heterodimerization activityMembrane primary amine oxidaseHomo sapiens (human)
quinone bindingMembrane primary amine oxidaseHomo sapiens (human)
aliphatic amine oxidase activityMembrane primary amine oxidaseHomo 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)
cytidine deaminase activitySingle-stranded DNA cytosine deaminaseHomo sapiens (human)
protein bindingSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
zinc ion bindingSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
ubiquitin protein ligase bindingSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
identical protein bindingSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
RNA bindingSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (39)

Processvia Protein(s)Taxonomy
chromatinLysine-specific histone demethylase 1AHomo sapiens (human)
nucleusLysine-specific histone demethylase 1AHomo sapiens (human)
chromosome, telomeric regionLysine-specific histone demethylase 1AHomo sapiens (human)
nucleusLysine-specific histone demethylase 1AHomo sapiens (human)
nucleoplasmLysine-specific histone demethylase 1AHomo sapiens (human)
transcription regulator complexLysine-specific histone demethylase 1AHomo sapiens (human)
protein-containing complexLysine-specific histone demethylase 1AHomo sapiens (human)
DNA repair complexLysine-specific histone demethylase 1AHomo 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)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C8Homo sapiens (human)
plasma membraneCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
cytoplasmCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo 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)
cytosolIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
smooth muscle contractile fiberIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
stereocilium bundleIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
cytoplasmIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial envelopeAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] BHomo sapiens (human)
dendriteAmine oxidase [flavin-containing] BHomo sapiens (human)
neuronal cell bodyAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytoplasmMembrane primary amine oxidaseHomo sapiens (human)
plasma membraneMembrane primary amine oxidaseHomo sapiens (human)
microvillusMembrane primary amine oxidaseHomo sapiens (human)
cell surfaceMembrane primary amine oxidaseHomo sapiens (human)
membraneMembrane primary amine oxidaseHomo sapiens (human)
early endosomeMembrane primary amine oxidaseHomo sapiens (human)
endoplasmic reticulumMembrane primary amine oxidaseHomo sapiens (human)
Golgi apparatusMembrane primary amine oxidaseHomo sapiens (human)
early endosomeMembrane primary amine oxidaseHomo sapiens (human)
plasma membraneMembrane primary amine oxidaseHomo sapiens (human)
endoplasmic reticulumMembrane primary amine oxidaseHomo sapiens (human)
Golgi apparatusMembrane primary amine oxidaseHomo 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)
nucleusSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
cytoplasmSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
cytosolSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
protein-containing complexSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
nucleusSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
cytoplasmSingle-stranded DNA cytosine deaminaseHomo sapiens (human)
P-bodySingle-stranded DNA cytosine deaminaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (152)

Assay IDTitleYearJournalArticle
AID1800332GST-LSD1 Enzymatic Assays from Article 10.1021/cb500018s: \\A Selective Phenelzine Analogue Inhibitor of Histone Demethylase LSD1.\\2014ACS chemical biology, Jun-20, Volume: 9, Issue:6
A selective phenelzine analogue inhibitor of histone demethylase LSD1.
AID1800333MAO-A/B Activity and Inhibition Assay from Article 10.1021/cb500018s: \\A Selective Phenelzine Analogue Inhibitor of Histone Demethylase LSD1.\\2014ACS chemical biology, Jun-20, Volume: 9, Issue:6
A selective phenelzine analogue inhibitor of histone demethylase LSD1.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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]
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
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]
AID1459579Inhibition of recombinant human MAO-B assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate after 20 mins by fluorometric assay2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Acacetin from Calea urticifolia with Inhibitory Properties against Human Monoamine Oxidase-A and -B.
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.
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).
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.
AID512128Selectivity ratio of IC50 for rat liver MAO to IC50 for human recombinant VAP-12010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Synthesis, in vitro activity, and three-dimensional quantitative structure-activity relationship of novel hydrazine inhibitors of human vascular adhesion protein-1.
AID1184071Inhibition of mouse TDO expressed in mouse P815B cells using L-tryptophan substrate incubated for 24 hrs by HPLC based cellular assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.
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.
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.
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.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID749472Induction of adipogenesis in human bone marrow MSC assessed as formation of intracellular lipid droplets at 10 uM after 15 days by oil red O staining in IDX condition relative to control2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
The opposite effect of isotype-selective monoamine oxidase inhibitors on adipogenesis in human bone marrow mesenchymal stem cells.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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.
AID363907Inhibition of rat brain monoamine oxidase A2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
N-Propynyl analogs of beta-phenylethylidenehydrazines: synthesis and evaluation of effects on glycine, GABA, and monoamine oxidase.
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]
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.
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.
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).
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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
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.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1459586Mixed-type inhibition of recombinant human MAO-A assessed as reduction in 4-hydroxyquinoline formation using varying levels of kynuramine as substrate after 20 mins by Lineweaver-Burk plot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Acacetin from Calea urticifolia with Inhibitory Properties against Human Monoamine Oxidase-A and -B.
AID255326In vitro percentage inhibition activity against GABA-T enzyme at a concentration of 1.25 uM after 6 h2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
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.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
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).
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).
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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.
AID678719Metabolic stability in human liver microsomes assessed as medium signal/noise ratio (S/N of 10 to 100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID589253Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using a recombinant system2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID589252Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using human liver microsomes2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1459588Mixed-type inhibition of recombinant human MAO-B assessed as reduction in 4-hydroxyquinoline formation using varying levels of kynuramine as substrate after 20 mins by Lineweaver-Burk plot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Acacetin from Calea urticifolia with Inhibitory Properties against Human Monoamine Oxidase-A and -B.
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.
AID512126Inhibition of human recombinant VAP-1 expressed in CHO cells after 30 mins by coupled colorimetric method2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Synthesis, in vitro activity, and three-dimensional quantitative structure-activity relationship of novel hydrazine inhibitors of human vascular adhesion protein-1.
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.
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.
AID639764Inhibition of LSD12011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Lysine demethylases inhibitors.
AID126694In vitro ability to inhibit Monoamine oxidase B activity in rat whole brain in vitro2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Synthesis of N-propargylphenelzine and analogues as neuroprotective agents.
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.
AID1192622Inhibition of human recombinant soluble MAO-B expressed in Pichia pastoris incubated for 30 mins prior to substrate addition measured after 60 mins by MAO-Glo assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Reversible and irreversible small molecule inhibitors of monoamine oxidase B (MAO-B) investigated by biophysical techniques.
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.
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]
AID256304Ex vitro percentage inhibition activity against GABA-T enzyme at a concentration of 1.25 uM after 3 h2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1459578Inhibition of recombinant human MAO-A assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate after 20 mins by fluorometric assay2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Acacetin from Calea urticifolia with Inhibitory Properties against Human Monoamine Oxidase-A and -B.
AID1184072Cytotoxicity against mouse P815B cells after 24 hrs by MTS/PMS assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.
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).
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1459719Inhibition of LSD1 (unknown origin)2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.
AID512127Inhibition of rat liver MAO after 30 mins by coupled colorimetric method2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Synthesis, in vitro activity, and three-dimensional quantitative structure-activity relationship of novel hydrazine inhibitors of human vascular adhesion protein-1.
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).
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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.
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]
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).
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.
AID749466Inhibition of adipogenesis in human bone marrow MSC assessed as reduction in adiponectin production at 1 to 10 uM after 14 days by ELISA2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
The opposite effect of isotype-selective monoamine oxidase inhibitors on adipogenesis in human bone marrow mesenchymal stem cells.
AID125712In vitro ability to inhibit Monoamine oxidase A activity in rat whole brain in vitro2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Synthesis of N-propargylphenelzine and analogues as neuroprotective agents.
AID639765Ratio of Kinact to Ki for LSD12011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Lysine demethylases inhibitors.
AID256307Ex vitro percentage inhibition activity against GABA-T enzyme at a concentration of 1.25 uM after 4.5 h2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
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.
AID1184068Inhibition of IDO1 (unknown origin) using L-tryptophan substrate incubated for 60 mins by HPLC2014European journal of medicinal chemistry, Sep-12, Volume: 84Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.
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.
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).
AID256305Ex vitro percentage inhibition activity against GABA-T enzyme at a concentration of 1.25 uM after 6 h2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID1192633Inhibition of human recombinant soluble MAO-B assessed as change in melting temperature at 100 uM after 20 mins by SYPRO orange staining-based fluorescence assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Reversible and irreversible small molecule inhibitors of monoamine oxidase B (MAO-B) investigated by biophysical techniques.
AID255325In vitro percentage inhibition activity against GABA-T enzyme at a concentration of 1.25 uM after 3 h2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID1184075Inhibition of IDO1 (unknown origin) at highest soluble concentration using L-tryptophan substrate incubated for 60 mins by HPLC2014European journal of medicinal chemistry, Sep-12, Volume: 84Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.
AID255331In vitro percentage inhibition activity against GABA-T enzyme at a concentration of 1.25 uM after 4.5 h2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
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.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' 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
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.
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.
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).
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID604075Inhibition of LSD12011Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
Inhibitors of histone demethylases.
AID1184074Solubility of the compound in pH 6.5 phosphate buffer containing 5% DMSO2014European journal of medicinal chemistry, Sep-12, Volume: 84Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.
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).
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' 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.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1184069Inhibition of IDO1 (unknown origin) using L-tryptophan substrate incubated for 60 mins in presence of 0.01% Triton-X by HPLC2014European journal of medicinal chemistry, Sep-12, Volume: 84Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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).
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).
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1184070Inhibition of mouse IDO1 expressed in mouse P815B cells using L-tryptophan substrate incubated for 18 hrs by HPLC based cellular assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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).
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).
AID134973Compound tested for the prevention of DSP- 4- induced depletion of noradrenaline (NA) in mouse hippocampus ex vivo2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Synthesis of N-propargylphenelzine and analogues as neuroprotective agents.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
AID1345202Human CYP2C8 (CYP2 family)2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1345977Human Monoamine oxidase B (Catecholamine turnover)2008Biochemistry, May-20, Volume: 47, Issue:20
Structural and mechanistic studies of arylalkylhydrazine inhibition of human monoamine oxidases A and B.
AID1346943Human SERT (Monoamine transporter subfamily)1997European journal of pharmacology, Dec-11, Volume: 340, Issue:2-3
Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
AID1346963Human DAT (Monoamine transporter subfamily)1997European journal of pharmacology, Dec-11, Volume: 340, Issue:2-3
Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
AID1346971Human NET (Monoamine transporter subfamily)1997European journal of pharmacology, Dec-11, Volume: 340, Issue:2-3
Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,331)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990925 (69.50)18.7374
1990's220 (16.53)18.2507
2000's88 (6.61)29.6817
2010's82 (6.16)24.3611
2020's16 (1.20)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 71.19

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 Index71.19 (24.57)
Research Supply Index7.38 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index127.16 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (71.19)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials203 (14.43%)5.53%
Reviews79 (5.61%)6.00%
Case Studies244 (17.34%)4.05%
Observational0 (0.00%)0.25%
Other881 (62.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (8)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase I Parallel Group Study in Healthy Subjects to Evaluate the Effect of Multiple Oral Doses of BI 1467335 and Phenelzine as Positive Control on Blood Pressure Response to Oral Tyramine (Double-blind, Randomised, Placebo-controlled Design for BI 14673 [NCT03979820]Phase 153 participants (Actual)Interventional2019-07-31Terminated(stopped due to Study discontinued - testing of highest dose obsolete)
A Phase 1, Randomized, Double-Blind, Placebo- and Positive-Controlled Study to Evaluate the Effect of Ozanimod on Pressor Response to Oral Tyramine in Healthy Adult Subjects [NCT03694119]Phase 192 participants (Actual)Interventional2018-07-24Completed
A Phase Ib Safety and Pharmacokinetics (PK)/ Pharmacodynamics (PD) Study to Determine the Dosage of Abraxane in Combination With Phenelzine Sulfate in Metastatic or Inoperable Locally Advanced Breast Cancer [NCT03505528]Phase 18 participants (Actual)Interventional2017-08-17Completed
Neuroimaging MAO-B in Medication Free and Treatment Resistant Major Depressive Disorder Using Novel MAO-B Tracer [NCT02153281]8 participants (Actual)Interventional2014-06-30Completed
A Phase 1, Randomized, Double-blind, Placebo- and Positive-controlled Study to Evaluate the Effect of Ozanimod on Pressor Response to Oral Tyramine in Healthy Adult Subjects [NCT04978298]Phase 1128 participants (Actual)Interventional2021-07-19Completed
A Phase II Study of MAOA Inhibitor Plus Docetaxel in Patients Receiving and Progressing on Docetaxel Therapy [NCT01253642]Phase 211 participants (Actual)Interventional2010-07-12Terminated(stopped due to low enrollment)
Phase 2 Trial of Phenelzine in Non-metastatic Recurrent Prostate Cancer [NCT02217709]Phase 226 participants (Actual)Interventional2014-09-08Completed
Efficacy of Hydroxyzine Versus Treatment as Usual for Panic Disorder: An Eight-Week, Open Label, Pilot, Randomized Controlled Trial. [NCT05737511]Phase 480 participants (Anticipated)Interventional2023-12-30Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01253642 (7) [back to overview]Duration of Progression Free Survival After Initiation of Combination Phenelzine and Docetaxel Therapy
NCT01253642 (7) [back to overview]Frequency of MAOA (Monoamine Oxidase A) Overexpression in CRPC (Castration-Resistant Prostate Cancer) Tumors That Are Progressing on Docetaxel
NCT01253642 (7) [back to overview]Maximum Change in PSA
NCT01253642 (7) [back to overview]Proportion of Patients Who Experience a PSA (Prostate-Specific Antigen) Decline of at Least 30%
NCT01253642 (7) [back to overview]Response Rate in Measurable Disease by RECIST (Response Evaluation Criteria In Solid Tumors) Criteria
NCT01253642 (7) [back to overview]Time to Death From All Causes
NCT01253642 (7) [back to overview]Toxicity of the Regimen
NCT03979820 (1) [back to overview]Tyramine Sensitivity Factor (TSF)

Duration of Progression Free Survival After Initiation of Combination Phenelzine and Docetaxel Therapy

Progression free survival is calculated as the time from Day 1 of Combination therapy to first evidence of progression (by PSA, Measureable Disease, or Clinical Progression). For subjects who did not meet progression criteria, date of new therapy or date of death was used. Outcome is reported as mean. (NCT01253642)
Timeframe: Up to 6 years

Interventiondays (Mean)
Combination Phenelzine and Docetaxel77.9

[back to top]

Frequency of MAOA (Monoamine Oxidase A) Overexpression in CRPC (Castration-Resistant Prostate Cancer) Tumors That Are Progressing on Docetaxel

Reported as Number of participants with MAOA expression greater than 5%. (NCT01253642)
Timeframe: Baseline

InterventionParticipants (Count of Participants)
Combination Phenelzine and Docetaxel8

[back to top]

Maximum Change in PSA

Measured from Day 1 of Combination therapy to PSA at 12 Weeks on therapy (or earlier if subject not on therapy for 12 weeks). (NCT01253642)
Timeframe: 12 weeks (or earlier in patients who discontinued early)

Interventionpercentage of PSA change (Median)
Combination Phenelzine and Docetaxel14.24

[back to top]

Proportion of Patients Who Experience a PSA (Prostate-Specific Antigen) Decline of at Least 30%

PSA response: A ≥ 30% reduction from baseline within 12 weeks of initiation of therapy (confirmed on a second measurement at least 3 weeks later). (NCT01253642)
Timeframe: Within 12 weeks

InterventionParticipants (Count of Participants)
Combination Phenelzine and Docetaxel2

[back to top]

Response Rate in Measurable Disease by RECIST (Response Evaluation Criteria In Solid Tumors) Criteria

Response in measurable disease is defined as a 30% decrease in the sum of diameters of target lesions (as described by RECIST 1.1). (NCT01253642)
Timeframe: Up to 6 years

InterventionParticipants (Count of Participants)
Combination Phenelzine and Docetaxel0

[back to top]

Time to Death From All Causes

Time to death is calculated from Day 1 of Combination therapy to death from any cause. (NCT01253642)
Timeframe: Up to 6 years

Interventiondays (Median)
Combination Phenelzine and Docetaxel191.0

[back to top]

Toxicity of the Regimen

Number of participants who experienced an Adverse Event. Detail of Adverse Events is reported in the Adverse Event Section (NCT01253642)
Timeframe: Up to 6 years

InterventionParticipants (Count of Participants)
Combination Phenelzine and Docetaxel11

[back to top]

Tyramine Sensitivity Factor (TSF)

TSF was defined as ratio of the tyramine dose causing an increase of systolic blood pressure (SBP) ≥ 30 millimetre of mercury (mmHg) for at least 3 consecutive measurements (TYR30) at baseline and at steady state of BI 1467335, placebo or phenelzine. Geometric Mean is the Geometric Least Squares Mean and is extracted from the ANOVA model that includes all treatments. Standard error is the geometric standard error of the mean (gSE) and is extracted from the ANOVA model that includes all treatments. (NCT03979820)
Timeframe: "At baseline (Day -11 up to Day-2) and at steady state (Day 29 up to Day 39 for the Placebo/Placebo + Tyramine and 10 mg BI 1467335/10 mg BI 1467335 + Tyramine arms, Day 8 up to Day 19 for the Phenelzine/ Phenelzine + Tyramine arm)."

InterventionRatio of tyramine dose (Geometric Least Squares Mean)
Placebo/Placebo + Tyramine0.98
Phenelzine/Phenelzine + Tyramine5.31
10 mg BI 1467335/10 mg BI 1467335 + Tyramine1.20

[back to top]