Page last updated: 2024-12-05

phenothiazine

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Description

Phenothiazine is a heterocyclic organic compound that serves as a core structure for a variety of pharmaceutical drugs. It is a tricyclic compound consisting of two benzene rings linked by a sulfur atom and a nitrogen atom. Phenothiazine derivatives, such as chlorpromazine, are known for their antipsychotic and antiemetic properties. They are often used to treat schizophrenia and other psychotic disorders, as well as nausea and vomiting. The synthesis of phenothiazine involves a multi-step process that typically starts with diphenylamine and sulfur. The compound exhibits a variety of pharmacological effects, including antihistamine, anticholinergic, and antipsychotic actions. It is widely studied for its potential therapeutic applications, particularly in the treatment of mental health conditions. Researchers are continuously exploring new phenothiazine derivatives with improved efficacy and reduced side effects.'

10H-phenothiazine : The 10H-tautomer of phenothiazine. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID7108
CHEMBL ID828
CHEBI ID37931
CHEBI ID37932
CHEBI ID38093
SCHEMBL ID9114
SCHEMBL ID2395921
MeSH IDM0099235

Synonyms (168)

Synonym
BIDD:GT0831
MLS002152928
HMS3394I13
thiodifenylamine
reconox
penthazine
phenothiazine
orimon
phenoxur
padophene
dibenzo-p-thiazine
souframine
dibenzothiazine
helmetina
early bird wormer
afi-tiazin
fentiazin
phenegic
feeno
nemazene
thiodiphenylamin
phenthiazine
wln: t c666 bm isj
10h-phenothiazine
92-84-2
contaverm
nemazine
wurm-thional
phenzeen
tiodifenilamina
fenothiazine
lethelmin
ent 38
nexarbol
xl-50
thiodiphenylamine
nsc-2037
antiverm
agrazine
nsc2037
fenoverm
phenovis
phenoverm
dibenzo-1,4-thiazine
phenosan
fenotiazina
smr000059045
MLS000069413 ,
phenothiazine (inn)
nemazine [veterinary] (tn)
D02601
10h-phenothiazin
CHEBI:37931 ,
OPREA1_495637
inchi=1/c12h9ns/c1-3-7-11-9(5-1)13-10-6-2-4-8-12(10)14-11/h1-8,13
NCGC00091146-01
fenotiazina [italian]
ai3-00038
epa pesticide chemical code 064501
brn 0143237
thiodifenylamine [dutch]
phenothiazine [inn]
tiodifenilamina [italian]
fenotiazina [inn-spanish]
thiodiphenylamin [german]
biverm
dibenzoparathiazine
nsc 2037
hsdb 5279
ccris 5877
fenothiazine [dutch]
einecs 202-196-5
phenothiazinum [inn-latin]
caswell no. 652
phenthiazinum
phenothiazine, >=98%
NCGC00091146-02
SR-01000721844-3
STK205834
HMS2052I13
AC-10429
danikoropa
CHEMBL828 ,
ent-38
FT-0654203
HMS1607G06
P0106
2,3:5,6-dibenzo-1,4-thiazine
sr-01000721844
SR-01000721844-4
bdbm50012855
cid_7108
AKOS000119180
NCGC00091146-05
NCGC00091146-04
NCGC00091146-03
4-27-00-01214 (beilstein handbook reference)
ec 202-196-5
phenothiazinum
gs9ex7qnu6 ,
phenothiazine [inn:nf]
unii-gs9ex7qnu6
dtxsid5021126 ,
cas-92-84-2
tox21_400010
dtxcid301126
BBL011728
MLS003166904
nsc-760392
pharmakon1600-01506171
nsc760392
MLS001424182
tox21_111090
HMS2230N12
S4251
CCG-101115
PS-3980
phenothiazine [hsdb]
phenothiazine [green book]
phenothiazine [who-dd]
phenothiazine [mi]
promethazine hydrochloride impurity a [ep impurity]
phenothiazine [usp-rs]
alimemazine hemitartrate impurity c [ep impurity]
HMS3372C18
NC00365
SCHEMBL9114
tox21_111090_1
NCGC00091146-08
phenothiazin
SCHEMBL2395921
W-100270
OPERA_ID_1719
AB00572590_12
mfcd00005015
phenothiazine, purum, >=98.0% (gc)
phenothiazine, united states pharmacopeia (usp) reference standard
phenothiazine, saj first grade
phenothiazine, vetranal(tm), analytical standard
HMS3652J21
phenothiazine, vetec(tm) reagent grade, 98%
HMS3715J12
SY004343
SW197745-2
CS-0008338
phenothiazine,c12h9ns,92-84-2
Q410846
F0266-2850
DB11447
EN300-19084
HMS3885P13
AMY33413
a phenothiazine
75788-67-9
HY-Y0055
alimemazine hemitartrate impurity c (ep impurity)
fenotiazina (inn-spanish)
chebi:37932
contraverm
promethazine hydrochloride impurity a (ep impurity)
chebi:38093
phenothiazinum (inn-latin)
nemazine (veterinary)
phenothiazine (usp-rs)
Z104472694
BP-31210
F90393
phenothiazine, reference standard

Research Excerpts

Overview

Phenothiazine (PTZ) is a heterocyclic thiazine compound used for industrial and medical purposes. Phenothiazines are a class of antipsychotics that share the same tricyclic structure and are widely used in clinical settings.

ExcerptReferenceRelevance
"Phenothiazines (PTZs) are a group of compounds characterized by the presence of the 10H-dibenzo-[b,e]-1,4-thiazine system. "( New phenothiazine conjugates as apoptosis inducing agents: Design, synthesis, In-vitro anti-cancer screening and
El-Haggar, RS; Elsayed, NA; Haffez, H; Sarhan, MO; Zaghary, WA, 2023
)
2.91
"Phenothiazine (PTZ) is a heterocyclic thiazine compound used for industrial and medical purposes. "( Sex-Specific Differences of Steroid Receptors Following Exposure to Environmentally Relevant Concentrations of Phenothiazine in Fundulus heteroclitus.
Calvitto, G; Chiari, JB; Laperche, JM; March, N; McGinnis, CL; Patel, R; Pylypiw, HM, 2020
)
2.21
"Phenothiazines are a class of antipsychotics that share the same tricyclic structure and are widely used in clinical settings. "( Phenothiazine antipsychotics exhibit dual properties in pseudo-allergic reactions: Activating MRGPRX2 and inhibiting the H
Cao, J; Che, D; Fu, J; He, H; Hou, Y; Wang, C; Wei, D; Xie, Y; Zhang, K; Zhou, N, 2019
)
3.4
"Phenothiazines are a commercially available class of psychotropic drugs known to show antituberculosis activity. "( Novel non-neuroleptic phenothiazines inhibit Mycobacterium tuberculosis replication.
Hsu, NJ; Jacobs, M; Jardine, A; Salie, S; Semenya, D, 2014
)
2.16
"The phenothiazine unit proved to be an important bulky unit in the structure of the synthesized inhibitors."( Peptide chemistry applied to a new family of phenothiazine-containing inhibitors of human farnesyltransferase.
Belei, D; Bîcu, E; Dubois, J; Dumitriu, GM; Farce, A; Ghinet, A; Rigo, B, 2014
)
1.14
"Phenothiazine is an aromatic tricyclic compound that first emerged from the furtive chemical activity surrounding the aniline dye industry at the latter half of the 19th century. "( Phenothiazine: the parent molecule.
Mitchell, SC, 2006
)
3.22

Effects

Phenothiazine has been found to be a strong antioxidant in eukaryotic cells in vitro and in invertebrates in vivo. Phenothiazines have been used as antipsychotics and as adjunct antiemetics during cancer chemotherapy.

ExcerptReferenceRelevance
"Phenothiazine compounds have been identified as a potential inhibitor of type IV pilus production in multiple Gram-negative bacterial species."( Type IV Pilus-Mediated Inhibition of
Piepenbrink, KH; Sidner, BS; Vo, N; Yu, Y, 2023
)
1.63
"Phenothiazine has been shown to act similarly to endocrine disrupting chemicals."( Sex-Specific Differences of Steroid Receptors Following Exposure to Environmentally Relevant Concentrations of Phenothiazine in Fundulus heteroclitus.
Calvitto, G; Chiari, JB; Laperche, JM; March, N; McGinnis, CL; Patel, R; Pylypiw, HM, 2020
)
1.49
"Phenothiazine drugs have been the subject of great interest due to their interesting aggregation properties and ability to interact with surfactants, model lipid bilayers, and biomembranes. "( Interactions of phenothiazine drugs with surfactants: a detailed physicochemical overview.
Mahajan, RK; Mahajan, S, 2013
)
2.18
"Phenothiazine has been found to be a strong antioxidant in eukaryotic cells in vitro and in invertebrates in vivo."( The antioxidative, non-psychoactive tricyclic phenothiazine reduces brain damage after experimental traumatic brain injury in mice.
Engelhard, K; Luh, C; Moosmann, B; Songarj, P; Staib-Lasarzik, I; Thal, SC, 2015
)
1.4
"The phenothiazine group has been identified as a suitable A ring in the structure of tubulin polymerization inhibitors. "( Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
Bîcu, E; Dubois, J; Farce, A; Ghinet, A; Moise, IM; Rigo, B, 2016
)
0.99
"Phenothiazines have been used as antipsychotics and as adjunct antiemetics during cancer chemotherapy and more recently have been reported to have anticancer properties."( In vitro differential sensitivity of melanomas to phenothiazines is based on the presence of codon 600 BRAF mutation.
Blower, PE; Durinck, S; Futreal, AP; Ikediobi, ON; Reimers, M; Stratton, MR; Weinstein, JN, 2008
)
1.32
"Phenothiazines have been associated with various ocular adverse effects, in particular cataract and corneal deposits. "( Phenothiazine deposits in corneo and lens.
Choong, YY; Lim, KS, 2001
)
3.2
"Phenothiazines have been demonstrated to cause elevated serum prolactin levels."( Benign papilloma of the male breast following chronic phenothiazine therapy.
Gottfried, MR; Sara, AS, 1987
)
1.24

Actions

ExcerptReferenceRelevance
"Phenothiazines inhibit major antioxidant defense mechanisms in trypanosomatids and exhibit potent cytotoxic effects in vitro. "( Could phenothiazine-benznidazole combined chemotherapy be effective in controlling heart parasitism and acute infectious myocarditis?
Caldas, IS; Diniz, LF; Gonçalves, RV; Gonçalves-Santos, E; González-Lozano, KJ; Mendonça, AAS; Novaes, RD; Souza-Silva, TG, 2020
)
2.48

Treatment

Phenothiazine treatment did not affect biliary excretion of indocyanine green and pravastatin. It increased biliary sulphobromophthalein-glutathione excretion. Treatment had little effect on the KIT/AKT/mammalian target of rapamycin (mTOR) pathway.

ExcerptReferenceRelevance
"phenothiazine or vehicle treatment. Brain lesion, neurofunctional impairment, body weight, and markers of cerebral inflammation were determined 24h after the insult."( The antioxidative, non-psychoactive tricyclic phenothiazine reduces brain damage after experimental traumatic brain injury in mice.
Engelhard, K; Luh, C; Moosmann, B; Songarj, P; Staib-Lasarzik, I; Thal, SC, 2015
)
1.4
"Phenothiazine treatment did not affect biliary excretion of indocyanine green and pravastatin, but it increased biliary sulphobromophthalein-glutathione excretion."( Effects of colchicine and phenothiazine on biliary excretion of organic anions in rats.
Akimoto, K; Ogasawara, T; Sano, N; Takikawa, H; Yamanaka, M, 1998
)
1.32
"Treatment with phenothiazine had little effect on the KIT/AKT/mammalian target of rapamycin (mTOR) pathway, but instead upregulated extracellular‑signal‑regulated kinase (ERK) activity."( Identification of phenothiazine as an ETV1‑targeting agent in gastrointestinal stromal tumors using the Connectivity Map.
Chao, Y; Chen, LT; Chen, SC; Chen, YC; Chua, WY; Fletcher, JA; Li, CF; Lin, YC; Yang, MH; Yen, CC; Yen, CH, 2019
)
1.19

Toxicity

ExcerptReferenceRelevance
" The two compounds are commercially available, approved for usage in cattle and have been reported to reverse some of the toxic effects associated with the intake of Acremonium coenophialum-infested fescue forage by cattle."( Effects of phenothiazine and thiabendazole on bovine dorsal pedal vein contractility induced by ergonovine and serotonin; potential for alleviation of fescue toxicity.
Abney, LK; Linnabary, RD; Oliver, JW; Robinson, AJ, 1992
)
0.67
" The PTZ alone was not toxic and did not inhibit EACE activity."( Toxicity and interaction of topical organophosphate insecticide dichlorvoscrotoxyphos and phenothiazine anthelmintic in sheep previously exposed to both drugs.
Mohammad, FK; St Omer, VV, 1985
)
0.49
" Drug-related toxic effects on the retina described in humans and animals are unrelated to melanin binding: melanin binding and retinal toxicity are two separate entities, the latter being related to the intrinsic toxicity of the compound rather than its ability to bind."( Binding of drugs to eye melanin is not predictive of ocular toxicity.
Davies, T; Hanton, G; Jezequel, S; Leblanc, B; Taradach, C, 1998
)
0.3
" 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

Compound-Compound Interactions

ExcerptReferenceRelevance
"The potential for drug-drug interactions in psychiatry and patients with epilepsy is very high."( Antiepileptic-antipsychotic drug interactions: a critical review of the evidence.
Monaco, F; Mula, M,
)
0.13
"A high performance thin-layer chromatography (HPTLC) method combined with densitometry for determination of phenothiazine derivatives is described."( Determination of phenothiazine derivatives by high performance thin-layer chromatography combined with densitometry.
Matysik, A; Skalska, A; Wójciak-Kosior, M, 2006
)
0.89

Bioavailability

ExcerptReferenceRelevance
"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

There was a negative correlation between the daily dosage of phenothiazine and the percentages of the polyunsaturated fatty acids arachidonic acid and alpha-linolenic acid in thrombocytes. Thiabendazole at a dosage of 44 mg/kg was tested in 8 foals, oxfendazoles at 10mg/kg were tested in 4 foals.

ExcerptRelevanceReference
" There was a negative correlation between the daily dosage of phenothiazine and the percentages of the polyunsaturated fatty acids arachidonic acid and alpha-linolenic acid+eicosapentaenoic acid+docosahexaenoic acid in thrombocytes (r = -0."( Schizophrenic patients treated with high dose phenothiazine or thioxanthene become deficient in polyunsaturated fatty acids in their thrombocytes.
Fischer, S; Kissling, W; Kuss, HJ, 1992
)
0.78
" Thiabendazole at a dosage of 44 mg/kg was tested in 8 foals, oxfendazole at 10 mg/kg was tested in 4 foals, and phenothiazine at 55 mg/kg, cambendazole at 20 mg/kg, and fenbendazole at 5 mg/kg were tested in 1 foal each."( Resistance of population-B equine strongyles to thiabendazole, oxfendazole, and phenothiazine (1981 to 1987).
Drudge, JH; Lyons, ET; Tolliver, SC, 1991
)
0.72
"The presence of a polypeptide conjugate fraction in the urine of young calves after oral dosing with phenothiazine has been confirmed."( The metabolism of phenothiazine in the neonatal calf: identification of drug-polypeptide conjugates from urine.
Mitchell, SC; Waring, RH, 1985
)
0.82
" PTZ-induced photosensitivity was widespread in the first group due to over-dosage of medicament by the dispenser and was suspected in one calf in the manually dosed group."( Low-dosage phenothiazine in the prophylaxis of trichostrongylid infection in calves.
Downey, NE; O'Shea, J, 1984
)
0.66
" After a medical prescription of the recommended dosage of 12."( [Abuse of tianeptine. A case report].
Bizouard, P; Bonin, B; Regina, W; Sechter, D; Vandel, P,
)
0.13
" Dose-response curves conducted at 30-min incubation time showed that chlorpromazine potently inhibited labelling of diacylglycerol and diacyglycerol-derived lipids (triacyglycerol and phosphatidylcholine) by the 3H-labelled precursors."( Chlorpromazine and human platelet glycerolipid metabolism: precursor specificity and significance of drug-platelet interaction time.
Daasvatn, KO; Holmsen, H, 1999
)
0.3
" The cultures and controls were incubated at 28 degrees C with shaking and dosed with 16."( Oxidation of phenothiazine and phenoxazine by Cunninghamella elegans.
Freeman, JP; Heinze, TM; Moody, JD; Parshikov, IA; Sutherland, JB; Williams, AJ; Zhang, D, 2001
)
0.68
" Each was used in four dosage levels (thioridazine and chlorpromazine: 200, 400, 800 and 1200 mg."( THE EFFECT OF PHENOTHIAZINES ON THE ELECTROCARDIOGRAM.
BAN, TA; STJEAN, A, 1964
)
0.6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
plant metaboliteAny eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms.
radical scavengerA role played by a substance that can react readily with, and thereby eliminate, radicals.
ferroptosis inhibitorAny substance that inhibits the process of ferroptosis (a type of programmed cell death dependent on iron and characterized by the accumulation of lipid peroxides) in organisms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
phenothiazine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (89)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency7.94330.004023.8416100.0000AID485290
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency50.11870.631035.7641100.0000AID504339
LuciferasePhotinus pyralis (common eastern firefly)Potency41.78180.007215.758889.3584AID1224835
interleukin 8Homo sapiens (human)Potency74.97800.047349.480674.9780AID651758
acetylcholinesteraseHomo sapiens (human)Potency79.64070.002541.796015,848.9004AID1347398
15-lipoxygenase, partialHomo sapiens (human)Potency6.30960.012610.691788.5700AID887
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency0.00103.189029.884159.4836AID1224846
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.48560.006038.004119,952.5996AID1159521
USP1 protein, partialHomo sapiens (human)Potency4.90190.031637.5844354.8130AID504865; AID743255
TDP1 proteinHomo sapiens (human)Potency20.89130.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency27.30600.000714.592883.7951AID1259369
Microtubule-associated protein tauHomo sapiens (human)Potency17.78280.180013.557439.8107AID1460
AR proteinHomo sapiens (human)Potency25.27910.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID588516; AID743042; AID743054
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency35.48130.707912.194339.8107AID720542
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency18.21670.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency9.51800.000417.946075.1148AID1346784; AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.32480.01237.983543.2770AID1346984; AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency17.12610.000214.376460.0339AID720691; AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency30.63790.003041.611522,387.1992AID1159552
retinoid X nuclear receptor alphaHomo sapiens (human)Potency13.80060.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency28.25380.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency17.75170.375827.485161.6524AID743217; AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency35.15530.005428.02631,258.9301AID1346982; AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency29.14900.000229.305416,493.5996AID588514; AID743069; AID743075; AID743079
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency12.58930.707936.904389.1251AID504333
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency77.60620.001024.504861.6448AID743215
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency22.98760.001019.414170.9645AID588537; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency0.00310.023723.228263.5986AID743223
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.10610.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency38.38430.000723.06741,258.9301AID743085
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency21.13300.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency21.11120.001628.015177.1139AID1224843; AID1224895; AID1259385
activating transcription factor 6Homo sapiens (human)Potency48.96620.143427.612159.8106AID1159516
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency20.79330.057821.109761.2679AID1159526; AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency36.97660.039147.5451146.8240AID1224845; AID1224896
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency17.78280.036619.637650.1187AID2100
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency24.80331.000012.232631.6228AID1452
chromobox protein homolog 1Homo sapiens (human)Potency25.11890.006026.168889.1251AID540317
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency50.11873.548119.542744.6684AID743266
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency9.83440.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency38.08630.000323.4451159.6830AID743065; AID743066
DNA polymerase betaHomo sapiens (human)Potency89.12510.022421.010289.1251AID485314
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency44.42890.000627.21521,122.0200AID651741; AID720636; AID743202
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency12.58930.00798.23321,122.0200AID2551
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency31.62280.031610.279239.8107AID884; AID885
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency31.62280.00419.962528.1838AID2675
lethal factor (plasmid)Bacillus anthracis str. A2012Potency15.84890.020010.786931.6228AID912
lamin isoform A-delta10Homo sapiens (human)Potency0.00090.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency5.01190.316212.765731.6228AID881
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency5.01190.00638.235039.8107AID881
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency25.11890.009610.525035.4813AID1479145
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
NADPH oxidase 1Homo sapiens (human)IC50 (µMol)0.35890.04401.26095.5000AID2538; AID2808
rac GTPase-activating protein 1 isoform aHomo sapiens (human)IC50 (µMol)18.50007.390057.8904301.2400AID624330
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)2.23600.00011.00768.7800AID625218
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki1.17100.00000.887110.0000AID625218
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)0.01600.00011.774010.0000AID625245
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)0.46100.00041.877310.0000AID625207
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.45700.00322.28879.3160AID625207
Adenosine receptor A3Homo sapiens (human)IC50 (µMol)25.64000.00001.89408.5470AID625196
Adenosine receptor A3Homo sapiens (human)Ki14.49200.00000.930610.0000AID625196
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50 (µMol)1.40000.00462.018210.0000AID6824
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC50 (µMol)4.64300.11003.26419.0330AID625146
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)25.64000.00021.874210.0000AID625196
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki14.49200.00010.949010.0000AID625196
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)0.59200.00002.37899.7700AID625150
Cannabinoid receptor 1Homo sapiens (human)IC50 (µMol)24.85700.00010.275310.0000AID625235
Cannabinoid receptor 1Homo sapiens (human)Ki19.62400.00010.50779.6000AID625235
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)0.19600.00021.557410.0000AID625243
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)0.46100.00081.541620.0000AID625207
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.45700.00031.465610.0000AID625207
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)2.23600.00011.03029.0000AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki1.17100.00010.954910.0000AID625218
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CIC50 (µMol)400.00001.30003.37279.6000AID581672
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)0.53200.00010.995010.0000AID625244
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50 (µMol)0.94000.00291.786810.0000AID160880
Alpha-synucleinHomo sapiens (human)IC50 (µMol)26.00000.19003.82049.8000AID674590
Alpha-synucleinHomo sapiens (human)Ki0.50000.08440.08440.0844AID674590
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)25.64000.00001.819410.0000AID625196
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki14.49200.00000.965010.0000AID625196
Sodium-dependent dopamine transporter Homo sapiens (human)IC50 (µMol)18.63600.00071.841946.0000AID625256
Sodium-dependent dopamine transporter Homo sapiens (human)Ki14.80700.00021.11158.0280AID625256
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.94000.00291.823210.0000AID160880
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Snq2pSaccharomyces cerevisiae EC1118INH90.00003.20006.26008.8000AID581808
Pleiotropic ABC efflux transporter of multiple drugsSaccharomyces cerevisiae S288CINH433.00004.20006.18338.3000AID581806
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (254)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo 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)
positive regulation of acute inflammatory response to antigenic stimulusCannabinoid receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerCannabinoid receptor 1Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayCannabinoid receptor 1Homo sapiens (human)
spermatogenesisCannabinoid receptor 1Homo sapiens (human)
axonal fasciculationCannabinoid receptor 1Homo sapiens (human)
response to nutrientCannabinoid receptor 1Homo sapiens (human)
memoryCannabinoid receptor 1Homo sapiens (human)
positive regulation of neuron projection developmentCannabinoid receptor 1Homo sapiens (human)
negative regulation of serotonin secretionCannabinoid receptor 1Homo sapiens (human)
positive regulation of fever generationCannabinoid receptor 1Homo sapiens (human)
negative regulation of fatty acid beta-oxidationCannabinoid receptor 1Homo sapiens (human)
regulation of synaptic transmission, GABAergicCannabinoid receptor 1Homo sapiens (human)
response to lipopolysaccharideCannabinoid receptor 1Homo sapiens (human)
negative regulation of mast cell activationCannabinoid receptor 1Homo sapiens (human)
negative regulation of dopamine secretionCannabinoid receptor 1Homo sapiens (human)
response to nicotineCannabinoid receptor 1Homo sapiens (human)
cannabinoid signaling pathwayCannabinoid receptor 1Homo sapiens (human)
response to cocaineCannabinoid receptor 1Homo sapiens (human)
glucose homeostasisCannabinoid receptor 1Homo sapiens (human)
positive regulation of apoptotic processCannabinoid receptor 1Homo sapiens (human)
response to ethanolCannabinoid receptor 1Homo sapiens (human)
negative regulation of action potentialCannabinoid receptor 1Homo sapiens (human)
negative regulation of blood pressureCannabinoid receptor 1Homo sapiens (human)
positive regulation of blood pressureCannabinoid receptor 1Homo sapiens (human)
regulation of insulin secretionCannabinoid receptor 1Homo sapiens (human)
regulation of synaptic transmission, glutamatergicCannabinoid receptor 1Homo sapiens (human)
maternal process involved in female pregnancyCannabinoid receptor 1Homo sapiens (human)
regulation of feeding behaviorCannabinoid receptor 1Homo sapiens (human)
regulation of penile erectionCannabinoid receptor 1Homo sapiens (human)
retrograde trans-synaptic signaling by endocannabinoidCannabinoid receptor 1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationCannabinoid receptor 1Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionCannabinoid receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayCannabinoid receptor 1Homo sapiens (human)
regulation of metabolic processCannabinoid receptor 1Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo sapiens (human)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (72)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo 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 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo 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)
cannabinoid receptor activityCannabinoid receptor 1Homo sapiens (human)
protein bindingCannabinoid receptor 1Homo sapiens (human)
identical protein bindingCannabinoid receptor 1Homo sapiens (human)
G protein-coupled receptor activityCannabinoid receptor 1Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo sapiens (human)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (51)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo 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)
mitochondrial outer membraneCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 1Homo sapiens (human)
actin cytoskeletonCannabinoid receptor 1Homo sapiens (human)
growth coneCannabinoid receptor 1Homo sapiens (human)
presynaptic membraneCannabinoid receptor 1Homo sapiens (human)
membrane raftCannabinoid receptor 1Homo sapiens (human)
glutamatergic synapseCannabinoid receptor 1Homo sapiens (human)
GABA-ergic synapseCannabinoid receptor 1Homo sapiens (human)
plasma membraneCannabinoid receptor 1Homo sapiens (human)
cytoplasmCannabinoid receptor 1Homo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (102)

Assay IDTitleYearJournalArticle
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
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.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
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.
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.
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.
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.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary 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.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
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A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
AID293683Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis inhibition time at 50.8 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
AID346025Binding affinity to beta cyclodextrin2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Convenient QSAR model for predicting the complexation of structurally diverse compounds with beta-cyclodextrins.
AID547804Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID581806Inhibition of Saccharomyces cerevisiae MKPDR5h multidrug transporter Pdr5p assessed as concentration required to threefold increase in rate of fluorescence signal relative to absence of inhibitor by fluorescein diacetate based high-throughput screening sp2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
New high-throughput screening assay to reveal similarities and differences in inhibitory sensitivities of multidrug ATP-binding cassette transporters.
AID293658Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis time at 37.3 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
AID1766052Inhibition of human GluN1-1a/NR2B receptor expressed in transgenic mouse fibroblast cells assessed as inhibition of L-glutamate-induced excitotoxicity at 20 uM by measuring LDH activity by cell based assay2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors.
AID167130In vitro inhibition of iron-dependent peroxidation of rabbit brain vesicular membrane lipids1992Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4
Phenothiazines as lipid peroxidation inhibitors and cytoprotective agents.
AID160880In vitro inhibition of Prostaglandin G/H synthase pathway in rat basophilic leukemia (RBL-1) cells1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
1,2-Dihydro-1-oxopyrrolo[3,2,1-kl]phenothiazine-2-carboxamides and congeners, dual cyclooxygenase/5-lipoxygenase inhibitors with antiinflammatory activity.
AID293680Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis inhibition time at 20.3 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
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.
AID293659Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis time at 50.8 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
AID410171Stimulation of DNA triplet repeat slippage synthesis using p33-labeled (ATT)3 and unlabeled (AAT)5 template assessed as number of base pairs2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
A bulge binding agent with novel wedge-shape topology for stimulation of DNA triplet repeat strand slippage synthesis.
AID605844Antiproliferative activity against human K562 cells after 48 hrs by hemocytometric analysis2011Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization.
AID581808Inhibition of Saccharomyces cerevisiae MKSNQ2h multidrug transporter Snq2p assessed as concentration required to threefold increase in rate of fluorescence signal relative to absence of inhibitor by fluorescein diacetate based high-throughput screening sp2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
New high-throughput screening assay to reveal similarities and differences in inhibitory sensitivities of multidrug ATP-binding cassette transporters.
AID1766060Solubility of the compound in buffer at > 20 uM2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors.
AID293660Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis time at 61 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
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.
AID214489Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase; No inhibition at 1000 uM1998Journal of medicinal chemistry, Jan-15, Volume: 41, Issue:2
Phenothiazine inhibitors of trypanothione reductase as potential antitrypanosomal and antileishmanial drugs.
AID674590Binding affinity to human alpha-synuclein expressed in Escherichia coli BL21 (DE3) cells after 1 hr by thioflavin T fluorescence assay2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Synthesis and in vitro evaluation of α-synuclein ligands.
AID420787Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced inward Na+ current at >= 10 uM2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Molecular properties of psychopharmacological drugs determining non-competitive inhibition of 5-HT3A receptors.
AID673777Cytotoxicity in UV-irradiated human U937 cells exposed to photosensitizer for 2 hrs before irradiation for 20 mins by WST-1 assay2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
Type 1 Phototherapeutic Agents. 2. Cancer Cell Viability and ESR Studies of Tricyclic Diarylamines.
AID293135Antimicrobial activity against Bacillus subtilis2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
Design, synthesis, and evaluation of efflux substrate-metal chelator conjugates as potential antimicrobial agents.
AID581807Inhibition of Saccharomyces cerevisiae MKCDR1h multidrug transporter Cdr1p assessed as concentration required to threefold increase in rate of fluorescence signal relative to absence of inhibitor by fluorescein diacetate based high-throughput screening sp2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
New high-throughput screening assay to reveal similarities and differences in inhibitory sensitivities of multidrug ATP-binding cassette transporters.
AID678816TP_TRANSPORTER: Northern blot in vivo Fischer male rat1988Journal of the National Cancer Institute, Nov-02, Volume: 80, Issue:17
Coinduction of MDR-1 multidrug-resistance and cytochrome P-450 genes in rat liver by xenobiotics.
AID581672Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
New high-throughput screening assay to reveal similarities and differences in inhibitory sensitivities of multidrug ATP-binding cassette transporters.
AID1161121Bactericidal activity against Mycobacterium smegmatis at 8.9 uM after 3 to 24 hrs by colony forming unit count method2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Incorporation of triphenylphosphonium functionality improves the inhibitory properties of phenothiazine derivatives in Mycobacterium tuberculosis.
AID547621Cytotoxicity against BESM cells after 88 hrs by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID1766057Inhibition of recombinant equine BChE at 20 uM by Ellman's method relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors.
AID293681Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis inhibition time at 30.5 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
AID293656Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis time at 20.3 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
AID1161116Antimicrobial activity against Mycobacterium smegmatis (MC2) 155 after 24 hrs by serial macrobroth dilution method2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Incorporation of triphenylphosphonium functionality improves the inhibitory properties of phenothiazine derivatives in Mycobacterium tuberculosis.
AID1161117Antimicrobial activity against Mycobacterium tuberculosis H37Ra after 5 days by serial macrobroth dilution method2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Incorporation of triphenylphosphonium functionality improves the inhibitory properties of phenothiazine derivatives in Mycobacterium tuberculosis.
AID293657Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis time at 30.5 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
AID625295Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in Pfizer data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID293682Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis inhibition time at 37.3 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
AID547622Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID1727546Inhibition of erastin-induced ferroptosis in human HT-1080 cells assessed as cell viability incubated for 48 hrs by MTT assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Structure-activity relationship studies of phenothiazine derivatives as a new class of ferroptosis inhibitors together with the therapeutic effect in an ischemic stroke model.
AID6824In vitro inhibition of 5-lipoxygenase pathway in rat basophilic leukemia (RBL-1) cells1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
1,2-Dihydro-1-oxopyrrolo[3,2,1-kl]phenothiazine-2-carboxamides and congeners, dual cyclooxygenase/5-lipoxygenase inhibitors with antiinflammatory activity.
AID1766055Inhibition of recombinant human AChE expressed in HEK293 cells at 20 uM by Ellman's method relative to control2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors.
AID1161119Inhibition of NDH2 in Mycobacterium smegmatis (MC2) 155 membranes assessed NADH oxidation relative to control2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Incorporation of triphenylphosphonium functionality improves the inhibitory properties of phenothiazine derivatives in Mycobacterium tuberculosis.
AID605956Inhibition of pig tubulin polymerization determined after 45 mins at 37 degC by turbidimetric analysis2011Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization.
AID410167Binding affinity to ATT-bulge-DNA by surface plasmon resonance based assay2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
A bulge binding agent with novel wedge-shape topology for stimulation of DNA triplet repeat strand slippage synthesis.
AID293684Inhibition of AAPH-induced hemolysis in human erythrocytes assessed as hemolysis inhibition time at 61 uM2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Free-radical-scavenging effect of carbazole derivatives on AAPH-induced hemolysis of human erythrocytes.
AID1766050Inhibition of human GluN1-1a/NR2A receptor expressed in transgenic mouse fibroblast cells assessed as inhibition of L-glutamate-induced excitotoxicity at 50 uM by measuring LDH activity by cell based assay2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
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AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
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[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,375)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902020 (85.05)18.7374
1990's47 (1.98)18.2507
2000's92 (3.87)29.6817
2010's168 (7.07)24.3611
2020's48 (2.02)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 79.94

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 Index79.94 (24.57)
Research Supply Index7.85 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index144.80 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (79.94)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (0.27%)5.53%
Reviews57 (2.23%)6.00%
Case Studies21 (0.82%)4.05%
Observational0 (0.00%)0.25%
Other2,468 (96.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Prospective, Open Label, Non-comparative Trial to Determine the Incidence of Chemotherapy-Induced Nausea and Vomiting (CINV) Associated With the Docetaxel-Cyclophosphamide Regimen in Early Breast Cancer Patients [NCT01298193]Phase 4212 participants (Actual)Interventional2011-05-31Completed
Safety of Artesunate-amodiaquine Combined With Methylene Blue or Primaquine for Falciparum Malaria Treatment in African Children: A Randomised Controlled Trial [NCT02851108]Phase 2100 participants (Actual)Interventional2016-10-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01298193 (9) [back to overview]Number of Participants With Complete Response (CR)
NCT01298193 (9) [back to overview]Number of Participants With Complete Response (CR) in Cycle 2 for Patient Without Complete Response in Cycle 1
NCT01298193 (9) [back to overview]Number of Participants With Treatment Related Adverse Events (AE) at Cycle 2
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2
NCT01298193 (9) [back to overview]Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1
NCT01298193 (9) [back to overview]Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2
NCT02851108 (1) [back to overview]Change in Haemoglobin Compared to the Baseline

Number of Participants With Complete Response (CR)

Complete response is defined as no vomiting and no use of rescue treatment within the first cycle of Docetaxel-Cyclophosphamide for the treatment of early-stage breast cancer patients. A vomiting episode is defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retches (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes are, by definition, separated by the absence of emesis and retching for at least 1 minute. The timing (date and time) of each vomiting episode will be recorded by the patient in each cycle diary at the time of occurrence. Assessments of efficacy will begin at the initiation of chemotherapy infusion (0 hours) until the morning of Day 6 (approximately 120 hours) after chemotherapy during 1-2 cycles. (NCT01298193)
Timeframe: Up to 21 days after cycle 1 of chemotherapy treatment

InterventionParticipants (Count of Participants)
Observational Phase (First Cycle):161

[back to top]

Number of Participants With Complete Response (CR) in Cycle 2 for Patient Without Complete Response in Cycle 1

To evaluate in cycle 2 the efficacy of aprepitant (days 1, 2 and 3) as secondary prevention in patients without complete response in cycle 1. A vomiting episode is defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retches (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes are, by definition, separated by the absence of emesis and retching for at least 1 minute. The timing (date and time) of each vomiting episode will be recorded by the patient in each cycle diary at the time of occurrence. Assessments of efficacy will begin at the initiation of chemotherapy infusion (0 hours) until the morning of Day 6 (approximately 120 hours) after chemotherapy during 1-2 cycles. (NCT01298193)
Timeframe: Up to cycle 2, and average of 6 weeks

InterventionParticipants (Count of Participants)
Aprepitant NCR12

[back to top] [back to top]

Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1

"To determine the incidence of nausea associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Chemotherapy-Induced Nausea and vomiting on daily life. There are 9 nausea-related items, each on a 7-point scale. Results are reported as a nausea score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 1 pre-chemotherapy NCR patientsCycle 1 post-chemotherapy NCR patientsCycle 1 pre-chemotherapy CR patientsCycle 1 post-chemotherapy CR patients
Aprepitant19.8531.7318.9320.27

[back to top]

Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2

"To determine the incidence of Nausea associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Nausea on daily life. There are 9 items, each on a 7-point scale. Results are reported as a nausea score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 2 pre-chemotherapy NCR patientsCycle 2 post-chemotherapy NCR patientsCycle 2 pre-chemotherapy CR patientsCycle 2 post-chemotherapy CR patients
Aprepitant NCR17.7136.1619.5724.30

[back to top]

Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1

"To determine the incidence of vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of vomiting on daily life. There are 9 vomiting-related items, each on a 7-point scale. Results are reported as a vomiting score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of vomiting (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 1 pre-chemotherapy NCR patientsCycle 1 post-chemotherapy NCR patientsCycle 1 pre-chemotherapy CR patientsCycle 1 post-chemotherapy CR patients
Aprepitant23.8627.4623.5324.15

[back to top]

Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2

"To determine the incidence of vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of vomiting on daily life. There are 9 items, each on a 7-point scale. Results are reported as a vomiting score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of vomiting (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 2 pre-chemotherapy NCR patientsCycle 2 post-chemotherapy NCR patientsCycle 2 pre-chemotherapy CR patientsCycle 2 post-chemotherapy CR patients
Aprepitant NCR20.0928.1923.7123.43

[back to top]

Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1

"To determine the incidence of Chemotherapy-Induced Nausea and Vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Chemotherapy-Induced Nausea and Vomiting on daily life. There are 18 items, each on a 7-point scale. Results are reported as a total score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea or vomiting (better outcome) (Maximum 126, Minimum 18)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 1 pre-chemotherapy NCR patientsCycle 1 post-chemotherapy NCR patientsCycle 1 pre-chemotherapy CR patientsCycle 1 post-chemotherapy CR patients
Aprepitant43.759.242.544.22

[back to top]

Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2

"To determine the total incidence of Chemotherapy-Induced Nausea and Vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Chemotherapy-Induced Nausea and Vomiting on daily life. There are 18 items, each on a 7-point scale. Results are reported as a total score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea or vomiting (better outcome) (Maximum 126, Minimum 18)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 2 pre-chemotherapy NCR patientsCycle 2 post-chemotherapy NCR patientsCycle 2 pre-chemotherapy CR patientsCycle 2 post-chemotherapy CR patients
Aprepitant NCR37.864.443.2847.7

[back to top]

Change in Haemoglobin Compared to the Baseline

Haemoglobin concentrations will be measured in the field using a HemoCue® (HemoCue® AB, Angelholm, Sweden) (NCT02851108)
Timeframe: 7 days

Interventiong/dl (Mean)
AS-AQ-MB0.18
AS-AQ-PQ0.54

[back to top]