Page last updated: 2024-11-05

chlorquinaldol

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Description

Chlorquinaldol: Local anti-infective agent used for skin, gastrointestinal, and vaginal infections with fungi, protozoa, and certain bacteria. In animals, it causes central nervous system damage and is not administered parenterally. It is also used as antiseptic, fungistat, or deodorant. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

chlorquinaldol : A monohydroxyquinoline that is quinolin-8-ol which is substituted by a methyl group at position 2 and by chlorine at positions 5 and 7. An antifungal and antibacterial, it was formerly used for topical treatment of skin conditions and vaginal infections. [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 CID6301
CHEMBL ID224325
CHEBI ID74500
SCHEMBL ID301405
MeSH IDM0004208

Synonyms (119)

Synonym
clorquinaldol [inn-spanish]
chlorquinaldolum [inn-latin]
chlorchinaldolum
sterosan
siogene
5,7-dichloro-8-hydroxyquinaldine
5,7-dichloro-2-methyl-8-hydroxyquinoline
chlorquinaldol [inn:ban:dcf]
hydroxydichloroquinaldine
clorchinaldolo [dcit]
steroxin
chloroquinaldol
siasteran
einecs 200-789-3
gyno-sterosan
5,7-dichloro-8-quinaldinol
chlorchinaldol
brn 0156683
siosteran
8-quinolinol, 5,7-dichloro-2-methyl-
chlorquinaldol
OPREA1_721210
BSPBIO_002764
chlorquinaldol (inn)
D07208
5,7-dichloro-2-methyl-quinolin-8-ol
72-80-0
5,7-dichloro-2-methyl-8-quinolinol
5,7-dichloro-8-hydroxy-2-methylquinoline
NCGC00095795-02
5,7-dichloro-8-hydroxy-2-methylquinoline, 98%
NCGC00095795-01
KBIOGR_001846
KBIO3_001984
SPECTRUM3_001092
SPECTRUM2_000524
SPECTRUM4_001263
SPBIO_000507
SPECTRUM212151
NCGC00095795-03
chlorquinaldol, chlorquinaldol (5,7-dichloro-2-methyl-8-quinolinol)
smr001549973
MLS002695929 ,
clorquinaldol
CHEMBL224325
nsc-755830
chebi:74500 ,
5,7-dichloro-2-methylquinolin-8-ol
AKOS000119838
A837624
NCGC00095795-04
HMS3264I07
5-21-03-00346 (beilstein handbook reference)
d6vhc87lls ,
unii-d6vhc87lls
nsc 755830
HMS3089A18
dtxsid3048998 ,
tox21_113490
cas-72-80-0
dtxcid3028924
pharmakon1600-00212151
nsc755830
clorchinaldolo
chlorquinaldolum
S4192
CCG-39580
FT-0623717
2-methyl-5,7-dichloro-8-hydroxyquinoline
chlorquinaldol [inn]
chlorquinaldol [mart.]
chlorquinaldol [who-dd]
chlorquinaldol [mi]
S10253
SCHEMBL301405
tox21_113490_1
NCGC00095795-06
cid_6301
5,7-bis(chloranyl)-2-methyl-quinolin-8-ol
bdbm76302
CS-4899
W-104478
hydroxydichloroquinaldinol
vagisteran
gynotherax
siosept
florabina
saprosan
siogen
quesil
siogeno
chloquinan
chlorchinaldin
sterozan
siogenal
quinolin-8-ol, 5,7-dichloro-2-methyl-
siogenon
chlorguinaldon
PS-7753
HY-B1360
AC-29743
AB00443827_06
AB00443827_07
mfcd00023984
SR-01000872737-1
sr-01000872737
HMS3652H09
SBI-0207012.P001
SW220230-1
STL502989
Z104475058
DB13306
5-bromo 2-isobutoxy benzonitirle
BCP11865
Q1645622
A16448
5,7-dichloro-8-hydroxyquinaldine 5,7-dichloro-2-methyl-8-hydroxyquinoline
SY015325
EN300-19748

Research Excerpts

Overview

Chlorquinaldol (CQD) is a topical antimicrobial agent used to treat skin infections.

ExcerptReferenceRelevance
"Chlorquinaldol (CQD) is a topical antimicrobial agent used to treat skin infections."( Chlorquinaldol targets the β-catenin and T-cell factor 4 complex and exerts anti-colorectal cancer activity.
Deng, K; Gong, L; Li, H; Liu, S; Lu, D; Sayed, S; Song, J; Su, Z; Sun, Q; Wang, L; Wang, Z; Zhou, L; Zhu, H, 2020
)
2.72

Effects

ExcerptReferenceRelevance
"As chlorquinaldol has no known anti-inflammatory activity, we attribute this improvement to difluocortolone valerate."( Therapeutic use of topical corticosteroids in the vesiculobullous lesions of incontinentia pigmenti.
Ikizoglu, G; Kaya, TI; Tursen, U, 2009
)
0.87

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

ExcerptRelevanceReference
"8, but display excellent solubility at low pH, suggesting that oral dosing may be possible."( Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
Barlow, DJ; Benoni, G; Bompiani, KM; Caglič, D; Dickerson, TJ; Houseknecht, KL; Krutein, MC; Lairson, LL; Pelletier, JC; Reitz, AB; Smith, GR, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
antiseptic drugA substance used locally on humans and other animals to destroy harmful microorganisms or to inhibit their activity (cf. disinfectants, which destroy microorganisms found on non-living objects, and antibiotics, which can be transported through the lymphatic system to destroy bacteria within the body).
antiprotozoal drugAny antimicrobial drug which is used to treat or prevent protozoal infections.
[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 (2)

ClassDescription
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
monohydroxyquinolineA hydroxyquinoline carrying a single hydroxy substituent.
[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 (33)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nrf2Homo sapiens (human)Potency22.38720.09208.222223.1093AID624171
glp-1 receptor, partialHomo sapiens (human)Potency2.51190.01846.806014.1254AID624417
RAR-related orphan receptor gammaMus musculus (house mouse)Potency5.30800.006038.004119,952.5996AID1159521
GLS proteinHomo sapiens (human)Potency17.78280.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency4.88530.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency0.02510.180013.557439.8107AID1468
AR proteinHomo sapiens (human)Potency6.61380.000221.22318,912.5098AID743036; AID743042; AID743053; AID743054
Smad3Homo sapiens (human)Potency12.58930.00527.809829.0929AID588855
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency1.77830.707912.194339.8107AID720542
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency37.90830.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency21.88130.000214.376460.0339AID720691; AID720692
estrogen nuclear receptor alphaHomo sapiens (human)Potency10.40730.000229.305416,493.5996AID743069; AID743075; AID743079; AID743080; AID743091
67.9K proteinVaccinia virusPotency20.08500.00018.4406100.0000AID720579; AID720580
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency9.34130.001019.414170.9645AID743094; AID743140
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency40.99030.016525.307841.3999AID602332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency13.33320.001723.839378.1014AID743083
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency1.23850.000323.4451159.6830AID743065; AID743066; AID743067
importin subunit beta-1 isoform 1Homo sapiens (human)Potency44.66845.804836.130665.1308AID540263
snurportin-1Homo sapiens (human)Potency44.66845.804836.130665.1308AID540263
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency84.92140.425612.059128.1838AID504891
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency0.72680.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency15.45940.004611.374133.4983AID624296; AID624297
VprHuman immunodeficiency virus 1Potency10.00001.584919.626463.0957AID651644
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency6.30960.025911.239831.6228AID602313
Glycoprotein hormones alpha chainHomo sapiens (human)Potency3.16234.46688.344810.0000AID624291
Cellular tumor antigen p53Homo sapiens (human)Potency2.67800.002319.595674.0614AID651631; AID720552
TAR DNA-binding protein 43Homo sapiens (human)Potency35.48131.778316.208135.4813AID652104
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency5.63190.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency5.95570.011912.222168.7989AID651632
[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)
Botulinum neurotoxin type A Clostridium botulinumIC50 (µMol)10.10000.50003.16927.2000AID1068575
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LAP4Saccharomyces cerevisiae (brewer's yeast)EC50 (µMol)5.38500.45008.371433.0000AID488823
RPL19ASaccharomyces cerevisiae (brewer's yeast)EC50 (µMol)14.74000.42005.576025.3600AID488814
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (170)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of cell population proliferationGlycoprotein hormones alpha chainHomo sapiens (human)
hormone-mediated signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
regulation of signaling receptor activityGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of steroid biosynthetic processGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of cell migrationGlycoprotein hormones alpha chainHomo sapiens (human)
thyroid gland developmentGlycoprotein hormones alpha chainHomo sapiens (human)
luteinizing hormone secretionGlycoprotein hormones alpha chainHomo sapiens (human)
organ growthGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlycoprotein hormones alpha chainHomo sapiens (human)
negative regulation of organ growthGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone secretionGlycoprotein hormones alpha chainHomo sapiens (human)
thyroid hormone generationGlycoprotein hormones alpha chainHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (47)

Processvia Protein(s)Taxonomy
hormone activityGlycoprotein hormones alpha chainHomo sapiens (human)
protein bindingGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone activityGlycoprotein hormones alpha chainHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
protein transmembrane transporter activityBotulinum neurotoxin type A Clostridium botulinum
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
extracellular regionGlycoprotein hormones alpha chainHomo sapiens (human)
extracellular spaceGlycoprotein hormones alpha chainHomo sapiens (human)
Golgi lumenGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone complexGlycoprotein hormones alpha chainHomo sapiens (human)
pituitary gonadotropin complexGlycoprotein hormones alpha chainHomo sapiens (human)
extracellular spaceGlycoprotein hormones alpha chainHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (71)

Assay IDTitleYearJournalArticle
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.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1824261Inhibition of recombinant NDM-1 (unknown origin) using fluorocillin as substrate at 10 uM incubated for 30 mins by fluorescence based assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
AID1068572Half life in human liver microsomes at 1 uM by reversed phase LC/MS analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID1068571Metabolic stability in human plasma assessed as compound remaining at 1 uM measured at 3 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID1068575Inhibition of Clostridium botulinum BoNT/A LC expressed in Escherichia coli assessed as cleavage of SNAPtide preincubated for 5 mins followed by SNAPtide addition measured for 105 mins by fluorescence assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID1824264Inhibition of recombinant VIM-1 (unknown origin) using fluorocillin as substrate at 10 uM incubated for 30 mins by fluorescence based assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
AID1068573Drug metabolism in human liver microsomes assessed as metabolic rate at 1 uM by reversed phase LC/MS analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1068566Metabolic stability in Sprague-Dawley rat plasma assessed as compound remaining at 1 uM measured at 3 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID1068565Aqueous solubility of the compound at pH 6.8 after 24 hrs by shake flask method2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID1068568Half life in Sprague-Dawley rat liver microsomes at 1 uM by reversed phase LC/MS analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID1824268Inhibition of recombinant IMP-1 (unknown origin) using fluorocillin as substrate at 3 uM incubated for 30 mins by fluorescence based assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
AID1824267Inhibition of recombinant IMP-1 (unknown origin) using fluorocillin as substrate at 10 uM incubated for 30 mins by fluorescence based assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
AID1824260Inhibition of recombinant NDM-1 (unknown origin) using fluorocillin as substrate at 30 uM incubated for 30 mins by fluorescence based assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
AID1824262Inhibition of recombinant NDM-1 (unknown origin) using fluorocillin as substrate at 3 uM incubated for 30 mins by fluorescence based assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
AID1824263Inhibition of recombinant VIM-1 (unknown origin) using fluorocillin as substrate at 30 uM incubated for 30 mins by fluorescence based assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
AID1068563Aqueous solubility of the compound at pH 1 after 24 hrs by shake flask method2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID1068570Half life in human plasma at 1 uM by LC-MS/MS analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID1068569Drug metabolism in Sprague-Dawley rat liver microsomes assessed as metabolic rate at 1 uM by reversed phase LC/MS analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1824265Inhibition of recombinant VIM-1 (unknown origin) using fluorocillin as substrate at 3 uM incubated for 30 mins by fluorescence based assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
AID1824266Inhibition of recombinant IMP-1 (unknown origin) using fluorocillin as substrate at 30 uM incubated for 30 mins by fluorescence based assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Nitroxoline and its derivatives are potent inhibitors of metallo-β-lactamases.
AID283249Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 by microplate alamar blue assay2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of cloxyquin (5-chloroquinolin-8-ol) against Mycobacterium tuberculosis.
AID1068567Half life in Sprague-Dawley rat plasma at 1 uM by LC-MS/MS analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745849Viability Counterscreen for CMV-Luciferase Assay of Inhibitors of ATXN expression
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.
AID1745850Viability Counterscreen for Confirmatory qHTS for Inhibitors of ATXN expression
AID1745847CMV-Luciferase Counterscreen for Inhibitors of ATXN expression
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.
AID1745848Confirmatory qHTS for Inhibitors of ATXN expression
AID1745846Firefly Luciferase Counterscreen for Inhibitors of ATXN expression
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (139)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990100 (71.94)18.7374
1990's10 (7.19)18.2507
2000's6 (4.32)29.6817
2010's13 (9.35)24.3611
2020's10 (7.19)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 36.30

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

MetricThis Compound (vs All)
Research Demand Index36.30 (24.57)
Research Supply Index5.09 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index53.49 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (36.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (10.96%)5.53%
Reviews6 (4.11%)6.00%
Case Studies6 (4.11%)4.05%
Observational1 (0.68%)0.25%
Other117 (80.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Use of Colposeptine in Bacterial Vaginosis. A Randomized, Controlled Study [NCT01153958]Phase 4133 participants (Actual)Interventional2010-07-31Terminated
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01153958 (6) [back to overview]Number of Participants With Adverse Events (AEs)
NCT01153958 (6) [back to overview]Percentage of Participants Cured
NCT01153958 (6) [back to overview]Percentage of Participants With Relapse 1 Month Post-treatment
NCT01153958 (6) [back to overview]Percentage of Participants With Relapse 2 Months Post-treatment
NCT01153958 (6) [back to overview]Change From Baseline in Nugent Score at 2 Months Post-treatment
NCT01153958 (6) [back to overview]Change From Baseline in Number of Participants With Each Grade of Lactobacilli at 2 Months Post-treatment

Number of Participants With Adverse Events (AEs)

An AE was defined as any untoward medical occurrence in the form of signs, symptoms, abnormal laboratory findings, or diseases that emerges or worsens relative to baseline during a clinical study with an Investigational Medicinal Product (IMP), regardless of causal relationship and even if no IMP has been administered. (NCT01153958)
Timeframe: Up to 2 months post-treatment

Interventionparticipants (Number)
Colposeptine8
Metronidazole8

[back to top]

Percentage of Participants Cured

Cure was defined as Nugent score less than 7, no symptoms of vaginal irritation (for example, pain, burning, odour or abnormal vaginal discharge). Nugent score was calculated by assessing for presence of large Gram-positive rods (Lactobacillus morphotypes; decrease in Lactobacillus scored as 0-4), small Gram-variable rods (Gardnerella vaginalis morphotypes; scored as 0-4), and curved Gram-variable rods (Mobiluncus species morphotypes; scored as 0-2). Total score range: 0-10. Score of 7-10 indicated bacterial vaginosis. (NCT01153958)
Timeframe: 1 week post-treatment

Interventionpercentage of participants (Number)
Colposeptine22.9
Metronidazole17.8

[back to top]

Percentage of Participants With Relapse 1 Month Post-treatment

Relapse: recurrence of the symptoms of bacterial vaginosis [BV] (Nugent score greater than or equal to 7, symptoms of vaginal irritation for example, pain, burning, odour or abnormal vaginal discharge) after a period of improvement. Nugent score was calculated by assessing for presence of large Gram-positive rods (Lactobacillus morphotypes; decrease in Lactobacillus scored as 0-4), small Gram-variable rods (Gardnerella vaginalis morphotypes; scored as 0-4), and curved Gram-variable rods (Mobiluncus species morphotypes; scored as 0-2). Total score range: 0-10. Score of 7-10 indicated BV. (NCT01153958)
Timeframe: 1 month post-treatment

Interventionpercentage of participants (Number)
Colposeptine16.0
Metronidazole10.7

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Percentage of Participants With Relapse 2 Months Post-treatment

Relapse: recurrence of the symptoms of bacterial vaginosis [BV] (Nugent score greater than or equal to 7, symptoms of vaginal irritation for example, pain, burning, odour or abnormal vaginal discharge) after a period of improvement. Nugent score was calculated by assessing for presence of large Gram-positive rods (Lactobacillus morphotypes; decrease in Lactobacillus scored as 0-4), small Gram-variable rods (Gardnerella vaginalis morphotypes; scored as 0-4), and curved Gram-variable rods (Mobiluncus species morphotypes; scored as 0-2). Total score range: 0-10. Score of 7-10 indicated BV. (NCT01153958)
Timeframe: 2 months post-treatment

Interventionpercentage of participants (Number)
Colposeptine23.3
Metronidazole17.2

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Change From Baseline in Nugent Score at 2 Months Post-treatment

Nugent score was calculated by assessing for presence of large Gram-positive rods (Lactobacillus morphotypes; decrease in Lactobacillus scored as 0-4), small Gram-variable rods (Gardnerella vaginalis morphotypes; scored as 0-4), and curved Gram-variable rods (Mobiluncus species morphotypes; scored as 0-2). Total score range: 0-10. Score of 7-10 indicate bacterial vaginosis. (NCT01153958)
Timeframe: Baseline and Month 2 post-treatment

,
Interventionunits on a scale (Mean)
Baseline (n= 66, 67)Change at Month 2 (n= 25, 29)
Colposeptine7.863.20
Metronidazole8.014.03

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Change From Baseline in Number of Participants With Each Grade of Lactobacilli at 2 Months Post-treatment

The grades of Lactobacilli in vaginal discharge were Grade 1 (Normal): Lactobacillus morphotypes predominate; Grade 2 (Intermediate): Mixed flora with some Lactobacilli present, but Gardnerella or Mobiluncus morphotypes also present; Grade 3 (Bacterial Vaginosis): Predominantly Gardnerella and/or Mobiluncus morphotypes, few or absent Lactobacilli. (NCT01153958)
Timeframe: Baseline and Month 2 post-treatment

,
Interventionparticipants (Number)
Baseline, Grade 1 (n= 66, 66)Baseline, Grade 2 (n= 66, 66)Baseline, Grade 3 (n= 66, 66)Month 2, Grade 1 (n= 25, 29)Month 2, Grade 2 (n= 25, 29)Month 2, Grade 3 (n= 25, 29)
Colposeptine03631177
Metronidazole01659146

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