Page last updated: 2024-12-05

dibucaine

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

Description

Dibucaine is a local anesthetic drug that is widely used in medical practice. It is synthesized through a multi-step process that involves the reaction of 2-chloro-4-nitroaniline with 2-diethylaminoethanol. Dibucaine has potent anesthetic properties, blocking nerve impulses by inhibiting the sodium channels responsible for signal transmission. Its importance lies in its ability to effectively relieve pain and numb tissues, making it useful in various medical procedures, including dental procedures, ophthalmic surgery, and spinal anesthesia. Dibucaine is studied extensively for its mechanism of action, potential therapeutic applications, and its role in pain management. Research investigates its efficacy, safety profile, and interactions with other drugs.'

Dibucaine: A local anesthetic of the amide type now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local anesthetics and its parenteral use is restricted to spinal anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1006) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cinchocaine : A monocarboxylic acid amide that is the 2-(diethylamino)ethyl amide of 2-butoxyquinoline-4-carboxylic acid. One of the most potent and toxic of the long-acting local anesthetics, its parenteral use was restricted to spinal anesthesia. It is now generally only used (usually as the hydrochloride) in creams and ointments and in suppositories for temporary relief of pain and itching associated with skin and anorectal conditions. [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 CID3025
CHEMBL ID1086
CHEBI ID247956
SCHEMBL ID34473
SCHEMBL ID23412539
MeSH IDM0006256

Synonyms (169)

Synonym
AC-2093
CHEMBL1086
MLS001148085
BRD-K99121711-001-03-5
BRD-K99121711-003-02-3
2-butoxy-quinoline-4-carboxylic acid (2-diethylamino-ethyl)-amide
MLS000028425 ,
smr000058391
DIVK1C_000332
KBIO1_000332
cincocaina [dcit]
cincain
hsdb 3312
nupercainal (van)
dibucainum
cinchocainum [inn-latin]
brn 0275489
cinchoninamide, 2-butoxy-n-(2-(diethylamino)ethyl)-
nsc 159055
dibucaine [usp]
percamine
einecs 201-632-1
4-quinolinecarboxamide, 2-butoxy-n-(2-(diethylamino)ethyl)-
cincainum
cincocainio [inn-spanish]
SPECTRUM_000928
PRESTWICK_164
cas-85-79-0
NCGC00016338-01
PRESTWICK2_000076
BSPBIO_002167
PRESTWICK3_000076
BPBIO1_000321
BSPBIO_000291
SPECTRUM5_000865
IDI1_000332
quinoline,2-butoxy,4-carboxy,(n-triethylamino) amide cinchocain
2-butoxy-n-[2-(diethylamino)ethyl]quinoline-4-carboxamide
inchi=1/c20h29n3o2/c1-4-7-14-25-19-15-17(16-10-8-9-11-18(16)22-19)20(24)21-12-13-23(5-2)6-3/h8-11,15h,4-7,12-14h2,1-3h3,(h,21,24
AB00053453
85-79-0
C07879
dibucaine
n-[2-(diethylamino)ethyl]-2-butoxycinchoninamide
2-butoxy-n-(.beta.-diethylaminoethyl)cinchoninamide
sovcaine
cinchocaine
dibucain
2-butoxyquinoline-4-carboxylic acid diethylaminoethylamide
cinchoninamide, 2-butoxy-n-[2-(diethylamino)ethyl]-
2-butoxy-n-[2-(diethylamino)ethyl]cinchoninamide
dibucaine base
nupercaine
.alpha.-butyloxycinchoninic acid diethylethylenediamide
4-quinolinecarboxamide, 2-butoxy-n-[2-(diethylamino)ethyl]-
nupercainal
wln: t66 bnj co4 evm2n2&2
nsc159055
dermacaine
nsc-159055
DB00527
alpha-butyloxycinchoninic acid diethylethylenediamide
alpha-butyloxycinchonic acid-gamma-diethylethylenediamine
2-butoxy-n-(beta-diethylaminoethyl)cinchoninamide
2-butoxy-n-(2-(diethylamino)ethyl)cinchoninamide
2-butoxy-n-(alpha-diethylaminoethyl)cinchoninamide
n-(2-(diethylamino)ethyl)-2-butoxycinchoninamide
2-n-butoxy-n-(2-diethylaminoethyl)cinchoninamide
2-butoxy-n-[2-(diethylamino)ethyl]-4-quinolinecarboxamide
dibucaine (usp)
D00733
nupercaine (tn)
cinchocaine (inn)
KBIO2_001408
KBIOGR_001049
KBIOSS_001408
KBIO3_001387
KBIO2_006544
KBIO2_003976
SPECTRUM4_000505
PRESTWICK1_000076
PRESTWICK0_000076
SPECTRUM2_001001
SPBIO_002212
SPBIO_001121
SPECTRUM3_000384
NINDS_000332
NCGC00016338-02
NCGC00016338-03
HMS1568O13
2-butoxy-n-(2-diethylaminoethyl)quinoline-4-carboxamide
cinchocainum
cincocainio
chebi:247956 ,
HMS2095O13
dtxsid3045271 ,
tox21_110381
dtxcid1025271
HMS2233F03
NCGC00016338-06
NCGC00016338-04
NCGC00016338-07
NCGC00016338-05
4-22-00-02284 (beilstein handbook reference)
l6jw2tjg99 ,
cincocaina
unii-l6jw2tjg99
cinchocaine [inn]
FT-0603086
2-butoxy-n-(2-diethylaminoethyl)cinchoninamide
dibucaine [hsdb]
dibucaine [usp monograph]
2-butoxy-n-(2-(diethylamino)ethyl)-4-quinolinecarboxamide
dibucaine [usp impurity]
cinchocaine [mart.]
4-quinolinecarboxamide, 2-butoxy-n-(2-(diethylamino)ethyl)
dibucaine [vandf]
dibucaine [mi]
cinchocaine [who-dd]
AKOS015897110
S5534
2-butoxy-n-[2-(diethylamino)ethyl]quinoline-4-carboximidic acid
gtpl7159
HMS3370I12
STL483757
CCG-220076
HY-B0552
SCHEMBL34473
tox21_110381_1
NCGC00016338-10
2-butoxy-n-(2-(diethylamino)ethyl)quinoline-4-carboxamide
2-butoxy-n-[2-(diethylamino)ethyl]quinoline-4-carboxamide;hydrochloride
bdbm48532
2-butoxy-n-[2-(diethylamino)ethyl]-4-quinolinecarboxamide;hydrochloride
cid_521951
2-butoxy-n-[2-(diethylamino)ethyl]cinchoninamide;hydrochloride
cinchocaine(dibucaine)
Q-100863
2-butoxy-n-[2-(diethylamino)ethyl]-4-quinolinecarboxamide #
PUFQVTATUTYEAL-UHFFFAOYSA-N
OPERA_ID_192
AB00053453_25
AB00053453_24
mfcd00047595
sr-01000003037
SR-01000003037-6
SBI-0051340.P003
HMS3712O13
Q417603
SY107339
AS-17426
BRD-K99121711-003-12-2
HMS3886I10
SCHEMBL23412539
EN300-18536764
cincocainio (inn-spanish)
n01bb06
c05ad04
4-quinolinecarboxamide, 2-butoxy-n-(2-(diethylamino)ethyl-
cvs hemorrhoidal topical analgesic
dibucaine topical anesthetic 1% hemorrhoidal
cinchocaine (mart.)
s01ha06
dibucaine (usp monograph)
dibucaine (usp impurity)
cinchocainum (inn-latin)
dibucaine 1%
s02da04
d04ab02

Research Excerpts

Overview

Dibucaine is a potent amide anesthetic available in over-the-counter preparations. It acts as a weak protonophore in cytochrome c oxidase proteoliposomes.

ExcerptReferenceRelevance
"Dibucaine is a potent, long-lasting local anesthetic (LA). "( Dibucaine toxicosis in a dog.
Hanzlicek, AS; Van der Merwe, D, 2010
)
3.25
"Dibucaine acts as a weak protonophore in cytochrome c oxidase proteoliposomes. "( Dibucaine interacts differently with membrane and protein in cytochrome c oxidase systems.
He, J; Nicholls, P,
)
3.02
"Dibucaine is a potent amide anesthetic available in over-the-counter preparations. "( Fatal accidental dibucaine poisoning in children.
Crouch, BI; Dayan, PS; Klein, BL; Litovitz, TL; Scalzo, AJ, 1996
)
2.08

Effects

Oral dibucaine toxicosis has been reported in children and includes gastrointestinal upset and neurologic and cardiovascular dysfunction. Dibucane has little effect on the Tm of the aqueous domain, but it decreases the TM of the transmembrane domain with Kd approximately equal to 4.1 x 10(-4) M.

ExcerptReferenceRelevance
"Oral dibucaine toxicosis has been reported in children and includes gastrointestinal upset and neurologic and cardiovascular dysfunction."( Dibucaine toxicosis in a dog.
Hanzlicek, AS; Van der Merwe, D, 2010
)
2.26
"Dibucaine has little effect on the Tm of the aqueous domain, but it decreases the Tm of the transmembrane domain with Kd approximately equal to 4.1 x 10(-4) M and a cooperativity of approximately 1.6, implying that destabilization is due to the binding of dibucaine to sites of intermediate or moderately high affinity.(ABSTRACT TRUNCATED AT 250 WORDS)"( Interaction of dibucaine with the transmembrane domain of the Ca(2+)-ATPase of sarcoplasmic reticulum.
Anteneodo, C; Heynen, ML; Lepock, JR; Meiering, E; Rodahl, AM; Sennisterra, GA, 1994
)
1.36
"Dibucaine has been reported to inhibit the enzyme activity competitively with phosphatidylserine."( [Effect of dibucaine on the association of protein kinase C with liposome].
Irita, K, 1991
)
1.39

Actions

ExcerptReferenceRelevance
"Dibucaine promotes an inhibition of the Ca2+-induced increase in mitochondrial H2O2 generation measured by the oxidation of scopoletin in the presence of horseradish peroxidase."( Ca2+-stimulated mitochondrial reactive oxygen species generation and permeability transition are inhibited by dibucaine or Mg2+.
Castilho, RF; Kowaltowski, AJ; Naia-da-Silva, ES; Vercesi, AE, 1998
)
1.23

Treatment

Dibucaine-treated platelets increased the peak of factor VIII clotting activity by 2-fold compared to activity with untreated platelets. Treatment also reduces to varying degrees the stimulatory effect of N-ethylmaleimide on the subsequent leucine uptake.

ExcerptReferenceRelevance
"Dibucaine-treated, ergosterol-replaced Tetrahymena cells had marked alterations in their plasma membranes."( Effect of the local anesthetic dibucaine on the surface membrane in sterol-manipulated Tetrahymena pyriformis studied by freeze-fracture electron microscopy.
Nozawa, Y; Sekiya, T, 1984
)
1.27
"Dibucaine-treated platelets increased the peak of factor VIII clotting activity by 2-fold compared to activity with untreated platelets."( Dibucaine elicits platelet procoagulant activity in factor VIII and factor X activation by a mechanism involving a sulfhydryl-dependent enzyme.
Hennessey, J; Hultin, MB; Morrison, SA, 1992
)
2.45
"Treatment with dibucaine, a phospholipid-interacting drug, also reduces to varying degrees (depending on its concentration) the stimulatory effect of N-ethylmaleimide on the subsequent leucine uptake, although pretreatment with dibucaine can stimulate the Na+-independent leucine uptake itself."( Effect of N-ethylmaleimide on leucine transport in the Chang liver cell. II. Effect on the kinetics of Na+-independent transport.
Mohri, T; Takadera, T, 1983
)
0.61

Toxicity

Dibucaine is considered one of the most potent and consequently toxic amide anesthetics available. Despite withdrawal from the US market as a spinal anesthetic, it remains accessible as an over-the-counter preparation in the United States.

ExcerptReferenceRelevance
"There have been reports of toxic reactions to ester-type local anesthetics in patients with genetic anomalies of plasma cholinesterase in so-called dibucaine-resistant homozygotes or heterozygotes."( Survey of local anesthetic toxicity in the families of patients with atypical plasma cholinesterase.
Eilderton, TE; Zsigmond, EK, 1975
)
0.45
" In most cases, the toxic effect was estimated by the amount of cells detached quantitatively."( Toxicity of local anaesthetics on myogenic cells in culture.
Hagiwara, Y; Ozawa, E, 1985
)
0.27
"2 micromol/L UCB for 10 min prior to the incubation with toxic concentrations of TFP (0."( Effect of bilirubin on toxicity induced by trifluoperazine, dibucaine and praziquantel to erythrocytes.
Brites, D; Brito, MA; Malheiros, SV; Meirelles, NC, 2001
)
0.55
"Dibucaine is considered one of the most potent and consequently toxic amide anesthetics available, and despite withdrawal from the US market as a spinal anesthetic, it remains accessible as an over-the-counter preparation in the United States."( Severe central nervous system and cardiovascular toxicity in a pediatric patient after ingestion of an over-the-counter local anesthetic.
Bernad, J; Dougherty, M; Holland, M; Marraffa, J; Nelsen, J; Stork, C, 2009
)
1.8

Compound-Compound Interactions

ExcerptReferenceRelevance
"Fifteen extraction sockets packed with a new drug combination which includes a local anaesthetic (cincain chloride), a local antiseptic (tri-iodomethane) and two drugs with a potent antifibrinolytic activity (tranexamic acid and propyl-hydroxy-benzoic acid) in an absorbable gelatin sponge (Gelfoam) as a vehicle, were histologically assessed with special reference to the parameters related to wound healing."( The effects on extraction wound healing of a new drug combination introduced for use in the prevention of post-extraction complications. A preliminary report.
Syrjänen, KJ; Syrjänen, SM, 1981
)
0.26

Bioavailability

ExcerptReferenceRelevance
"The choice of vehicle for patch test materials is important for the bioavailability and stability of the allergens."( Aspects of pharmaceutical and chemical standardization of patch test materials.
Hansen, J; Kreilgård, B, 1989
)
0.28
" Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have been proposed as drug-delivery systems to increase the bioavailability of local anesthetics."( Electron Paramagnetic Resonance and Small-Angle X-ray Scattering Characterization of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Dibucaine Encapsulation.
Barbosa, LRS; Barbosa, RM; Casadei, BR; de Paula, E; Duarte, EL; Duran, N; Severino, P, 2018
)
0.68
"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
" For example, intermittent application of a particular dosage results in lower blood levels, and allowing sufficient time between doses reduces the amount necessary to obtain the desired anesthesia."( Local anesthesia in otolaryngology. A re-evaluation.
Schenck, NL,
)
0.13
" In addition, the Ca2+ dose-response curves of both activities in intact platelets, obtained by stimulation with A23187 in the presence of Ca2+/HEDTA-buffers, were compared."( Correlation between calpain-mediated cytoskeletal degradation and expression of platelet procoagulant activity. A role for the platelet membrane-skeleton in the regulation of membrane lipid asymmetry?
Bevers, EM; Comfurius, P; Verhallen, PF; Zwaal, RF, 1987
)
0.27
" Dose-response curves for lignocaine, mepivacaine, bupivacaine, amethocaine and cinchocaine were obtained after single intrathecal injection to the mouse."( A methodological study of spinal (subarachnoid) anaesthesia in the rat and the mouse.
Akerman, SB, 1985
)
0.27
" All three drugs inhibited norepinephrine (NE) and KCl dose-response curves in a concentration-dependent manner."( Spasmolytic action of verapamil, D600 and cinchocaine on the rat vas deferens.
Lin, CS; Swamy, VC, 1980
)
0.26
" A tetracaine dose-response curve for HVA-ICa indicated an apparent dissociation constant of 79."( Local anesthetics depress the calcium current of rat sensory neurons in culture.
Muteki, T; Sugiyama, K, 1994
)
0.29
" The optimized methods proved to be specific and accurate for the analysis of the cited drugs in laboratory-prepared mixtures and dosage forms."( Column and thin-layer chromatographic methods for the simultaneous determination of acediasulfone in the presence of cinchocaine, and cefuroxime in the presence of its hydrolytic degradation products.
Aly, SM; El-Anwar, FM; Mohammad, MA; Zawilla, NH,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
topical anaestheticA local anesthetic that is used to numb the surface of a body part.
[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 (3)

ClassDescription
monocarboxylic acid amideA carboxamide derived from a monocarboxylic acid.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
aromatic etherAny ether in which the oxygen is attached to at least one aryl 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]

Pathways (1)

PathwayProteinsCompounds
Dibucaine Action Pathway3111

Protein Targets (33)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency17.48820.177814.390939.8107AID2147
glp-1 receptor, partialHomo sapiens (human)Potency14.12540.01846.806014.1254AID624417
USP1 protein, partialHomo sapiens (human)Potency44.66840.031637.5844354.8130AID743255
TDP1 proteinHomo sapiens (human)Potency17.08060.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency16.89680.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency31.10850.000221.22318,912.5098AID1259243; AID1259247
Smad3Homo sapiens (human)Potency10.00000.00527.809829.0929AID588855
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency8.91250.011212.4002100.0000AID1030
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency14.12540.01237.983543.2770AID1346984
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.84930.003041.611522,387.1992AID1159553
retinoid X nuclear receptor alphaHomo sapiens (human)Potency16.88420.000817.505159.3239AID1159527; AID1159531
pregnane X nuclear receptorHomo sapiens (human)Potency11.88320.005428.02631,258.9301AID1346982
cytochrome P450 2D6Homo sapiens (human)Potency8.70900.00108.379861.1304AID1645840
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency0.01060.023723.228263.5986AID743222
IDH1Homo sapiens (human)Potency20.59620.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency35.48130.035520.977089.1251AID504332
thyroid stimulating hormone receptorHomo sapiens (human)Potency26.60320.001628.015177.1139AID1259385
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency26.83250.057821.109761.2679AID1159528
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency7.94330.00207.533739.8107AID891
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency11.22020.036619.637650.1187AID1466; AID2242
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency15.84890.001815.663839.8107AID894
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency4.46680.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency10.32150.000323.4451159.6830AID743065; AID743067
gemininHomo sapiens (human)Potency21.75320.004611.374133.4983AID624296; AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.00110.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency0.89130.125912.234435.4813AID1458
lamin isoform A-delta10Homo sapiens (human)Potency0.00710.891312.067628.1838AID1487
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency19.95260.316212.765731.6228AID881
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.22023.548118.039535.4813AID1466
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.22023.548118.039535.4813AID1466
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency19.95260.00638.235039.8107AID881
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency14.12540.009610.525035.4813AID1479145
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)41.65000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

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)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

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)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

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)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (118)

Assay IDTitleYearJournalArticle
AID1589662Cytotoxicity against human A172 cells after 3 days by neutral red dye-based photometric method2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID698548Antihemolytic activity against hypotonic hemolysis in Wistar rat erythrocytes at 100 uM after 10 mins relative to control2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis of new chiral xanthone derivatives acting as nerve conduction blockers in the rat sciatic nerve.
AID1589639Cytotoxicity against human RD cells after 3 days by neutral red dye-based photometric method2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1589668Selectivity index, ratio of CC50 for human A172 cells to EC50 for Enterovirus D68 US/MO/14-18947 infected in human A172 cells2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589655Selectivity index, ratio of CC50 for human RD cells to EC50 for Enterovirus D68 US/MO/14-18949 infected in RD human cells2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID312896Partition coefficient, log P by UPLC method2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID1589651Antiviral activity against Enterovirus D68 US/IL/14-18956 infected in human RD cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric meth2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589660Cytotoxicity against human HeLa cells after 3 days by neutral red dye-based photometric method2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID23971logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1589670Selectivity index, ratio of CC50 for human SH-SY5Y cells to EC50 for Enterovirus D68 US/MO/14-18947 infected in human SH-SY5Y cells2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589652Antiviral activity against Enterovirus D68 US/MO/14-18947 infected in human RD cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric meth2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589665Selectivity index, ratio of CC50 for human SH-SY5Y cells to EC50 for Enterovirus D68 US/KY/14-18953 infected in human SH-SY5Y cells2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589641Inhibition of 2C protein in Enterovirus D68 US/KY/14-18953 infected in human RD cells assessed as reduction of VP1 expression at 3 uM measured at 9 hrs post infection by DAPI-staining based microscopy2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID311935Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1589649Antiviral activity against Influenza A virus (A/California/07/2009(H1N1)) at 10 uM after 2 days by plaque assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1703105Selectivity index, ratio of CC50 for human RD cells infected with Enterovirus A71 to EC50 for Enterovirus A71 infected in human RD cells2020European journal of medicinal chemistry, Sep-15, Volume: 202Identification of dibucaine derivatives as novel potent enterovirus 2C helicase inhibitors: In vitro, in vivo, and combination therapy study.
AID698550Antihemolytic activity against hypotonic hemolysis in Wistar rat erythrocytes after 10 mins2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis of new chiral xanthone derivatives acting as nerve conduction blockers in the rat sciatic nerve.
AID1061889Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID751710Displacement of [3H]Batrachotoxin from sodium channel site 2 in Wistar rat brain at 10 uM after 60 mins relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID751645Displacement of [3H]Batrachotoxin from sodium channel site 2 in Wistar rat brain after 60 mins2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID1589669Antiviral activity against Enterovirus D68 US/MO/14-18947 infected in human SH-SY5Y cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID311934Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID23965logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1589659Cytotoxicity against human A549 cells after 3 days by neutral red dye-based photometric method2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID23959logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID26296Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID450269Displacement of [3H]-BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore.
AID1589650Antiviral activity against Influenza B virus (B/Brisbane/60/2008) at 10 uM after 2 days by plaque assay2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID23961logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1589653Selectivity index, ratio of CC50 for human RD cells to EC50 for Enterovirus D68 US/MO/14-18947 infected in human RD cells2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589663Selectivity index, ratio of CC50 for human A172 cells to EC50 for Enterovirus D68 US/KY/14-18953 infected in human A172 cells2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589647Inhibition of sodium channel in rat dorsal root ganglia neurons assessed as reduction in veratridine-induced intracellular calcium influx at 20 to 50 uM after overnight incubation by Fura-2AM dye based fluorescence microscopy2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589661Antiviral activity against Enterovirus D68 US/KY/14-18953 infected in human A172 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric me2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID23973Partition coefficient (logD, measured by HPLC, log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1589643Inhibition of 2C protein in Enterovirus D68 US/KY/14-18953 infected in human RD cells assessed as reduction of VP1 expression at 1 uM measured at 9 hrs post infection by Western blot analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589664Antiviral activity against Enterovirus D68 US/KY/14-18953 infected in human SH-SY5Y cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID1589640Selectivity index, ratio of CC50 for human RD cells to EC50 for Enterovirus D68 US/KY/14-18953 infected in human RD cells2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID312895Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID1589656Selectivity index, ratio of CC50 for human RD cells to EC50 for Enterovirus D68 US/IL/14-18956 infected in human RD cells2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID23963logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1589654Antiviral activity against Enterovirus D68 US/MO/14-18949 infected in human RD cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric meth2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1703103Antiviral activity against Enterovirus A71 infected in human RD cells assessed as inhibition of viral replication measured by CCK-8 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Identification of dibucaine derivatives as novel potent enterovirus 2C helicase inhibitors: In vitro, in vivo, and combination therapy study.
AID450273Lipophilicity, log P of the compound2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore.
AID1589642Inhibition of 2C protein in Enterovirus D68 US/KY/14-18953 infected in human RD cells assessed as reduction of VP1 expression at 3 uM measured at 9 hrs post infection by Western blot analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1703104Cytotoxicity against human RD cells infected with Enterovirus A71 assessed as reduction in cell viability measured by CCK-8 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Identification of dibucaine derivatives as novel potent enterovirus 2C helicase inhibitors: In vitro, in vivo, and combination therapy study.
AID698552Inhibition of amplitude of compound action potential in isolated Wistar rat sciatic nerve at 0.1 to 3 uM after 15 mins by electrophysiology assay2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis of new chiral xanthone derivatives acting as nerve conduction blockers in the rat sciatic nerve.
AID1589657Antiviral activity against Enterovirus D68 UA/IL/14-18952 infected in human RD cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric meth2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID23970logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID310931Partition coefficient, log P of the compound2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities.
AID1589638Antiviral activity against Enterovirus D68 US/KY/14-18953 infected in human RD cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric meth2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589666Cytotoxicity against human SH-SY5Y cells after 3 days by neutral red dye-based photometric method2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID241212Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Defining determinant molecular properties for the blockade of the apamin-sensitive SKCa channel in guinea-pig hepatocytes: the influence of polarizability and molecular geometry.
AID23968logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1589658Selectivity index, ratio of CC50 for human RD cells to EC50 for Enterovirus D68 UA/IL/14-18952 infected in human RD cells2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589646Inhibition of 2C protein in Enterovirus D68 US/KY/14-18953 infected in human RD cells assessed as reduction of viral RNA level at 3 uM measured at 9 hrs post infection by RT-qPCR method relative to control2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
AID1589667Antiviral activity against Enterovirus D68 US/MO/14-18947 infected in human A172 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 mins under shaking condition and measured after 3 days by neutral red dye-based photometric me2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Discovery of Quinoline Analogues as Potent Antivirals against Enterovirus D68 (EV-D68).
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (982)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990681 (69.35)18.7374
1990's138 (14.05)18.2507
2000's92 (9.37)29.6817
2010's58 (5.91)24.3611
2020's13 (1.32)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 40.46

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 Index40.46 (24.57)
Research Supply Index7.01 (2.92)
Research Growth Index4.21 (4.65)
Search Engine Demand Index105.05 (26.88)
Search Engine Supply Index3.22 (0.95)

This Compound (40.46)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials34 (3.17%)5.53%
Reviews22 (2.05%)6.00%
Case Studies62 (5.78%)4.05%
Observational0 (0.00%)0.25%
Other955 (89.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]