Page last updated: 2024-11-13

roquinimex

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

Description

roquinimex: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID54676478
CHEMBL ID11672
CHEBI ID92056
SCHEMBL ID42132
SCHEMBL ID1651117
MeSH IDM0131769

Synonyms (67)

Synonym
HMS3267L20
BRD-K03384561-001-01-9
roquinimex
linomide ,
pnu-212616
fcf-89
ls-2616 ,
tocris-1461
NCGC00025172-01
D05756
84088-42-6
roquinimex (usan/inn)
fcf 89
1,2-dihydro-4-hydroxy-n,1-dimethyl-2-oxo-3-quinolinecarboxanilide
roquinimexum [latin]
3-quinolinecarboxamide, 1,2-dihydro-4-hydroxy-n,1-dimethyl-2-oxo-n-phenyl
roquinimex [usan:inn]
ls 2616
ccris 7673
CHEMBL11672
4-hydroxy-n,1-dimethyl-2-oxo-n-phenyl-1,2-dihydroquinoline-3-carboxamide
roquinimexum
372t2944c0 ,
unii-372t2944c0
cas-84088-42-6
tox21_110951
dtxsid4045680 ,
dtxcid2025680
FT-0630924
S2307
CS-3169
HY-13743
SCHEMBL42132
tox21_110951_1
NCGC00025172-02
roquinimex [mi]
roquinimex [mart.]
roquinimex [who-dd]
roquinimex [inn]
roquinimex [usan]
SCHEMBL1651117
SGOOQMRIPALTEL-UHFFFAOYSA-N
n-methyl-n-phenyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxo-quinoline-3-carboxamide
1,2-dihydro-4-hydroxy-n,n-dimethyl-2-oxo-n-phenyl-3-quinolinecarboxamide
AKOS024456612
n-phenyl-n-methyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxo-quinoline-3-carboxamide
mfcd00866331
sr-01000597567
SR-01000597567-1
4-hydroxy-n,1-dimethyl-2-oxo-n-phenyl-3-quinolinecarboxamide
CHEBI:92056
ls2616;fcf89
roquinimex(linomide)
DB11366
bdbm50248187
abr 21261
HMS3676D07
L0270
HMS3412D07
Q964482
BCP29884
abr212616
fcf89
ls2616
D91260
A854171
4-hydroxy-n,1-dimethyl-2-oxo-n-phenylquinoline-3-carboxamide

Research Excerpts

Overview

Roisinimex (Roq) is an immunomodulator known to stimulate cellular immune responses. It has been shown to attenuate induction of several inflammatory and autoimmune diseases. Roquinimex is an orally active drug with immunostimulating activities demonstrated in vitro and clinically.

ExcerptReferenceRelevance
"Roquinimex is a modulator of the immune system and has been shown to attenuate induction of several inflammatory and autoimmune diseases. "( Roquinimex inhibits dextran sodium sulfate-induced murine colitis.
Andersson, G; Hedlund, G; Liu, Q; Thorlacius, H; Wan, MX; Wang, Y; Zhang, XW, 2003
)
3.2
"Roquinimex is an immunomodulator that can effectively inhibit the development of several autoimmune diseases in animal models, but the mechanism is still unknown. "( Roquinimex-mediated protection effect on the development of chronic graft-versus-host disease in mice is associated with induction of Th1 cytokine production and inhibition of proinflammatory cytokine production.
Cheng, JP; He, JF; Xiao, ZY; Yang, RF; Yun, LH; Zhang, YX; Zhou, WX, 2007
)
3.23
"Roquinimex (Roq) is an immunomodulator known to stimulate cellular immune responses. "( Enhanced lymphokine-activated killer cell activity by an immunomodulator, Roquinimex.
Ascensao, JL; Silva, MR; Vaz, F, 1995
)
1.96
"Roquinimex is an orally active drug with immunostimulating activities demonstrated in vitro and clinically."( Phase II study of roquinimex in myelodysplastic syndrome.
Nilsson, B; Rosenfeld, CS; Shadduck, RK; Zeigler, ZR, 1997
)
1.35
"Roquinimex seems to be an active immunomodulator with manageable toxicity."( The first clinical pilot study of roquinimex (Linomide) in cancer patients with special focus on immunological effects.
Bergh, JC; Gunnarsson, PO; Nilsson, BI; Strandgarden, KA; Termander, BC; Tötterman, TH, 1997
)
1.3
"Roquinimex, Linomide, is a quinoline derivative with pleiotropic immunomodulatory activities which has been shown to enhance NK function. "( Natural effector cells in patients with acute myeloid leukemia treated with the immunomodulator Linomide after autologous bone marrow transplantation.
Bengtsson, M; Hokland, M; Hokland, P; Holm, MS; Jørgensen, H; Nilsson, B; Simonsson, B, 1999
)
1.75
"Roquinimex (Linomide) is an immunotherapeutic agent used in conjunction with autologous bone marrow transplantation (ABMT) for treatment of acute and chronic myelogenous leukemia (AML and CML). "( Dermatologic changes associated with roquinimex immunotherapy after autologous bone marrow transplant.
Burns, RP; Gaspari, AA; Liesveld, J; Ohsuga, Y; Rowe, JM, 2000
)
2.02

Effects

ExcerptReferenceRelevance
"Roquinimex (Linomide) has been demonstrated to suppress tumor growth in animal models. "( The first clinical pilot study of roquinimex (Linomide) in cancer patients with special focus on immunological effects.
Bergh, JC; Gunnarsson, PO; Nilsson, BI; Strandgarden, KA; Termander, BC; Tötterman, TH, 1997
)
2.02

Actions

ExcerptReferenceRelevance
"Roquinimex is known to enhance T cell, NK cell and macrophage activity."( Treatment of chronic myelogenous leukemia with autologous bone marrow transplantation followed by roquinimex.
Abboud, CN; DiPersio, JF; Duerst, RE; Liesveld, JL; Linder, T; Nilsson, BI; Packman, CH; Rapoport, AP; Rowe, JM; Ryan, DH; Simonsson, B; Wang, N, 1999
)
1.24

Treatment

Rquinimex treatment suppressed the production of IFN-gamma and IL-10 in HSV-infected BALB/c mice. The treatment restored the Th1/Th2 cytokine balance, although only a minimal effect was observed on interleukin (IL)-4 secretion.

ExcerptReferenceRelevance
"Roquinimex treatment suppressed the production of IFN-gamma and also the production of IL-10 in HSV-infected BALB/c mice."( Immunomodulation by roquinimex decreases the expression of IL-23 (p19) mRNA in the brains of herpes simplex virus type 1 infected BALB/c mice.
Broberg, EK; Eralinna, JP; Halenius, A; Hukkanen, V; Peltoniemi, J; Roytta, M; Salmi, AA; Setala, N, 2004
)
1.37
"Roquinimex treatment, however, induced IFN-gamma production and restored the Th1/Th2 cytokine balance, although only a minimal effect of roquinimex on interleukin (IL)-4 secretion was observed."( Roquinimex-mediated protection effect on the development of chronic graft-versus-host disease in mice is associated with induction of Th1 cytokine production and inhibition of proinflammatory cytokine production.
Cheng, JP; He, JF; Xiao, ZY; Yang, RF; Yun, LH; Zhang, YX; Zhou, WX, 2007
)
2.5

Pharmacokinetics

ExcerptReferenceRelevance
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
" Our study suggests that treatment aimed at abrogation of autoimmunity combined with expansion of beta-cell mass constitutes a potential therapeutic approach for treatment of insulin-dependent diabetes mellitus."( Amelioration of diabetes in nonobese diabetic mice with advanced disease by linomide-induced immunoregulation combined with Reg protein treatment.
Clark, A; Gross, DJ; Okamoto, H; Reibstein, I; Slavin, S; van den Brand, J; Weiss, L, 1998
)
0.3

Bioavailability

ExcerptReferenceRelevance
"In order to investigate the bioavailability and the rate-limiting step of the absorption of roquinimex, an oral solution and a tablet formulation (Linomide(R)) were given to healthy volunteers."( Dissolution rate-limited absorption and complete bioavailability of roquinimex in man.
Gunnarsson, PO; Höglund, P; Nordle, O; Polacek, J; Strandgârden, K; Wännman, H, 1999
)
0.76
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"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
" Dose-response analysis demonstrated that a Linomide blood level of 50-100 microM is optimal for such chemoprevention."( Antiangiogenic treatment with linomide as chemoprevention for prostate, seminal vesicle, and breast carcinogenesis in rodents.
Isaacs, JT; Joseph, IB; Vukanovic, J, 1996
)
0.29
" In spite of selection of favourable prognosis patients and an optimal daily dosing schedule, linomide was not an effective treatment in renal cell carcinoma."( EORTC phase II study of daily oral linomide in metastatic renal cell carcinoma patients with good prognostic factors.
de Mulder, PH; de Wit, R; Fosså, SD; Paridaens, R; Pawinsky, A; Stoter, G; Svedberg, A; van Oosterom, AT, 1997
)
0.3
"L-W rats with small induced P-SV tumors were treated with a recommended dosage of linomide (100 mg/kg BW/day) by the intraperitoneal and oral routes."( Effects of linomide on advanced prostate-seminal vesicle cancers in Lobund-Wistar rats.
Pollard, M, 1998
)
0.3
" The dosage of linomide used showed evidence of toxicity."( Effects of linomide on advanced prostate-seminal vesicle cancers in Lobund-Wistar rats.
Pollard, M, 1998
)
0.3
" Furthermore, bropirimine was most efficacious when dosing was begun 5-10 days after injection of myelin basic protein, the protein isolated from the central nervous system and used for inducing EAE in our model."( Pharmacology of the biological response modifier bropirimine (PNU-54461) on experimental autoimmune encephalomyelitis (EAE) in mice.
Brideau, RJ; Buxser, SE; Chapman, DL; Decker, DE; Dunn, CJ; Galinet, LA; Ready, KA; Vroegop, SM, 1999
)
0.3
" The duration and dosage of Linomide required to obtain these effects is similar to those required for EAE inhibition."( Inhibition of autoimmune disease by the immunomodulator linomide correlates with the ability to activate macrophages.
Andersson, M; Björk, A; Brunmark, C; Dahlén, E; Dawe, K; Hedlund, G; Tellander, AC, 2000
)
0.31
", 30- to 60-fold more potent than linomide) in these assays and its lack of a proinflammation in the Beagle-dog, ABR-215050 (tasquinimod), Figure 1, was characterized for dose-response ability to inhibit the growth of a series of four additional human and rodent prostate cancer models in mice."( Identification of ABR-215050 as lead second generation quinoline-3-carboxamide anti-angiogenic agent for the treatment of prostate cancer.
Björk, A; Dalrymple, SL; Garrison, JB; Isaacs, JT; Kyprianou, N; Leanderson, T; Olsson, A; Pili, R; Qian, DZ, 2006
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic amideAn amide in which the amide linkage is bonded directly to an aromatic system.
[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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency25.11890.007215.758889.3584AID411
acetylcholinesteraseHomo sapiens (human)Potency0.77620.002541.796015,848.9004AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency33.49150.006038.004119,952.5996AID1159521
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency15.84890.01237.983543.2770AID1346984
pregnane X nuclear receptorHomo sapiens (human)Potency29.84930.005428.02631,258.9301AID1346982
aryl hydrocarbon receptorHomo sapiens (human)Potency33.49150.000723.06741,258.9301AID743085
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (41)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (87)

Assay IDTitleYearJournalArticle
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID115400Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 32 mg/kg in MRL/1 mice2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID251725In vitro percent inhibition of ConA induced T-cell proliferation at the dose 10 ug/mL2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
AID123898In vivo effect of compound on VEGF-induced angiogenesis in blood volume of mice2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Modified synthesis and antiangiogenic activity of linomide.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID115401Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 32 mg/kg in murine2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID251851In vitro percent inhibition of tumor necrosis factor, alpha secreted by macrophage at the dose 10 ug/mL2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
AID115546Percent inhibition of proteinuria by compound dose of 10 mg/kg given perorally to MRL/1 mice2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID115398Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 100 mg/kg in murine2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID251732In vitro percent inhibition of ConA induced T-cell proliferation at the dose 100 ug/mL2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
AID115393Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 1 mg/kg in MRL/1 mice2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID116493Activity expressed as percent inhibition of anti-TNP IgM level in TNP-LPS immunized mice, at a dose of 10 mg/kg perorally2002Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
Quinoline-3-carbothioamides and related compounds as novel immunomodulating agents.
AID251861In vitro percent inhibition of tumor necrosis factor, alpha secreted by macrophage at the dose 100 ug/mL2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
AID115548Percent inhibition of proteinuria by compound dose of 100 mg/kg given perorally to MRL/1 mice2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID116492Activity was expressed as percent inhibition of anti-TNP IgM level in TNP-LPS immunized mice, at a dose of 1 mg/kg perorally2002Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
Quinoline-3-carbothioamides and related compounds as novel immunomodulating agents.
AID156156Antiproliferative activity against PC-3 prostate cancer cells2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Structure-activity relationships studies of the anti-angiogenic activities of linomide.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID251719In vitro percent inhibition of LPS induced B-cell proliferation at the dose 10 ug/mL2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID116494Activity was expressed as percent inhibition of anti-TNP IgM level in TNP-LPS immunized mice, at a dose of 100 mg/kg perorally2002Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
Quinoline-3-carbothioamides and related compounds as novel immunomodulating agents.
AID251718In vitro percent inhibition of ConA induced T-cell proliferation at the dose 1 ug/mL2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
AID52145Effective concentration for inhibiting blood vessel formation in the CAM (Chicken chorioallantoic membrane) angiogenesis assay.2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Structure-activity relationships studies of the anti-angiogenic activities of linomide.
AID115395Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 10 mg/kg in MRL/1 mice2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID115550Percent inhibition of proteinuria by compound dose of 100 mg/kg given perorally to murine in chronic graft-versus-host-disease test2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID84809Inhibitory concentration against Human umbilical vein endothelial cell (HUVEC) proliferation2003Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
Structure-activity relationships studies of the anti-angiogenic activities of linomide.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID115554Percent inhibition of proteinuria by compound dose of 32 mg/kg given perorally to MRL/1 mice2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID115553Percent inhibition of proteinuria by compound dose of 3.2 mg/kg given perorally to MRL/1 mice; Inactive2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID115544Percent inhibition of proteinuria by compound dose of 1 mg/kg given perorally to MRL/1 mice; Inactive2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID115059Inhibition of acute experimental autoimmune encephalomyelitis in SJL/N mice by 0.2 mg/kg/day p.o./s.c.2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Synthesis and biological evaluation of new 1,2-dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for treatment of autoimmune disorders: structure-activity relationship.
AID115396Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 10 mg/kg in murine2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID115551Percent inhibition of proteinuria by compound dose of 10 mg/kg given perorally to murine in chronic graft-versus-host-disease test2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID115053Inhibition of acute experimental autoimmune encephalomyelitis (aEAE) in SJL/N mice at a dose of 5 mg/kg/day, (po/sc) was determined2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Synthesis and biological evaluation of new 1,2-dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for treatment of autoimmune disorders: structure-activity relationship.
AID251708In vitro percent inhibition of LPS induced B-cell proliferation at the dose 1 ug/mL2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
AID115399Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 3.2 mg/kg in MRL/1 mice2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID115555Percent inhibition of proteinuria in mice, perorally dose of 32 mg/kg2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID251836In vitro percent inhibition of tumor necrosis factor, alpha secreted by macrophage at the dose 1 ug/mL2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID115397Percent inhibition of anti-DNA antibody was evaluated by ELISA technique as a measure of auto-immune disease after injection of compound dose of 100 mg/kg in MRL/1 mice2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID251726In vitro percent inhibition of LPS induced B-cell proliferation at the dose 100 ug/mL2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator.
AID115052Inhibition of acute experimental autoimmune encephalomyelitis (aEAE) in SJL/N mice at a dose of 1 mg/kg/day, (po/sc) was determined2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Synthesis and biological evaluation of new 1,2-dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for treatment of autoimmune disorders: structure-activity relationship.
AID110850In vivo effect of compound on VEGF-induced angiogenesis in blood vessels of mice2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Modified synthesis and antiangiogenic activity of linomide.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (195)

TimeframeStudies, This Drug (%)All Drugs %
pre-199017 (8.72)18.7374
1990's122 (62.56)18.2507
2000's41 (21.03)29.6817
2010's8 (4.10)24.3611
2020's7 (3.59)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.02

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

MetricThis Compound (vs All)
Research Demand Index19.02 (24.57)
Research Supply Index5.43 (2.92)
Research Growth Index5.15 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.02)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials25 (12.38%)5.53%
Reviews15 (7.43%)6.00%
Case Studies2 (0.99%)4.05%
Observational0 (0.00%)0.25%
Other160 (79.21%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]