Page last updated: 2024-12-06

fentiazac

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

Cross-References

ID SourceID
PubMed CID28871
CHEMBL ID589092
CHEBI ID94523
SCHEMBL ID24355
MeSH IDM0048266

Synonyms (70)

Synonym
[4-(4-chlorophenyl)-2-phenyl-1,3-thiazol-5-yl]acetic acid
nsc-282191
nsc282191
5-thiazoleacetic acid, 4-(p-chlorophenyl)-2-phenyl-
18046-21-4
mls003115545 ,
norvedan
donorest
br 700
4-(p-chlorophenyl)-2-phenyl-5-thiazoleacetic acid
flogene
fentiazac
5-thiazoleacetic acid, 4-(4-chlorophenyl)-2-phenyl-
fentiazac (jan/usan/inn)
D01975
4-(4-chlorophenyl)-2-phenyl-5-thiazoleacetic acid
ch 800
einecs 241-958-1
wy 21,894
fentiazacum [inn-latin]
brn 1083610
fentiazaco [inn-spanish]
nsc 282191
HMS2089J20
smr001831119
CHEMBL589092 ,
wy-21,894
wy-21894
jiekmacrvqtprc-uhfffaoysa-
inchi=1/c17h12clno2s/c18-13-8-6-11(7-9-13)16-14(10-15(20)21)22-17(19-16)12-4-2-1-3-5-12/h1-9h,10h2,(h,20,21)
2-(4-(4-chlorophenyl)-2-phenylthiazol-5-yl)acetic acid
bdbm50309254
2-[4-(4-chlorophenyl)-2-phenyl-1,3-thiazol-5-yl]acetic acid
NCGC00183868-01
NCGC00182976-01
0yhf6e6nls ,
unii-0yhf6e6nls
fentiazac [usan:inn:ban:jan]
fentiazacum
fentiazaco
cas-18046-21-4
tox21_113219
tox21_111788
tox21_113218
dtxcid803050
dtxsid8023050 ,
FT-0630446
fentiazac [inn]
fentiazac [mart.]
fentiazac [mi]
fentiazac [jan]
fentiazac [usan]
fentiazac [who-dd]
CCG-220474
SCHEMBL24355
NCGC00183868-02
tox21_111788_1
AB01087413-03
AKOS027446367
sr-05000001476
SR-05000001476-2
2-[4-(4-chlorophenyl)-2-phenyl-5-thiazolyl]acetic acid
CHEBI:94523
SR-05000001476-1
HMS3713O10
Q3742491
DB13217
18046-21-4 (free acid)
CS-0068397
HY-118752

Research Excerpts

Overview

Fentiazac was shown to be an effective analgesic for use in this painful inflammatory condition.

ExcerptReferenceRelevance
"Fentiazac was shown to be an effective analgesic for use in this painful inflammatory condition."( Single-blind clinical trial comparing use of fentiazac and paracetamol in postendodontic periodontitis.
Leguen, MA, 1985
)
1.25

Toxicity

ExcerptReferenceRelevance
" Five (26%) fentiazac-treated patients and four (21%) diclofenac sodium-treated patients reported adverse effects, mostly gastro-intestinal."( The efficacy and safety of fentiazac and diclofenac sodium in peri-arthritis of the shoulder: a multi-centre, double-blind comparison.
Kolarz, G; Mayrhofer, F; Scherak, O; Thumb, N,
)
0.81
" The adverse effect on the gastrointestinal membrane was less with Compd."( Studies on the anti-inflammatory activity and ulcerogenic adverse effect of thiazole derivatives, especially 2-amino-thiazoleacetic acid derivatives.
Ando, K; Nagatomi, H, 1984
)
0.27

Pharmacokinetics

ExcerptReferenceRelevance
" The drug, rapidly absorbed by the gastrointestinal system, shows a long maintenance in the body, with a long half-life in both animal species."( Pharmacokinetics of fentiazac in rats and monkeys.
Bianchi, E; De Marchi, G; Giachetti, C; Gomarasca, P; Mondino, A; Segre, G; Silvestri, S; Zanolo, G, 1981
)
0.59
" In clinical settings, the magnitude of the pharmacokinetic difference may warrant dose adjustment to avoid toxic effects of FT when administered with CM."( Effect of cimetidine on the pharmacokinetics of fentiazac in rats.
Kweon, DS; Lee, MH; Shim, CK, 1993
)
0.54
" The terminal half-life (7."( Pharmacokinetic study of fentiazac and its main metabolite hydroxyfentiazac in the elderly.
Akbaraly, JP; Beck, H; Campistron, G; Coulais, Y; Grislain, L; Houin, G; Lapeyre, C; Rochas, MA; Tufenkji, AE, 1993
)
0.59

Bioavailability

ExcerptReferenceRelevance
" Absorption was quite rapid, though some inter-subject variation in rates of absorption and bioavailability was observed."( The pharmacokinetics of fentiazac and its metabolite, p-hydroxyfentiazac, after twice-daily oral administration to male volunteers.
Dowell, PS; Franklin, RA; Harries, H; Norris, R; Pierce, DM; Whiteland, H, 1984
)
0.57
" The bioavailability resulting from the epicutaneous administration is markedly lower than that provided by the oral administration."( Serum and urinary levels of fentiazac after a single oral and epicutaneous administration in human subjects.
Giachetti, C; Mondino, A; Quattrini, M; Silvestri, S; Zanolo, G, 1981
)
0.56
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" The degree of gastric or intestinal irritation seen with dosing of other drugs was as follows; indomethacin greater than diclofenac Na greater than ibuprofen greater than aspirin greater than phenylbutazone or indomethacin greater than CH-800 = diclofenac Na greater than ibuprofen greater than phenylbutazone, respectively."( [Irritative activity of a new anti-inflammatory agent 4-(p-chorophenyl)-2-phenyl-5-thiazoleacetic acid (CH-800) on the gastrointestinal tract in rats (author's transl)].
Ohtsuki, H; Okabe, S; Tabata, K, 1979
)
0.26
" 29 especially gave the preferable results with almost no gastric damage at the higher dosage together with its good anti-edematous activity."( Studies on the anti-inflammatory activity and ulcerogenic adverse effect of thiazole derivatives, especially 2-amino-thiazoleacetic acid derivatives.
Ando, K; Nagatomi, H, 1984
)
0.27
" Both dosage regimens were equally efficacious, and no advantage except convenience was found for one dosage schedule over the other."( Fentiazac in osteoarthritis: comparison of BID and QID regimens.
Molina-López, J, 1983
)
1.71
" The two pharmaceutical dosage forms were given to same subjects at a one-week interval according to a cross-over design."( Serum and urinary levels of fentiazac after a single oral and epicutaneous administration in human subjects.
Giachetti, C; Mondino, A; Quattrini, M; Silvestri, S; Zanolo, G, 1981
)
0.56
" The findings suggest that the dosage regimen of this drug should be decreased in the elderly."( Pharmacokinetic study of fentiazac and its main metabolite hydroxyfentiazac in the elderly.
Akbaraly, JP; Beck, H; Campistron, G; Coulais, Y; Grislain, L; Houin, G; Lapeyre, C; Rochas, MA; Tufenkji, AE, 1993
)
0.59
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
thiazolesAn azole in which the five-membered heterocyclic aromatic skeleton contains a N atom and one S atom.
[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 (27)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency28.69540.007215.758889.3584AID624030
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
SMAD family member 2Homo sapiens (human)Potency21.31380.173734.304761.8120AID1346859
Fumarate hydrataseHomo sapiens (human)Potency14.12540.00308.794948.0869AID1347053
SMAD family member 3Homo sapiens (human)Potency21.31380.173734.304761.8120AID1346859
TDP1 proteinHomo sapiens (human)Potency31.29560.000811.382244.6684AID686978
AR proteinHomo sapiens (human)Potency15.45890.000221.22318,912.5098AID743036; AID743042; AID743053; AID743054; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency19.24320.000657.913322,387.1992AID1259377; AID1259378
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency16.93010.000214.376460.0339AID720692
retinoid X nuclear receptor alphaHomo sapiens (human)Potency10.68220.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency33.49150.001530.607315,848.9004AID1224848; AID1224849; AID1259403
estrogen nuclear receptor alphaHomo sapiens (human)Potency11.56380.000229.305416,493.5996AID743069; AID743075; AID743078
GVesicular stomatitis virusPotency4.89750.01238.964839.8107AID1645842
polyproteinZika virusPotency14.12540.00308.794948.0869AID1347053
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency3.57310.001019.414170.9645AID743094; AID743140; AID743191
aryl hydrocarbon receptorHomo sapiens (human)Potency15.53950.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency33.49150.001723.839378.1014AID743083
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency18.28070.057821.109761.2679AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency24.65540.039147.5451146.8240AID1224845
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency2.51190.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency28.83330.000323.4451159.6830AID743065; AID743067
Interferon betaHomo sapiens (human)Potency4.89750.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency4.89750.01238.964839.8107AID1645842
Guanine nucleotide-binding protein GHomo sapiens (human)Potency19.95261.995325.532750.1187AID624287
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency4.89750.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency4.89750.01238.964839.8107AID1645842
[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)
Prostaglandin D2 receptor 2Homo sapiens (human)IC50 (µMol)0.65250.00040.10090.9600AID458064; AID458065; AID458406; AID458407
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (56)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
chemotaxisProstaglandin D2 receptor 2Homo sapiens (human)
immune responseProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
calcium-mediated signalingProstaglandin D2 receptor 2Homo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
negative regulation of male germ cell proliferationProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (25)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin F receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide bindingProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
neuron projectionProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (68)

Assay IDTitleYearJournalArticle
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID458065Antagonist activity at human CRTH2 receptor expressed in HEK285-7 cells assessed as inhibition of beta arrestin translocation by bioluminescence resonance energy transfer assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID458064Displacement of[3H]PGD2 from human CRTH2 receptor expressed in HEK385-7 cells2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID458085Antagonist activity at human CRTH2 receptor expressed in HEK285-7 cells assessed as inhibition of beta arrestin translocation by bioluminescence resonance energy transfer assay relative to control2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID458406Antagonist activity at human CRTH2 receptor expressed in HEK285-7 cells assessed as inhibition of beta arrestin translocation by bioluminescence resonance energy transfer assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID458408Antagonist activity at human CRTH2 receptor expressed in HEK285-7 cells assessed as inhibition of beta arrestin translocation by bioluminescence resonance energy transfer assay relative to control2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID717844Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 20 uM after 45 mins by spectrophotometric analysis relative to control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID458407Displacement of[3H]PGD2 from human CRTH2 receptor expressed in african green monkey COS7 cells2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
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.
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.
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.
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.
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.
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.
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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
AID1745845Primary 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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (62)

TimeframeStudies, This Drug (%)All Drugs %
pre-199045 (72.58)18.7374
1990's2 (3.23)18.2507
2000's1 (1.61)29.6817
2010's8 (12.90)24.3611
2020's6 (9.68)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.54

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 Index27.54 (24.57)
Research Supply Index4.41 (2.92)
Research Growth Index4.76 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.54)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials15 (22.73%)5.53%
Reviews0 (0.00%)6.00%
Case Studies1 (1.52%)4.05%
Observational0 (0.00%)0.25%
Other50 (75.76%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]