Page last updated: 2024-11-13

rolitetracycline

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Description

Rolitetracycline: A pyrrolidinylmethyl TETRACYCLINE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

rolitetracycline : A derivative of tetracycline in which the amide function is substituted with a pyrrolidinomethyl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID54682938
CHEMBL ID1237046
CHEBI ID63334
SCHEMBL ID155640
SCHEMBL ID21831095
MeSH IDM0019254

Synonyms (86)

Synonym
gh9iw85221 ,
unii-gh9iw85221
rolitetracycline [usan:usp:inn:ban:jan]
nsc 759177
reverin
superciclin
synotodecin
prm-tc
velacycline
rolitetraciclina [inn-spanish]
2-naphthacenecarboxamide, 4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-n-(1-pyrrolidinylmethyl)-, (4s-(4alpha,4aalpha,5aalpha,6beta,12aalpha))-
einecs 212-031-9
4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-n-(1-pyrrolidinylmethyl)-2-naphthacenecarboxamide
tetracycline, pyrrolidinomethyl-
n-pyrrolidino-methyl-tetracycline
syntetrex
velacicline
bristacin
pirrolidinometil-tetraciclina [italian]
sq 15,659
rolitetracyclinum [inn-latin]
751-97-3
tetracycline, n-(pyrrolidinylmethyl)-
68060-64-0
rolitetracycline
solvocillin
syntetrin
aat 4
kinteto
(4s,4as,5as,6s,12as)-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-n-(pyrrolidin-1-ylmethyl)-4,4a,5,5a-tetrahydrotetracene-2-carboxamide
sq 15659
DB01301
pyrrolidino-methyl-tetracycline
n-(pyrrolidinomethyl)tetracycline
n-(1-pyrrolidinylmethyl)-tetracycline
synterin (tn)
rolitetracycline (jan/usan/inn)
D02282
HMS2094O15
[(4s,6s,12as,4as,5as)-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-6-methyl-1, 11-dioxo(4,5,6,12a,4a,5a-hexahydronaphthacen-2-yl)]-n-(pyrrolidinylmethyl)carb oxamide
pharmakon1600-01505684
nsc759177
nsc-759177
rolitetracyclinum
pirrolidinometil-tetraciclina
rolitetraciclina
CHEMBL1237046
so 15,659
sq-15659
CHEBI:63334 ,
(4s,4as,5as,6s,12as)-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-n-(pyrrolidin-1-ylmethyl)-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
synterin
rolitetracycline [who-dd]
rolitetracycline [usan]
rolitetracycline [mi]
rolitetracycline [mart.]
rolitetracycline [inn]
rolitetracycline [jan]
2-naphthacenecarboxamide, 4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-n-(1-pyrrolidinylmethyl)-, (4s-(4.alpha.,4a.alpha.,5a.alpha.,6.beta.,12a.alpha))
CCG-213512
HMEYVGGHISAPJR-IAHYZSEUSA-N
SCHEMBL155640
AKOS024284365
AB01563105_02
AB01563105_01
sr-05000001744
SR-05000001744-1
bdbm50477463
so-15659
rolitetracycline, analytical standard
SBI-0206901.P001
(4s,5as,6s,12as)-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-n-(pyrrolidin-1-ylmethyl)-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
NCGC00263906-01
BCP15881
Q3940320
SCHEMBL21831095
(4s,4as,5as,6s,12ar)-4-(dimethylamino)-1,6,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-n-(pyrrolidin-1-ylmethyl)-4,4a,5,5a-tetrahydrotetracene-2-carboxamide
pyrrolidinylmethyltetracycline
gtpl12760
HY-18257
CS-0007350
(4s,4as,5as,6s,12as)-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-n-(1-pyrrolidinylmethyl)-2-naphthacenecarboxamide
EN300-19651952
(4s,4as,5as,6s,12as)-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-n-[(pyrrolidin-1-yl)methyl]-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
n-(pyrrolidin-1-ylmethyl)tetracycline
PD132300

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The calculations of pharmacokinetic parameters were performed using the Hewlett-Packard 9830B computer and fitting the concentrations of the antibiotic in blood to the general biexponential equation."( Effect of unilateral nephrectomy on the pharmacokinetics of rolitetracycline in rabbits.
Gawrońska-Szklarz, B; Górnik, W; Kardel-Mizerska, T; Wójcicki, J, 1981
)
0.5
"Comparative studies on some selected pharmacokinetic parameters of rolitetracycline (effective antimicrobial activity levels) in sheep, pigs, rabbits, chickens and pigeons were carried out after intravenous administration of the drug at a dose of 5 mg/kg."( Species specific pharmacokinetics of rolitetracycline.
Kanelov, I; Lashev, L; Pashov, D, 1995
)
0.8
" 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

Dosage Studied

The dosage applied was about 10-20 times higher than the therapeutical single dose of doxycycline. It is assumed that the dosage regimen of rolitetracycline should be changed in subjects possessing one kidney.

ExcerptRelevanceReference
" Up to this time, amoxicillin has not been commercially available as an injectable dosage form."( Pneumococcal meningitis-therapeutic studies in mice.
Hirth, RS; Price, KE; Tsai, YH; Williams, EB, 1975
)
0.25
" The higher dosage administered orally had no greater influence on the sputum concentration."( [Tetracycline levels in the sputum in chronic obstructive bronchitis (author's transl)].
Ritzerfeld, W; Ulmer, WT; Zimmermann, I, 1977
)
0.26
" The dosage applied was about 10-20 times higher than the therapeutical single dose of doxycycline and about 4-8 times higher than the single dose of rolitetracycline."( [On the circulation compatibility of doxycycline and rolitetracycline in conscious minipigs (author's transl)].
Mehren, W; Mergler, G; Moussawi, M; Schoog, M; Tauberger, G, 1978
)
0.71
" Serum levels following one shot intravenous injection of DOTC iv in glucose solution showed a good dose-response comparable with that of the same dose injection of pyrrolidinomethyltetracycline (PRM-TC)."( [Studies on the absorption and excretion of doxycycline for intravenous use (author's transl)].
Fukaya, K; Kitamoto, O; Kunii, O; Mashimo, K, 1975
)
0.25
" It is assumed that the dosage regimen of rolitetracycline should be changed in subjects possessing one kidney."( Effect of unilateral nephrectomy on the pharmacokinetics of rolitetracycline in rabbits.
Gawrońska-Szklarz, B; Górnik, W; Kardel-Mizerska, T; Wójcicki, J, 1981
)
0.77
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
microphthalmia-associated transcription factor isoform 9Homo sapiens (human)IC50 (µMol)4.46360.00481.37104.9290AID1259371; AID1259373; AID1259375
Insulin-degrading enzymeHomo sapiens (human)IC50 (µMol)100.00000.01402.35207.0000AID1600069
DNA repair protein RAD52 homologHomo sapiens (human)IC50 (µMol)29.00000.25502.63016.7000AID1639797
Integrase Human immunodeficiency virus 1IC50 (µMol)31.00000.00051.544310.0000AID307121; AID307122
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (27)

Processvia Protein(s)Taxonomy
proteolysisInsulin-degrading enzymeHomo sapiens (human)
insulin receptor signaling pathwayInsulin-degrading enzymeHomo sapiens (human)
bradykinin catabolic processInsulin-degrading enzymeHomo sapiens (human)
ubiquitin recyclingInsulin-degrading enzymeHomo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IInsulin-degrading enzymeHomo sapiens (human)
protein catabolic processInsulin-degrading enzymeHomo sapiens (human)
positive regulation of protein bindingInsulin-degrading enzymeHomo sapiens (human)
hormone catabolic processInsulin-degrading enzymeHomo sapiens (human)
peptide catabolic processInsulin-degrading enzymeHomo sapiens (human)
positive regulation of protein catabolic processInsulin-degrading enzymeHomo sapiens (human)
symbiont entry into host cellInsulin-degrading enzymeHomo sapiens (human)
amyloid-beta metabolic processInsulin-degrading enzymeHomo sapiens (human)
proteolysis involved in protein catabolic processInsulin-degrading enzymeHomo sapiens (human)
amyloid-beta clearanceInsulin-degrading enzymeHomo sapiens (human)
amyloid-beta clearance by cellular catabolic processInsulin-degrading enzymeHomo sapiens (human)
insulin metabolic processInsulin-degrading enzymeHomo sapiens (human)
insulin catabolic processInsulin-degrading enzymeHomo sapiens (human)
regulation of aerobic respirationInsulin-degrading enzymeHomo sapiens (human)
DNA double-strand break processing involved in repair via single-strand annealingDNA repair protein RAD52 homologHomo sapiens (human)
cellular response to oxidative stressDNA repair protein RAD52 homologHomo sapiens (human)
regulation of nucleotide-excision repairDNA repair protein RAD52 homologHomo sapiens (human)
DNA recombinase assemblyDNA repair protein RAD52 homologHomo sapiens (human)
double-strand break repairDNA repair protein RAD52 homologHomo sapiens (human)
DNA recombinationDNA repair protein RAD52 homologHomo sapiens (human)
double-strand break repair via homologous recombinationDNA repair protein RAD52 homologHomo sapiens (human)
mitotic recombinationDNA repair protein RAD52 homologHomo sapiens (human)
double-strand break repair via single-strand annealingDNA repair protein RAD52 homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
virus receptor activityInsulin-degrading enzymeHomo sapiens (human)
endopeptidase activityInsulin-degrading enzymeHomo sapiens (human)
metalloendopeptidase activityInsulin-degrading enzymeHomo sapiens (human)
protein bindingInsulin-degrading enzymeHomo sapiens (human)
ATP bindingInsulin-degrading enzymeHomo sapiens (human)
zinc ion bindingInsulin-degrading enzymeHomo sapiens (human)
peptide bindingInsulin-degrading enzymeHomo sapiens (human)
protein homodimerization activityInsulin-degrading enzymeHomo sapiens (human)
insulin bindingInsulin-degrading enzymeHomo sapiens (human)
DNA bindingDNA repair protein RAD52 homologHomo sapiens (human)
single-stranded DNA bindingDNA repair protein RAD52 homologHomo sapiens (human)
protein bindingDNA repair protein RAD52 homologHomo sapiens (human)
identical protein bindingDNA repair protein RAD52 homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
nucleusInsulin-degrading enzymeHomo sapiens (human)
extracellular spaceInsulin-degrading enzymeHomo sapiens (human)
nucleusInsulin-degrading enzymeHomo sapiens (human)
cytoplasmInsulin-degrading enzymeHomo sapiens (human)
mitochondrionInsulin-degrading enzymeHomo sapiens (human)
peroxisomeInsulin-degrading enzymeHomo sapiens (human)
peroxisomal matrixInsulin-degrading enzymeHomo sapiens (human)
cytosolInsulin-degrading enzymeHomo sapiens (human)
external side of plasma membraneInsulin-degrading enzymeHomo sapiens (human)
cell surfaceInsulin-degrading enzymeHomo sapiens (human)
basolateral plasma membraneInsulin-degrading enzymeHomo sapiens (human)
extracellular exosomeInsulin-degrading enzymeHomo sapiens (human)
peroxisomal matrixInsulin-degrading enzymeHomo sapiens (human)
mitochondrionInsulin-degrading enzymeHomo sapiens (human)
cytosolInsulin-degrading enzymeHomo sapiens (human)
nucleusDNA repair protein RAD52 homologHomo sapiens (human)
nucleoplasmDNA repair protein RAD52 homologHomo sapiens (human)
protein-containing complexDNA repair protein RAD52 homologHomo sapiens (human)
protein-DNA complexDNA repair protein RAD52 homologHomo sapiens (human)
nucleusDNA repair protein RAD52 homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (53)

Assay IDTitleYearJournalArticle
AID1347168HepG2 cells viability 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.
AID1347152Confirmatory screen NINDS 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.
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.
AID1347169Tertiary RLuc qRT-PCR qHTS assay 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.
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.
AID1347153Confirmatory 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.
AID1347167Vero cells viability 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.
AID1347149Furin counterscreen 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.
AID1347161Confirmatory screen NINDS Rhodamine 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.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
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.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID307118Antiviral activity against HIV1 3B in CEM cells assessed as inhibition of viral-induced cytopathicity2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Newer tetracycline derivatives: synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase.
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.
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]
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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.
AID322957Inhibition of synthetic amyloid beta-42 fibrillation by ThT fluorescence analysis relative to control2007The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14
Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct.
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.
AID307122Inhibition of HIV1 recombinant integrase strand transfer activity2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Newer tetracycline derivatives: synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase.
AID307119Cytotoxicity against CEM cells after 5 days by MTT method2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Newer tetracycline derivatives: synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID307121Inhibition of HIV1 recombinant integrase 3'-processing activity2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Newer tetracycline derivatives: synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase.
AID307123Antimycobacterial activity against Mycobacterium tuberculosis by agar dilution method2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Newer tetracycline derivatives: synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase.
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]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1594144Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme acti2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules.
AID1600069Inhibition of human recombinant IDE expressed in Escherichia coli BL21 (DE3) cells using ATTO 655- Cys-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Trp as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by spectrophotometri2019European journal of medicinal chemistry, Oct-01, Volume: 179Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID540235Phospholipidosis-negative literature compound
AID475504Binding affinity to amyloid beta (1 to 42) fibrils by change in fluorescence at 100 uM after 10 mins2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' 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]
AID475505Binding affinity to amyloid beta (1 to 42) oligomers by change in fluorescence at 100 uM after 10 mins2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta.
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]
AID322958Inhibition of synthetic amyloid beta-42 fibrillation by light scattering analysis relative to control2007The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14
Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct.
AID322956Inhibition of synthetic amyloid beta42 oligomer formation by Western blot2007The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14
Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct.
AID322955Inhibition of synthetic amyloid beta-42 oligomerization by ELISA2007The Journal of biological chemistry, Apr-06, Volume: 282, Issue:14
Small molecule inhibitors of aggregation indicate that amyloid beta oligomerization and fibrillization pathways are independent and distinct.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1594145Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity 2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID540211Fraction unbound 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.
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
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
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]
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]
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (349)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990323 (92.55)18.7374
1990's7 (2.01)18.2507
2000's8 (2.29)29.6817
2010's8 (2.29)24.3611
2020's3 (0.86)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 36.01

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index36.01 (24.57)
Research Supply Index5.97 (2.92)
Research Growth Index4.43 (4.65)
Search Engine Demand Index50.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (36.01)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (1.83%)5.53%
Reviews4 (1.05%)6.00%
Case Studies13 (3.40%)4.05%
Observational0 (0.00%)0.25%
Other358 (93.72%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]