Page last updated: 2024-12-10

demycarosylturimycin h

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 CID5289394
CHEMBL ID453514
MeSH IDM0067757
PubMed CID6440717
CHEBI ID85260
MeSH IDM0067757

Synonyms (36)

Synonym
nsc-64393
leucomycin v, 9-o-(5-(dimethylamino)tetrahydro-6-methyl-2h-pyran-2-yl)-, (9(2r,5s,6r))-
il-5902
il 5902
provamycin
espiramicin
sequamycin
CHEMBL453514
rp-5337
rovamicina
rovamycine
nsc-758472
nsc-55926
AB00514638
foromacidin a
unii-033ech6ifg
033ech6ifg ,
spiramycin i [mi]
S5744
AC-32598
leucomycin v,9-o-[(2r,5s,6r)-5-(dimethylamino)tetrahydro-6-methyl-2h-pyran-2-yl]-
DTXSID9023594
CS-8166
[(4r,5s,6s,7r,9r,10r,11e,13e,16r)-6-{[(2s,3r,4r,5s,6r)-5-{[(2s,4r,5s,6s)-4,5-dihydroxy-4,6-dimethyltetrahydro-2h-pyran-2-yl]oxy}-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2h-pyran-2-yl]oxy}-10-{[(2r,5s,6r)-5-(dimethylamino)-6-methyltetrahydro-2h-pyra
HY-100593
CCG-270525
foromacidine a
spiramycin 1
demycarosylturimycin h
spiramycin a
rovamycinetrade mark
2-[(4r,5s,6s,7r,9r,10r,11e,13e,16r)-6-[(2s,3r,4r,5s,6r)-5-[(2s,4r,5s,6s)-4,5-dihydroxy-4,6-dimethyl-tetrahydropyran-2-yl]oxy-4-(dimethylamino)-3-hydroxy-6-methyl-tetrahydropyran-2-yl]oxy-10-[(2r,5s,6s)-5-(dimethylamino)-6-methyl-tetrahydropyran-2-yl]oxy-4
CHEBI:85260
[(4r,5s,6s,7r,9r,10r,11e,13e,16r)-6-{[(2s,3r,4r,5s,6r)-5-{[(2s,4r,5s,6s)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy}-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy}-10-{[(2r,5s,6s)-5-(dimethylamino)-6-methyloxan-2-yl]oxy}-4-hydroxy-5-methoxy-9,16-dimethyl
J-015730
DB06145
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
bacterial metaboliteAny prokaryotic metabolite produced during a metabolic reaction in bacteria.
antibacterial drugA drug used to treat or prevent bacterial infections.
antimicrobial agentA substance that kills or slows the growth of microorganisms, including bacteria, viruses, fungi and protozoans.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
macrolideA macrocyclic lactone with a ring of twelve or more members derived from a polyketide.
etherAn organooxygen compound with formula ROR, where R is not hydrogen.
aldehydeA compound RC(=O)H, in which a carbonyl group is bonded to one hydrogen atom and to one R group.
disaccharide derivativeA carbohydrate derivative that is formally obtained from a disaccharide.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[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 (4)

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 (142)

Assay IDTitleYearJournalArticle
AID1632118Antibacterial activity against Staphylococcus epidermidis ATCC 12228 after 18 hrs by serial microdilution method2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID529873Antimicrobial activity against Staphylococcus aureus RN4220 harboring pAT392 containing mph(B) and rdmC-like genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID529867Antimicrobial activity against Streptococcus uberis UCN61 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID369555Hepatic uptake clearance in Bcrp gene knockout C57BL/6 mouse at 1 uM administered through single-pass liver perfusion for 15 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID423268Antibacterial activity against azithromycin-resistant 0.01 MOI Chlamydia psittaci 6BC BCRBAZ1 harboring A2059G mutation in bacterial 23S rRNA gene infected in mouse L2 cells treated 2 hrs after infection measured on day 7 by plaque assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Frequency of development and associated physiological cost of azithromycin resistance in Chlamydia psittaci 6BC and C. trachomatis L2.
AID369399Drug excretion in Bcrp gene knockout C57BL/6 mouse assessed as drug recovery in outflow perfusate and bile at 1 uM administered through single-pass liver perfusion for 15 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID143746Inhibition of N-acetylphenylalanine-tRNA peptide bond formation by puromycin reaction at 10E-6 M1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Synthesis and biological activity of photoactive derivatives of erythromycin.
AID1755474Volume of distribution at steady state in human at 0.5 g, iv2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID369403Drug level in C57BL/6 mouse bile at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW9182007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
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.
AID369412Drug excretion in C57BL/6 mouse assessed as drug recovery in bile at 1 uM administered through single-pass liver perfusion for 15 mins relative to total liver drug content at the end of infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID733658Antimicrobial activity against Escherichia coli ATTC-25922 at 100 ug after overnight incubation by disk-diffusion method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis, crystal structure and antibacterial activity of new highly functionalized ionic compounds based on the imidazole nucleus.
AID733657Antimicrobial activity against Staphylococcus aureus ATTC-25923 at 100 ug after overnight incubation by disk-diffusion method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis, crystal structure and antibacterial activity of new highly functionalized ionic compounds based on the imidazole nucleus.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID369414Drug excretion in Mrp2 gene knockout C57BL/6 mouse assessed as drug recovery in bile at 1 uM administered through single-pass liver perfusion for 15 mins relative to total liver drug content at the end of infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID1755480Cmax in human serum at 2 g, po2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID733655Antimicrobial activity against Salmonella typhimurium ATCC 07095 at 100 ug after overnight incubation by disk-diffusion method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis, crystal structure and antibacterial activity of new highly functionalized ionic compounds based on the imidazole nucleus.
AID519669Inhibition of PAR2-mediated SLIGKV-NH2-induced interleukin-8 production in normal human epidermal keratinocytes preincubated for 24 hrs by ELISA2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Effect of 14-membered-ring macrolides on production of interleukin-8 mediated by protease-activated receptor 2 in human keratinocytes.
AID1632119Antibacterial activity against Staphylococcus epidermidis ATCC 49134 after 18 hrs by serial microdilution method2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID534111Antibacterial activity against Pasteurella multocida pm1980 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID143744Inhibition of N-acetylphenylalanine-tRNA peptide bond formation by fragment reaction at 10e-5 M1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Synthesis and biological activity of photoactive derivatives of erythromycin.
AID369410Drug excretion in Bcrp gene knockout C57BL/6 mouse assessed as drug recovery in outflow perfusate at 1 uM administered through single-pass liver perfusion for 15 mins relative to total liver drug content at the end of infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID369409Drug excretion in Mrp2 gene knockout C57BL/6 mouse assessed as drug recovery in outflow perfusate at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW918 relative to total liver drug content at the 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID396002Antimicrobial activity against Mycoplasma putrefaciens KS1 after 24 hrs by twofold serial dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro susceptibilities of Mycoplasma putrefaciens field isolates.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID423267Antibacterial activity against azithromycin-resistant 0.01 MOI Chlamydia psittaci 6BC BCRBAZ5 harboring A2059C mutation in bacterial 23S rRNA gene infected in mouse L2 cells treated 2 hrs after infection measured on day 7 by plaque assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Frequency of development and associated physiological cost of azithromycin resistance in Chlamydia psittaci 6BC and C. trachomatis L2.
AID523010Activity at macrolide 2'-phosphotransferase 1 by PK/LDH-coupled assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Nucleotide selectivity of antibiotic kinases.
AID369402Drug level in Bcrp gene knockout C57BL/6 mouse bile at 1 uM administered through single-pass liver perfusion for 15 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID1632114Antibacterial activity against Bacillus subtilis ATCC 6633 after 18 hrs by serial microdilution method2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1632116Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 1 after 18 hrs by serial microdilution method2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID529869Antimicrobial activity against Escherichia coli AG100A harboring pAT392 containing mph(B) gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID529878Antimicrobial activity against Staphylococcus aureus RN4220 harboring empty vector by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID369413Drug excretion in C57BL/6 mouse assessed as drug recovery in bile at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW918 relative to total liver drug content at the end of infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID1632120Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 18 hrs by serial microdilution method2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID534112Ratio of MIC for Pasteurella multocida AL435 to MIC for TolC deficient Pasteurella multocida pm19802008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID1755469Cmax in human at 2 g, po2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1755470Tmax in human at 2 g, po2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID369411Drug excretion in Bcrp gene knockout C57BL/6 mouse assessed as drug recovery in outflow perfusate at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW918 relative to total liver drug content at the 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID518965Induction of erm(C) expression in Escherichia coli JM109 harboring Staphylococcus aureus erm(C)-containing pERMZalpha reporter plasmid at 10 mg/ml after 36 hrs at 37 degC by disc-based beta-galactosidase reporter gene assay2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Induction of erm(C) expression by noninducing antibiotics.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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.
AID1632126Cytotoxicity against HDF assessed as reduction in cell survival after 72 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID1632130Selectivity index, ratio of IC50 for HDF to IC50 for human MCF7 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID423273Antibacterial activity against azithromycin-tolerant 0.01 MOI Chlamydia trachomatis L2AZM#23 harboring mutation in bacterial ribosomal protein L4 infected in mouse L2 cells treated 2 hrs after infection measured on day 7 by plaque assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Frequency of development and associated physiological cost of azithromycin resistance in Chlamydia psittaci 6BC and C. trachomatis L2.
AID596021Antiparasitic activity against clindamycin-resistant Toxoplasma gondii 4 infected in HFF assessed as reduction of ycf24/UPRT genes copy number ratio at 5 uM treated for 48 hrs immediately after infection followed by reinoculated into fresh HFF monolayers 2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Chemistry and biology of macrolide antiparasitic agents.
AID369415Drug excretion in Mrp2 gene knockout C57BL/6 mouse assessed as drug recovery in bile at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW918 relative to total liver drug content at the end of infusi2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID1632129Selectivity index, ratio of IC50 for HDF to IC50 for human KB cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID1632125Cytotoxicity against human HepG2 cells assessed as reduction in cell survival after 72 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID423265Antibacterial activity against 0.01 MOI wild type Chlamydia psittaci 6BC BCRB infected in mouse L2 cells treated 2 hrs after infection measured on day 7 by plaque assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Frequency of development and associated physiological cost of azithromycin resistance in Chlamydia psittaci 6BC and C. trachomatis L2.
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.
AID369401Drug level in Mrp2 gene knockout C57BL/6 mouse bile at 1 uM administered through single-pass liver perfusion for 15 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID529866Antimicrobial activity against Streptococcus uberis UCN60 expressing mph(B) and rdmC-like genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID369553Hepatic uptake clearance in Mrp2 gene knockout C57BL/6 mouse at 1 uM administered through single-pass liver perfusion for 15 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
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]
AID529870Antimicrobial activity against Escherichia coli AG100A harboring pAT392 containing mph(B) and rdmC-like genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID1755472Protein binding in human plasma at 2 g, po2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID396001Antimicrobial activity against Mycoplasma putrefaciens Jordanian isolates after 24 hrs by twofold serial dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro susceptibilities of Mycoplasma putrefaciens field isolates.
AID423274Antibacterial activity against azithromycin-tolerant 0.01 MOI Chlamydia trachomatis L2AZM#31 harboring mutation in bacterial ribosomal protein L4 infected in mouse L2 cells treated 2 hrs after infection measured on day 7 by plaque assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Frequency of development and associated physiological cost of azithromycin resistance in Chlamydia psittaci 6BC and C. trachomatis L2.
AID369400Drug level in C57BL/6 mouse bile at 1 uM administered through single-pass liver perfusion for 15 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1755483Drug excretion in human urine at 2 g, po measured within 24 hrs2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID520735Antimicrobial activity against Staphylococcus aureus RN4220 harboring erm(B) and cfr gene by disk diffusion assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors.
AID596087Antiparasitic activity against green fluorescent protein expressing hwgprt deficient Toxoplasma gondii RH infected in HFF assessed as reduction of ycf24/UPRT genes copy number ratio at 5 uM treated for 48 hrs after 6 hrs infection followed by reinoculated2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Chemistry and biology of macrolide antiparasitic agents.
AID733656Antimicrobial activity against Pseudomonas aeruginosa ATCC 27853 at 100 ug after overnight incubation by disk-diffusion method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis, crystal structure and antibacterial activity of new highly functionalized ionic compounds based on the imidazole nucleus.
AID369404Drug level in Mrp2 gene knockout C57BL/6 mouse bile at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW9182007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
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]
AID1695933Antibacterial activity against constitutively-resistant Staphylococcus aureus2019European journal of medicinal chemistry, Apr-15, Volume: 168Comprehensive review on the anti-bacterial activity of 1,2,3-triazole hybrids.
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.
AID1632128Selectivity index, ratio of IC50 for HDF to IC50 for human HeLa cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID369408Drug excretion in Mrp2 gene knockout C57BL/6 mouse assessed as drug recovery in outflow perfusate at 1 uM administered through single-pass liver perfusion for 15 mins relative to total liver drug content at the end of infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID520740Antimicrobial activity against erm(B)-deficient Staphylococcus aureus RN4220 harboring cfr gene by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors.
AID1632132Solubility of compound in water2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID529874Antimicrobial activity against Enterococcus faecalis JH2-2 harboring pAT392 containing rdmC-like gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID423272Antibacterial activity against 0.01 MOI wild type Chlamydia trachomatis L2/LGV/434/Bu infected in mouse L2 cells treated 2 hrs after infection measured on day 7 by plaque assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Frequency of development and associated physiological cost of azithromycin resistance in Chlamydia psittaci 6BC and C. trachomatis L2.
AID369416Drug excretion in Bcrp gene knockout C57BL/6 mouse assessed as drug recovery in bile at 1 uM administered through single-pass liver perfusion for 15 mins relative to total liver drug content at the end of infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID534110Antibacterial activity against TolC deficient Pasteurella multocida pm1980 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID534109Ratio of MIC for Pasteurella multocida AL435 to MIC for TolC deficient Pasteurella multocida pm05272008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID596020Antiparasitic activity against green fluorescent protein expressing hwgprt deficient Toxoplasma gondii RH infected in HFF assessed as reduction of ycf24/UPRT genes copy number ratio at 5 uM treated for 48 hrs immediately after infection followed by reinoc2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Chemistry and biology of macrolide antiparasitic agents.
AID369397Drug excretion in C57BL/6 mouse assessed as drug recovery in outflow perfusate and bile at 1 uM administered through single-pass liver perfusion for 15 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID529868Antimicrobial activity against Escherichia coli AG100A harboring pAT392 containing rdmC-like gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID529877Antimicrobial activity against Escherichia coli AG100A harboring empty vector by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
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.
AID1755475Renal clearance in human at 0.5 g, iv2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1632123Cytotoxicity against human KB cells assessed as reduction in cell survival after 72 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID369554Hepatic uptake clearance in Mrp2 gene knockout C57BL/6 mouse at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW9182007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID1632122Cytotoxicity against human HeLa cells assessed as reduction in cell survival after 72 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID1755477Total clearance in human at 0.5 g, iv2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID534108Antibacterial activity against Pasteurella multocida pm0527 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
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.
AID1755479Half life in human at 0.5 g, iv2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID369552Hepatic uptake clearance in C57BL/6 mouse at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW9182007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID534106Antibacterial activity against Pasteurella multocida AL435 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID369417Drug excretion in Bcrp gene knockout C57BL/6 mouse assessed as drug recovery in bile at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW918 relative to total liver drug content at the end of infusi2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID529871Antimicrobial activity against Staphylococcus aureus RN4220 harboring pAT392 containing rdmC-like gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1755476Non-renal clearance in human at 0.5 g, iv2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID369405Drug level in Bcrp gene knockout C57BL/6 mouse bile at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW9182007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID529879Antimicrobial activity against Enterococcus faecalis JH2-2 harboring empty vector by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1755471Half life in human at 2 g, po2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID396000Antimicrobial activity against Mycoplasma putrefaciens French isolates after 24 hrs by twofold serial dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro susceptibilities of Mycoplasma putrefaciens field isolates.
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]
AID1695932Antibacterial activity against inducibly-resistant Staphylococcus aureus2019European journal of medicinal chemistry, Apr-15, Volume: 168Comprehensive review on the anti-bacterial activity of 1,2,3-triazole hybrids.
AID523012Ratio of Kcat to Km for macrolide 2'-phosphotransferase 1 by PK/LDH-coupled assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Nucleotide selectivity of antibiotic kinases.
AID1632131Selectivity index, ratio of IC50 for HDF to IC50 for human HepG2 cells2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID1755473Cmax in human at 0.5 g, iv2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID369551Hepatic uptake clearance in C57BL/6 mouse at 1 uM administered through single-pass liver perfusion for 15 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID520736Antimicrobial activity against erm(B) and cfr-deficient Staphylococcus aureus RN4220 harboring plasmid LI50 by disk diffusion assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors.
AID423266Antibacterial activity against azithromycin-resistant 0.01 MOI Chlamydia psittaci 6BC BCRBAZ2 harboring A2058C mutation in bacterial 23S rRNA gene infected in mouse L2 cells treated 2 hrs after infection measured on day 7 by plaque assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Frequency of development and associated physiological cost of azithromycin resistance in Chlamydia psittaci 6BC and C. trachomatis L2.
AID1755478Drug excretion in human urine at 0.5 g, iv measured within 24 hrs2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1632121Octanol-water partition coefficient, log P of compound after 1 hr by UV-visible spectrophotometric analysis2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID1632115Antibacterial activity against Micrococcus luteus ATCC 10240 after 18 hrs by serial microdilution method2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
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]
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1755468Oral bioavailability in human at 2 g2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID143745Inhibition of N-acetylphenylalanine-tRNA peptide bond formation by puromycin reaction at 10E-5 M1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Synthesis and biological activity of photoactive derivatives of erythromycin.
AID1632124Cytotoxicity against human MCF7 cells assessed as reduction in cell survival after 72 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID369556Hepatic uptake clearance in Bcrp gene knockout C57BL/6 mouse at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW9182007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID534107Antibacterial activity against TolC deficient Pasteurella multocida pm0527 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID1755481AUC (0 to infinity) in human serum at 2 g, po2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
AID1632117Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 2 after 18 hrs by serial microdilution method2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm.
AID529872Antimicrobial activity against Staphylococcus aureus RN4220 harboring pAT392 containing mph(B) gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
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]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID529876Antimicrobial activity against Enterococcus faecalis JH2-2 harboring pAT392 containing mph(B) and rdmC-like gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID1695931Antibacterial activity against methicillin-resistant Staphylococcus aureus2019European journal of medicinal chemistry, Apr-15, Volume: 168Comprehensive review on the anti-bacterial activity of 1,2,3-triazole hybrids.
AID596088Antiparasitic activity against clindamycin-resistant Toxoplasma gondii 4 infected in HFF assessed as reduction of ycf24/UPRT genes copy number ratio at 5 uM treated for 48 hrs after 6 hrs infection followed by reinoculated into fresh HFF monolayers measur2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Chemistry and biology of macrolide antiparasitic agents.
AID1755482Tmax in human serum at 2 g, po2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
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.
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
AID369407Drug excretion in C57BL/6 mouse assessed as drug recovery in outflow perfusate at 1 uM administered through single-pass liver perfusion for 15 mins coinfused with Pgp and Bcrp inhibitor GW918 relative to total liver drug content at the end of infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID529875Antimicrobial activity against Enterococcus faecalis JH2-2 harboring pAT392 containing mph(B) gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Emergence of macrolide resistance gene mph(B) in Streptococcus uberis and cooperative effects with rdmC-like gene.
AID520741Antimicrobial activity against cfr-deficient Staphylococcus aureus RN4220 harboring erm(B) gene by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID369406Drug excretion in C57BL/6 mouse assessed as drug recovery in outflow perfusate at 1 uM administered through single-pass liver perfusion for 15 mins relative to total liver drug content at the end of infusion2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID369398Drug excretion in Mrp2 gene knockout C57BL/6 mouse assessed as drug recovery in outflow perfusate and bile at 1 uM administered through single-pass liver perfusion for 15 mins2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Roles of P-glycoprotein, Bcrp, and Mrp2 in biliary excretion of spiramycin in mice.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (27)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (3.70)18.7374
1990's3 (11.11)18.2507
2000's10 (37.04)29.6817
2010's12 (44.44)24.3611
2020's1 (3.70)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.23

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

MetricThis Compound (vs All)
Research Demand Index11.23 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.23)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews2 (10.53%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other17 (89.47%)84.16%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]