Page last updated: 2024-11-12

archazolid a

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Description

archazolid A: inhibits vacuolar-type ATPase; isolated from Archangium gephyra; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16680454
CHEMBL ID241106
MeSH IDM0509807

Synonyms (6)

Synonym
archazolid a
CHEMBL241106
bdbm50178305
Q44002843
(1s)-1-{4-[(2s,3s,4e,6e,8s,9s,10r,11e,13z,15z,17s,18s,19e,22e)-10,18-dihydroxy-8-methoxy-3,7,9,13,15,17,20,23-octamethyl-24-oxo-1-oxacyclotetracosa-4,6,11,13,15,19,22-heptaen-2-yl]-1,3-thiazol-2-yl}-3-methylbutyl methylcarbamate
[(1s)-1-[4-[(2s,3s,4e,6e,8s,9s,10r,11e,13z,15z,17s,18s,19e,22e)-10,18-dihydroxy-8-methoxy-3,7,9,13,15,17,20,23-octamethyl-24-oxo-1-oxacyclotetracosa-4,6,11,13,15,19,22-heptaen-2-yl]-1,3-thiazol-2-yl]-3-methylbutyl] n-methylcarbamate
[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)
Neutrophil elastaseHomo sapiens (human)IC50 (µMol)0.35200.00632.073422.3780AID1583536
Adenosine receptor A3Homo sapiens (human)Ki0.96700.00000.930610.0000AID1583535
P2X purinoceptor 3Homo sapiens (human)IC50 (µMol)0.08610.00000.20301.5136AID1583534
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile acid receptorHomo sapiens (human)EC50 (µMol)0.20000.00401.419110.0000AID1305701
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (100)

Processvia Protein(s)Taxonomy
proteolysisNeutrophil elastaseHomo sapiens (human)
negative regulation of transcription by RNA polymerase IINeutrophil elastaseHomo sapiens (human)
response to yeastNeutrophil elastaseHomo sapiens (human)
leukocyte migration involved in inflammatory responseNeutrophil elastaseHomo sapiens (human)
biosynthetic process of antibacterial peptides active against Gram-negative bacteriaNeutrophil elastaseHomo sapiens (human)
proteolysisNeutrophil elastaseHomo sapiens (human)
intracellular calcium ion homeostasisNeutrophil elastaseHomo sapiens (human)
response to UVNeutrophil elastaseHomo sapiens (human)
extracellular matrix disassemblyNeutrophil elastaseHomo sapiens (human)
protein catabolic processNeutrophil elastaseHomo sapiens (human)
response to lipopolysaccharideNeutrophil elastaseHomo sapiens (human)
negative regulation of chemokine productionNeutrophil elastaseHomo sapiens (human)
negative regulation of interleukin-8 productionNeutrophil elastaseHomo sapiens (human)
positive regulation of interleukin-8 productionNeutrophil elastaseHomo sapiens (human)
defense response to bacteriumNeutrophil elastaseHomo sapiens (human)
positive regulation of MAP kinase activityNeutrophil elastaseHomo sapiens (human)
positive regulation of smooth muscle cell proliferationNeutrophil elastaseHomo sapiens (human)
negative regulation of inflammatory responseNeutrophil elastaseHomo sapiens (human)
positive regulation of immune responseNeutrophil elastaseHomo sapiens (human)
negative regulation of chemotaxisNeutrophil elastaseHomo sapiens (human)
pyroptosisNeutrophil elastaseHomo sapiens (human)
neutrophil-mediated killing of gram-negative bacteriumNeutrophil elastaseHomo sapiens (human)
neutrophil-mediated killing of fungusNeutrophil elastaseHomo sapiens (human)
positive regulation of leukocyte tethering or rollingNeutrophil elastaseHomo sapiens (human)
phagocytosisNeutrophil elastaseHomo sapiens (human)
acute inflammatory response to antigenic stimulusNeutrophil elastaseHomo sapiens (human)
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo sapiens (human)
response to hypoxiaP2X purinoceptor 3Homo sapiens (human)
signal transductionP2X purinoceptor 3Homo sapiens (human)
neuromuscular synaptic transmissionP2X purinoceptor 3Homo sapiens (human)
response to heatP2X purinoceptor 3Homo sapiens (human)
response to coldP2X purinoceptor 3Homo sapiens (human)
response to mechanical stimulusP2X purinoceptor 3Homo sapiens (human)
response to carbohydrateP2X purinoceptor 3Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 3Homo sapiens (human)
urinary bladder smooth muscle contractionP2X purinoceptor 3Homo sapiens (human)
peristalsisP2X purinoceptor 3Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 3Homo sapiens (human)
regulation of synaptic plasticityP2X purinoceptor 3Homo sapiens (human)
behavioral response to painP2X purinoceptor 3Homo sapiens (human)
positive regulation of calcium-mediated signalingP2X purinoceptor 3Homo sapiens (human)
sensory perception of tasteP2X purinoceptor 3Homo sapiens (human)
establishment of localization in cellP2X purinoceptor 3Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 3Homo sapiens (human)
protein homotrimerizationP2X purinoceptor 3Homo sapiens (human)
cellular response to ATPP2X purinoceptor 3Homo sapiens (human)
inorganic cation transmembrane transportP2X purinoceptor 3Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 3Homo sapiens (human)
negative regulation of very-low-density lipoprotein particle remodelingBile acid receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionBile acid receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
nitrogen catabolite activation of transcription from RNA polymerase II promoterBile acid receptorHomo sapiens (human)
intracellular glucose homeostasisBile acid receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
inflammatory responseBile acid receptorHomo sapiens (human)
cell-cell junction assemblyBile acid receptorHomo sapiens (human)
Notch signaling pathwayBile acid receptorHomo sapiens (human)
bile acid metabolic processBile acid receptorHomo sapiens (human)
negative regulation of tumor necrosis factor-mediated signaling pathwayBile acid receptorHomo sapiens (human)
regulation of low-density lipoprotein particle clearanceBile acid receptorHomo sapiens (human)
intracellular receptor signaling pathwayBile acid receptorHomo sapiens (human)
negative regulation of type II interferon productionBile acid receptorHomo sapiens (human)
negative regulation of interleukin-1 productionBile acid receptorHomo sapiens (human)
negative regulation of interleukin-2 productionBile acid receptorHomo sapiens (human)
negative regulation of interleukin-6 productionBile acid receptorHomo sapiens (human)
negative regulation of tumor necrosis factor productionBile acid receptorHomo sapiens (human)
positive regulation of interleukin-17 productionBile acid receptorHomo sapiens (human)
toll-like receptor 9 signaling pathwayBile acid receptorHomo sapiens (human)
regulation of urea metabolic processBile acid receptorHomo sapiens (human)
intracellular triglyceride homeostasisBile acid receptorHomo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusBile acid receptorHomo sapiens (human)
bile acid signaling pathwayBile acid receptorHomo sapiens (human)
intracellular bile acid receptor signaling pathwayBile acid receptorHomo sapiens (human)
cholesterol homeostasisBile acid receptorHomo sapiens (human)
defense response to bacteriumBile acid receptorHomo sapiens (human)
negative regulation of apoptotic processBile acid receptorHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionBile acid receptorHomo sapiens (human)
innate immune responseBile acid receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBile acid receptorHomo sapiens (human)
positive regulation of insulin receptor signaling pathwayBile acid receptorHomo sapiens (human)
fatty acid homeostasisBile acid receptorHomo sapiens (human)
regulation of insulin secretion involved in cellular response to glucose stimulusBile acid receptorHomo sapiens (human)
regulation of bile acid biosynthetic processBile acid receptorHomo sapiens (human)
cellular response to lipopolysaccharideBile acid receptorHomo sapiens (human)
cellular response to fatty acidBile acid receptorHomo sapiens (human)
cellular response to organonitrogen compoundBile acid receptorHomo sapiens (human)
negative regulation of monocyte chemotactic protein-1 productionBile acid receptorHomo sapiens (human)
regulation of cholesterol metabolic processBile acid receptorHomo sapiens (human)
cellular response to bile acidBile acid receptorHomo sapiens (human)
positive regulation of adipose tissue developmentBile acid receptorHomo sapiens (human)
positive regulation of phosphatidic acid biosynthetic processBile acid receptorHomo sapiens (human)
positive regulation of glutamate metabolic processBile acid receptorHomo sapiens (human)
positive regulation of ammonia assimilation cycleBile acid receptorHomo sapiens (human)
cell differentiationBile acid receptorHomo sapiens (human)
negative regulation of inflammatory responseBile acid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (26)

Processvia Protein(s)Taxonomy
protease bindingNeutrophil elastaseHomo sapiens (human)
transcription corepressor activityNeutrophil elastaseHomo sapiens (human)
endopeptidase activityNeutrophil elastaseHomo sapiens (human)
serine-type endopeptidase activityNeutrophil elastaseHomo sapiens (human)
protein bindingNeutrophil elastaseHomo sapiens (human)
heparin bindingNeutrophil elastaseHomo sapiens (human)
peptidase activityNeutrophil elastaseHomo sapiens (human)
cytokine bindingNeutrophil elastaseHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 3Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 3Homo sapiens (human)
ATP bindingP2X purinoceptor 3Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingBile acid receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingBile acid receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificBile acid receptorHomo sapiens (human)
transcription coregulator bindingBile acid receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificBile acid receptorHomo sapiens (human)
DNA-binding transcription factor activityBile acid receptorHomo sapiens (human)
nuclear receptor activityBile acid receptorHomo sapiens (human)
protein bindingBile acid receptorHomo sapiens (human)
zinc ion bindingBile acid receptorHomo sapiens (human)
nuclear receptor bindingBile acid receptorHomo sapiens (human)
bile acid bindingBile acid receptorHomo sapiens (human)
bile acid receptor activityBile acid receptorHomo sapiens (human)
sequence-specific DNA bindingBile acid receptorHomo sapiens (human)
nuclear retinoid X receptor bindingBile acid receptorHomo sapiens (human)
chenodeoxycholic acid bindingBile acid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
extracellular regionNeutrophil elastaseHomo sapiens (human)
extracellular spaceNeutrophil elastaseHomo sapiens (human)
cytoplasmNeutrophil elastaseHomo sapiens (human)
cytosolNeutrophil elastaseHomo sapiens (human)
cell surfaceNeutrophil elastaseHomo sapiens (human)
secretory granuleNeutrophil elastaseHomo sapiens (human)
azurophil granule lumenNeutrophil elastaseHomo sapiens (human)
specific granule lumenNeutrophil elastaseHomo sapiens (human)
phagocytic vesicleNeutrophil elastaseHomo sapiens (human)
collagen-containing extracellular matrixNeutrophil elastaseHomo sapiens (human)
extracellular exosomeNeutrophil elastaseHomo sapiens (human)
transcription repressor complexNeutrophil elastaseHomo sapiens (human)
extracellular spaceNeutrophil elastaseHomo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo sapiens (human)
plasma membraneP2X purinoceptor 3Homo sapiens (human)
axonP2X purinoceptor 3Homo sapiens (human)
Schaffer collateral - CA1 synapseP2X purinoceptor 3Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseP2X purinoceptor 3Homo sapiens (human)
postsynapseP2X purinoceptor 3Homo sapiens (human)
receptor complexP2X purinoceptor 3Homo sapiens (human)
plasma membraneP2X purinoceptor 3Homo sapiens (human)
nucleoplasmBile acid receptorHomo sapiens (human)
chromatinBile acid receptorHomo sapiens (human)
euchromatinBile acid receptorHomo sapiens (human)
receptor complexBile acid receptorHomo sapiens (human)
RNA polymerase II transcription regulator complexBile acid receptorHomo sapiens (human)
nucleusBile acid receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (49)

Assay IDTitleYearJournalArticle
AID717488Solubility of the compound in 5:95 MeOH-d4:D2O solution at 0.5 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID717489Solubility of the compound in 10:90 DMSO-d6:D2O solution at 0.5 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583542Inhibition of human A2B adenosine receptor incubated for 60 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID306128Inhibition of tobacco hornworm midgut vacuolar ATPase V1/V0 holoenzyme2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Design, synthesis, and biological evaluation of novel analogues of archazolid: a highly potent simplified V-ATPase inhibitor.
AID1583535Displacement of [3H]PSB-11 from human A3 adenosine receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583539Inhibition of Calcium channel (unknown origin) at 10 uM relative to control2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583536Inhibition of human leukocyte elastase assessed as reduction in pNA release using chromogenic MeO-Suc-Ala-Ala-Pro-Val-pNA substrate measured over 10 mins by spectrophotometry2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID717484Solubility of the compound in 10:90 MeOH-d4:D2O solution at 0.5 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583541Inhibition of human A2A adenosine receptor incubated for 60 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583531Inhibition of human P2X1 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by calcium 5 dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID717480Solubility in 4 mM LDAO at 1 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583548Inhibition of human P2Y12 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583553Inhibition of human P2X7 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583549Inhibition of human P2Y14 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583532Growth inhibition of human 1321N1 cells incubated for 72 hrs by MTT assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583552Inhibition of human P2X4 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID601539Inhibition of Manduca sexta V-ATPase V1/Vo holoenzyme activity assessed as inorganic phosphate production pretreated for 5 mins2011Journal of natural products, May-27, Volume: 74, Issue:5
Archazolid A-15-O-β-D-glucopyranoside and iso-archazolid B: potent V-ATPase inhibitory polyketides from the myxobacteria Cystobacter violaceus and Archangium gephyra.
AID1583533Inhibition of Manduca sexta V-type proton ATPase assessed as reduction in inorganic phosphate production pre-inucubated for 5 mins before Tris-ATP addition and measured after 2 mins2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583560Inhibition of chymotrypsin (unknown origin) assessed as reduction in pNA release using chromogenic Suc-Ala-Ala-Pro-Phe-pNA substrate measured over 12.5 mins by spectrophotometry2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID717479Solubility in 3 mM DPC at 0.5 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583557Inhibition of trypsin (unknown origin) assessed as reduction in pNA release using chromogenic Suc-Ala-Ala-Pro-Arg-pNA substrate measured over 10 mins by spectrophotometry2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583550Inhibition of human GPR17 at 10 uM by Oregon-green BAPTA-1/AM dye based calcium mobilization assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID601540Antiproliferative activity against mouse L929 cells assessed as growth inhibition after 5 days by MTT assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Archazolid A-15-O-β-D-glucopyranoside and iso-archazolid B: potent V-ATPase inhibitory polyketides from the myxobacteria Cystobacter violaceus and Archangium gephyra.
AID1583546Inhibition of human P2Y6 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583538Inhibition of human PPARgamma at 10 uM relative to control2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583558Inhibition of cathepsin B (unknown origin) assessed as reduction in pNA release using chromogenic Z-Arg-Arg-pNA substrate measured over 1 hr by spectrophotometry2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID717490Solubility of the compound in 50:50 DMSO-d6:D2O solution at 1 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583544Inhibition of human P2Y2 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID717487Solubility of the compound in 5:95 EtOH-d6:D2O solution at 1 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID717482Solubility of the compound in 42:9:49 EtOH-d6:CNCD3:D2O solution at <0.5 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID717486Solubility of the compound in 5:95 CNCD3-d6:D2O solution at 1 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583551Inhibition of human P2X2 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583537Ratio of IC50 for inhibition of Manduca sexta V-type proton ATPase assessed as reduction in inorganic phosphate production pre-inucubated for 5 mins before Tris-ATP addition and measured after 2 mins to IC50 for inhibition of human 1321N1 cells incubated 2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID306129Growth inhibition of mouse L929 cells by MTT assay2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Design, synthesis, and biological evaluation of novel analogues of archazolid: a highly potent simplified V-ATPase inhibitor.
AID1583559Inhibition of cathepsin L (unknown origin) assessed as reduction in pNA release using chromogenic Z-Phe-Arg-pNA substrate measured over 1 hr by spectrophotometry2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID717481Solubility in 17 mM DHPC at 1 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID717485Solubility of the compound in 5:95 EtOH-d6:D2O solution at 0.5 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583547Inhibition of human P2Y11 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID717477Solubility in 50 mM OG at 0.5 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1305701Agonist activity at farnesoid x receptor(unknown origin)2016Bioorganic & medicinal chemistry, Aug-01, Volume: 24, Issue:15
Novel approaches to map small molecule-target interactions.
AID717478Solubility in 2 mM LMPC at 0.5 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583534Inhibition of human P2X3 assessed as reduction in agonist-induced intracellular Ca2+ concentration pre-incubated for 30 mins before agonist addition by calcium 5 dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID717483Solubility of the compound in 40:40:1 CDCl3:MeOH-d4:D2O at 1 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583554Non-competitive inhibition of human P2X3 expressed in human 1321N1 cells assessed as reduction in maximal effect of ATP-induced intracellular Ca2+ concentration pre-incubated for 30 mins before agonist addition by calcium 5 dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID717476Solubility in 0.4 mM OG at 0.5 mM by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID717475Binding affinity to tobacco hornworm V-ATPase c subunit in 4:4:1 CDCl3:MeOH-d4:D2O by NMR analysis2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
AID1583543Inhibition of human P2Y1 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583540Inhibition of human A1 adenosine receptor incubated for 60 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
AID1583545Inhibition of human P2Y4 assessed as reduction in agonist-induced intracellular Ca2+ concentration at 10 uM pre-incubated for 30 mins before agonist addition by FLUO-4 AM dye based fluorescence assay2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (25)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (24.00)29.6817
2010's17 (68.00)24.3611
2020's2 (8.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.59

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 Index11.59 (24.57)
Research Supply Index3.26 (2.92)
Research Growth Index4.84 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.59)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other24 (96.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]