Page last updated: 2024-11-13

gallinamide a

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Description

gallinamide A: antimalarial peptide from marine cyanobacteria [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25209862
CHEMBL ID541700
MeSH IDM0528969

Synonyms (11)

Synonym
CHEMBL541700
gallinamide a
symplostatin 4
1208232-55-6
DTXSID50153030
bdbm50033762
[(1s)-1-[[(1s)-1-[[(e,1s)-4-[(2s)-3-methoxy-2-methyl-5-oxo-2h-pyrrol-1-yl]-1-methyl-4-oxo-but-2-enyl]carbamoyl]-3-methyl-butyl]carbamoyl]-3-methyl-butyl] (2s,3s)-2-(dimethylamino)-3-methyl-pentanoate
CS-0255808
[(2s)-1-[[(2s)-1-[[(e,2s)-5-[(2s)-3-methoxy-2-methyl-5-oxo-2h-pyrrol-1-yl]-5-oxopent-3-en-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl] (2s,3s)-2-(dimethylamino)-3-methylpentanoate
EX-A5200
HY-N10109
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cathepsin L2Homo sapiens (human)IC50 (µMol)0.30000.07502.214110.0000AID1063745; AID1063746
Procathepsin LMus musculus (house mouse)Ki0.00530.00530.00530.0053AID1898760
Procathepsin LHomo sapiens (human)IC50 (µMol)0.01540.00021.66619.5100AID1063747; AID1063748; AID1526360; AID1526361
Procathepsin LHomo sapiens (human)Ki0.00800.00001.10139.3000AID1898758
Cathepsin BHomo sapiens (human)IC50 (µMol)1.96910.00021.845310.0000AID1063743; AID1063744; AID1898750
Cathepsin BHomo sapiens (human)Ki0.11700.00001.21808.6000AID1898759
Pro-cathepsin HHomo sapiens (human)IC50 (µMol)30.00000.12592.740410.0000AID1063741; AID1063742
CruzipainTrypanosoma cruziIC50 (µMol)0.00080.00022.04508.0000AID1526368; AID1902912
Cysteine proteinase falcipain 2a Plasmodium falciparum (malaria parasite P. falciparum)IC50 (µMol)0.00850.00580.44035.0000AID1171535; AID1171536
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (44)

Processvia Protein(s)Taxonomy
apoptotic processCathepsin L2Homo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IICathepsin L2Homo sapiens (human)
extracellular matrix disassemblyCathepsin L2Homo sapiens (human)
immune responseCathepsin L2Homo sapiens (human)
positive regulation of apoptotic signaling pathwayCathepsin L2Homo sapiens (human)
positive regulation of peptidase activityCathepsin L2Homo sapiens (human)
proteolysis involved in protein catabolic processCathepsin L2Homo sapiens (human)
adaptive immune responseProcathepsin LHomo sapiens (human)
proteolysisProcathepsin LHomo sapiens (human)
protein autoprocessingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host plasma membraneProcathepsin LHomo sapiens (human)
receptor-mediated endocytosis of virus by host cellProcathepsin LHomo sapiens (human)
antigen processing and presentationProcathepsin LHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IIProcathepsin LHomo sapiens (human)
collagen catabolic processProcathepsin LHomo sapiens (human)
zymogen activationProcathepsin LHomo sapiens (human)
enkephalin processingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host endosome membraneProcathepsin LHomo sapiens (human)
CD4-positive, alpha-beta T cell lineage commitmentProcathepsin LHomo sapiens (human)
symbiont entry into host cellProcathepsin LHomo sapiens (human)
antigen processing and presentation of peptide antigenProcathepsin LHomo sapiens (human)
proteolysis involved in protein catabolic processProcathepsin LHomo sapiens (human)
elastin catabolic processProcathepsin LHomo sapiens (human)
macrophage apoptotic processProcathepsin LHomo sapiens (human)
cellular response to thyroid hormone stimulusProcathepsin LHomo sapiens (human)
positive regulation of apoptotic signaling pathwayProcathepsin LHomo sapiens (human)
positive regulation of peptidase activityProcathepsin LHomo sapiens (human)
immune responseProcathepsin LHomo sapiens (human)
proteolysisCathepsin BHomo sapiens (human)
thyroid hormone generationCathepsin BHomo sapiens (human)
collagen catabolic processCathepsin BHomo sapiens (human)
epithelial cell differentiationCathepsin BHomo sapiens (human)
regulation of apoptotic processCathepsin BHomo sapiens (human)
decidualizationCathepsin BHomo sapiens (human)
symbiont entry into host cellCathepsin BHomo sapiens (human)
proteolysis involved in protein catabolic processCathepsin BHomo sapiens (human)
cellular response to thyroid hormone stimulusCathepsin BHomo sapiens (human)
metanephros developmentPro-cathepsin HHomo sapiens (human)
T cell mediated cytotoxicityPro-cathepsin HHomo sapiens (human)
adaptive immune responsePro-cathepsin HHomo sapiens (human)
immune response-regulating signaling pathwayPro-cathepsin HHomo sapiens (human)
proteolysisPro-cathepsin HHomo sapiens (human)
apoptotic processPro-cathepsin HHomo sapiens (human)
positive regulation of cell population proliferationPro-cathepsin HHomo sapiens (human)
positive regulation of gene expressionPro-cathepsin HHomo sapiens (human)
positive regulation of epithelial cell migrationPro-cathepsin HHomo sapiens (human)
neuropeptide catabolic processPro-cathepsin HHomo sapiens (human)
bradykinin catabolic processPro-cathepsin HHomo sapiens (human)
positive regulation of peptidase activityPro-cathepsin HHomo sapiens (human)
antigen processing and presentationPro-cathepsin HHomo sapiens (human)
positive regulation of cell migrationPro-cathepsin HHomo sapiens (human)
zymogen activationPro-cathepsin HHomo sapiens (human)
protein destabilizationPro-cathepsin HHomo sapiens (human)
response to retinoic acidPro-cathepsin HHomo sapiens (human)
membrane protein proteolysisPro-cathepsin HHomo sapiens (human)
negative regulation of apoptotic processPro-cathepsin HHomo sapiens (human)
surfactant homeostasisPro-cathepsin HHomo sapiens (human)
positive regulation of angiogenesisPro-cathepsin HHomo sapiens (human)
dichotomous subdivision of terminal units involved in lung branchingPro-cathepsin HHomo sapiens (human)
ERK1 and ERK2 cascadePro-cathepsin HHomo sapiens (human)
cellular response to thyroid hormone stimulusPro-cathepsin HHomo sapiens (human)
positive regulation of apoptotic signaling pathwayPro-cathepsin HHomo sapiens (human)
proteolysis involved in protein catabolic processPro-cathepsin HHomo sapiens (human)
immune responsePro-cathepsin HHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
cysteine-type endopeptidase activityCathepsin L2Homo sapiens (human)
serine-type endopeptidase activityCathepsin L2Homo sapiens (human)
protein bindingCathepsin L2Homo sapiens (human)
cysteine-type peptidase activityCathepsin L2Homo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processCathepsin L2Homo sapiens (human)
fibronectin bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityProcathepsin LHomo sapiens (human)
protein bindingProcathepsin LHomo sapiens (human)
collagen bindingProcathepsin LHomo sapiens (human)
cysteine-type peptidase activityProcathepsin LHomo sapiens (human)
histone bindingProcathepsin LHomo sapiens (human)
proteoglycan bindingProcathepsin LHomo sapiens (human)
serpin family protein bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityCathepsin BHomo sapiens (human)
protein bindingCathepsin BHomo sapiens (human)
collagen bindingCathepsin BHomo sapiens (human)
peptidase activityCathepsin BHomo sapiens (human)
cysteine-type peptidase activityCathepsin BHomo sapiens (human)
proteoglycan bindingCathepsin BHomo sapiens (human)
endopeptidase activityPro-cathepsin HHomo sapiens (human)
aminopeptidase activityPro-cathepsin HHomo sapiens (human)
cysteine-type endopeptidase activityPro-cathepsin HHomo sapiens (human)
serine-type endopeptidase activityPro-cathepsin HHomo sapiens (human)
protein bindingPro-cathepsin HHomo sapiens (human)
peptidase activityPro-cathepsin HHomo sapiens (human)
cysteine-type peptidase activityPro-cathepsin HHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processPro-cathepsin HHomo sapiens (human)
HLA-A specific activating MHC class I receptor activityPro-cathepsin HHomo sapiens (human)
thyroid hormone bindingPro-cathepsin HHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
extracellular regionCathepsin L2Homo sapiens (human)
lysosomal lumenCathepsin L2Homo sapiens (human)
extracellular spaceCathepsin L2Homo sapiens (human)
lysosomeCathepsin L2Homo sapiens (human)
extracellular regionProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
nucleusProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
multivesicular bodyProcathepsin LHomo sapiens (human)
Golgi apparatusProcathepsin LHomo sapiens (human)
plasma membraneProcathepsin LHomo sapiens (human)
apical plasma membraneProcathepsin LHomo sapiens (human)
endolysosome lumenProcathepsin LHomo sapiens (human)
chromaffin granuleProcathepsin LHomo sapiens (human)
lysosomal lumenProcathepsin LHomo sapiens (human)
intracellular membrane-bounded organelleProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixProcathepsin LHomo sapiens (human)
extracellular exosomeProcathepsin LHomo sapiens (human)
endocytic vesicle lumenProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular regionCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
external side of plasma membraneCathepsin BHomo sapiens (human)
apical plasma membraneCathepsin BHomo sapiens (human)
endolysosome lumenCathepsin BHomo sapiens (human)
melanosomeCathepsin BHomo sapiens (human)
perinuclear region of cytoplasmCathepsin BHomo sapiens (human)
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular exosomeCathepsin BHomo sapiens (human)
peptidase inhibitor complexCathepsin BHomo sapiens (human)
ficolin-1-rich granule lumenCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
extracellular regionPro-cathepsin HHomo sapiens (human)
extracellular spacePro-cathepsin HHomo sapiens (human)
lysosomePro-cathepsin HHomo sapiens (human)
cytosolPro-cathepsin HHomo sapiens (human)
secretory granule lumenPro-cathepsin HHomo sapiens (human)
cytoplasmic ribonucleoprotein granulePro-cathepsin HHomo sapiens (human)
intracellular membrane-bounded organellePro-cathepsin HHomo sapiens (human)
collagen-containing extracellular matrixPro-cathepsin HHomo sapiens (human)
extracellular exosomePro-cathepsin HHomo sapiens (human)
alveolar lamellar bodyPro-cathepsin HHomo sapiens (human)
multivesicular body lumenPro-cathepsin HHomo sapiens (human)
tertiary granule lumenPro-cathepsin HHomo sapiens (human)
ficolin-1-rich granule lumenPro-cathepsin HHomo sapiens (human)
extracellular spacePro-cathepsin HHomo sapiens (human)
lysosomePro-cathepsin HHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (81)

Assay IDTitleYearJournalArticle
AID1063748Inhibition of recombinant human Cathepsin L using Z-Phe-Arg-aminomethylcoumarin as substrate2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1898769Inhibition of recombinant human Cathepsin B in African green monkey Vero E6 using Z-Phe-Arg-AMC as substrate for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1405437Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156A novel Anti-Cancer Stem Cells compound optimized from the natural symplostatin 4 scaffold inhibits Wnt/β-catenin signaling pathway.
AID1063734Irreversible inhibition of recombinant human Cathepsin L using Z-Phe-Arg-aminomethylcoumarin as substrate assessed as residual activity at 10 fold IC50 preincubated for 30 mins followed by 100 fold dilution measured for 2 hrs by fluorescence assay2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1063749Inhibition of recombinant human Cathepsin L assessed as inhibition of activity-based probe DCG-04 labelling preincubated for 30 mins followed by DCG-04 addition measured after 30 mins2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1898770Inhibition of recombinant human Cathepsin B expressed in African green monkey Vero E6 using Z-Phe-Arg-AMC as substrate followed by CA-074 addition incubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID423033Cytotoxicity against human NCI-H460 cells at 16.9 uM2009Journal of natural products, Jan, Volume: 72, Issue:1
Antimalarial peptides from marine cyanobacteria: isolation and structural elucidation of gallinamide A.
AID1405436Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156A novel Anti-Cancer Stem Cells compound optimized from the natural symplostatin 4 scaffold inhibits Wnt/β-catenin signaling pathway.
AID1898752Inhibition of human recombinant Cathepsin S assessed remaining activity using Z-FR-AMC as substrate incubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1063743Inhibition of human Cathepsin B using Z-Phe-Arg-aminomethylcoumarin as substrate preincubated for 30 mins followed by substrate addition2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1898758Inhibition of human recombinant Cathepsin L assessed as Apparent inhibition constant using Z-FR-AMC as substrate inubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1405434Antiproliferative activity against mouse 4T1 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156A novel Anti-Cancer Stem Cells compound optimized from the natural symplostatin 4 scaffold inhibits Wnt/β-catenin signaling pathway.
AID1526363Inhibition of human cathepsin L assessed as Kinact /Ki ratio using fluorogenic substrate cbz-FR-AMC monitored for 90 to 120 mins by spectrophotometry
AID1171534Inhibition of FP1 in Plasmodium falciparum trophozoite stage after 1 hr by SDS-PAGE analysis2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials.
AID1526369Cytotoxicity in mouse C2C12 cells assessed as reduction in cell viability incubated for 3 days
AID1898751Inhibition of human recombinant Cathepsin V assessed remaining activity using Z-FR-AMC as substrate incubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898761Inhibition of human recombinant Cathepsin L assessed as ratio of Kinact/Kiapp using Z-FR-AMC as substrate inubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID423031Antileishmanial activity against Leishmania donovani2009Journal of natural products, Jan, Volume: 72, Issue:1
Antimalarial peptides from marine cyanobacteria: isolation and structural elucidation of gallinamide A.
AID1063740Selectivity index, ratio of IC50 for human Cathepsin V to IC50 for recombinant human Cathepsin L using Z-Phe-Arg-aminomethylcoumarin as substrate2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1898768Inhibition of SARS-CoV-2 PLpro at 10 uM assessed as remaining activity using Z-RLRGG-AMC as substrate at 10 uM incubated for 15 mins followed by substrate addition by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898764Cytotoxicity against cells African green monkey Vero E6 cells incubated for 24 to 72 hrs by alamar blue assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1902912Inhibition of Trypanosoma cruzi cruzain using Z-FR-AMC as substrate preincubated for 10 mins followed by substrate addition by fluorimetric analysis2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Intramolecular Interactions Enhance the Potency of Gallinamide A Analogues against
AID1526367Antitrypanosomal activity against Trypanosoma cruzi amastigote stage forms infected in mouse C2C12 cells incubated for 3 days by 4',6-diamidino-2-phenylindole staining based microscopy
AID1405430Antiproliferative activity against human HeLa cells2018European journal of medicinal chemistry, Aug-05, Volume: 156A novel Anti-Cancer Stem Cells compound optimized from the natural symplostatin 4 scaffold inhibits Wnt/β-catenin signaling pathway.
AID1898759Inhibition of human recombinant Cathepsin B assessed as Apparent inhibition constant using Z-FR-AMC as substrate inubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898781Inhibition of recombinant human Cathepsin L in African green monkey Vero E6 at 20 uM using Z-Phe-Arg-AMC as substrate for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898763Inhibition of mouse Cathepsin L assessed as ratio of Kinact/Kiapp using Z-FR-AMC as substrate inubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1405431Antiproliferative activity against human HT-29 cells2018European journal of medicinal chemistry, Aug-05, Volume: 156A novel Anti-Cancer Stem Cells compound optimized from the natural symplostatin 4 scaffold inhibits Wnt/β-catenin signaling pathway.
AID1063739Selectivity index, ratio of IC50 for human Cathepsin V to IC50 for recombinant human Cathepsin L using Z-Phe-Arg-aminomethylcoumarin as substrate preincubated for 30 mins followed by substrate addition2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1898777Inhibition of recombinant human furin assessed as remaining activity at 50 uM using pERTKR-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1171537Inhibition of FP3 in Plasmodium falciparum trophozoite stage after 1 hr by SDS-PAGE analysis2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials.
AID1898750Inhibition of human recombinant Cathepsin B assessed remaining activity using Z-FR-AMC as substrate incubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898754Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as inhibition of viral infection pre incubated for 30 minutes followed by viral infection and measured after 72 hrs by Nucblue dye based fluorometric analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1063742Inhibition of human Cathepsin H using Arg-aminomethylcoumarin as substrate2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1405433Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156A novel Anti-Cancer Stem Cells compound optimized from the natural symplostatin 4 scaffold inhibits Wnt/β-catenin signaling pathway.
AID1898748Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as inhibition of viral entry at 0.5 uM for >= 60 mins post infection by Alexa Fluor 488 and Hoechst dye based fluorescence microscopy2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898767Inhibition of SARS-CoV-2 main protease assessed as remaining activity using Mu-HSSKLQ-AMC as substrate at 10 uM incubated for 15 mins followed by substrate addition by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID423029Antimalarial activity against chloroquine-resistant Plasmodium falciparum W22009Journal of natural products, Jan, Volume: 72, Issue:1
Antimalarial peptides from marine cyanobacteria: isolation and structural elucidation of gallinamide A.
AID1526365Irreversible inhibition of human cathepsin L assessed as residual enzyme activity using fluorogenic substrate cbz-FR-AMC incubated for 30 mins followed by 100 fold dilution and measured after 1 hrs by spectrophotometry
AID1898765Anti viral activity against SARS-CoV-2 infected in African green monkey veroE6 assessed as reduction in viral load2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID423030Cytotoxicity against african green monkey Vero cells2009Journal of natural products, Jan, Volume: 72, Issue:1
Antimalarial peptides from marine cyanobacteria: isolation and structural elucidation of gallinamide A.
AID1898780Inhibition of recombinant human TMPRSS2 assessed as remaining activity at 50 uM using Boc-QAR-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID423034Cytotoxicity against mouse Neuro2a cells at 16.9 uM2009Journal of natural products, Jan, Volume: 72, Issue:1
Antimalarial peptides from marine cyanobacteria: isolation and structural elucidation of gallinamide A.
AID1898762Inhibition of human recombinant Cathepsin B assessed as ratio of Kinact/Kiapp using Z-FR-AMC as substrate inubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1063741Inhibition of human Cathepsin H using Arg-aminomethylcoumarin as substrate preincubated for 30 mins followed by substrate addition2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1902914Cytotoxicity against mouse C2C12 cells assessed as lethal dose2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Intramolecular Interactions Enhance the Potency of Gallinamide A Analogues against
AID1063737Selectivity index, ratio of IC50 for human Cathepsin B to IC50 for recombinant human Cathepsin L after 30 mins using Z-Phe-Arg-aminomethylcoumarin as substrate preincubated for 30 mins followed by substrate addition2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1898766Antiviral activity against SARS-CoV-2 infected in human A549 cells overexpressing ACE2 assessed as reduction in virus-induced cytopathic effect at 625 nM incubated for 1 hr followed by viral infection measured after 96 hrs by inverted microscopy2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898779Antiviral activity against SARS-CoV-2 infected in human MRC5 cells expressing ACE2/TMPRSS2 assessed as inhibition of viral entry at 32 uM2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1063738Selectivity index, ratio of IC50 for human Cathepsin B to IC50 for recombinant human Cathepsin L using Z-Phe-Arg-aminomethylcoumarin as substrate2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1898776Binding affinity to Cathepsin L in African green monkey VeroE6 cell lysates assessed as covalent adducts by quantitative mass spectrometry2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1526368Inhibition of recombinant Trypanosoma cruzi Cruzain expressed in Pichia pastoris using Z-Phe-Arg-AMC substrate incubated for 30 mins by fluorescence based assay
AID1526364Irreversible inhibition of human cathepsin L assessed as residual enzyme activity using fluorogenic substrate cbz-FR-AMC incubated for 30 mins followed by 100 fold dilution and measured after 2 hrs by spectrophotometry
AID1063744Inhibition of human Cathepsin B using Z-Phe-Arg-aminomethylcoumarin as substrate2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1405435Antiproliferative activity against human A375 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156A novel Anti-Cancer Stem Cells compound optimized from the natural symplostatin 4 scaffold inhibits Wnt/β-catenin signaling pathway.
AID1898755Inhibition of human recombinant Cathepsin L assessed as Kinact using Z-FR-AMC as substrate inubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898756Inhibition of human recombinant Cathepsin B assessed as Kinact using Z-FR-AMC as substrate inubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1526361Inhibition of human cathepsin L using fluorogenic substrate cbz-FR-AMC monitored for 90 to 120 mins by spectrophotometry
AID1526360Inhibition of human cathepsin L
AID1898783Synergistic antiviral activity against SARS-CoV-2 infected in human HEK293 cells expressing TMPRSS2 as inhibition of viral entry in presence of Na-famostat mesylate2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1171533Antiplasmodial activity against Plasmodium falciparum 3D72014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials.
AID1063735Irreversible inhibition of recombinant human Cathepsin L using Z-Phe-Arg-aminomethylcoumarin as substrate assessed as residual activity at 10 fold IC50 preincubated for 30 mins followed by 100 fold dilution measured immediately after dilution by fluoresce2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1063746Inhibition of human Cathepsin V using Z-Phe-Arg-aminomethylcoumarin as substrate2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1171535Inhibition of FP2 in Plasmodium falciparum trophozoite stage after 1 hr by SDS-PAGE analysis2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials.
AID1898775Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as inhibition of viral entry at 0.5 uM pretreated for 30 mins with cells followed by viral infection and measured after 24 hrs post infection by Alexa Fluor 488 2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898782Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as inhibition of viral entry at 0.5 uM and measured after 24 hrs post infection by Alexa Fluor 488 and Hoechst dye based fluorescence microscopy2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898774Antiviral activity against SARS-CoV-2 infected in human HEK293 cells expressing TMPRSS2 as inhibition of viral entry2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898749Inhibition of human recombinant Cathepsin L assessed remaining activity using Z-FR-AMC as substrate incubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898757Inhibition of mouse Cathepsin L assessed as Kinact using Z-FR-AMC as substrate inubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1405432Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156A novel Anti-Cancer Stem Cells compound optimized from the natural symplostatin 4 scaffold inhibits Wnt/β-catenin signaling pathway.
AID1063745Inhibition of human Cathepsin V using Z-Phe-Arg-aminomethylcoumarin as substrate preincubated for 30 mins followed by substrate addition2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1171536Inhibition of FP2' in Plasmodium falciparum trophozoite stage after 1 hr by SDS-PAGE analysis2014Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials.
AID1063747Inhibition of recombinant human Cathepsin L using Z-Phe-Arg-aminomethylcoumarin as substrate preincubated for 30 mins followed by substrate addition2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID423032Antitrypanosomal activity against Trypanosoma cruzi at 16.9 uM2009Journal of natural products, Jan, Volume: 72, Issue:1
Antimalarial peptides from marine cyanobacteria: isolation and structural elucidation of gallinamide A.
AID1898771Inhibition of recombinant human Cathepsin B expressed in huamn A549 using Z-Phe-Arg-AMC as substrate incubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898753Inhibition of human recombinant Cathepsin K assessed remaining activity using Z-FR-AMC as substrate incubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1405438Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156A novel Anti-Cancer Stem Cells compound optimized from the natural symplostatin 4 scaffold inhibits Wnt/β-catenin signaling pathway.
AID1898773Antiviral activity against SARS-CoV-2 infected in African Green monkey Vero E6 cells expressing TMPRSS2 as inhibition of viral entry2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1898760Inhibition of mouse Cathepsin L assessed as Apparent inhibition constant using Z-FR-AMC as substrate inubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
AID1063736Irreversible inhibition of recombinant human cathepsin L using Z-Phe-Arg-aminomethylcoumarin as substrate2014Journal of natural products, Jan-24, Volume: 77, Issue:1
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
AID1898772Inhibition of recombinant human Cathepsin B expressed in human A549 using Z-Phe-Arg-AMC as substrate followed by CA-074 addition incubated for 30 mins by fluorometric assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (14.29)29.6817
2010's9 (64.29)24.3611
2020's3 (21.43)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.83

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

MetricThis Compound (vs All)
Research Demand Index19.83 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index4.90 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.83)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]