Page last updated: 2024-10-15

cyclic guanosine monophosphate-adenosine monophosphate

Description

c-GMP-AMP : A cyclic purine dinucleotide that consists of AMP and GMP units cyclised via 3',5'-linkages. [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]

2'-3'-cGAMP : A cyclic purine dinucleotide that consists of AMP and GMP units cyclised via 3',5'- and 2',5'-linkages respectively. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID135471108
CHEMBL ID4449584
CHEBI ID71580
SCHEMBL ID19940046
MeSH IDM0588853
PubMed CID135564529
CHEMBL ID4465054
CHEBI ID75947
SCHEMBL ID17325409
SCHEMBL ID24649405
MeSH IDM0588853

Synonyms (72)

Synonym
cgamp
3',5'-cyclic gmp-amp
2-amino-9-[(2r,3r,3as,7ar,9r,10r,10as,14ar)-9-(6-amino-9h-purin-9-yl)-3,5,10,12-tetrahydroxy-5,12-dioxidooctahydro-2h,7h-difuro[3,2-d:3',2'-j][1,3,7,9,2,8]tetraoxadiphosphacyclododecin-2-yl]-1,9-dihydro-6h-purin-6-one
CHEBI:71580
c-gmp-amp
3',3'-cgamp
c[g(3',5')pa(3',5')p]
3'3'-cyclic guanosine monophosphate-adenosine monophosphate
CS-3892
4bw ,
2-amino-9-[(2r,3r,3as,5r,7ar,9r,10r,10as,12r,14ar)-9-(6-amino-9h-purin-9-yl)-3,5,10,12-tetrahydroxy-5,12-dioxidooctahydro-2h,7h-difuro[3,2-d:3',2'-j][1,3,7,9,2,8]tetraoxadiphosphacyclododecin-2-yl]-1,9-dihydro-6h-purin-6-one
HY-12512
AKOS030526925
849214-04-6
CHEMBL4449584 ,
SCHEMBL19940046
2-amino-9-((2r,3r,3as,7ar,9r,10r,10as,14ar)-9-(6-amino-9h-purin-9-yl)-3,5,10,12-tetrahydroxy-5,12-dioxidooctahydro-2h,7h-difuro[3,2-d:3',2'-j][1,3,7,9]tetraoxa[2,8]diphosphacyclododecin-2-yl)-3,9-dihydro-6h-purin-6-one
3',3' cgamp; c-gmp-amp; c[g(3',5')pa(3',5')p]
2-amino-9-[(1s,6r,8r,9r,10s,15r,17r,18r)-17-(6-aminopurin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1h-purin-6-one
Q27139728
EX-A2911
cgamp; c-gpap
C76713
bdbm50509401
DTXSID401045334
1sy ,
2',3'-cgamp
cgamp(2'-5')
cyclic gp(2'-5')ap(3'-5')
C20640 ,
cyclic guanosine monophosphate-adenosine monophosphate
c[g(2',5')pa(3',5')p]
CHEBI:75947 ,
2'-3'-cgamp
1441190-66-4
2-amino-9-[(5r,7r,8r,12ar,14r,15r,15as,16r)-14-(6-amino-9h-purin-9-yl)-2,10,15,16-tetrahydroxy-2,10-dioxidooctahydro-12h-5,8-methanofuro[3,2-l][1,3,6,9,11,2,10]pentaoxadiphosphacyclotetradecin-7-yl]-1,9-dihydro-6h-purin-6-one
cyclic (guanosine-(2'->5')-monophosphate-adenosine-(3'->5')-monophosphate)
2'-o,5'-o-[(adenosine-3'-o,5'-o-diyl)bisphosphinico]guanosine
2',5'-3',5'-cgamp
2'3'-cyclic guanosine monophosphate-adenosine monophosphate
SCHEMBL17325409
c(g(2',5')pa(3',5')p)
j3.180.146j ,
unii-552y49k43e
552y49k43e ,
2'-o,5'-o-((adenosine-3'-o,5'-o-diyl)bisphosphinico)guanosine
2'-guanylic acid, adenylyl-(3'->5')-, cyclic nucleotide
2-amino-9-((5r,7r,8r,12ar,14r,15r,15as,16r)-14-(6-amino-9h-purin-9-yl)-2,10,15,16-tetrahydroxy-2,10-dioxidooctahydro-12h-5,8-methanofuro(3,2-l)(1,3,6,9,11,2,10)pentaoxadiphosphacyclotetradecin-7-yl)-1,9-dihydro-6h-purin-6-one
2-amino-9-((2r,5r,7r,8r,10s,12ar,14r,15r,15as,16r)-14-(6-amino-9h-purin-9-yl)-2,10,15,16-tetrahydroxy-2,10-dioxidooctahydro-12h-5,8-methanofuro(3,2-l)(1,3,6,9,11,2,10)pentaoxadiphosphacyclotetradecin-7-yl)-3,9-dihydro-6h-purin-6-one
2-amino-9-((1r,6r,8r,9r,10s,15r,17r,18r)-8-(6-amino-9h-purin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxido-2,4,7,11,13,16-hexaoxa-3,12-diphosphatricyclo(13.2.1.06,10)octadec-17-yl)-1,9-dihydro-6h-purin-6-one
6h-purin-6-one, 2-amino-9-((5r,7r,8r,12ar,14r,15r,15as,16r)-14-(6-amino-9h-purin-9-yl)octahydro-2,10,15,16-tetrahydroxy-2,10-dioxido-5,8-methano-12h-furo(3,2-l)-1,3,6,9,11,2,10-pentaoxadiphosphacyclot etradecin-7-yl)-1,9-dihydro-
5'-o,2'-o-(3',5'-dideoxyadenosine-3',5'-diylbis(oxy(hydroxyphosphinylidene)))guanosine
2'3'-cgamp
AC-33623
cyclic [g(2',5')pa(3',5')p]
gtpl9207
CHEMBL4465054 ,
bdbm50506263
2',3'-cgamp sodium salt, >=98% (hplc)
2',3' cgamp; c-gmp-amp; c[g(2',5')pa(3',5')p]
2-amino-9-[(2r,5r,7r,8r,10s,12ar,14r,15r,15as,16r)-14-(6-amino-9h-purin-9-yl)-2,10,15,16-tetrahydroxy-2,10-dioxidooctahydro-12h-5,8-methanofuro[3,2-l][1,3,6,9,11,2,10]pentaoxadiphosphacyclotetradecin-7-yl]-3,9-dihydro-6h-purin-6-one
Q17143195
SCHEMBL24649405
2-amino-9-[(1r,6r,8r,9r,10s,15r,17r,18r)-8-(6-aminopurin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1h-purin-6-one
2-amino-9-[(1r,6r,8r,9r,10s,15r,17r,18r)-8-(6-amino-9h-purin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxido-2,4,7,11,13,16-hexaoxa-3,12-diphosphatricyclo[13.2.1.06,10]octadec-17-yl]-1,9-dihydro-6h-purin-6-one
A901660
2/'3/'-cgamp
2-3-cgamp
2'-3'-cyclic gmp-amp;2',3'-cgamp
PD039600
(1r,6r,8r,9r,10s,15r,17r,18r)-17-(2-amino-6-oxo-6,9-dihydro-1h-purin-9-yl)-8-(6-amino-9h-purin-9-yl)-3,9,12,18-tetrahydroxy-2,4,7,11,13,16-hexaoxa-3,12-diphosphatricyclo[13.2.1.0,octadecane-3,12-dione
AKOS040732256

Bioavailability

ExcerptReference
" The orally bioavailable modulators of gap junctions meclofenamate and tonabersat break this paracrine loop, and we provide proof-of-principle that these drugs could be used to treat established brain metastasis."( Carcinoma-astrocyte gap junctions promote brain metastasis by cGAMP transfer.
Boire, A; Chen, Q; Cross, JR; Er, EE; Jacob, L; Jin, X; Lopez-Soto, A; Massagué, J; Patwa, R; Shah, H; Valiente, M; Xu, K, 2016
)
" However, natural CDNs are hydrophilic small molecules with negative charges and are susceptible to enzymatic degradation, leading to low bioavailability in target tissues yet unwanted toxicities and narrow therapeutic windows."( STING activation in cancer immunotherapy.
Lin, S; Su, T; Valerie, K; Wang, XY; Zhang, Y; Zhu, G, 2019
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (3)

ClassDescription
adenyl ribonucleotideA purine riboncleotide where adenine is the purine.
cyclic purine dinucleotide
guanyl ribonucleotideA purine ribonucleotide where the purine is guanine.
cyclic purine dinucleotide
guanyl ribonucleotideA purine ribonucleotide where the purine is guanine.
adenyl ribonucleotideA purine riboncleotide where adenine is the purine.
[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]

Pathways (3)

PathwayProteinsCompounds
Cytosolic DNA-sensing pathway01
STING pathway in Kawasaki-like disease and COVID-1904
Mitochondrial immune response to SARS-CoV-285

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Stimulator of interferon genes proteinHomo sapiens (human)IC50 (µMol)0.00360.00180.00360.0055AID1528522; AID1905855
[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)
Stimulator of interferon genes proteinMus musculus (house mouse)EC50 (µMol)0.02000.02000.02000.0200AID1575508
Stimulator of interferon genes proteinHomo sapiens (human)EC50 (µMol)50.43090.00581.36117.2000AID1541395; AID1541396; AID1541397; AID1541399; AID1541400; AID1814337; AID1814342; AID1814344; AID1814346; AID1814347; AID1852608; AID1852613
Stimulator of interferon genes proteinHomo sapiens (human)Kd0.78100.00381.31315.2000AID1546606; AID1575505; AID1575507; AID1861452
Stimulator of interferon genes proteinMus musculus (house mouse)EC50 (µMol)18.80000.02000.02000.0200AID1714249
Stimulator of interferon genes proteinMus musculus (house mouse)Kd0.00000.00001.42253.5000AID1905864
Stimulator of interferon genes proteinHomo sapiens (human)EC50 (µMol)13.09840.00581.36117.2000AID1528518; AID1541395; AID1541396; AID1541397; AID1541399; AID1541400; AID1714251; AID1714253; AID1714255; AID1749739; AID1816900; AID1852608; AID1852613; AID1861453; AID1905663
Stimulator of interferon genes proteinHomo sapiens (human)Kd9.16080.00381.31315.2000AID1546606; AID1575505; AID1575509; AID1861452; AID1905860
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
protein complex oligomerizationStimulator of interferon genes proteinHomo sapiens (human)
autophagosome assemblyStimulator of interferon genes proteinHomo sapiens (human)
activation of innate immune responseStimulator of interferon genes proteinHomo sapiens (human)
pattern recognition receptor signaling pathwayStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of defense response to virus by hostStimulator of interferon genes proteinHomo sapiens (human)
cytoplasmic pattern recognition receptor signaling pathwayStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of macroautophagyStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of protein bindingStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of type I interferon productionStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of interferon-beta productionStimulator of interferon genes proteinHomo sapiens (human)
cellular response to interferon-betaStimulator of interferon genes proteinHomo sapiens (human)
innate immune responseStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIStimulator of interferon genes proteinHomo sapiens (human)
regulation of inflammatory responseStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityStimulator of interferon genes proteinHomo sapiens (human)
protein complex oligomerizationStimulator of interferon genes proteinHomo sapiens (human)
defense response to virusStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of type I interferon-mediated signaling pathwayStimulator of interferon genes proteinHomo sapiens (human)
reticulophagyStimulator of interferon genes proteinHomo sapiens (human)
protein localization to endoplasmic reticulumStimulator of interferon genes proteinHomo sapiens (human)
cellular response to exogenous dsRNAStimulator of interferon genes proteinHomo sapiens (human)
cellular response to organic cyclic compoundStimulator of interferon genes proteinHomo sapiens (human)
antiviral innate immune responseStimulator of interferon genes proteinHomo sapiens (human)
cGAS/STING signaling pathwayStimulator of interferon genes proteinHomo sapiens (human)
proton transmembrane transportStimulator of interferon genes proteinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIInterferon regulatory factor 3Homo sapiens (human)
cytoplasmic pattern recognition receptor signaling pathwayInterferon regulatory factor 3Homo sapiens (human)
apoptotic processInterferon regulatory factor 3Homo sapiens (human)
DNA damage responseInterferon regulatory factor 3Homo sapiens (human)
signal transduction involved in regulation of gene expressionInterferon regulatory factor 3Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayInterferon regulatory factor 3Homo sapiens (human)
positive regulation of type I interferon productionInterferon regulatory factor 3Homo sapiens (human)
positive regulation of interferon-alpha productionInterferon regulatory factor 3Homo sapiens (human)
positive regulation of interferon-beta productionInterferon regulatory factor 3Homo sapiens (human)
toll-like receptor 4 signaling pathwayInterferon regulatory factor 3Homo sapiens (human)
TRIF-dependent toll-like receptor signaling pathwayInterferon regulatory factor 3Homo sapiens (human)
MDA-5 signaling pathwayInterferon regulatory factor 3Homo sapiens (human)
regulation of apoptotic processInterferon regulatory factor 3Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionInterferon regulatory factor 3Homo sapiens (human)
innate immune responseInterferon regulatory factor 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon regulatory factor 3Homo sapiens (human)
regulation of inflammatory responseInterferon regulatory factor 3Homo sapiens (human)
defense response to virusInterferon regulatory factor 3Homo sapiens (human)
type I interferon-mediated signaling pathwayInterferon regulatory factor 3Homo sapiens (human)
positive regulation of type I interferon-mediated signaling pathwayInterferon regulatory factor 3Homo sapiens (human)
cellular response to exogenous dsRNAInterferon regulatory factor 3Homo sapiens (human)
macrophage apoptotic processInterferon regulatory factor 3Homo sapiens (human)
programmed necrotic cell deathInterferon regulatory factor 3Homo sapiens (human)
cellular response to virusInterferon regulatory factor 3Homo sapiens (human)
cGAS/STING signaling pathwayInterferon regulatory factor 3Homo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseInterferon regulatory factor 3Homo sapiens (human)
regulation of transcription by RNA polymerase IIInterferon regulatory factor 3Homo sapiens (human)
immune system processInterferon regulatory factor 3Homo sapiens (human)
protein complex oligomerizationStimulator of interferon genes proteinHomo sapiens (human)
autophagosome assemblyStimulator of interferon genes proteinHomo sapiens (human)
activation of innate immune responseStimulator of interferon genes proteinHomo sapiens (human)
pattern recognition receptor signaling pathwayStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of defense response to virus by hostStimulator of interferon genes proteinHomo sapiens (human)
cytoplasmic pattern recognition receptor signaling pathwayStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of macroautophagyStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of protein bindingStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of type I interferon productionStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of interferon-beta productionStimulator of interferon genes proteinHomo sapiens (human)
cellular response to interferon-betaStimulator of interferon genes proteinHomo sapiens (human)
innate immune responseStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIStimulator of interferon genes proteinHomo sapiens (human)
regulation of inflammatory responseStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityStimulator of interferon genes proteinHomo sapiens (human)
protein complex oligomerizationStimulator of interferon genes proteinHomo sapiens (human)
defense response to virusStimulator of interferon genes proteinHomo sapiens (human)
positive regulation of type I interferon-mediated signaling pathwayStimulator of interferon genes proteinHomo sapiens (human)
reticulophagyStimulator of interferon genes proteinHomo sapiens (human)
protein localization to endoplasmic reticulumStimulator of interferon genes proteinHomo sapiens (human)
cellular response to exogenous dsRNAStimulator of interferon genes proteinHomo sapiens (human)
cellular response to organic cyclic compoundStimulator of interferon genes proteinHomo sapiens (human)
antiviral innate immune responseStimulator of interferon genes proteinHomo sapiens (human)
cGAS/STING signaling pathwayStimulator of interferon genes proteinHomo sapiens (human)
proton transmembrane transportStimulator of interferon genes proteinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
protein bindingStimulator of interferon genes proteinHomo sapiens (human)
proton channel activityStimulator of interferon genes proteinHomo sapiens (human)
protein kinase bindingStimulator of interferon genes proteinHomo sapiens (human)
ubiquitin protein ligase bindingStimulator of interferon genes proteinHomo sapiens (human)
cyclic-di-GMP bindingStimulator of interferon genes proteinHomo sapiens (human)
signaling adaptor activityStimulator of interferon genes proteinHomo sapiens (human)
identical protein bindingStimulator of interferon genes proteinHomo sapiens (human)
protein homodimerization activityStimulator of interferon genes proteinHomo sapiens (human)
2',3'-cyclic GMP-AMP bindingStimulator of interferon genes proteinHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingStimulator of interferon genes proteinHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingInterferon regulatory factor 3Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificInterferon regulatory factor 3Homo sapiens (human)
DNA-binding transcription activator activityInterferon regulatory factor 3Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificInterferon regulatory factor 3Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificInterferon regulatory factor 3Homo sapiens (human)
DNA bindingInterferon regulatory factor 3Homo sapiens (human)
DNA-binding transcription factor activityInterferon regulatory factor 3Homo sapiens (human)
protein bindingInterferon regulatory factor 3Homo sapiens (human)
protein domain specific bindingInterferon regulatory factor 3Homo sapiens (human)
identical protein bindingInterferon regulatory factor 3Homo sapiens (human)
protein homodimerization activityInterferon regulatory factor 3Homo sapiens (human)
sequence-specific DNA bindingInterferon regulatory factor 3Homo sapiens (human)
sequence-specific double-stranded DNA bindingInterferon regulatory factor 3Homo sapiens (human)
promoter-specific chromatin bindingInterferon regulatory factor 3Homo sapiens (human)
protein bindingStimulator of interferon genes proteinHomo sapiens (human)
proton channel activityStimulator of interferon genes proteinHomo sapiens (human)
protein kinase bindingStimulator of interferon genes proteinHomo sapiens (human)
ubiquitin protein ligase bindingStimulator of interferon genes proteinHomo sapiens (human)
cyclic-di-GMP bindingStimulator of interferon genes proteinHomo sapiens (human)
signaling adaptor activityStimulator of interferon genes proteinHomo sapiens (human)
identical protein bindingStimulator of interferon genes proteinHomo sapiens (human)
protein homodimerization activityStimulator of interferon genes proteinHomo sapiens (human)
2',3'-cyclic GMP-AMP bindingStimulator of interferon genes proteinHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingStimulator of interferon genes proteinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
Golgi membraneStimulator of interferon genes proteinHomo sapiens (human)
endoplasmic reticulum membraneStimulator of interferon genes proteinHomo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membraneStimulator of interferon genes proteinHomo sapiens (human)
Golgi membraneStimulator of interferon genes proteinHomo sapiens (human)
autophagosome membraneStimulator of interferon genes proteinHomo sapiens (human)
nucleoplasmStimulator of interferon genes proteinHomo sapiens (human)
mitochondrial outer membraneStimulator of interferon genes proteinHomo sapiens (human)
endosomeStimulator of interferon genes proteinHomo sapiens (human)
autophagosomeStimulator of interferon genes proteinHomo sapiens (human)
peroxisomeStimulator of interferon genes proteinHomo sapiens (human)
endoplasmic reticulum membraneStimulator of interferon genes proteinHomo sapiens (human)
cytosolStimulator of interferon genes proteinHomo sapiens (human)
plasma membraneStimulator of interferon genes proteinHomo sapiens (human)
cytoplasmic vesicle membraneStimulator of interferon genes proteinHomo sapiens (human)
secretory granule membraneStimulator of interferon genes proteinHomo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membraneStimulator of interferon genes proteinHomo sapiens (human)
perinuclear region of cytoplasmStimulator of interferon genes proteinHomo sapiens (human)
serine/threonine protein kinase complexStimulator of interferon genes proteinHomo sapiens (human)
STING complexStimulator of interferon genes proteinHomo sapiens (human)
autophagosomeStimulator of interferon genes proteinHomo sapiens (human)
nucleusInterferon regulatory factor 3Homo sapiens (human)
cytoplasmInterferon regulatory factor 3Homo sapiens (human)
nucleusInterferon regulatory factor 3Homo sapiens (human)
nucleoplasmInterferon regulatory factor 3Homo sapiens (human)
cytoplasmInterferon regulatory factor 3Homo sapiens (human)
mitochondrionInterferon regulatory factor 3Homo sapiens (human)
cytosolInterferon regulatory factor 3Homo sapiens (human)
chromatinInterferon regulatory factor 3Homo sapiens (human)
Golgi membraneStimulator of interferon genes proteinHomo sapiens (human)
endoplasmic reticulum membraneStimulator of interferon genes proteinHomo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membraneStimulator of interferon genes proteinHomo sapiens (human)
Golgi membraneStimulator of interferon genes proteinHomo sapiens (human)
autophagosome membraneStimulator of interferon genes proteinHomo sapiens (human)
nucleoplasmStimulator of interferon genes proteinHomo sapiens (human)
mitochondrial outer membraneStimulator of interferon genes proteinHomo sapiens (human)
endosomeStimulator of interferon genes proteinHomo sapiens (human)
autophagosomeStimulator of interferon genes proteinHomo sapiens (human)
peroxisomeStimulator of interferon genes proteinHomo sapiens (human)
endoplasmic reticulum membraneStimulator of interferon genes proteinHomo sapiens (human)
cytosolStimulator of interferon genes proteinHomo sapiens (human)
plasma membraneStimulator of interferon genes proteinHomo sapiens (human)
cytoplasmic vesicle membraneStimulator of interferon genes proteinHomo sapiens (human)
secretory granule membraneStimulator of interferon genes proteinHomo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membraneStimulator of interferon genes proteinHomo sapiens (human)
perinuclear region of cytoplasmStimulator of interferon genes proteinHomo sapiens (human)
serine/threonine protein kinase complexStimulator of interferon genes proteinHomo sapiens (human)
STING complexStimulator of interferon genes proteinHomo sapiens (human)
autophagosomeStimulator of interferon genes proteinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (136)

Assay IDTitleYearJournalArticle
AID1546606Binding affinity to wild type human STING (139 to 379 residues) by ITC assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Targeting Stimulator of Interferon Genes (STING): A Medicinal Chemistry Perspective.
AID1852617Cytotoxicity against human PBMC cells2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1575507Binding affinity to wild type human STING C-terminal domain (139 to 379 residues) expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetric method2019MedChemComm, Dec-01, Volume: 10, Issue:12
Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.
AID1541396Activation of recombinant human wild-type STING expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1852607Binding affinity to human wild type STING assessed as change in melting temperature by differential scanning fluorimetry (DSF) method2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1852616Induction of IFNalpha secretion in human PBMC incubated for 16 hrs2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541402Activation of STING in human PBMC assessed as induction of INFgamma secretion at 12.5 uM incubated for 16 hrs by ProcartaPlex assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1814339Activation of human STING REF mutant expressed in digitonin treated HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation by luciferase reporter gene assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1814349Induction of INF-alpha production in healthy human PBMC incubated for 16 hrs2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1852610Agonist activity at human STING REF expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1861452Agonist activity at wild type human STING C-terminal domain (139 to 379 residues) assessed as dissociation constant by isothermal titration calorimetry analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration.
AID1575508Inhibition of STING in mouse L929 cells assessed as reduction in cGAMP induce IFNbeta expression measured after 4 hrs by qRT-PCR2019MedChemComm, Dec-01, Volume: 10, Issue:12
Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.
AID1814342Activation of wild-type human STING expressed in HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation measured after 30 mins by luciferase reporter gene assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1852614Induction of IFNgamma secretion in human PBMC incubated for 16 hrs2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541400Activation of recombinant human STING haplotype R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541395Activation of recombinant human wild-type STING expressed in 293T cells incubated for 7 hrs in absence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1814340Activation of human STING QA mutant expressed in digitonin treated HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation by luciferase reporter gene assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1541411Cytotoxicity against human PBMC-derived CD3-positive T cells assessed as effect on cell viability at 12.5 uM incubated for 16 hrs by Zombie-NIR staining-based flow cytometry2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541398Activation of recombinant human STING haplotype R232H mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541403Activation of STING in human PBMC assessed as induction of TNFalpha secretion at 12.5 uM incubated for 16 hrs by ProcartaPlex assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1814341Activation of human STING Q mutant expressed in digitonin treated HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation by luciferase reporter gene assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1541409Activation of recombinant human STING haplotype G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1814346Activation of wild-type human STING expressed in digitonin treated human THP1-Dual cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation measured after 30 mins by luciferase reporter gene assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1852608Agonist activity at human wild type STING expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541394Binding affinity to recombinant human wild-type STING assessed as change in melting temperature at 150 uM by SYPRO orange dye based differential scanning fluorimetric method2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1814347Activation of wild-type human STING expressed in human THP1-Dual cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation measured after 7 hrs by luciferase reporter gene assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1814344Activation of wild-type human STING expressed in HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation measured after 7 hrs by luciferase reporter gene assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1861454Agonist activity at human STING H232 variant assessed as dissociation constant2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration.
AID1814353Induction of TNF-alpha production in healthy human PBMC incubated for 16 hrs2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1814351Induction of INF-gamma production in healthy human PBMC incubated for 16 hrs2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1541405Ratio of EC50 for recombinant human wild-type STING expressed in 293T cells in absence of digitonin A to EC50 for recombinant human wild-type STING expressed in 293T cells in presence of digitonin A2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541399Activation of recombinant human STING haplotype G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1852609Agonist activity at human STING HAQ expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541407Activation of recombinant human STING haplotype R71H/G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541406Activation of recombinant human wild-type STING expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541408Activation of recombinant human STING haplotype R232H mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541401Cytotoxicity against human PBMC-derived monocytes assessed as CD3-negative CD14 positive monocyte viability at 12.5 uM incubated for 16 hrs by Zombie-NIR staining-based flow cytometry relative to control2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1546605Binding affinity to human STING H232 mutant by ITC assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Targeting Stimulator of Interferon Genes (STING): A Medicinal Chemistry Perspective.
AID1814338Activation of human STING HAQ mutant expressed in digitonin treated HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation by luciferase reporter gene assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1575505Binding affinity to human STING expressed in Escherichia coli by isothermal titration calorimetric method2019MedChemComm, Dec-01, Volume: 10, Issue:12
Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.
AID1852613Agonist activity at human wild type full length STING expressed in 293T cells incubated for 7 hrs by luciferase/cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541410Activation of recombinant human STING haplotype R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541387Activation of STING in human PBMC assessed as induction of INFalpha secretion at 12.5 uM incubated for 16 hrs by ProcartaPlex assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1852615Induction of TNFalpha secretion in human PBMC incubated for 16 hrs2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1814337Activation of wild-type human STING expressed in digitonin treated HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation by luciferase reporter gene assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING Agonist 3',3'-c-Di(2'F,2'dAMP).
AID1852612Agonist activity at human STING Q expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1852611Agonist activity at human STING AQ expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541397Activation of recombinant human STING haplotype R71H/G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1905863Binding affinity to human STING HAQ variant assessed as half life by Surface plasmon resonance assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1528528Agonist activity at STING in human PBMC cells assessed as increase in IL6 production at 139 uM measured after 4 hrs by ELISA2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1528529Agonist activity at STING in human PBMC cells assessed as increase in IFNbeta mRNA level at 69.6 uM measured after 4 hrs by qRT-PCR analysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1852608Agonist activity at human wild type STING expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1905885Antitumor immunity in mouse MC38 cells implanted in C57BL/6J mouse assessed as increase in TNF-alpha level in injected tumor at 100 to 500 ug,IT administrated in right flank on day 0 measured after 4 hrs by mesoscale assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1852615Induction of TNFalpha secretion in human PBMC incubated for 16 hrs2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541408Activation of recombinant human STING haplotype R232H mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1546606Binding affinity to wild type human STING (139 to 379 residues) by ITC assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Targeting Stimulator of Interferon Genes (STING): A Medicinal Chemistry Perspective.
AID1601375Antitumor activity against mouse B16-OVA cells implanted in mouse assessed as tumour regression in contralateral flank at 10 ug administered intratumorally on day 6, 9 and 12 post implantation2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy.
AID1541406Activation of recombinant human wild-type STING expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541399Activation of recombinant human STING haplotype G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1905854Displacement of radiolabeled [3H]-2',3'-cGAMP from human STING HAQ variant incubated for 2 hrs by scintillation counting method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1816900Binding affinity to human STING incubated for 60 mins measured by competitive TR-FRET assay2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
AID1575505Binding affinity to human STING expressed in Escherichia coli by isothermal titration calorimetric method2019MedChemComm, Dec-01, Volume: 10, Issue:12
Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.
AID1714253Activation of STING in human THP-1-Dual cells assessed as induction of type I IFNs by measuring stimulation of NF-kappaB pathway incubated for 48 hrs by luciferase reporter gene assay
AID1816905Stability in human serum assessed as half life measured upto 120 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
AID1816904Stability in rat serum assessed as half life measured upto 120 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
AID1528521Cytotoxicity against STING knockout human THP1 cells assessed as reduction in cell viability by MTS assay2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1861452Agonist activity at wild type human STING C-terminal domain (139 to 379 residues) assessed as dissociation constant by isothermal titration calorimetry analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration.
AID1852609Agonist activity at human STING HAQ expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1905879Antitumor immunity in mouse MC38 cells implanted in C57BL/6J mouse assessed as increase in IL-6 level in injected tumor at 100 to 500 ug,IT administrated in right flank on day 0 measured after 4 hrs by mesoscale assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1905856Binding affinity to human STING HAQ variant assessed as melting temperature by thermal shift assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1905865Binding affinity to wild type mouse STING assessed as half life by Surface plasmon resonance assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1541400Activation of recombinant human STING haplotype R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1852614Induction of IFNgamma secretion in human PBMC incubated for 16 hrs2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541394Binding affinity to recombinant human wild-type STING assessed as change in melting temperature at 150 uM by SYPRO orange dye based differential scanning fluorimetric method2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541411Cytotoxicity against human PBMC-derived CD3-positive T cells assessed as effect on cell viability at 12.5 uM incubated for 16 hrs by Zombie-NIR staining-based flow cytometry2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1905862Binding affinity to human STING HAQ variant assessed as dissociation constant by Surface plasmon resonance assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1905861Binding affinity to wild type human STING assessed as half life by Surface plasmon resonance assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1541403Activation of STING in human PBMC assessed as induction of TNFalpha secretion at 12.5 uM incubated for 16 hrs by ProcartaPlex assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541407Activation of recombinant human STING haplotype R71H/G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1905864Binding affinity to wild type mouse STING assessed as dissociation constant by Surface plasmon resonance assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1905860Binding affinity to wild type human STING assessed as dissociation constant by Surface plasmon resonance assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1714243Stability in presence of nuclease P1 assessed as parent compound remaining level at 7 ug incubated for 2 hrs by HPLC analysis
AID1905663Agonist activity at STING in human wild-type THP1-Dual cells co-expressing ISRE reporter assessed as IRF-mediated immune response incubated for 24 hrs by QUANTI Luc based microplate reader method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor.
AID1905858Agonist activity at STING HAQ variant in human THP1 cell assessed as maximum human INF-beta production incubated for 5 hrs by mesoscale assay relative to control2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1905875Antitumor activity against mouse MC38 cells implanted in C57BL/6J mouse assessed as tumor growth inhibition in non-injected left flank at 100 ug,IT administrated in left flank on day 0,3,7 and 10 measured after 15 days2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1541398Activation of recombinant human STING haplotype R232H mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1905894Antitumor immunity in mouse MC38 cells implanted in C57BL/6J mouse assessed as increase in IFN-gamma level in injected tumor at 100 to 500 ug,IT administrated in right flank on day 0 measured after 4 hrs by ELISA2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1541396Activation of recombinant human wild-type STING expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1861453Agonist activity at STING (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration.
AID1905664Cytotoxicity against human wild type THP1-Dual cells assessed as residual cell viability by CellTiter96 Aqueous One Solution Cell Proliferation Assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor.
AID1905889Agonist activity at STING HAQ variant in mouse BMDC cells assessed as maximum mouse INF-beta production incubated for 5 hrs by ELISA relative to control2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1714242Induction of type I IFN production in mouse RAW-Lucia ISG-KO-STING cells at 0.08 to 60 ug/ml incubated for 48 hrs by luciferase reporter gene assay
AID1575509Binding affinity to human C-terminal STING domain (139 to 378 residues) by microscale thermophoresis method2019MedChemComm, Dec-01, Volume: 10, Issue:12
Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.
AID1714249Activation of STING in mouse RAW-Lucia ISG cells assessed as induction of type I IFNs stimulation by measuring induction of IRF pathway incubated for 48 hrs by luciferase reporter gene assay
AID1905857Binding affinity to wild type human STING assessed as melting temperature by thermal shift assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1528519Induction of IRF3 pathway in STING knockout human THP1 cells measured after 20 hrs by luciferase reporter gene assay2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1816903Agonist activity at STING HAQ mutant in human THP-1 dual cells incubated for 20 hrs by luciferase reporter gene assay2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
AID1528518Agonist activity at STING in human THP1 cells assessed as stimulation of IRF3 pathway measured after 20 hrs by luciferase reporter gene assay2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1541397Activation of recombinant human STING haplotype R71H/G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541409Activation of recombinant human STING haplotype G230A/R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1601371Antitumor activity against mouse B16-OVA cells implanted in mouse assessed as tumour regression in injected flank at 10 ug administered intratumorally on day 6, 9 and 12 post implantation2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy.
AID1528522Inhibition of anti 6His antibody-labeled terbium cryptate binding to human wild-type full-length 6His-tagged d2-labeled STING measured after 4 hrs by HTRF assay2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1528520Cytotoxicity against human THP1 cells assessed as reduction in cell viability by MTS assay2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1714255Activation of STING in human blood assessed as induction of type I IFNs incubated for 18 to 20 hrs by QUANTI-Blue assay
AID1541405Ratio of EC50 for recombinant human wild-type STING expressed in 293T cells in absence of digitonin A to EC50 for recombinant human wild-type STING expressed in 293T cells in presence of digitonin A2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1852612Agonist activity at human STING Q expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1852616Induction of IFNalpha secretion in human PBMC incubated for 16 hrs2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1905855Displacement of radiolabeled [3H]-2',3'-cGAMP from wild type human STING incubated for 2 hrs by scintillation counting method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1861454Agonist activity at human STING H232 variant assessed as dissociation constant2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration.
AID1714247Stability in presence of snake venom phosphodiesterase assessed as parent compound remaining level at 7 ug incubated for 2 hrs by HPLC analysis
AID1905884Antitumor immunity in mouse MC38 cells implanted in C57BL/6J mouse assessed as increase in IFN-beta level in injected tumor at 100 to 500 ug,IT administrated in right flank on day 0 measured after 4 hrs by ELISA2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1816902Agonist activity at human STING R232 mutant transfected in HEK293T cells co-expressing ISRE Nano-Luc incubated for 20 hrs by luciferase reporter gene assay2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
AID1905859Agonist activity at STING HAQ variant in human THP1 cell assessed as increase in human INF-beta production incubated for 5 hrs by mesoscale assay2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1852611Agonist activity at human STING AQ expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1852613Agonist activity at human wild type full length STING expressed in 293T cells incubated for 7 hrs by luciferase/cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1528531Agonist activity at STING in human PBMC cells assessed as increase in IL6 mRNA level at 69.6 uM measured after 4 hrs by qRT-PCR analysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1714257Stability in presence of ENPP1 ( unknown origin) assessed as half life by HPLC analysis
AID1528524Agonist activity at STING in human PBMC cells assessed as increase in IFNbeta release at 1.39 to 139 uM measured after 4 hrs by ELISA2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1714251Activation of STING in human THP-1-Dual cells assessed as induction of type I IFNs by measuring stimulation of IRF pathway incubated for 48 hrs by luciferase reporter gene assay
AID1528530Agonist activity at STING in human PBMC cells assessed as increase in CXCL10 mRNA level at 69.6 uM measured after 4 hrs by qRT-PCR analysis2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
AID1852607Binding affinity to human wild type STING assessed as change in melting temperature by differential scanning fluorimetry (DSF) method2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541387Activation of STING in human PBMC assessed as induction of INFalpha secretion at 12.5 uM incubated for 16 hrs by ProcartaPlex assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1905888Agonist activity at STING HAQ variant in mouse BMDC cells assessed as increase in mouse INF-beta production incubated for 5 hrs by ELISA2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1905876Antitumor activity against mouse MC38 cells implanted in C57BL/6J mouse assessed as tumor growth inhibition in non-injected left flank at 50 ug,IT administrated in left flank on day 0,3,7 and 10 measured after 15 days2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
AID1816901Agonist activity at human STING R232 mutant transfected in HEK293T cells co-expressing ISRE Nano-Luc incubated for 30 mins in presence of digitonin by luciferase reporter gene assay2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
AID1541410Activation of recombinant human STING haplotype R293Q mutant expressed in 293T cells measured after 30 mins in presence of digitonin A by bright Glo-luciferase reporter gene assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1905659Induction of STING dependent immune response in human wild type THP1-Dual cells co-expressing ISRE reporter assessed as normalized luciferase gene expression by measuring relative luciferase units at 50 uM incubated for 24 hrs by QUANTI Luc based micropla2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor.
AID1541395Activation of recombinant human wild-type STING expressed in 293T cells incubated for 7 hrs in absence of digitonin A by bright Glo-luciferase reporter gene assay2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1541402Activation of STING in human PBMC assessed as induction of INFgamma secretion at 12.5 uM incubated for 16 hrs by ProcartaPlex assay relative to 2'3'cGAMP2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1546605Binding affinity to human STING H232 mutant by ITC assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Targeting Stimulator of Interferon Genes (STING): A Medicinal Chemistry Perspective.
AID1749739Binding affinity to 6His-tagged human STING measured after 3 hrs by HTRF assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Structure-Activity Relationship Study of Amidobenzimidazole Analogues Leading to Potent and Systemically Administrable Stimulator of Interferon Gene (STING) Agonists.
AID1852610Agonist activity at human STING REF expressed in 293T cells by digitonin cell based assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1852617Cytotoxicity against human PBMC cells2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
AID1541401Cytotoxicity against human PBMC-derived monocytes assessed as CD3-negative CD14 positive monocyte viability at 12.5 uM incubated for 16 hrs by Zombie-NIR staining-based flow cytometry relative to control2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.
AID1601376Antitumor activity against mouse B16-OVA cells implanted in mouse assessed as higher number of mouse cured of tumors at 10 ug administered intratumorally on day 6, 9 and 12 post implantation2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Discovery of IACS-8803 and IACS-8779, potent agonists of stimulator of interferon genes (STING) with robust systemic antitumor efficacy.
AID1346267Human transmembrane protein 173 (Other pattern recognition receptors)2013Molecular cell, Jul-25, Volume: 51, Issue:2
Cyclic GMP-AMP containing mixed phosphodiester linkages is an endogenous high-affinity ligand for STING.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (327)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's161 (49.24)24.3611
2020's166 (50.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials1 (0.30%)5.53%
Reviews2 (33.33%)6.00%
Reviews39 (11.89%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other4 (66.67%)84.16%
Other288 (87.80%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]