Page last updated: 2024-10-15

bis(3',5')-cyclic diguanylic acid

Cross-References

ID SourceID
PubMed CID135440063
CHEMBL ID1231573
CHEBI ID49537
SCHEMBL ID17974376
MeSH IDM0171847

Synonyms (43)

Synonym
CHEMBL1231573 ,
9,9'-[(2r,3r,3as,5s,7ar,9r,10r,10as,12s,14ar)-3,5,10,12-tetrahydroxy-5,12-dioxidooctahydro-2h,7h-difuro[3,2-d:3',2'-j][1,3,7,9,2,8]tetraoxadiphosphacyclododecine-2,9-diyl]bis(2-amino-1,9-dihydro-6h-purin-6-one)
c2e ,
bis-(3',5')-cyclic digmp
cyclic di-3',5'-guanylate
61093-23-0
3',5'-cyclic diguanylic acid
3',5'-cyclic digmp
cdigmp
5GP-5GP ,
cyclic di-3',5'-guanylic acid
cyclic di-gmp
bis(3',5')-cyclic diguanylic acid
cyclic-bis(3'->5') dimeric gmp
c-di-gmp ,
CHEBI:49537 ,
cyclic-bis(3',5')diguanylic acid
cgpgp
bis-(3'-5')-cyclic dimeric guanosine monophosphate
9,9'-[(2r,3r,3as,7ar,9r,10r,10as,14ar)-3,5,10,12-tetrahydroxy-5,12-dioxidooctahydro-2h,7h-difuro[3,2-d:3',2'-j][1,3,7,9,2,8]tetraoxadiphosphacyclododecine-2,9-diyl]bis(2-amino-1,9-dihydro-6h-purin-6-one)
cyclic diguanylic acid
guanylyl-(3'->5')-3'-guanylic acid, cyclic 3'->5'''-nucleotide
cyclic dinucleotide di-gmp
3',5'-cyclic di-gmp
c-(gpgp)
cyclic diguanylate
bdbm50436163
cyclic-di-gmp
CS-7977
HY-107780
SCHEMBL17974376
PKFDLKSEZWEFGL-MHARETSRSA-N
c-di-gmp; cyclic diguanosine monophosphate
EX-A6951
Q2649761
(1s,6r,8r,9r,10s,15r,17r,18r)-8,17-bis(2-amino-6-hydroxypurin-9-yl)-3,12-dihydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecane-9,18-diol
cyclicdiguanylate
2-amino-9-[(1s,6r,8r,9r,10s,15r,17r,18r)-17-(2-amino-6-oxo-1h-purin-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
DTXSID801027528
(1s,6r,8r,9r,10s,15r,17r,18r)-8,17-bis(2-amino-6-oxo-6,9-dihydro-1h-purin-9-yl)-3,9,12,18-tetrahydroxy-2,4,7,11,13,16-hexaoxa-3,12-diphosphatricyclo[13.3.0.0,octadecane-3,12-dione
BP-58810
AKOS040732890
c-di-gmp (disodium)

Toxicity

ExcerptReference
" Whereas wild-type cells tolerated a sudden exposure to a toxic concentration of toluene, a tolR mutant strain or a strain overexpressing a diguanylate cyclase gene lost viability upon toluene shock."( Degradation of cyclic diguanosine monophosphate by a hybrid two-component protein protects Azoarcus sp. strain CIB from toluene toxicity.
Baraquet, C; Blázquez, B; Díaz, E; Harwood, CS; Martín-Moldes, Z; Zamarro, MT, 2016
)

Compound-Compound Interactions

ExcerptReference
" In this study, a murine model was used to compare sublingual administration with intranasal and intramuscular administration of influenza H5N1 virosomes (2 µg haemagglutinin; HA) in combination with the mucosal adjuvant (3',5')-cyclic dimeric guanylic acid (c-di-GMP)."( Evaluation of the sublingual route for administration of influenza H5N1 virosomes in combination with the bacterial second messenger c-di-GMP.
Bredholt, G; Cox, RJ; Ebensen, T; Gjeraker, IH; Guzmán, CA; Pedersen, GK; Svindland, S, 2011
)

Bioavailability

ExcerptReference
" However, the bioavailability of iron is low due to its insolubility under aerobic conditions."( The Iron Tug-of-War between Bacterial Siderophores and Innate Immunity.
Golonka, R; Vijay-Kumar, M; Yeoh, BS, 2019
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
immunomodulatorBiologically active substance whose activity affects or plays a role in the functioning of the immune system.
signalling moleculeA molecular messenger in which the molecule is specifically involved in transmitting information between cells. Such molecules are released from the cell sending the signal, cross over the gap between cells by diffusion, and interact with specific receptors in another cell, triggering a response in that cell by activating a series of enzyme controlled reactions which lead to changes inside the cell.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
cyclic purine dinucleotide
guanyl ribonucleotideA purine ribonucleotide where the purine is guanine.
[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 (5)

PathwayProteinsCompounds
Immune System91482
Innate Immune System41475
Cytosolic sensors of pathogen-associated DNA4712
STING mediated induction of host immune responses166
IRF3-mediated induction of type I IFN134

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RocRPseudomonas aeruginosa PAO1IC50 (µMol)0.02000.02000.02000.0200AID755392
[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)Kd0.11000.00001.42253.5000AID1575511
Stimulator of interferon genes proteinHomo sapiens (human)EC50 (µMol)40.02830.00581.36117.2000AID1541395; AID1541396; AID1541397; AID1541399; AID1541400; AID1814337
Stimulator of interferon genes proteinHomo sapiens (human)Kd2.20750.00381.31315.2000AID1546606; AID1575505; AID1575512; AID1861452
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (45)

Assay IDTitleYearJournalArticle
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.
AID1693330Antibacterial activity against Streptococcus mutans NBRC13955 assessed as bacterial cell density at 500 uM relative to control2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Amine skeleton-based c-di-GMP derivatives as biofilm formation inhibitors.
AID1693328Antibacterial activity against Pseudomonas aeruginosa NBRC13275 assessed as bacterial cell density at 500 uM relative to control2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Amine skeleton-based c-di-GMP derivatives as biofilm formation inhibitors.
AID1693329Antibacterial activity against Staphylococcus aureus NBRC13276 assessed as bacterial cell density at 500 uM relative to control2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Amine skeleton-based c-di-GMP derivatives as biofilm formation inhibitors.
AID755394Allosteric inhibition of Pseudomonas aeruginosa WspR using [32P]-GTP as substrate measured for 1 hr by thin layer chromatographic analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Potent suppression of c-di-GMP synthesis via I-site allosteric inhibition of diguanylate cyclases with 2'-F-c-di-GMP.
AID1251971Inhibition of Caulobacter crescentus PleD2015Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
Synthesis of Triazole-Linked Analogues of c-di-GMP and Their Interactions with Diguanylate Cyclase.
AID755388Inhibition of Pseudomonas aeruginosa PA14 PvrR using [32P]-GTP as substrate at 100 uM after 120 mins by thin layer chromatographic analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Potent suppression of c-di-GMP synthesis via I-site allosteric inhibition of diguanylate cyclases with 2'-F-c-di-GMP.
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.
AID755395Inhibition of Pseudomonas aeruginosa WspR using [32P]-GTP as substrate at 100 uM after 120 mins by thin layer chromatographic analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Potent suppression of c-di-GMP synthesis via I-site allosteric inhibition of diguanylate cyclases with 2'-F-c-di-GMP.
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).
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.
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).
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.
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.
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.
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.
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.
AID1693327Antibacterial activity against Escherichia coli DH5alpha assessed as bacterial cell density at 500 uM relative to control2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Amine skeleton-based c-di-GMP derivatives as biofilm formation inhibitors.
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.
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.
AID755393Competitive binding affinity to Pseudomonas aeruginosa WspR after 5 mins in presence of [32P]-c-di-GMP2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Potent suppression of c-di-GMP synthesis via I-site allosteric inhibition of diguanylate cyclases with 2'-F-c-di-GMP.
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).
AID1693323Antibiofilm activity against Escherichia coli DH5alpha assessed as inhibition of biofilm formation at 500 uM incubated for 24 hrs by crystal violet staining based microtiter plate reader assay relative to control2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Amine skeleton-based c-di-GMP derivatives as biofilm formation inhibitors.
AID1693326Antibiofilm activity against Streptococcus mutans NBRC13955 assessed as inhibition of biofilm formation at 500 uM incubated for 24 hrs by crystal violet staining based microtiter plate reader assay relative to control2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Amine skeleton-based c-di-GMP derivatives as biofilm formation inhibitors.
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.
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.
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.
AID755391Competitive binding affinity to Pseudomonas aeruginosa Alg44 PilZ domain after 5 mins in presence of [32P]-c-di-GMP2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Potent suppression of c-di-GMP synthesis via I-site allosteric inhibition of diguanylate cyclases with 2'-F-c-di-GMP.
AID755390Inhibition of Pseudomonas aeruginosa PA14 diguanylate cyclase PA1107 using [32P]-GTP as substrate at 100 uM after 120 mins by thin layer chromatographic analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Potent suppression of c-di-GMP synthesis via I-site allosteric inhibition of diguanylate cyclases with 2'-F-c-di-GMP.
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.
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.
AID1575511Binding affinity to mouse C-terminal STING domain (139 to 378 residues) by isothermal titration calorimetric method2019MedChemComm, Dec-01, Volume: 10, Issue:12
Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.
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.
AID1575512Binding affinity to human C-terminal STING domain (139 to 379 residues) by isothermal titration calorimetric method2019MedChemComm, Dec-01, Volume: 10, Issue:12
Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules.
AID755389Inhibition of Pseudomonas aeruginosa PAO1 His6-tagged RocR expressed in Escherichia coli BL21 (DE3) using [32P]-GTP as substrate at 100 uM after 120 mins by thin layer chromatographic analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Potent suppression of c-di-GMP synthesis via I-site allosteric inhibition of diguanylate cyclases with 2'-F-c-di-GMP.
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.
AID755392Competitive binding affinity to Pseudomonas aeruginosa PAO1 His6-tagged RocR expressed in Escherichia coli BL21 (DE3) after 5 mins in presence of [32P]-c-di-GMP2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Potent suppression of c-di-GMP synthesis via I-site allosteric inhibition of diguanylate cyclases with 2'-F-c-di-GMP.
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.
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.
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).
AID1693324Antibiofilm activity against Pseudomonas aeruginosa NBRC13275 assessed as inhibition of biofilm formation at 500 uM incubated for 6 hrs by crystal violet staining based microtiter plate reader assay relative to control2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Amine skeleton-based c-di-GMP derivatives as biofilm formation inhibitors.
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.
AID1693325Antibiofilm activity against Staphylococcus aureus NBRC13276 assessed as inhibition of biofilm formation at 500 uM incubated for 24 hrs by crystal violet staining based microtiter plate reader assay relative to control2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Amine skeleton-based c-di-GMP derivatives as biofilm formation inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,099)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.09)18.7374
1990's10 (0.91)18.2507
2000's129 (11.74)29.6817
2010's734 (66.79)24.3611
2020's225 (20.47)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 (%)
Trials1 (0.09%)5.53%
Reviews129 (11.60%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other982 (88.31%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]