General Information of the Protein
Protein ID
PT03644
Protein Name
Stimulator of interferon genes protein
Secondarily
Protein Name
Endoplasmic reticulum interferon stimulator
Mediator of IRF3 activation
Transmembrane protein 173
Gene Name
STING1
Secondarily
Gene Name
ERIS
MITA
STING
TMEM173
Sequence
MPHSSLHPSIPCPRGHGAQKAALVLLSACLVTLWGLGEPPEHTLRYLVLHLASLQLGLLLNGVCSLAEELRHIHSRYRGSYWRTVRACLGCPLRRGALLLLSIYFYYSLPNAVGPPFTWMLALLGLSQALNILLGLKGLAPAEISAVCEKGNFNVAHGLAWSYYIGYLRLILPELQARIRTYNQHYNNLLRGAVSQRLYILLPLDCGVPDNLSMADPNIRFLDKLPQQTGDHAGIKDRVYSNSIYELLENGQRAGTCVLEYATPLQTLFAMSQYSQAGFSREDRLEQAKLFCRTLEDILADAPESQNNCRLIAYQEPADDSSFSLSQEVLRHLRQEEKEEVTVGSLKTSAVPSTSTMSQEPELLISGMEKPLPLRTDFS
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Organism
Homo sapiens, Human
Protein Classification
Unclassified protein
Function
Facilitator of innate immune signaling that acts as a sensor of cytosolic DNA from bacteria and viruses and promotes the production of type I interferon (IFN-alpha and IFN-beta) (PubMed:18724357, PubMed:18818105, PubMed:19433799, PubMed:19776740, PubMed:23027953, PubMed:23910378, PubMed:23747010, PubMed:29973723, PubMed:30842659, PubMed:35045565, PubMed:27801882, PubMed:36808561). Innate immune response is triggered in response to non-CpG double-stranded DNA from viruses and bacteria delivered to the cytoplasm (PubMed:26300263). Acts by binding cyclic dinucleotides: recognizes and binds cyclic di-GMP (c-di-GMP), a second messenger produced by bacteria, and cyclic GMP-AMP (cGAMP), a messenger produced by CGAS in response to DNA virus in the cytosol (PubMed:21947006, PubMed:23258412, PubMed:23707065, PubMed:23722158, PubMed:26229117, PubMed:23910378, PubMed:23747010, PubMed:30842659). Upon binding of c-di-GMP or cGAMP, STING1 oligomerizes, translocates from the endoplasmic reticulum and is phosphorylated by TBK1 on the pLxIS motif, leading to recruitment and subsequent activation of the transcription factor IRF3 to induce expression of type I interferon and exert a potent anti-viral state (PubMed:22394562, PubMed:25636800, PubMed:29973723, PubMed:30842653, PubMed:35045565). In addition to promote the production of type I interferons, plays a direct role in autophagy (PubMed:30568238, PubMed:30842662). Following cGAMP-binding, STING1 buds from the endoplasmic reticulum into COPII vesicles, which then form the endoplasmic reticulum-Golgi intermediate compartment (ERGIC) (PubMed:30842662). The ERGIC serves as the membrane source for WIPI2 recruitment and LC3 lipidation, leading to formation of autophagosomes that target cytosolic DNA or DNA viruses for degradation by the lysosome (PubMed:30842662). The autophagy- and interferon-inducing activities can be uncoupled and autophagy induction is independent of TBK1 phosphorylation (PubMed:30568238, PubMed:30842662). Autophagy is also triggered upon infection by bacteria: following c-di-GMP-binding, which is produced by live Gram-positive bacteria, promotes reticulophagy (By similarity). Exhibits 2',3' phosphodiester linkage-specific ligand recognition: can bind both 2'-3' linked cGAMP (2'-3'-cGAMP) and 3'-3' linked cGAMP but is preferentially activated by 2'-3' linked cGAMP (PubMed:26300263, PubMed:23910378, PubMed:23747010). The preference for 2'-3'-cGAMP, compared to other linkage isomers is probably due to the ligand itself, whichs adopts an organized free-ligand conformation that resembles the STING1-bound conformation and pays low energy costs in changing into the active conformation (PubMed:26150511). May be involved in translocon function, the translocon possibly being able to influence the induction of type I interferons (PubMed:18724357). May be involved in transduction of apoptotic signals via its association with the major histocompatibility complex class II (MHC-II) (By similarity).
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Uniprot ID
Primary ID:
Q86WV6

Secondarily ID:
A8K3P6
B6EB35
D6RBX0
D6RE01
D6RID9
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Ensembl ID
ENSG00000184584
HGNC ID
HGNC:27962
Subcellular Location
Endoplasmic reticulum membrane
Cytoplasm
Perinuclear region
Endoplasmic reticulum-Golgi intermediate compartment membrane
Golgi apparatus membrane
Cytoplasmic vesicle
Autophagosome membrane
Mitochondrion outer membrane
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000025 , HEK-293T
Compound ID Compound Name Compound Formula
CP0534896
CHEMBL5078036
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C20H22F2N10O9P2S
 1
1
EC50 = 7 nM
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CP0968949
Cyclo-4-amino-5-methyl-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]-pyrimidine5'-O-Phosphate(3'->5')Guanosine5'-O-Phosphate(2'->5')
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C22H27N9O13P2
 2
1
EC50 = 9 nM
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2
EC50 = 31300 nM
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CP0160320
2-amino-9-[(1R,6R,8R,9R,10S,15S,17R)-8-(6-aminopurin-9-yl)-3,9,12-trihydroxy-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
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C20H24N10O12P2
 4
1
EC50 = 10 nM
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2
EC50 = 30 nM
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3
EC50 = 120 nM
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4
EC50 = 21600 nM
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CP0177170
2-amino-9-[(1S,6R,8R,10S,15R,17R,18R)-8-(6-aminopurin-9-yl)-18-fluoro-3,12-dihydroxy-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
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C20H23FN10O11P2
 5
1
EC50 = 10 nM
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2
EC50 = 20 nM
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3
EC50 = 40 nM
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4
EC50 = 60 nM
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5
EC50 = 15100 nM
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CP0224779
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-8-(4-aminopyrrolo[2,3-d]pyrimidin-7-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
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C21H25N9O13P2
 4
1
EC50 = 10 nM
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2
EC50 = 20 nM
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3
EC50 = 160 nM
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4
EC50 = 66400 nM
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CP0239509
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-3,9,12,18-tetrahydroxy-8-(6-methylsulfanylpurin-9-yl)-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
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C21H25N9O13P2S
 4
1
EC50 = 10 nM
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2
EC50 = 60 nM
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3
EC50 = 1230 nM
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4
EC50 = 13300 nM
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CP0326362
2-amino-9-[(1R,6R,8R,9R,10R,15R,17R,18R)-8-(6-aminopurin-9-yl)-9-fluoro-3,12,18-trihydroxy-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
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C20H23FN10O12P2
 5
1
EC50 = 10 nM
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2
EC50 = 20 nM
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3
EC50 = 30 nM
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4
EC50 = 13800 nM
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5
EC50 = 37560 nM
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CP0220338
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
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C20H23N9O13P2
 4
1
EC50 = 10 nM
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2
EC50 = 20 nM
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3
EC50 = 30 nM
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4
EC50 = 29900 nM
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CP0330295
2-amino-9-[(1S,6R,8R,9R,10S,15R,17R,18R)-8-(6-aminopurin-9-yl)-18-fluoro-3,9,12-trihydroxy-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
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C20H23FN10O12P2
 4
1
EC50 = 10 nM
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2
EC50 = 20 nM
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3
EC50 = 40 nM
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4
EC50 = 16700 nM
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CP0534891
[(1R,3R,6R,8R,9R,10R,12R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-12-(2-ethylbutanoyloxymethoxy)-9,18-difluoro-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl 2-ethylbutanoate
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C34H46F2N10O14P2
 2
1
EC50 = 10 nM
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2
EC50 = 70 nM
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CP0950476
Cyclo-4-amino-5-(biphenyl-4-yl)-7-beta-D-ribofuranosyl-7Hpyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
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C33H33N9O13P2
 2
1
EC50 = 13 nM
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2
EC50 = 2950 nM
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CP0134444
2-amino-9-[(1R,6R,8R,10S,15R,17R,18R)-8-(6-aminopurin-9-yl)-3,12,18-trihydroxy-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
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C20H24N10O12P2
 5
1
EC50 = 20 nM
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2
EC50 = 30 nM
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3
EC50 = 60 nM
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4
EC50 = 340 nM
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5
EC50 = 31900 nM
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CP0145547
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-8-(2,6-diaminopurin-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
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C20H25N11O13P2
 5
1
EC50 = 20 nM
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2
EC50 = 40 nM
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3
EC50 = 50 nM
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4
EC50 = 310 nM
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5
EC50 = 35900 nM
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CP0158277
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
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C20H24N10O13P2
 5
1
EC50 = 20 nM
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2
EC50 = 40 nM
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3
EC50 = 50 nM
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4
EC50 = 13700 nM
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5
EC50 = 28370 nM
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CP0160045
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-9-amino-8-(6-aminopurin-9-yl)-3,12,18-trihydroxy-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
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C20H25N11O12P2
 3
1
EC50 = 20 nM
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2
EC50 = 30 nM
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3
EC50 = 240 nM
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CP0160321
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-3,9,12,18-tetrahydroxy-8-[6-(methylamino)purin-9-yl]-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
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C21H26N10O13P2
 4
1
EC50 = 20 nM
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2
EC50 = 60 nM
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3
EC50 = 1200 nM
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4
EC50 = 63700 nM
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CP0160322
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-8-(2-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
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C20H24N10O13P2
 4
1
EC50 = 20 nM
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2
EC50 = 40 nM
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3
EC50 = 700 nM
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4
EC50 = 53900 nM
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CP0177171
2-amino-9-[(1R,6R,8R,9R,10R,15R,17R,18R)-8-(2,6-diaminopurin-9-yl)-9-fluoro-3,12,18-trihydroxy-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
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C20H24FN11O12P2
 5
1
EC50 = 20 nM
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2
EC50 = 30 nM
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3
EC50 = 40 nM
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4
EC50 = 130 nM
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5
EC50 = 27600 nM
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CP0239512
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]-1-methylpurin-6-one
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C21H26N10O13P2
 4
1
EC50 = 20 nM
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2
EC50 = 40 nM
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3
EC50 = 780 nM
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4
EC50 = 40000 nM
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CP0323317
2-amino-9-[(1R,6R,8R,9R,10R,15S,17R)-8-(6-aminopurin-9-yl)-9-fluoro-3,12-dihydroxy-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
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C20H23FN10O11P2
 5
1
EC50 = 20 nM
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2
EC50 = 40 nM
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3
EC50 = 50 nM
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4
EC50 = 180 nM
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5
EC50 = 10700 nM
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CP0326226
2-amino-9-[(1S,6R,8R,9R,10R,15R,17R,18R)-8-(6-aminopurin-9-yl)-9,18-difluoro-3,12-dihydroxy-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
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C20H22F2N10O11P2
 5
1
EC50 = 20 nM
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2
EC50 = 50 nM
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3
EC50 = 90 nM
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4
EC50 = 200 nM
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5
EC50 = 13300 nM
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CP0330296
2-amino-9-[(1R,6R,8R,9R,10R,15R,17R,18R)-8-(6-amino-2-fluoropurin-9-yl)-9-fluoro-3,12,18-trihydroxy-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
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C20H22F2N10O12P2
 4
1
EC50 = 20 nM
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2
EC50 = 30 nM
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3
EC50 = 80 nM
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4
EC50 = 11000 nM
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CP0323318
2-amino-9-[(1R,6R,8R,9R,14R,16R,17R,18R)-16-(6-aminopurin-9-yl)-3,11,17,18-tetrahydroxy-3,11-dioxo-2,4,7,10,12,15-hexaoxa-3lambda5,11lambda5-diphosphatricyclo[12.2.1.16,9]octadecan-8-yl]-1H-purin-6-one
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C20H24N10O13P2
 7
1
EC50 = 20 nM
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2
EC50 = 30 nM
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3
EC50 = 170 nM
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4
EC50 = 260 nM
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5
EC50 = 11680 nM
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6
EC50 = 39200 nM
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7
EC50 = 85110 nM
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CP0546127
9-[(1R,6R,8R,9R,10R,15R,17R,18R)-17-(6-aminopurin-9-yl)-9,18-difluoro-3,12-dihydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]purin-6-amine
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C20H22F2N10O10P2
 3
1
EC50 = 20 nM
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2
EC50 = 7990 nM
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3
EC50 = 96500 nM
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   TS
CP0558309
9-[(1R,6R,8R,9R,10R,15R,17R,18R)-17-(6-aminopurin-9-yl)-9,18-difluoro-3-hydroxy-12-oxo-12-sulfanyl-3-sulfanylidene-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]purin-6-amine
   Show/Hide
C20H22F2N10O8P2S2
 2
1
EC50 = 20 nM
   TI
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   TS
2
EC50 = 520 nM
   TI
   LI
   LO
   TS
CP0528017
[(1R,3R,6R,8R,9R,10R,12R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-12-(2,2-dimethylpropanoyloxymethoxy)-9,18-difluoro-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl 2,2-dimethylpropanoate
   Show/Hide
C32H42F2N10O14P2
 2
1
EC50 = 20 nM
   TI
   LI
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   TS
2
EC50 = 30 nM
   TI
   LI
   LO
   TS
CP0915723
Cyclo-4-amino-5-ethynyl-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]-pyrimidine5'-O-Phosphate(3'->5')Guanosine5'-O-Phosphate(2'->5')
   Show/Hide
C23H25N9O13P2
 1
1
EC50 = 20 nM
   TI
   LI
   LO
   TS
CP0952826
Cyclo-4-amino-5-(furan-2-yl)-7-beta-D-ribofuranosyl-7H-pyrrolo-[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-Ophosphate(2'->5')
   Show/Hide
C25H27N9O14P2
 2
1
EC50 = 25 nM
   TI
   LI
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   TS
2
EC50 = 41300 nM
   TI
   LI
   LO
   TS
CP0965688
Cyclo-4-amino-7-beta-D-ribofuranosyl-5-(thiophen-2-yl)-7Hpyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
   Show/Hide
C25H27N9O13P2S
 2
1
EC50 = 28 nM
   TI
   LI
   LO
   TS
2
EC50 = 27300 nM
   TI
   LI
   LO
   TS
CP0160318
2-amino-9-[(1R,6R,8R,10S,15S,17R)-8-(6-aminopurin-9-yl)-3,12-dihydroxy-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
   Show/Hide
C20H24N10O11P2
 4
1
EC50 = 30 nM
   TI
   LI
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   TS
2
EC50 = 40 nM
   TI
   LI
   LO
   TS
3
EC50 = 60 nM
   TI
   LI
   LO
   TS
4
EC50 = 75400 nM
   TI
   LI
   LO
   TS
CP0528008
[(1R,3S,6R,8R,9R,10R,12R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-12-(2-ethylbutanoyloxymethoxy)-9,18-difluoro-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl 2-ethylbutanoate
   Show/Hide
C34H46F2N10O14P2
 2
1
EC50 = 30 nM
   TI
   LI
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   TS
2
EC50 = 230 nM
   TI
   LI
   LO
   TS
CP0528018
[(1R,3R,6R,8R,9R,10R,12R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-9,18-difluoro-3,12-dioxo-12-(propan-2-yloxycarbonyloxymethoxy)-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl propan-2-yl carbonate
   Show/Hide
C30H38F2N10O16P2
 2
1
EC50 = 30 nM
   TI
   LI
   LO
   TS
2
EC50 = 310 nM
   TI
   LI
   LO
   TS
CP0965687
Cyclo-4-amino-5-(4-(naphthalen-2-yl)phenyl)-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
   Show/Hide
C37H35N9O13P2
 2
1
EC50 = 32 nM
   TI
   LI
   LO
   TS
2
EC50 = 3060 nM
   TI
   LI
   LO
   TS
CP0964233
Cyclo-4-amino-5-(benzothiophen-2-yl)-7-beta-D-ribofuranosyl-7Hpyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
   Show/Hide
C29H29N9O13P2S
 2
1
EC50 = 35 nM
   TI
   LI
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   TS
2
EC50 = 8690 nM
   TI
   LI
   LO
   TS
CP0145548
2-amino-7-[(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]-3H-pyrrolo[2,3-d]pyrimidin-4-one
   Show/Hide
C21H25N9O13P2
 5
1
EC50 = 40 nM
   TI
   LI
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   TS
2
EC50 = 60 nM
   TI
   LI
   LO
   TS
3
EC50 = 100 nM
   TI
   LI
   LO
   TS
4
EC50 = 1100 nM
   TI
   LI
   LO
   TS
5
EC50 = 40400 nM
   TI
   LI
   LO
   TS
CP0224760
2-amino-9-[(1R,6R,8R,9S,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
   Show/Hide
C20H24N10O13P2
 3
1
EC50 = 40 nM
   TI
   LI
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   TS
2
EC50 = 80 nM
   TI
   LI
   LO
   TS
3
EC50 = 90 nM
   TI
   LI
   LO
   TS
CP0357410
9-[(1R,6R,8R,9R,10R,15R,17R,18R)-17-(6-aminopurin-9-yl)-9,18-difluoro-3-hydroxy-12-oxo-12-sulfanyl-3-sulfanylidene-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]purin-6-amine
   Show/Hide
C20H22F2N10O8P2S2
 2
1
EC50 = 40 nM
   TI
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2
EC50 = 7020 nM
   TI
   LI
   LO
   TS
CP0569885
CHEMBL5071466
   Show/Hide
C20H22F2N10O9P2S
 1
1
EC50 = 40 nM
   TI
   LI
   LO
   TS
CP0528019
[(1R,3S,6R,8R,9R,10R,12S,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-12-(2,2-dimethylpropanoyloxymethylsulfanyl)-9,18-difluoro-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]sulfanylmethyl 2,2-dimethylpropanoate
   Show/Hide
C32H42F2N10O12P2S2
 2
1
EC50 = 40 nM
   TI
   LI
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   TS
2
EC50 = 70 nM
   TI
   LI
   LO
   TS
CP0543907
[(1R,3S,6R,8R,9R,10R,12R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-12-(2,2-dimethylpropanoyloxymethylsulfanyl)-9,18-difluoro-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]sulfanylmethyl 2,2-dimethylpropanoate
   Show/Hide
C32H42F2N10O12P2S2
 1
1
EC50 = 40 nM
   TI
   LI
   LO
   TS
CP0528012
[(1R,3R,6R,8R,9R,10R,12S,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-12-(benzoyloxymethoxy)-9,18-difluoro-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl benzoate
   Show/Hide
C36H34F2N10O14P2
 2
1
EC50 = 40 nM
   TI
   LI
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   TS
2
EC50 = 250 nM
   TI
   LI
   LO
   TS
CP0528016
[(1R,3S,6R,8R,9R,10R,12R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-12-(2,2-dimethylpropanoyloxymethoxy)-9,18-difluoro-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl 2,2-dimethylpropanoate
   Show/Hide
C32H42F2N10O14P2
 2
1
EC50 = 40 nM
   TI
   LI
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   TS
2
EC50 = 70 nM
   TI
   LI
   LO
   TS
CP0952258
Cyclo-4-amino-5-[4-{(naphthalen-1-yloxy)methyl}phenyl]-7-beta-Dribofuranosyl-7H-pyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
   Show/Hide
C38H37N9O14P2
 2
1
EC50 = 43 nM
   TI
   LI
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   TS
2
EC50 = 2580 nM
   TI
   LI
   LO
   TS
CP0964231
Cyclo-4-amino-5-(naphthalen-2-yl)-7-beta-D-ribofuranosyl-7Hpyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
   Show/Hide
C31H31N9O13P2
 2
1
EC50 = 48 nM
   TI
   LI
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   TS
2
EC50 = 7630 nM
   TI
   LI
   LO
   TS
CP0239506
2-amino-9-[(1S,6R,8R,10S,15R,17R,18R)-8-(6-amino-2-fluoropurin-9-yl)-18-fluoro-3,12-dihydroxy-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
   Show/Hide
C20H22F2N10O11P2
 4
1
EC50 = 50 nM
   TI
   LI
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   TS
2
EC50 = 100 nM
   TI
   LI
   LO
   TS
3
EC50 = 170 nM
   TI
   LI
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   TS
4
EC50 = 700 nM
   TI
   LI
   LO
   TS
CP0239510
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-3,9,12,18-tetrahydroxy-3,12-dioxo-8-(6-oxo-1H-purin-9-yl)-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1H-purin-6-one
   Show/Hide
C20H23N9O14P2
 4
1
EC50 = 50 nM
   TI
   LI
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   TS
2
EC50 = 140 nM
   TI
   LI
   LO
   TS
3
EC50 = 300 nM
   TI
   LI
   LO
   TS
4
EC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0177159
2-amino-7-[(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]-3H-thieno[3,4-d]pyrimidin-4-one
   Show/Hide
C21H24N8O13P2S
 4
1
EC50 = 50 nM
   TI
   LI
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   TS
2
EC50 = 110 nM
   TI
   LI
   LO
   TS
3
EC50 = 250 nM
   TI
   LI
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   TS
4
EC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0224780
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-8-(6-aminopurin-9-yl)-3,9,12,18-tetrahydroxy-3-oxo-12-sulfanylidene-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1H-purin-6-one
   Show/Hide
C20H24N10O12P2S
 4
1
EC50 = 60 nM
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   LI
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   TS
2
EC50 = 110 nM
   TI
   LI
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   TS
3
EC50 = 120 nM
   TI
   LI
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   TS
4
EC50 = 140 nM
   TI
   LI
   LO
   TS
CP0323316
2-amino-9-[(1R,6R,8R,9S,10S,15R,17R,18R)-8-(6-amino-2-fluoropurin-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
   Show/Hide
C20H23FN10O13P2
 4
1
EC50 = 60 nM
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   TS
2
EC50 = 100 nM
   TI
   LI
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   TS
3
EC50 = 200 nM
   TI
   LI
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   TS
4
EC50 = 600 nM
   TI
   LI
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   TS
CP0955337
Cyclo-4-amino-5-(phenanthren-9-yl)-7-beta-D-ribofuranosyl-7Hpyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
   Show/Hide
C35H33N9O13P2
 2
1
EC50 = 61 nM
   TI
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   TS
2
EC50 = 65450 nM
   TI
   LI
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   TS
CP0915724
Cyclo-4-amino-5-phenyl-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]-pyrimidine5'-O-Phosphate(3'->5')Guanosine5'-O-Phosphate(2'->5')
   Show/Hide
C27H29N9O13P2
 2
1
EC50 = 63 nM
   TI
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   TS
2
EC50 = 40700 nM
   TI
   LI
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   TS
CP0969805
Cyclo-4-amino-5-cyclopropyl-7-beta-D-ribofuranosyl-7H-pyrrolo-[2,3-d]pyrimidine5'-O-Phosphate(3'->5')Guanosine5'-OPhosphate(2'->5')
   Show/Hide
C24H29N9O13P2
 1
1
EC50 = 64 nM
   TI
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   TS
CP0968475
Cyclo-4-amino-5-iodo-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]-pyrimidine5'-O-Phosphate(3'->5')Guanosine5'-O-Phosphate(2'->5')
   Show/Hide
C21H24IN9O13P2
 1
1
EC50 = 66 nM
   TI
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   TS
CP0160046
2-amino-9-[(1R,6R,8R,10S,15R,17R,18R)-8-(6-amino-2-chloropurin-9-yl)-3,12,18-trihydroxy-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
   Show/Hide
C20H23ClN10O12P2
 5
1
EC50 = 70 nM
   TI
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   TS
2
EC50 = 80 nM
   TI
   LI
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   TS
3
EC50 = 90 nM
   TI
   LI
   LO
   TS
4
EC50 = 960 nM
   TI
   LI
   LO
   TS
5
EC50 = 58200 nM
   TI
   LI
   LO
   TS
CP0915725
Cyclo-4-amino-5-(benzofuran-2-yl)-7-beta-D-ribofuranosyl-7Hpyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
   Show/Hide
C29H29N9O14P2
 2
1
EC50 = 76 nM
   TI
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   TS
2
EC50 = 10940 nM
   TI
   LI
   LO
   TS
CP0494967
CHEMBL5093161
   Show/Hide
C20H24N10O10P2S2
 2
1
EC50 = 80 nM
   TI
   LI
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   TS
2
EC50 = 3320 nM
   TI
   LI
   LO
   TS
CP0965689
Cyclo-4-amino-5-iodo-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]-pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(3'->5')
   Show/Hide
C21H24IN9O13P2
 1
1
EC50 = 101 nM
   TI
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   TS
CP0955338
Cyclo-4-amino-5-phenyl-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]-pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(3'->5')
   Show/Hide
C27H29N9O13P2
 1
1
EC50 = 110 nM
   TI
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   TS
CP0969450
Cyclo-4-amino-5-(pent-1-yn-1-yl)-7-beta-D-ribofuranosyl-7Hpyrrolo[2,3-d]pyrimidine5'-O-Phosphate(3'->5')Guanosine5'-O-Phosphate(2'->5')
   Show/Hide
C26H31N9O13P2
 1
1
EC50 = 116 nM
   TI
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   TS
CP0177169
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
   Show/Hide
C20H24N10O13P2
 6
1
EC50 = 120 nM
   TI
   LI
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   TS
2
EC50 = 121 nM
   TI
   LI
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   TS
3
EC50 = 260 nM
   TI
   LI
   LO
   TS
4
EC50 = 2060 nM
   TI
   LI
   LO
   TS
5
EC50 = 68370 nM
   TI
   LI
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   TS
6
EC50 = 70100 nM
   TI
   LI
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   TS
CP0546123
[(1R,3R,6R,8R,9R,10R,12R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-12-(2,2-dimethylpropanoyloxymethylsulfanyl)-9,18-difluoro-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]sulfanylmethyl 2,2-dimethylpropanoate
   Show/Hide
C32H42F2N10O12P2S2
 2
1
EC50 = 120 nM
   TI
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   TS
2
EC50 = 180 nM
   TI
   LI
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   TS
CP0177172
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]-3H-purine-2,6-dione
   Show/Hide
C20H23N9O14P2
 4
1
EC50 = 130 nM
   TI
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   TS
2
EC50 = 180 nM
   TI
   LI
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   TS
3
EC50 = 190 nM
   TI
   LI
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   TS
4
EC50 = 720 nM
   TI
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   TS
CP0546125
[(1R,3R,6R,8R,9R,10R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-9,18-difluoro-12-hydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl 2,2-dimethylpropanoate
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C26H32F2N10O12P2
 2
1
EC50 = 130 nM
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2
EC50 = 460 nM
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CP0224759
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-3,9,12,18-tetrahydroxy-3,12-dioxo-8-(6-sulfanylidene-3H-purin-9-yl)-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1H-purin-6-one
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C20H23N9O13P2S
 4
1
EC50 = 150 nM
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2
EC50 = 200 nM
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3
EC50 = 300 nM
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4
EC50 = 8300 nM
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CP0548439
CHEMBL5082153
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C20H22F2N10O8P2S2
 2
1
EC50 = 170 nM
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2
EC50 = 2280 nM
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CP0528009
[(1R,3S,6R,8R,9R,10R,12R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-9,18-difluoro-3,12-dioxo-12-(propan-2-yloxycarbonyloxymethoxy)-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl propan-2-yl carbonate
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C30H38F2N10O16P2
 2
1
EC50 = 170 nM
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2
EC50 = 940 nM
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CP0326358
CHEBI:71578
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C20H24N10O12P2
 5
1
EC50 = 200 nM
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2
EC50 = 260 nM
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3
EC50 = 300 nM
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4
EC50 = 7100 nM
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5
EC50 = 14900 nM
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CP0249594
5-amino-1-[(1R,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[13.2.1.06,10]octadecan-8-yl]imidazole-4-carboxamide
   Show/Hide
C19H25N9O14P2
 3
1
EC50 = 210 nM
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2
EC50 = 320 nM
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3
EC50 = 45300 nM
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CP0470841
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-8-(7-aminotriazolo[4,5-d]pyrimidin-3-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
   Show/Hide
C19H23N11O13P2
 4
1
EC50 = 210 nM
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2
EC50 = 230 nM
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3
EC50 = 310 nM
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4
EC50 = 5720 nM
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CP0330298
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-8-(2-amino-6-methylsulfanylpurin-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
   Show/Hide
C21H26N10O13P2S
 4
1
EC50 = 240 nM
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2
EC50 = 300 nM
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3
EC50 = 480 nM
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4
EC50 = 8500 nM
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CP0548438
[(1R,3R,6R,8R,9R,10R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-9,18-difluoro-12-hydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl propan-2-yl carbonate
   Show/Hide
C25H30F2N10O13P2
 2
1
EC50 = 320 nM
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2
EC50 = 1930 nM
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CP0952259
Cyclo-4-amino-5-(dibenzo[b,d]furan-4-yl)-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
   Show/Hide
C33H31N9O14P2
 2
1
EC50 = 367 nM
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2
EC50 = 19100 nM
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CP0366501
5-amino-1-[(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]imidazole-4-carboxamide
   Show/Hide
C19H25N9O13P2
 4
1
EC50 = 400 nM
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2
EC50 = 420 nM
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3
EC50 = 830 nM
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4
EC50 = 47200 nM
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CP0534892
[(1R,3R,6R,8R,9R,10R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-9,18-difluoro-12-hydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl benzoate
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C28H28F2N10O12P2
 2
1
EC50 = 400 nM
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2
EC50 = 3090 nM
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CP0548479
[(1R,3R,6R,8R,9R,10R,15R,17R,18R)-8,17-bis(6-aminopurin-9-yl)-9,18-difluoro-12-hydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-3-yl]oxymethyl 2-ethylbutanoate
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C27H34F2N10O12P2
 2
1
EC50 = 450 nM
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2
EC50 = 1360 nM
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CP0248590
benzyl N-[3-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazol-1-yl]propyl]carbamate
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C27H31N7O5
 1
1
EC50 = 630.96 nM
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CP0546907
tert-butyl N-[4-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazol-1-yl]butyl]carbamate
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C25H35N7O5
 1
1
EC50 = 794.33 nM
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CP0160324
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
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C20H24N10O14P2
 5
1
EC50 = 900 nM
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2
EC50 = 1100 nM
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3
EC50 = 4470 nM
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4
EC50 = 4500 nM
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5
EC50 > 45000 nM
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CP0552805
2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-(morpholin-4-ylmethoxy)-1-propylbenzimidazole-5-carboxamide
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C23H31N7O4
 1
1
EC50 = 1000 nM
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CP0557240
2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxy-1-propylbenzimidazole-5-carboxamide
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C19H24N6O3
 1
1
EC50 = 1000 nM
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CP0557241
1-butyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazole-5-carboxamide
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C20H26N6O3
 1
1
EC50 = 1000 nM
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CP0955336
Cyclo-4-amino-5-(naphthalen-1-yl)-7-beta-D-ribofuranosyl-7Hpyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
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C31H31N9O13P2
 2
1
EC50 = 1100 nM
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2
EC50 = 42450 nM
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CP0956914
Cyclo-4-amino-5-(1,2-dihydroacenaphthylen-5-yl)-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidine5'-O-phosphate(3'->5')Guanosine5'-O-phosphate(2'->5')
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C33H33N9O13P2
 1
1
EC50 = 1160 nM
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CP0330297
9-[(1R,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[13.2.1.06,10]octadecan-8-yl]-3H-purine-2,6-dione
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C20H23N9O15P2
 4
1
EC50 = 1700 nM
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2
EC50 = 1800 nM
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3
EC50 = 2000 nM
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4
EC50 = 32800 nM
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CP0556779
2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxy-1-prop-2-enylbenzimidazole-5-carboxamide
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C19H22N6O3
 1
1
EC50 = 2511.89 nM
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CP0912403
Cyclo-adenosine5'-O-Phosphate(3'->5')2-Amino-5-methyl-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-one5'-O-Phosphate(2'->5')
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C22H27N9O13P2
 1
1
EC50 = 3010 nM
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CP0421492
2-[(2,5-diethylpyrazole-3-carbonyl)amino]-7-methoxy-1-propylbenzimidazole-5-carboxamide
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C20H26N6O3
 1
1
EC50 = 3162.28 nM
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CP0424752
2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxy-1-(3-methylbutyl)benzimidazole-5-carboxamide
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C21H28N6O3
 1
1
EC50 = 3162.28 nM
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CP0543004
(1R,6R,8R,9R,10S,15R,17R,18R)-8,17-bis(4-amino-5-iodopyrrolo[2,3-d]pyrimidin-7-yl)-3,12-dihydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecane-9,18-diol
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C22H24I2N8O12P2
 1
1
EC50 = 3488 nM
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CP0553869
2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-(3-hydroxypropoxy)-1-propylbenzimidazole-5-carboxamide
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C21H28N6O4
 1
1
EC50 = 3981.07 nM
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CP0950857
Cyclo-4-amino-5-phenyl-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]-pyrimidine5'-O-phosphate(3'->5')2-Amino-5-phenyl-7-beta-Dribofuranosyl-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-one5'-O-phosphate(2'->5')
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C34H34N8O13P2
 1
1
EC50 = 6410 nM
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CP0556778
2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxy-1-(3-morpholin-4-ylpropyl)benzimidazole-5-carboxamide
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C23H31N7O4
 1
1
EC50 = 7943.28 nM
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CP0549819
(1R,6R,8R,9R,10S,15R,17R,18R)-8,17-bis(4-amino-5-phenylpyrrolo[2,3-d]pyrimidin-7-yl)-3,12-dihydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecane-9,18-diol
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C34H34N8O12P2
 1
1
EC50 > 45000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0248635
1-[(E)-4-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-(3-morpholin-4-ylpropoxy)benzimidazol-1-yl]but-2-enyl]-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazole-5-carboxamide
   Show/Hide
C42H51N13O7
 6
1 EC50 < 0.1 nM
2 EC50 = 11 nM
3 EC50 = 130 nM
4 EC50 = 190 nM
5 IC50 = 3.9 nM
6 IC50 = 7.1 nM
CP0158277
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
   Show/Hide
C20H24N10O13P2
 8
1 EC50 = 5.8 nM
2 EC50 = 50 nM
3 EC50 = 19600 nM
4 IC50 = 1.8 nM
5 IC50 = 5.5 nM
6 Kd = 6.2 nM
7 Kd = 3790 nM
8 Kd = 42000 nM
CP0228629
2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-1-[(E)-4-[2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxy-5-(1H-1,2,4-triazol-5-yl)benzimidazol-1-yl]but-2-enyl]-7-(3-morpholin-4-ylpropoxy)benzimidazole-5-carboxamide
   Show/Hide
C43H51N15O6
 2
1 EC50 = 6.2 nM
2 EC50 = 240 nM
CP0326358
CHEBI:71578
   Show/Hide
C20H24N10O12P2
 1
1 EC50 = 51.3 nM
CP0176928
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
   Show/Hide
C20H23N9O13P2
 4
1 EC50 = 62 nM
2 EC50 = 6800 nM
3 IC50 = 7.2 nM
4 IC50 = 200 nM
CP0964113
2-amino-9-[(2R,5R,7R,8R,10R,12aR,14R,15aS,16R)-16-hydroxy-2,10-dioxido-14(pyrimidin-4-ylamino)-2,10-disulfanyldecahydro-5,8-methanocyclopenta[l][1,3,6,9,11,2,10]pentaoxadiphosphacyclotetradecin-7-yl]-1,9-dihydro-6H-purin-6-one
   Show/Hide
C20H26N8O9P2S2
 1
1 EC50 = 85 nM
CP0965563
2-amino-9-[(2R,5R,7R,8R,10R,12aR,14R,15aS,16R)-16-hydroxy-2,10-dioxido-14(pyrimidin-4-yloxy)-2,10-disulfanyldecahydro-5,8-methanocyclopenta[l][1,3,6,9,11,2,10]pentaoxadiphosphacyclotetradecin-7-yl]-1,9-dihydro-6H-purin-6-one
   Show/Hide
C20H25N7O10P2S2
 1
1 EC50 = 102 nM
CP0130028
1-[(2-chloro-6-fluorophenyl)methyl]-3,3-dimethyl-2-oxo-N-[(2,4,6-trifluorophenyl)methyl]indole-6-carboxamide
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C25H19ClF4N2O2
 1
1 EC50 = 185 nM
CP0494967
CHEMBL5093161
   Show/Hide
C20H24N10O10P2S2
 2
1 EC50 = 700 nM
2 IC50 = 45.3 nM
CP0069083
1-[4-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]benzimidazol-1-yl]butyl]-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]benzimidazole-5-carboxamide
   Show/Hide
C34H38N12O4
 5
1 EC50 = 3100 nM
2 IC50 = 6.163 nM
3 IC50 = 20000 nM
4 Kd = 1.6 nM
5 Ki = 14 nM
CP0353766
N-[(5-chloro-7,9-dioxofuro[2,3-f][1,3]benzoxazin-2-yl)methyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
   Show/Hide
C18H10ClN5O5
 4
1 EC50 = 4900 nM
2 EC50 = 7100 nM
3 IC50 = 470 nM
4 IC50 = 1400 nM
CP0357335
N-[[5-chloro-7-(2H-tetrazol-5-yl)-1-benzofuran-2-yl]methyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
   Show/Hide
C17H11ClN8O2
 4
1 EC50 = 5900 nM
2 EC50 = 38000 nM
3 IC50 = 1700 nM
4 IC50 = 15000 nM
CP0353763
5-chloro-6-hydroxy-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
   Show/Hide
C17H11ClN4O5
 4
1 EC50 = 6000 nM
2 EC50 = 9200 nM
3 IC50 = 580 nM
4 IC50 = 2500 nM
CP0259616
4-(5,6-dimethoxybenzo[b]thiophen-2-yl)-4- oxobutanoic acid
   Show/Hide
C14H14O5S
 1
1 EC50 = 8300 nM
CP0344146
4-(4-fluoro-5,6-dimethoxybenzo[b]thiophen- 2-yl)-4-oxobutanoic acid
   Show/Hide
C14H13FO5S
 4
1 EC50 = 17000 nM
2 EC50 = 26000 nM
3 IC50 = 1300 nM
4 IC50 = 9400 nM
CP0260705
5-chloro-2-[(1,6-naphthyridine-8-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
   Show/Hide
C19H12ClN3O4
 4
1 EC50 = 18000 nM
2 EC50 = 21000 nM
3 IC50 = 5200 nM
4 IC50 = 23000 nM
CP0273542
5-chloro-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
   Show/Hide
C17H11ClN4O4
 4
1 EC50 = 26000 nM
2 EC50 = 57000 nM
3 IC50 = 5000 nM
4 IC50 = 20000 nM
CP0345476
3-chloro-5-methyl-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
   Show/Hide
C18H13ClN4O4
 4
1 EC50 = 32000 nM
2 EC50 = 52000 nM
3 IC50 = 11000 nM
4 IC50 = 28000 nM
CP0262000
2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
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C17H12N4O4
 4
1 EC50 = 50000 nM
2 EC50 = 71000 nM
3 IC50 = 14000 nM
4 IC50 = 40000 nM
CP0197694
AS-1404
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C17H14O4
 3
1 EC50 > 100000 nM
2 IC50 = 89000 nM
3 IC50 > 100000 nM
CP0260706
2,2,2-trifluoroethyl 5-fluoro-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylate
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C19H12F4N4O4
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0261999
methyl 2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylate
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C18H14N4O4
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0344145
[(2R)-1,1,1-trifluoropropan-2-yl] 5-chloro-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylate
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C20H14ClF3N4O4
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0355729
dimethyl 5-(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)benzene-1,3-dicarboxylate
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C17H14N4O5
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0357336
methyl 2-[(3-oxo-1H-pyrrolo[3,4-c]pyridin-2-yl)methyl]-1-benzofuran-7-carboxylate
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C18H14N2O4
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0550348
tert-butyl N-[3-[6-carbamoyl-3-[(E)-4-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazol-1-yl]but-2-enyl]-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]benzimidazol-4-yl]oxypropyl]carbamate
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C43H53N13O8
 1
1 IC50 = 0.0623 nM
CP0229599
2-ethyl-N-[1-[(E)-4-[2-(2-ethyl-5-methylpyrazole-3-carbonyl)imino-3-methyl-7-(piperidin-1-ylmethyl)benzimidazol-1-yl]but-2-enyl]-3-methylbenzimidazol-2-ylidene]-5-methylpyrazole-3-carboxamide
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C40H49N11O2
 1
1 IC50 < 1 nM
CP0229600
2-ethyl-N-[1-[(E)-4-[2-(2-ethyl-5-methylpyrazole-3-carbonyl)imino-4-(hydroxymethyl)-3-methylbenzimidazol-1-yl]but-2-enyl]-3-methylbenzimidazol-2-ylidene]-5-methylpyrazole-3-carboxamide
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C35H40N10O3
 1
1 IC50 < 1 nM
CP0311616
N-[1-[(E)-4-[7-(1,2-dihydroxyethyl)-2-(2-ethyl-5-methylpyrazole-3-carbonyl)imino-3-methylbenzimidazol-1-yl]but-2-enyl]-3-methylbenzimidazol-2-ylidene]-2-ethyl-5-methylpyrazole-3-carboxamide
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C36H42N10O4
 1
1 IC50 < 1 nM
CP0317724
2-ethyl-N-[1-[(E)-4-[2-(2-ethyl-5-methylpyrazole-3-carbonyl)imino-3-methyl-7-(morpholin-4-ylmethyl)benzimidazol-1-yl]but-2-enyl]-3-methylbenzimidazol-2-ylidene]-5-methylpyrazole-3-carboxamide
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C39H47N11O3
 1
1 IC50 < 1 nM
CP0543694
N-[1-[(E)-4-[7-(azepan-1-ylmethyl)-2-(2-ethyl-5-methylpyrazole-3-carbonyl)imino-3-methylbenzimidazol-1-yl]but-2-enyl]-3-methylbenzimidazol-2-ylidene]-2-ethyl-5-methylpyrazole-3-carboxamide
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C41H51N11O2
 1
1 IC50 < 1 nM
CP0576045
2-ethyl-N-[3-[(E)-4-[2-(2-ethyl-5-methylpyrazole-3-carbonyl)imino-7-(3-hydroxypropoxy)-3-methylbenzimidazol-1-yl]but-2-enyl]-4-methoxy-1-methylbenzimidazol-2-ylidene]-5-methylpyrazole-3-carboxamide
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C38H46N10O5
 1
1 IC50 < 1 nM
CP0508261
2-amino-9-[(1R,6S,8R,9R,15R,17R,18R)-8-(9-aminoimidazo[1,2-a]purin-3-yl)-18-fluoro-12-hydroxy-3-oxo-3-sulfanyl-12-sulfanylidene-2,4,11,13,16-pentaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,9]octadecan-17-yl]-1H-purin-6-one
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C23H26FN11O8P2S2
 1
1 IC50 = 2 nM
CP0547883
2-amino-9-[(1R,6R,8S,9R,10S,15S,17S,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
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C20H24N10O13P2
 4
1 IC50 = 4.6 nM
2 Kd = 0.2 nM
3 Kd = 42000 nM
4 Kd = 79000 nM
CP0248590
benzyl N-[3-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazol-1-yl]propyl]carbamate
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C27H31N7O5
 1
1 IC50 = 582.1 nM
CP0243314
benzyl N-[3-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-(3-morpholin-4-ylpropoxy)benzimidazol-1-yl]propyl]carbamate
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C33H42N8O6
 1
1 IC50 = 936.5 nM
CP0069029
tert-butyl N-[3-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazol-1-yl]propyl]carbamate
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C24H33N7O5
 1
1 IC50 = 1539 nM
CP0158278
2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-1-propylbenzimidazole-5-carboxamide
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C18H22N6O2
 1
1 IC50 = 1737 nM
CP0575979
2-methoxy-5,6-dimethyl-10H-acridin-9-one
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C16H15NO2
 2
1 IC50 = 1920 nM
2 Kd = 26400 nM
CP0394146
2-(6-tert-butyl-3-chloro-4-methoxy-9-oxoacridin-10-yl)acetic acid
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C20H20ClNO4
 1
1 IC50 < 20000 nM
CP0177169
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
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C20H24N10O13P2
 1
1 Kd = 1040 nM
CP0160324
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
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C20H24N10O14P2
 2
1 Kd = 1210 nM
2 Kd = 5200 nM
Clinical Information about the Protein
Target 1 ( Stimulator of interferon genes protein (TMEM173) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Aicardi-Goutieres syndrome [ICD-11: 5C55.2]
Investigative Drug(s) 2 Investigative Drugs  2
1 C-176 Investigative
Aicardi-Goutieres syndrome
2 C-178 Investigative
Aicardi-Goutieres syndrome