Compounds > cl 075
Page last updated: 2024-11-12

cl 075

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Cross-References

ID SourceID
PubMed CID10198719
CHEMBL ID512901
SCHEMBL ID482958
MeSH IDM0549461

Synonyms (24)

Synonym
L07 ,
2-propyl[1,3]thiazolo[4,5-c]quinolin-4-amine
CHEMBL512901 ,
cl-075
2-propylthiazolo[4,5-c]quinolin-4-amine
256922-53-9
AKOS016007272
bdbm50398245
NFYMGJSUKCDVJR-UHFFFAOYSA-N
2-propylthiazolo[4,5-c]quinolin4-amine
3M-002 ,
SCHEMBL482958
DTXSID80436686
cl075
2-propyl-[1,3]thiazolo[4,5-c]quinolin-4-amine
gtpl9270
mfcd09998898
cl 075
'cl075; 3m-002'
Q27073740
AS-33295
EX-A5490
HY-117066
CS-0063631
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Toll-like receptor 8Homo sapiens (human)EC50 (µMol)3.11000.48004.26369.0000AID1720360; AID706908
Toll-like receptor 7Homo sapiens (human)EC50 (µMol)18.00000.00721.57446.8000AID1720361
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
regulation of protein phosphorylationToll-like receptor 8Homo sapiens (human)
inflammatory responseToll-like receptor 8Homo sapiens (human)
response to virusToll-like receptor 8Homo sapiens (human)
immunoglobulin mediated immune responseToll-like receptor 8Homo sapiens (human)
negative regulation of interleukin-12 productionToll-like receptor 8Homo sapiens (human)
positive regulation of interferon-alpha productionToll-like receptor 8Homo sapiens (human)
positive regulation of interferon-beta productionToll-like receptor 8Homo sapiens (human)
positive regulation of type II interferon productionToll-like receptor 8Homo sapiens (human)
positive regulation of interleukin-1 beta productionToll-like receptor 8Homo sapiens (human)
positive regulation of interleukin-6 productionToll-like receptor 8Homo sapiens (human)
positive regulation of interleukin-8 productionToll-like receptor 8Homo sapiens (human)
toll-like receptor 8 signaling pathwayToll-like receptor 8Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionToll-like receptor 8Homo sapiens (human)
innate immune responseToll-like receptor 8Homo sapiens (human)
positive regulation of innate immune responseToll-like receptor 8Homo sapiens (human)
defense response to virusToll-like receptor 8Homo sapiens (human)
cellular response to mechanical stimulusToll-like receptor 8Homo sapiens (human)
toll-like receptor signaling pathwayToll-like receptor 8Homo sapiens (human)
canonical NF-kappaB signal transductionToll-like receptor 8Homo sapiens (human)
regulation of protein phosphorylationToll-like receptor 7Homo sapiens (human)
inflammatory responseToll-like receptor 7Homo sapiens (human)
canonical NF-kappaB signal transductionToll-like receptor 7Homo sapiens (human)
I-kappaB phosphorylationToll-like receptor 7Homo sapiens (human)
JNK cascadeToll-like receptor 7Homo sapiens (human)
positive regulation of chemokine productionToll-like receptor 7Homo sapiens (human)
positive regulation of interferon-alpha productionToll-like receptor 7Homo sapiens (human)
positive regulation of interferon-beta productionToll-like receptor 7Homo sapiens (human)
positive regulation of type II interferon productionToll-like receptor 7Homo sapiens (human)
positive regulation of interleukin-8 productionToll-like receptor 7Homo sapiens (human)
toll-like receptor 7 signaling pathwayToll-like receptor 7Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionToll-like receptor 7Homo sapiens (human)
innate immune responseToll-like receptor 7Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIToll-like receptor 7Homo sapiens (human)
positive regulation of inflammatory responseToll-like receptor 7Homo sapiens (human)
defense response to virusToll-like receptor 7Homo sapiens (human)
positive regulation of macrophage cytokine productionToll-like receptor 7Homo sapiens (human)
response to cGMPToll-like receptor 7Homo sapiens (human)
cellular response to mechanical stimulusToll-like receptor 7Homo sapiens (human)
cellular response to virusToll-like receptor 7Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionToll-like receptor 7Homo sapiens (human)
toll-like receptor signaling pathwayToll-like receptor 7Homo sapiens (human)
positive regulation of interleukin-6 productionToll-like receptor 7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
DNA bindingToll-like receptor 8Homo sapiens (human)
RNA bindingToll-like receptor 8Homo sapiens (human)
double-stranded RNA bindingToll-like receptor 8Homo sapiens (human)
single-stranded RNA bindingToll-like receptor 8Homo sapiens (human)
signaling receptor activityToll-like receptor 8Homo sapiens (human)
pattern recognition receptor activityToll-like receptor 8Homo sapiens (human)
double-stranded RNA bindingToll-like receptor 7Homo sapiens (human)
single-stranded RNA bindingToll-like receptor 7Homo sapiens (human)
protein bindingToll-like receptor 7Homo sapiens (human)
siRNA bindingToll-like receptor 7Homo sapiens (human)
pattern recognition receptor activityToll-like receptor 7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
Golgi membraneToll-like receptor 8Homo sapiens (human)
endoplasmic reticulum membraneToll-like receptor 8Homo sapiens (human)
external side of plasma membraneToll-like receptor 8Homo sapiens (human)
endosome membraneToll-like receptor 8Homo sapiens (human)
endolysosome membraneToll-like receptor 8Homo sapiens (human)
plasma membraneToll-like receptor 8Homo sapiens (human)
Golgi membraneToll-like receptor 7Homo sapiens (human)
cytoplasmToll-like receptor 7Homo sapiens (human)
lysosomeToll-like receptor 7Homo sapiens (human)
endosomeToll-like receptor 7Homo sapiens (human)
endoplasmic reticulumToll-like receptor 7Homo sapiens (human)
endoplasmic reticulum membraneToll-like receptor 7Homo sapiens (human)
plasma membraneToll-like receptor 7Homo sapiens (human)
endosome membraneToll-like receptor 7Homo sapiens (human)
early phagosomeToll-like receptor 7Homo sapiens (human)
endolysosome membraneToll-like receptor 7Homo sapiens (human)
receptor complexToll-like receptor 7Homo sapiens (human)
plasma membraneToll-like receptor 7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (64)

Assay IDTitleYearJournalArticle
AID766314Agonist activity at TLR8 in human PBMC assessed as increase of IFNA21 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID341159Toxic induction of IL1-beta level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Investigating Toll-like receptor agonists for potential to treat hepatitis C virus infection.
AID706907Induction of proinflammatory cytokine release in human PBMC after 12 hrs2012Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
Structure-activity relationships in human Toll-like receptor 8-active 2,3-diamino-furo[2,3-c]pyridines.
AID766294Agonist activity at TLR8 in human PBMC assessed as increase of IL18 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766301Agonist activity at TLR8 in human PBMC assessed as increase of IL1RN mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID341161Toxic induction of IL6 level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Investigating Toll-like receptor agonists for potential to treat hepatitis C virus infection.
AID766299Agonist activity at TLR8 in human PBMC assessed as increase of IL6 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766308Agonist activity at TLR8 in human PBMC assessed as increase of CXCL5 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID341171Increase in 2',5'-oligoadenylate synthase level in human PBMC after 24 hrs by PCR method relative to control2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Investigating Toll-like receptor agonists for potential to treat hepatitis C virus infection.
AID341174Antiviral activity against HCV infected human Huh7 replicon cells treated with 3 uM drug-induced human PBMC supernatants assessed as viral levels in presence of type I IFN receptor antibody by luciferase assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Investigating Toll-like receptor agonists for potential to treat hepatitis C virus infection.
AID766306Agonist activity at TLR8 in human PBMC assessed as increase of CXCL9 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766285Agonist activity at TLR8 in human PBMC assessed as increase of IL29 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID642644Pro-inflammatory activity in human whole blood assessed as TNF-alpha production upto 50 uM2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Potent adjuvantic activity of a CCR1-agonistic bis-quinoline.
AID766283Agonist activity at TLR8 in human PBMC assessed as increase of TNF mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766281Agonist activity at TLR8 in human PBMC assessed as increase of G-CSF level after 12 hrs2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID642647Pro-inflammatory activity in human whole blood assessed as IL-8 production upto 50 uM2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Potent adjuvantic activity of a CCR1-agonistic bis-quinoline.
AID766317Agonist activity at TLR8 in human PBMC assessed as increase of IFNA17 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766287Agonist activity at TLR8 in human PBMC assessed as increase of IL28A mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766311Agonist activity at TLR8 in human PBMC assessed as increase of CXCL1 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766289Agonist activity at TLR8 in human PBMC assessed as decrease of IL24 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766310Agonist activity at TLR8 in human PBMC assessed as increase of IFNG mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID642648Pro-inflammatory activity in human whole blood assessed as IL-12 production upto 50 uM2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Potent adjuvantic activity of a CCR1-agonistic bis-quinoline.
AID766291Agonist activity at TLR8 in human PBMC assessed as increase of IL20 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766292Agonist activity at TLR8 in human PBMC assessed as increase of IL22 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID1845954Reactivation of HIV-1 latency infected in GFP-fused human J-Lat 9.2 cells assessed as increase in GFP expression at 1 uM incubated for 24 hrs by flow cytometry2021European journal of medicinal chemistry, Mar-05, Volume: 213HIV latency reversal agents: A potential path for functional cure?
AID766284Agonist activity at TLR8 in human PBMC assessed as increase of IL32 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID341172Increase in IFNalpha level in human PBMC after 24 hrs relative to control2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Investigating Toll-like receptor agonists for potential to treat hepatitis C virus infection.
AID642646Pro-inflammatory activity in human whole blood assessed as IL-6 production upto 50 uM2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Potent adjuvantic activity of a CCR1-agonistic bis-quinoline.
AID766278Agonist activity at TLR8 in human PBMC assessed as increase of MIP1beta level after 12 hrs2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID642650Antiinflammatory activity in human whole blood assessed as IL-10 production upto 50 uM2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Potent adjuvantic activity of a CCR1-agonistic bis-quinoline.
AID766304Agonist activity at TLR8 in human PBMC assessed as increase of CXCL10 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766295Agonist activity at TLR8 in human PBMC assessed as decrease of IL16 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766280Agonist activity at TLR8 in human PBMC assessed as increase of GRO level after 12 hrs2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID1720361Agonist activity at TLR7 in human cryopreserved PBMC assessed as induction of IFNalpha production measured after 24 hrs2020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B.
AID766279Agonist activity at TLR8 in human PBMC assessed as increase of MIP1alpha level after 12 hrs2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID341169Antiviral activity against HCV infected human Huh7 replicon cells treated with drug-induced human PBMC supernatants assessed as viral levels by luciferase assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Investigating Toll-like receptor agonists for potential to treat hepatitis C virus infection.
AID766307Agonist activity at TLR8 in human PBMC assessed as increase of CXCL3 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766290Agonist activity at TLR8 in human PBMC assessed as increase of IL23A mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766298Agonist activity at TLR8 in human PBMC assessed as increase of IL12B mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766293Agonist activity at TLR8 in human PBMC assessed as increase of IL18RAP mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766300Agonist activity at TLR8 in human PBMC assessed as increase of IL4 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766319Agonist activity at TLR8 in human PBMC assessed as increase of IFNA1 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID642649Pro-inflammatory activity in human whole blood assessed as IL-18 production upto 50 uM2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Potent adjuvantic activity of a CCR1-agonistic bis-quinoline.
AID766313Agonist activity at TLR8 in human PBMC assessed as increase of IFNA8 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766318Agonist activity at TLR8 in human PBMC assessed as increase of IFNA1/IFNA13 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766288Agonist activity at TLR8 in human PBMC assessed as increase of IL27RA mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766309Agonist activity at TLR8 in human PBMC assessed as increase of CXCL2 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766305Agonist activity at TLR8 in human PBMC assessed as increase of CXCL11 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766286Agonist activity at TLR8 in human PBMC assessed as increase of IL28RA mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766297Agonist activity at TLR8 in human PBMC assessed as increase of IL13 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766303Agonist activity at TLR8 in human PBMC assessed as increase of IL1A mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID341177Toxic induction of TNFalpha level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Investigating Toll-like receptor agonists for potential to treat hepatitis C virus infection.
AID341160Induction of IFNalpha2a level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Investigating Toll-like receptor agonists for potential to treat hepatitis C virus infection.
AID642645Pro-inflammatory activity in human whole blood assessed as IL1-beta production upto 50 uM2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Potent adjuvantic activity of a CCR1-agonistic bis-quinoline.
AID766315Agonist activity at TLR8 in human PBMC assessed as increase of IFNA5 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID341170Antiviral activity against HCV infected human Huh7 replicon cells assessed as viral levels by luciferase assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Investigating Toll-like receptor agonists for potential to treat hepatitis C virus infection.
AID766296Agonist activity at TLR8 in human PBMC assessed as increase of IL15 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766302Agonist activity at TLR8 in human PBMC assessed as increase of IL1B mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID706908Agonist activity at human TLR8 expressed in HEK293 cells assessed as induction of NF-kappaB activity by measuring extracellular secreted alkaline phosphatase by HEK-blue reporter gene assay2012Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
Structure-activity relationships in human Toll-like receptor 8-active 2,3-diamino-furo[2,3-c]pyridines.
AID766316Agonist activity at TLR8 in human PBMC assessed as increase of IFNA10 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID766282Agonist activity at TLR8 in human PBMC assessed as increase of TNFAIP6 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID1720360Agonist activity at TLR8 in human cryopreserved PBMC assessed as inhibition of IL-12p40 production measured after 24 hrs2020Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B.
AID766312Agonist activity at TLR8 in human PBMC assessed as increase of IFNA7 mRNA level at 10 ug/mL after 2 hrs relative to negative control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exquisite selectivity for human toll-like receptor 8 in substituted furo[2,3-c]quinolines.
AID1345474Human TLR8 (Toll-like receptor family)2012Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
Structure-activity relationships in human Toll-like receptor 8-active 2,3-diamino-furo[2,3-c]pyridines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (7.14)29.6817
2010's24 (85.71)24.3611
2020's2 (7.14)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.46

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

MetricThis Compound (vs All)
Research Demand Index27.46 (24.57)
Research Supply Index3.37 (2.92)
Research Growth Index5.14 (4.65)
Search Engine Demand Index27.81 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.46)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (96.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.0710aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
juglone
juglone: structure. juglone : A hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone in which the hydrogen at position 5 has been replaced by a hydroxy group. A plant-derived 1,4-naphthoquinone with confirmed antibacterial and antitumor activities.		2.1110hydroxy-1,4-naphthoquinonegeroprotector;
herbicide;
reactive oxygen species generator
4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide
4-(dimethylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)benzamide: structure in first source. 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide : A benzamide resulting from the formal condensation of the carboxy group of 4-(dimethylamino)benzoic acid with the amino group of 7-amino-N-hydroxyheptanamide. It is a potent inhibitor of histone deacetylases and induces cell cycle arrest and apoptosis in several human cancer cell lines.		3.4110benzamides;
hydroxamic acid;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		3.4110dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
thiazoles
[no description available]		5.452201,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
azacitidine
Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia.		3.4110N-glycosyl-1,3,5-triazine;
nucleoside analogue		antineoplastic agent
formal glycol
[no description available]		2.1110cyclic acetal;
dioxolane
imiquimod
Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis.		2.7930imidazoquinolineantineoplastic agent;
interferon inducer
nicotine
(S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.		2.17103-(1-methylpyrrolidin-2-yl)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
glycidyl nitrate
glycidyl nitrate: a nitric oxide donor; structure in first source. peptidoglycan : A peptidoglycosaminoglycan formed by alternating residues of beta-(1->4)-linked N-acetylglucosamine and N-acetylmuramic acid {2-amino-3-O-[(S)-1-carboxyethyl]-2-deoxy-D-glucose} residues. Attached to the carboxy group of the muramic acid is a peptide chain of three to five amino acids.		2.0510
indolactam v
indolactam V: only the (-)-isomer of indolactam V showed carcinogenic activity; structure given in first source		3.4110indoles
resiquimod
S 28463: structure given in first source		3.5880imidazoquinoline
n-formylmethionine leucyl-phenylalanine
N-Formylmethionine Leucyl-Phenylalanine: A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated.. N-formyl-L-methionyl-L-leucyl-L-phenylalanine : A tripeptide composed of L-Met, L-Leu and L-Phe in a linear sequence with a formyl group at the amino terminus. It acts as a potent inducer of leucocyte chemotaxis and macrophage activator as well as a ligand for the FPR receptor.		2.1110tripeptide
trichostatin a
trichostatin A: chelates zinc ion in the active site of histone deacetylases, resulting in preventing histone unpacking so DNA is less available for transcription; do not confuse with TRICHOSANTHIN which is a protein; found in STREPTOMYCES		3.4110antibiotic antifungal agent;
hydroxamic acid;
trichostatin		bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector
12-deoxyphorbol 13-acetate
[no description available]		3.4110phorbol estermetabolite
naphthoquinones
Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.		2.1110
belinostat
[no description available]		3.4110hydroxamic acid;
olefinic compound;
sulfonamide		antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
panobinostat
Panobinostat: An indole and hydroxamic acid derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used as an antineoplastic agent in combination with BORTEZOMIB and DEXAMETHASONE for the treatment of MULTIPLE MYELOMA.. panobinostat : A hydroxamic acid obtained by formal condensation of the carboxy group of (2E)-3-[4-({[2-(2-methylindol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enoic acid with the amino group of hydroxylamine. A histone deacetylase inhibitor used (as its lactate salt) in combination with bortezomib and dexamethasone for the treatment of multiple myeloma.		3.4110cinnamamides;
hydroxamic acid;
methylindole;
secondary amino compound		angiogenesis modulating agent;
antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
n-(2-amino-5-fluorobenzyl)-4-(n-(pyridine-3-acrylyl)aminomethyl)benzamide
[no description available]		3.4110
lipid a
Lipid A: Lipid A is the biologically active component of lipopolysaccharides. It shows strong endotoxic activity and exhibits immunogenic properties.. lipid A : The glycolipid moiety of bacterial lipopolysaccharide (R can be either hydrogen or a fatty acyl group).		2.5220dodecanoate ester;
lipid A;
tetradecanoate ester		Escherichia coli metabolite
mart-1 antigen
MART-1 Antigen: A melanosome-specific protein that plays a role in the expression, stability, trafficking, and processing of GP100 MELANOMA ANTIGEN, which is critical to the formation of Stage II MELANOSOMES. The protein is used as an antigen marker for MELANOMA cells.		2.0510
sm360320
SM360320: Proc Natl Acad Sci U S A 2006 Feb 7;103(6):1828-33		2.0310
bi 2536
[no description available]		3.4110
vtx-2337
[no description available]		2.2510
angiotensinogen
Angiotensinogen: An alpha-globulin of about 453 amino acids, depending on the species. It is produced by the liver in response to lowered blood pressure and secreted into blood circulation. Angiotensinogen is the inactive precursor of the ANGIOTENSINS produced in the body by successive enzyme cleavages. Cleavage of angiotensinogen by RENIN yields the decapeptide ANGIOTENSIN I. Further cleavage of angiotensin I (by ANGIOTENSIN CONVERTING ENZYME) yields the potent vasoconstrictor octapeptide ANGIOTENSIN II; and then, via other enzymes, other angiotensins also involved in the hemodynamic-regulating RENIN-ANGIOTENSIN SYSTEM.		2.1110
oligonucleotides
[no description available]		2.0610
az 505
AZ 505: an SMYD2 inhibitor; structure in first source		3.4110
bix 01294
[no description available]		3.4110piperidines
gardiquimod
[no description available]		2.0510
unc 0638
UNC 0638: inhibits lysine methyltransferases G9a and GLP; structure in first source		3.4110quinazolines
jq1 compound
[no description available]		3.4110carboxylic ester;
organochlorine compound;
tert-butyl ester;
thienotriazolodiazepine		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
bromodomain-containing protein 4 inhibitor;
cardioprotective agent;
ferroptosis inducer
epz-6438
tazemetostat: a histone methyltransferase EZH2 inhibitor with antineoplastic activity		3.4110
gsk343
GSK343: an EZH2 methyltransferase inhibitor. GSK343 : A member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM).		3.4110aminopyridine;
indazoles;
N-alkylpiperazine;
N-arylpiperazine;
pyridone;
secondary carboxamide		antineoplastic agent;
apoptosis inducer;
EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor
2-methoxy-n-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide: a probe for bromo and extra C-terminal domain proteins; structure in first source		3.4110quinazolines
guanosine
ribonucleoside : Any nucleoside where the sugar component is D-ribose.		2.1110guanosines;
purines D-ribonucleoside		fundamental metabolite
loxoribine
[no description available]		2.1110
rvx 208
apabetalone: a bromodomain and extra-terminal domain protein (BET) inhibitor; prevents interactions between BET proteins and acetyl-lysine residues on histone tails to modify epigenetic regulation		3.4110
ConditionIndicatedRelationship StrengthStudiesTrials
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted
[description not available]		02.4720
Hepatitis C
INFLAMMATION of the LIVER in humans caused by HEPATITIS C VIRUS, a single-stranded RNA virus. Its incubation period is 30-90 days. Hepatitis C is transmitted primarily by contaminated blood parenterally and is often associated with transfusion and intravenous drug abuse. However, in a significant number of cases, the source of hepatitis C infection is unknown.		02.4720
Innate Inflammatory Response
[description not available]		02.0710
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.0710
Chronic Hepatitis B
[description not available]		02.2510
Hepatitis B, Chronic
INFLAMMATION of the LIVER in humans caused by HEPATITIS B VIRUS lasting six months or more. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.		02.2510
HIV Coinfection
[description not available]		04.6530
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		04.6530
E coli Infections
[description not available]		02.1510
Escherichia coli Infections
Infections with bacteria of the species ESCHERICHIA COLI.		02.1510
Co-infection
[description not available]		02.1310
Arthritides, Bacterial
[description not available]		02.1310
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.		02.1310
EBV Infections
[description not available]		02.1510
Sclerosis, Systemic
[description not available]		02.1510
Scleroderma, Systemic
A chronic multi-system disorder of CONNECTIVE TISSUE. It is characterized by SCLEROSIS in the SKIN, the LUNGS, the HEART, the GASTROINTESTINAL TRACT, the KIDNEYS, and the MUSCULOSKELETAL SYSTEM. Other important features include diseased small BLOOD VESSELS and AUTOANTIBODIES. The disorder is named for its most prominent feature (hard skin), and classified into subsets by the extent of skin thickening: LIMITED SCLERODERMA and DIFFUSE SCLERODERMA.		02.1510
Epstein-Barr Virus Infections
Infection with human herpesvirus 4 (HERPESVIRUS 4, HUMAN); which may facilitate the development of various lymphoproliferative disorders. These include BURKITT LYMPHOMA (African type), INFECTIOUS MONONUCLEOSIS, and oral hairy leukoplakia (LEUKOPLAKIA, HAIRY).		02.1510
Libman-Sacks Disease
[description not available]		02.0610
Lupus Erythematosus, Systemic
A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow.		02.0610
Jaundice, Cholestatic
[description not available]		02.0710
Cirrhosis, Liver
[description not available]		02.0710
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		02.0710
Jaundice, Obstructive
Jaundice, the condition with yellowish staining of the skin and mucous membranes, that is due to impaired BILE flow in the BILIARY TRACT, such as INTRAHEPATIC CHOLESTASIS, or EXTRAHEPATIC CHOLESTASIS.		02.0710