Page last updated: 2024-11-12

luf 6000

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID11711282
CHEMBL ID475346
SCHEMBL ID936823
MeSH IDM0499724

Synonyms (21)

Synonym
luf-6000
CHEMBL475346 ,
HY-13236
luf6000
CS-1158
890087-21-5
SCHEMBL936823
2-cyclohexyl-n-(3,4-dichlorophenyl)-1h-imidazo[4,5-c]quinolin-4-amine
DTXSID30470994
n-(3,4-dichloro-phenyl)-2-cyclohexyl-1h-imidazo[4,5-c]quinolin-4-amine
gtpl9446
2-cyclohexyl-n-(3,4-dichlorophenyl)-3h-imidazo[5,4-c]quinolin-4-amine
NCGC00378900-01
luf 6000
BCP25002
2-cyclohexyl-n-(3,4-dichlorophenyl)-3h-imidazo[4,5-c]quinolin-4-amine
A923164
F84893
MS-27099
bdbm50588808
AKOS040741978

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency6.00810.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency6.00810.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency6.00810.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency6.00810.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency6.00810.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine receptor A3Homo sapiens (human)Ki2.00000.00000.930610.0000AID1849483
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (56)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (30)

Assay IDTitleYearJournalArticle
AID265775Decrease in dissociation of [125I]I-AB-MECA from human adenosine A3 receptor in CHO membrane at 10 uM relative to control after 30 min2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
AID370762Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells at 10 uM2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
AID370767Intrinsic activity at human adenosine A3 receptor expressed in CHO cells assessed as increase in C1IB-MECA-stimulated inhibition of forskolin-induced cAMP release at 10 uM by TR-FRET assay2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
AID1849420Positive allosteric modulator activity in human A3AR opioid receptor stably expressed in human HEK293 cell membrane assessed as decrease in radioligand [125I]I-AB-MECA dissociation from A3AR receptor by measuring remaining radioligand-bound receptor at 10
AID265772Agonist activity at human adenosine A2B receptor assessed as inhibition of NECA-induced cAMP accumulation in CHO membrane at 10 uM2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
AID265774Displacement of [125I]I-AB-MECA from human adenosine A3 receptor in CHO membrane at 10 uM2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
AID418848Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells at 10 uM2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
AID370761Displacement of [125I]AB-MECA from human adenosine A1 receptor expressed in CHO cells at 10 uM2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
AID370764Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cells at 10 uM2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
AID1232373Positive allosteric modulator activity at human A3 adenosine receptor assessed as potentiation of maximum efficacy of Cl-IB-MECA2015Bioorganic & medicinal chemistry, Jul-15, Volume: 23, Issue:14
Understanding allosteric interactions in G protein-coupled receptors using Supervised Molecular Dynamics: A prototype study analysing the human A3 adenosine receptor positive allosteric modulator LUF6000.
AID418847Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293 cells at 10 uM2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
AID418850Increase in efficacy of stimulation of [35S]GTPgammaS binding to human adenosine A3 receptor expressed in CHO cells at 10 uM by liquid scintillation counting relative to C1-IB-MECA2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
AID370763Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells at 10 uM2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
AID265769Displacement of [3H]R-PIA from human adenosine A1 receptor in CHO membrane at 10 uM2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
AID370765Binding affinity to human adenosine A1 receptor expressed in CHO cells assessed as enhancement of DPCPX-induced displacement of [125I]AB-MECA from receptor at 10 uM after 90 mins relative to control2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
AID1849421Positive allosteric modulator activity in human A3AR opioid receptor stably expressed in human HEK293 cell membrane assessed as net change in radioligand [125I]I-AB-MECA equilibrium binding to A3AR receptor at 10 uM incubated for 18 hrs by radioligand com
AID370766Binding affinity to human adenosine A3 receptor expressed in CHO cells assessed as enhancement of C1IB-MECA-induced displacement of [125I]AB-MECA from receptor at 10 uM after 90 mins relative to control2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
AID1849422Positive allosteric modulator activity in wild type human A3AR opioid receptor stably expressed in human HEK293 cell membrane assessed as increase in CI-IB-MECA induced [35S]GTPGAgammaS binding to receptor at 1 uM preincubated for 1 hrs with CI-IB-MECA fu
AID418849Decrease in dissociation of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells at 10 uM after 60 mins relative to control2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
AID706373Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as potentiation of Cl-IB-MECA-induced [35S]GTPgammaS binding after 20 mins2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.
AID418846Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells at 10 uM2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
AID1849483Positive allosteric modulator activity in human wild type A3AR receptor stably expressed in human HEK293 cell membrane assessed as inhibition of radioligand [125I]-ABOPX orthosteric binding incubated for 18 hrs in presence of PSB603 by equilibrium radioli
AID265776Increase of efficacy at human adenosine A3 receptor in CHO membrane at 10 uM relative to 2-Cl-IB-MECA2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
AID265771Displacement of [3H]R-PIA from human adenosine A2A receptor in HEK293 cells at 10 uM2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1345822Human A3 receptor (Adenosine receptors)2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (33.33)29.6817
2010's3 (33.33)24.3611
2020's3 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.36

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.36 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.36)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]