Page last updated: 2024-12-10

5-chloro-7-[1-piperidinyl(2-pyridinyl)methyl]-8-quinolinol

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 CID3491105
CHEMBL ID1503729
CHEBI ID116455
SCHEMBL ID1239765

Synonyms (22)

Synonym
CCG-195355
OPREA1_323762
OPREA1_457202
MLS000774847 ,
smr000365462
CHEBI:116455
AKOS000808186
AKOS016290624
HMS2743M19
5-chloro-7-[piperidin-1-yl(pyridin-2-yl)methyl]quinolin-8-ol
STL228095
dndi1417601
CHEMBL1503729
5-chloro-7-(piperidin-1-yl(pyridin-2-yl)methyl)qui
F1031-0076
SCHEMBL1239765
bdbm57971
5-chloro-7-[1-piperidinyl(2-pyridinyl)methyl]-8-quinolinol
5-chloro-7-[piperidino(2-pyridyl)methyl]quinolin-8-ol
5-chloranyl-7-[piperidin-1-yl(pyridin-2-yl)methyl]quinolin-8-ol
cid_3491105
Q27199340
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
quinolinesA class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency44.66840.003245.467312,589.2998AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency7.07950.004023.8416100.0000AID485290
Chain A, Beta-lactamaseEscherichia coli K-12Potency0.63100.044717.8581100.0000AID485294
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency22.38720.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency35.48130.177814.390939.8107AID2147
glp-1 receptor, partialHomo sapiens (human)Potency11.22020.01846.806014.1254AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency89.12510.100020.879379.4328AID588453
ATAD5 protein, partialHomo sapiens (human)Potency6.51040.004110.890331.5287AID504467
TDP1 proteinHomo sapiens (human)Potency14.33940.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency11.22020.180013.557439.8107AID1460
thioredoxin glutathione reductaseSchistosoma mansoniPotency3.54810.100022.9075100.0000AID485364
Smad3Homo sapiens (human)Potency20.39410.00527.809829.0929AID588855; AID720534; AID720536
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency37.65050.011212.4002100.0000AID1030
hypothetical protein, conservedTrypanosoma bruceiPotency31.62280.223911.245135.4813AID624173
67.9K proteinVaccinia virusPotency2.81840.00018.4406100.0000AID720579
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency7.94330.707936.904389.1251AID504333
IDH1Homo sapiens (human)Potency14.58100.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency7.07950.035520.977089.1251AID504332
beta-2 adrenergic receptorHomo sapiens (human)Potency31.62280.00586.026332.6427AID492947
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency25.11890.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency44.66840.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency29.09290.00419.984825.9290AID504444
huntingtin isoform 2Homo sapiens (human)Potency25.11890.000618.41981,122.0200AID1688
flap endonuclease 1Homo sapiens (human)Potency44.66840.133725.412989.1251AID588795
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency29.93490.168316.404067.0158AID720504
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency11.22020.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency11.22020.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency11.22020.15855.287912.5893AID540303
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency4.22090.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency21.85280.004611.374133.4983AID624296; AID624297
VprHuman immunodeficiency virus 1Potency31.62281.584919.626463.0957AID651644
Guanine nucleotide-binding protein GHomo sapiens (human)Potency3.54811.995325.532750.1187AID624287
[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)
ADAM10Homo sapiens (human)IC50 (µMol)9.04600.03585.50189.0460AID743259
PPP5C protein, partialHomo sapiens (human)IC50 (µMol)42.34900.82781.69742.5670AID2422
nonstructural protein 1Influenza A virus (A/California/07/2009(H1N1))IC50 (µMol)8.01800.200024.4540100.0000AID504329
serine/threonine-protein phosphatase PP1-alpha catalytic subunit isoform 3Homo sapiens (human)IC50 (µMol)2.47702.47703.65556.6460AID2403
disintegrin and metalloproteinase domain-containing protein 17 isoform 1 preproproteinHomo sapiens (human)IC50 (µMol)17.00400.01153.04769.1060AID743260
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
alkaline phosphatase, tissue-nonspecific isozyme isoform 1 preproproteinHomo sapiens (human)EC50 (µMol)81.14800.227025.090486.8000AID1001
streptokinase A precursorStreptococcus pyogenes M1 GASEC50 (µMol)79.43900.06008.9128130.5170AID1902; AID1914
Estrogen receptorRattus norvegicus (Norway rat)EC50 (µMol)150.00000.006022.3670130.5170AID1914
Estrogen receptor betaRattus norvegicus (Norway rat)EC50 (µMol)150.00000.006022.3670130.5170AID1914
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
aryl hydrocarbon receptor nuclear translocatorHomo sapiens (human)AC501.33000.190023.3694115.5100AID651703
protein AF-9 isoform aHomo sapiens (human)AC501.84000.08008.380217.9800AID720495
transforming acidic coiled-coil-containing protein 3Homo sapiens (human)AC501.33000.190024.2333115.5100AID651703
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (28)

Processvia Protein(s)Taxonomy
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIHepcidinHomo sapiens (human)
myeloid cell homeostasisHepcidinHomo sapiens (human)
transcription by RNA polymerase IIHepcidinHomo sapiens (human)
intracellular iron ion homeostasisHepcidinHomo sapiens (human)
inflammatory responseHepcidinHomo sapiens (human)
immune responseHepcidinHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATHepcidinHomo sapiens (human)
response to iron ionHepcidinHomo sapiens (human)
protein catabolic processHepcidinHomo sapiens (human)
killing of cells of another organismHepcidinHomo sapiens (human)
iron ion transmembrane transportHepcidinHomo sapiens (human)
macrophage activationHepcidinHomo sapiens (human)
positive regulation of macrophage activationHepcidinHomo sapiens (human)
positive regulation of protein catabolic processHepcidinHomo sapiens (human)
negative regulation of bone resorptionHepcidinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHepcidinHomo sapiens (human)
negative regulation of inflammatory responseHepcidinHomo sapiens (human)
defense response to fungusHepcidinHomo sapiens (human)
establishment of localization in cellHepcidinHomo sapiens (human)
multicellular organismal-level iron ion homeostasisHepcidinHomo sapiens (human)
negative regulation of intestinal absorptionHepcidinHomo sapiens (human)
defense response to bacteriumHepcidinHomo sapiens (human)
negative regulation of iron ion transmembrane transportHepcidinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
hormone activityHepcidinHomo sapiens (human)
copper ion bindingHepcidinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
extracellular regionHepcidinHomo sapiens (human)
nucleusHepcidinHomo sapiens (human)
extracellular spaceHepcidinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (27)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745848Confirmatory qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745849Viability Counterscreen for CMV-Luciferase Assay of Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745847CMV-Luciferase Counterscreen for Inhibitors of ATXN expression
AID1745850Viability Counterscreen for Confirmatory qHTS for Inhibitors of ATXN expression
AID1745846Firefly Luciferase Counterscreen for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1911516Cytotoxicity against human MES-SA cells assessed as cell growth inhibition incubated for 72 hrs by PrestoBlue reagent based cell viability assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Structure-Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer.
AID1911522Cytotoxicity against human A-431 cells expressing ABCB1 assessed as cell growth inhibition incubated for 72 hrs by PrestoBlue reagent based cell viability assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Structure-Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer.
AID1911521Cytotoxicity against human A-431 cells assessed as cell growth inhibition after 72 hrs by PrestoBlue reagent based cell viability assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Structure-Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer.
AID1911523Selectivity ratio of IC50 for cytotoxicity against human A-431 cells assessed as cell growth inhibition to IC50 for cytotoxicity against human A-431 cells expressing ABCB1 assessed as cell growth inhibition2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Structure-Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer.
AID1911519Cytotoxicity against multidrug resistance human MES-SA/Dx5 cells assessed as cell growth inhibition incubated for 72 hrs in presence of P-gp inhibitor Tariquidar by PrestoBlue reagent based cell viability assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Structure-Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer.
AID1911517Selectivity ratio of IC50 for cytotoxicity against human MES-SA cells assessed as cell growth inhibition to IC50 for cytotoxicity against multidrug resistance human MES-SA/Dx5 cells assessed as cell growth inhibition2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Structure-Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer.
AID1911515Cytotoxicity against human MES-SA cells assessed as cell growth inhibition incubated for 72 hrs in presence of P-gp inhibitor Tariquidar by PrestoBlue reagent based cell viability assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Structure-Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer.
AID1911518Cytotoxicity against multidrug resistance human MES-SA/Dx5 cells assessed as cell growth inhibition incubated for 72 hrs by PrestoBlue reagent based cell viability assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Structure-Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer.
AID1911520Selectivity ratio of IC50 for cytotoxicity against human MES-SA cells assessed as cell growth inhibition in presence of P-gp inhibitor Tariquidar to IC50 for cytotoxicity against multidrug resistance human MES-SA/Dx5 cells assessed as cell growth inhibiti2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Structure-Activity Relationships of 8-Hydroxyquinoline-Derived Mannich Bases with Tertiary Amines Targeting Multidrug-Resistant Cancer.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (16.67)29.6817
2010's3 (50.00)24.3611
2020's2 (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: 12.41

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 Index12.41 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]