Page last updated: 2024-12-10

2-amino-6-methyl-4-(3-pyridinyl)-5,6,7,8-tetrahydroquinoline-3-carbonitrile

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 CID3835861
CHEMBL ID1409113
CHEBI ID121361
SCHEMBL ID19853152

Synonyms (33)

Synonym
2-amino-6-methyl-4-pyridin-3-yl-5,6,7,8-tetrahydroquinoline-3-carbonitrile
MLS000114823 ,
smr000092114
CHEBI:121361
AKOS001685617
2-amino-6-methyl-4-(pyridin-3-yl)-5,6,7,8-tetrahydroquinoline-3-carbonitrile
STL241555
HMS2255H20
CCG-24881
AKOS022008129
2-amino-6-methyl-4-(3-pyridinyl)-5,6,7,8-tetrahydroquinoline-3-carbonitrile
2-amino-6-methyl-4-(3-pyridyl)-5,6,7,8-tetrahydroquinoline-3-carbonitrile
cid_3835861
2-azanyl-6-methyl-4-pyridin-3-yl-5,6,7,8-tetrahydroquinoline-3-carbonitrile
bdbm62810
SCHEMBL19853152
CHEMBL1409113
Q27209899
SR-01000114347-1
sr-01000114347
642008-81-9
E73437
2-amino-5,6,7,8-tetrahydro-6-methyl-4-(3-pyridinyl)-3-quinolinecarbonitrile
brd 6989
S0771
brd 6989 - bio-x
EX-A3462
CS-0087276
HY-122586
brd6989
MS-23739
AC-36387
BB162589
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
bipyridinesCompounds containing a bipyridine group.
[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 (23)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency5.01190.044717.8581100.0000AID485294
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.18380.177814.390939.8107AID2147
acid sphingomyelinaseHomo sapiens (human)Potency25.118914.125424.061339.8107AID504937
glp-1 receptor, partialHomo sapiens (human)Potency0.89130.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency9.77550.004110.890331.5287AID504467; AID624248; AID624249; AID624251
TDP1 proteinHomo sapiens (human)Potency2.05960.000811.382244.6684AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency10.00000.316212.443531.6228AID902
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency5.17350.00419.984825.9290AID504444
huntingtin isoform 2Homo sapiens (human)Potency1.99530.000618.41981,122.0200AID1688
importin subunit beta-1 isoform 1Homo sapiens (human)Potency0.46115.804836.130665.1308AID540253
snurportin-1Homo sapiens (human)Potency0.46115.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency0.46115.804816.996225.9290AID540253
gemininHomo sapiens (human)Potency32.64270.004611.374133.4983AID624296
[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)
Cyclin-CHomo sapiens (human)IC50 (µMol)10.23700.00500.67925.9000AID1613760; AID1613761; AID1910409
Cyclin-dependent kinase 8Homo sapiens (human)IC50 (µMol)0.42770.00341.02755.9000AID1388681; AID1613760; AID1890141; AID1910409
Cyclin-dependent kinase 19Homo sapiens (human)IC50 (µMol)30.00000.00500.40852.2000AID1388682; AID1613761; AID1890142
[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)
Hsf1 proteinMus musculus (house mouse)EC50 (µMol)1.83400.160024.4900236.5000AID2382
Cyclin-CMus musculus (house mouse)EC50 (µMol)1.40001.40001.40001.4000AID1388683
Cyclin-dependent kinase 8Mus musculus (house mouse)EC50 (µMol)1.40000.02000.71001.4000AID1388683
[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)
Hsf1 proteinMus musculus (house mouse)AC5069.07000.171030.8718167.9780AID493083; AID493085
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
G0 to G1 transitionCyclin-CHomo sapiens (human)
negative regulation of Notch signaling pathwayCyclin-CHomo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-CHomo sapiens (human)
protein ubiquitinationCyclin-dependent kinase 8Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-dependent kinase 8Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 8Homo sapiens (human)
negative regulation of triglyceride metabolic processCyclin-dependent kinase 8Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 8Homo sapiens (human)
positive regulation of apoptotic processCyclin-dependent kinase 19Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 19Homo sapiens (human)
cellular response to lipopolysaccharideCyclin-dependent kinase 19Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 19Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
protein bindingCyclin-CHomo sapiens (human)
identical protein bindingCyclin-CHomo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-CHomo sapiens (human)
protein kinase activityCyclin-dependent kinase 8Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 8Homo sapiens (human)
protein bindingCyclin-dependent kinase 8Homo sapiens (human)
ATP bindingCyclin-dependent kinase 8Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 8Homo sapiens (human)
ubiquitin protein ligase activityCyclin-dependent kinase 8Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 8Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 8Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 19Homo sapiens (human)
ATP bindingCyclin-dependent kinase 19Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 19Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 19Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
cyclin-dependent protein kinase holoenzyme complexCyclin-CHomo sapiens (human)
nucleoplasmCyclin-CHomo sapiens (human)
CKM complexCyclin-CHomo sapiens (human)
nucleusCyclin-CHomo sapiens (human)
mediator complexCyclin-CHomo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 8Homo sapiens (human)
nucleusCyclin-dependent kinase 8Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 8Homo sapiens (human)
nucleolusCyclin-dependent kinase 8Homo sapiens (human)
CKM complexCyclin-dependent kinase 8Homo sapiens (human)
ubiquitin ligase complexCyclin-dependent kinase 8Homo sapiens (human)
mediator complexCyclin-dependent kinase 8Homo sapiens (human)
protein-containing complexCyclin-dependent kinase 8Homo sapiens (human)
nucleusCyclin-dependent kinase 8Homo sapiens (human)
nucleoplasmCyclin-CMus musculus (house mouse)
nucleoplasmCyclin-dependent kinase 8Mus musculus (house mouse)
nucleoplasmCyclin-dependent kinase 19Homo sapiens (human)
cytosolCyclin-dependent kinase 19Homo sapiens (human)
perinuclear region of cytoplasmCyclin-dependent kinase 19Homo sapiens (human)
CKM complexCyclin-dependent kinase 19Homo sapiens (human)
nucleusCyclin-dependent kinase 19Homo sapiens (human)
cytosolCyclin-dependent kinase 19Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (24)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1890141Inhibition of recombinant CDK8 (unknown origin)2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.
AID1388682Inhibition of CDK19 (unknown origin)2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1613761Inhibition of recombinant human GST/His-tagged CDK11 (1 to 502 residues)/cyclinC (1 to 283 residues) catalytic domain expressed in insect cells by Lantha screen eu binding assay2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1890181Selectivity index, ratio of IC50 for recombinant CDK19 (unknown origin) to IC50 for recombinant CDK8 (unknown origin)2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.
AID1910406Transcriptional activity of AP-1 in R848-stimulated mouse BMDC cells transfected with pAP1-luc assessed as ratio of AP-1 activity at 5 uM treated for 24 hrs followed by R484 stimulation for 4 hrs by luminescence based microplate reader analysis relative t2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Discovery and Anti-Inflammatory Activity Evaluation of a Novel CDK8 Inhibitor through Upregulation of IL-10 for the Treatment of Inflammatory Bowel Disease
AID1890142Inhibition of recombinant CDK19 (unknown origin)2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery Efforts.
AID1910405Anti-inflammatory activity against R848-stimulated mouse BMDC cells assessed as upregulation of IL-10 production at 5 uM treated for 24 hrs followed by R484 stimulation for 12 hrs by ELISA method (Rvb = 100 %)2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Discovery and Anti-Inflammatory Activity Evaluation of a Novel CDK8 Inhibitor through Upregulation of IL-10 for the Treatment of Inflammatory Bowel Disease
AID1613760Inhibition of recombinant full-length human His-tagged CDK8/cyclinC expressed in baculovirus expression system by Lantha screen assay2019European journal of medicinal chemistry, Feb-15, Volume: 164CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.
AID1910409Inhibition of recombinant full length His tagged human CDK8/Cyclin C expressed in Baculovirus incubated for 60 mins in presence of ATP by ADP-Glo kinase assay2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Discovery and Anti-Inflammatory Activity Evaluation of a Novel CDK8 Inhibitor through Upregulation of IL-10 for the Treatment of Inflammatory Bowel Disease
AID1388681Inhibition of CDK8 (unknown origin)2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
AID1388683Inhibition of CDK8/Cyclin-C in R848-stimulated mouse BMDC assessed as upregulation of IL-10 level2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
[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's1 (11.11)29.6817
2010's5 (55.56)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: 12.40

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 Index12.40 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.70 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.40)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (33.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]