Compounds > ly2857785
Page last updated: 2024-11-13

ly2857785

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Cross-References

ID SourceID
PubMed CID78357764
CHEMBL ID3940387
MeSH IDM000602425

Synonyms (20)

Synonym
S7511
ly2857785
CS-3336
HY-12293
1619903-54-6
CHEMBL3940387 ,
AKOS030526612
NCGC00390634-01
bdbm50193097
trans-n1-(4-(3-isopropyl-2-methyl-2h-indazol-5-yl)pyrimidin-2-yl)-n4-(tetrahydro-2h-pyran-4-yl)cyclohexane-1,4-diamine
BCP24053
ly-2857785;ly 2857785
EX-A1714
BS-15873
SB18859
1619903-55-7
4-n-[4-(2-methyl-3-propan-2-ylindazol-5-yl)pyrimidin-2-yl]-1-n-(oxan-4-yl)cyclohexane-1,4-diamine
CCG-269222
ly-2857785
AC-35707

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 (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency0.10440.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency37.90830.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency15.09160.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency21.31740.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency3.85120.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
[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)
Cyclin-T1Homo sapiens (human)IC50 (µMol)0.01100.00100.55858.0000AID1317358
Cyclin-CHomo sapiens (human)IC50 (µMol)0.01600.00500.67925.9000AID1317359
Cyclin-dependent kinase 8Homo sapiens (human)IC50 (µMol)0.01600.00341.02755.9000AID1317359
Cyclin-dependent kinase 7Homo sapiens (human)IC50 (µMol)0.24600.00010.91069.2000AID1317360
Cyclin-dependent kinase 9Homo sapiens (human)IC50 (µMol)0.01100.00100.62368.0000AID1317358
Cyclin-HHomo sapiens (human)IC50 (µMol)0.24600.00051.08239.2000AID1317360
CDK-activating kinase assembly factor MAT1Homo sapiens (human)IC50 (µMol)0.24600.00301.68929.2000AID1317360
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (83)

Processvia Protein(s)Taxonomy
regulation of cyclin-dependent protein serine/threonine kinase activityCyclin-T1Homo sapiens (human)
transcription by RNA polymerase IICyclin-T1Homo sapiens (human)
response to xenobiotic stimulusCyclin-T1Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IICyclin-T1Homo sapiens (human)
positive regulation by host of viral transcriptionCyclin-T1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-T1Homo sapiens (human)
cell divisionCyclin-T1Homo sapiens (human)
regulation of transcription by RNA polymerase IICyclin-T1Homo sapiens (human)
positive regulation of DNA-templated transcription, elongationCyclin-T1Homo sapiens (human)
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)
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)
DNA repairCyclin-dependent kinase 7Homo sapiens (human)
transcription by RNA polymerase IICyclin-dependent kinase 7Homo sapiens (human)
transcription initiation at RNA polymerase II promoterCyclin-dependent kinase 7Homo sapiens (human)
snRNA transcription by RNA polymerase IICyclin-dependent kinase 7Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-dependent kinase 7Homo sapiens (human)
protein stabilizationCyclin-dependent kinase 7Homo sapiens (human)
cell divisionCyclin-dependent kinase 7Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 7Homo sapiens (human)
regulation of G1/S transition of mitotic cell cycleCyclin-dependent kinase 7Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 7Homo sapiens (human)
regulation of mitotic cell cycleCyclin-dependent kinase 9Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 9Homo sapiens (human)
DNA repairCyclin-dependent kinase 9Homo sapiens (human)
regulation of DNA repairCyclin-dependent kinase 9Homo sapiens (human)
transcription by RNA polymerase IICyclin-dependent kinase 9Homo sapiens (human)
transcription initiation at RNA polymerase II promoterCyclin-dependent kinase 9Homo sapiens (human)
transcription elongation by RNA polymerase IICyclin-dependent kinase 9Homo sapiens (human)
cell population proliferationCyclin-dependent kinase 9Homo sapiens (human)
replication fork processingCyclin-dependent kinase 9Homo sapiens (human)
regulation of mRNA 3'-end processingCyclin-dependent kinase 9Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IICyclin-dependent kinase 9Homo sapiens (human)
positive regulation by host of viral transcriptionCyclin-dependent kinase 9Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-dependent kinase 9Homo sapiens (human)
regulation of muscle cell differentiationCyclin-dependent kinase 9Homo sapiens (human)
nucleus localizationCyclin-dependent kinase 9Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 9Homo sapiens (human)
cellular response to cytokine stimulusCyclin-dependent kinase 9Homo sapiens (human)
negative regulation of protein localization to chromatinCyclin-dependent kinase 9Homo sapiens (human)
positive regulation of protein localization to chromatinCyclin-dependent kinase 9Homo sapiens (human)
transcription elongation-coupled chromatin remodelingCyclin-dependent kinase 9Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 9Homo sapiens (human)
regulation of transcription by RNA polymerase IICyclin-HHomo sapiens (human)
transcription initiation at RNA polymerase II promoterCyclin-HHomo sapiens (human)
protein stabilizationCyclin-HHomo sapiens (human)
regulation of G1/S transition of mitotic cell cycleCyclin-HHomo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityCyclin-HHomo sapiens (human)
G1/S transition of mitotic cell cycleCDK-activating kinase assembly factor MAT1Homo sapiens (human)
nucleotide-excision repairCDK-activating kinase assembly factor MAT1Homo sapiens (human)
regulation of transcription by RNA polymerase IICDK-activating kinase assembly factor MAT1Homo sapiens (human)
transcription initiation at RNA polymerase II promoterCDK-activating kinase assembly factor MAT1Homo sapiens (human)
adult heart developmentCDK-activating kinase assembly factor MAT1Homo sapiens (human)
ventricular system developmentCDK-activating kinase assembly factor MAT1Homo sapiens (human)
negative regulation of apoptotic processCDK-activating kinase assembly factor MAT1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationCDK-activating kinase assembly factor MAT1Homo sapiens (human)
response to calcium ionCDK-activating kinase assembly factor MAT1Homo sapiens (human)
regulation of G1/S transition of mitotic cell cycleCDK-activating kinase assembly factor MAT1Homo sapiens (human)
DNA repairCDK-activating kinase assembly factor MAT1Homo 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 (42)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCyclin-T1Homo sapiens (human)
DNA bindingCyclin-T1Homo sapiens (human)
chromatin bindingCyclin-T1Homo sapiens (human)
protein bindingCyclin-T1Homo sapiens (human)
protein kinase bindingCyclin-T1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activator activityCyclin-T1Homo sapiens (human)
RNA polymerase bindingCyclin-T1Homo sapiens (human)
7SK snRNA bindingCyclin-T1Homo sapiens (human)
DNA-binding transcription factor bindingCyclin-T1Homo sapiens (human)
molecular condensate scaffold activityCyclin-T1Homo sapiens (human)
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)
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)
protein kinase activityCyclin-dependent kinase 7Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 7Homo sapiens (human)
protein bindingCyclin-dependent kinase 7Homo sapiens (human)
ATP bindingCyclin-dependent kinase 7Homo sapiens (human)
ATP-dependent activity, acting on DNACyclin-dependent kinase 7Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 7Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 7Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 7Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCyclin-dependent kinase 9Homo sapiens (human)
transcription coactivator bindingCyclin-dependent kinase 9Homo sapiens (human)
DNA bindingCyclin-dependent kinase 9Homo sapiens (human)
chromatin bindingCyclin-dependent kinase 9Homo sapiens (human)
transcription elongation factor activityCyclin-dependent kinase 9Homo sapiens (human)
protein kinase activityCyclin-dependent kinase 9Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 9Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 9Homo sapiens (human)
protein bindingCyclin-dependent kinase 9Homo sapiens (human)
ATP bindingCyclin-dependent kinase 9Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 9Homo sapiens (human)
kinase activityCyclin-dependent kinase 9Homo sapiens (human)
protein kinase bindingCyclin-dependent kinase 9Homo sapiens (human)
7SK snRNA bindingCyclin-dependent kinase 9Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 9Homo sapiens (human)
RNA polymerase II general transcription initiation factor activityCyclin-HHomo sapiens (human)
protein bindingCyclin-HHomo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-HHomo sapiens (human)
protein bindingCDK-activating kinase assembly factor MAT1Homo sapiens (human)
zinc ion bindingCDK-activating kinase assembly factor MAT1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activator activityCDK-activating kinase assembly factor MAT1Homo 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 (39)

Processvia Protein(s)Taxonomy
nucleolusCyclin-T1Homo sapiens (human)
nucleusCyclin-T1Homo sapiens (human)
nucleusCyclin-T1Homo sapiens (human)
nucleoplasmCyclin-T1Homo sapiens (human)
cytosolCyclin-T1Homo sapiens (human)
cyclin/CDK positive transcription elongation factor complexCyclin-T1Homo sapiens (human)
P-TEFb complexCyclin-T1Homo sapiens (human)
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)
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)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 7Homo sapiens (human)
fibrillar centerCyclin-dependent kinase 7Homo sapiens (human)
male germ cell nucleusCyclin-dependent kinase 7Homo sapiens (human)
nucleusCyclin-dependent kinase 7Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 7Homo sapiens (human)
cytosolCyclin-dependent kinase 7Homo sapiens (human)
plasma membraneCyclin-dependent kinase 7Homo sapiens (human)
perinuclear region of cytoplasmCyclin-dependent kinase 7Homo sapiens (human)
transcription factor TFIIH core complexCyclin-dependent kinase 7Homo sapiens (human)
transcription factor TFIIH holo complexCyclin-dependent kinase 7Homo sapiens (human)
CAK-ERCC2 complexCyclin-dependent kinase 7Homo sapiens (human)
transcription factor TFIIK complexCyclin-dependent kinase 7Homo sapiens (human)
cytoplasmCyclin-dependent kinase 7Homo sapiens (human)
nucleusCyclin-dependent kinase 7Homo sapiens (human)
nucleusCyclin-dependent kinase 9Homo sapiens (human)
nucleusCyclin-dependent kinase 9Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 9Homo sapiens (human)
cyclin/CDK positive transcription elongation factor complexCyclin-dependent kinase 9Homo sapiens (human)
membraneCyclin-dependent kinase 9Homo sapiens (human)
PML bodyCyclin-dependent kinase 9Homo sapiens (human)
cytoplasmic ribonucleoprotein granuleCyclin-dependent kinase 9Homo sapiens (human)
transcription elongation factor complexCyclin-dependent kinase 9Homo sapiens (human)
P-TEFb complexCyclin-dependent kinase 9Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-HHomo sapiens (human)
nucleoplasmCyclin-HHomo sapiens (human)
transcription factor TFIIH core complexCyclin-HHomo sapiens (human)
transcription factor TFIIH holo complexCyclin-HHomo sapiens (human)
CAK-ERCC2 complexCyclin-HHomo sapiens (human)
transcription factor TFIIK complexCyclin-HHomo sapiens (human)
nucleusCyclin-HHomo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCDK-activating kinase assembly factor MAT1Homo sapiens (human)
nucleoplasmCDK-activating kinase assembly factor MAT1Homo sapiens (human)
transcription factor TFIIH core complexCDK-activating kinase assembly factor MAT1Homo sapiens (human)
transcription factor TFIIH holo complexCDK-activating kinase assembly factor MAT1Homo sapiens (human)
CAK-ERCC2 complexCDK-activating kinase assembly factor MAT1Homo sapiens (human)
transcription factor TFIIK complexCDK-activating kinase assembly factor MAT1Homo 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 (11)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID1317359Inhibition of CDK8/cyclin C (unknown origin) using RBER-CHKStide as substrate after 60 mins in presence of 33P-ATP by microbeta scintillation counting analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
AID1317360Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using CDK7/9ptide as substrate after 60 mins in presence of 33P-ATP by microbeta scintillation 2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
AID1317358Inhibition of recombinant human full length C-terminal His6-tagged CDK9/cyclin T1 expressed in baculovirus infected Sf21 insect cells using CDK9ptide as substrate after 60 mins in presence of 33P-ATP by microbeta scintillation counting analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's2 (40.00)24.3611
2020's3 (60.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.35

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 Index20.35 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.35)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
bms 387032
N-(5-(((5-(1,1-dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide: a CDK2 inhibitor with antineoplastic activity; structure in first source. N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-4-carboxamide : A secondary carboxamide resulting from the formal condensation of the carboxy group of piperidine-4-carboxylic acid with the amino group of 5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-amine. It is an ATP-competitive inhibitor of CDK2, CDK7 and CDK9 kinases and exhibits anti-cancer properties.		2.13101,3-oxazoles;
1,3-thiazoles;
organic sulfide;
piperidinecarboxamide;
secondary carboxamide		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
alsterpaullone
alsterpaullone: structure in first source. alsterpaullone : An organic heterotetracyclic compound that is 1,3-dihydro-2H-1-benzazepin-2-one which shares its 4-5 bond with the 3-2 bond of 5-nitro-1H-indole.		2.1310C-nitro compound;
caprolactams;
organic heterotetracyclic compound		anti-HIV-1 agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor
alvocidib
alvocidib: structure given in first source. alvocidib : A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2' position (the (-)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation.		2.1310dihydroxyflavone;
hydroxypiperidine;
monochlorobenzenes;
tertiary amino compound		antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
palbociclib
[no description available]		2.1310aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
pik 75
PIK 75: structure in first source		2.1310
rgb 286638
[no description available]		2.1310
at 7519
4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-pyrazole-3-carboxamide : A member of the class of pryrazoles that is 4-amino-1H-pyrazole-3-carboxylic acid in which the primary amino group has been acylated by a 2,6-dichlorobenzoyl group and in which the carboxylic acid has been converted into a carboxamide by formal condensation with the primary amino group of 4-aminopiperidine.		2.1310dichlorobenzene;
piperidines;
pyrazoles;
secondary carboxamide		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene: has antineoplastic activity; also inhibits Fms-like tyrosine kinase-3; structure in first source		2.1310
p276-00
P276-00: antineoplastic, cyclin-dependent kinase inhibitor; structure in first source		2.1310
meriolin 3
meriolin 3: a cell death-inducing kinase inhibitor; structure in first source		2.1310
ldc067
[no description available]		2.1310
bay 1000394
roniciclib: an antineoplastic agent that inhibits cyclin-dependent kinases; structure in first source		2.1310
abemaciclib
[no description available]		2.1310
dinaciclib
[no description available]		2.1310pyrazolopyrimidine
ConditionIndicatedRelationship StrengthStudiesTrials
Benign Neoplasms
[description not available]		02.1310
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.1310
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510