Compounds > wz4003
Page last updated: 2024-11-13

wz4003

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Description

WZ4003: inhibits both NUAK1 and NUAK2; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID72200024
CHEMBL ID4303523
MeSH IDM0592038

Synonyms (35)

Synonym
S7317
n-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide
wz-4003
gtpl8047
HY-15802
wz4003
CS-3258
c25h29cln6o3
1214265-58-3
AKOS025142058
wz 4003
n-3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]propanamide
n-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)propionamide
n-(3-((5-chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)propionamide
AC-30128
HMS3653E12
wz4003, >=98% (hplc)
NCGC00386309-05
SW220181-1
A858198
n-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-propanamide
F20676
EX-A2485
Q27089237
BCP09218
HMS3674E13
NCGC00386309-07
CCG-264737
CHEMBL4303523 ,
AS-55863
bdbm50587675
n-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]propanamide
DTXSID601110474
EN300-20128562
n-{3-[(5-chloro-2-{[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)oxy]phenyl}propanamide

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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency10.68400.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency6.74120.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency3.37860.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency6.74120.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency6.74120.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency6.74120.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency6.74120.01238.964839.8107AID1645842
[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)
NUAK family SNF1-like kinase 1Homo sapiens (human)IC50 (µMol)0.01380.00130.29185.0900AID1845553; AID1913078
NUAK family SNF1-like kinase 2Homo sapiens (human)IC50 (µMol)0.10000.00170.56072.6000AID1845578; AID1913079
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (59)

Processvia Protein(s)Taxonomy
protein phosphorylationNUAK family SNF1-like kinase 1Homo sapiens (human)
DNA damage responseNUAK family SNF1-like kinase 1Homo sapiens (human)
cell adhesionNUAK family SNF1-like kinase 1Homo sapiens (human)
regulation of cell adhesionNUAK family SNF1-like kinase 1Homo sapiens (human)
regulation of myosin-light-chain-phosphatase activityNUAK family SNF1-like kinase 1Homo sapiens (human)
regulation of cell population proliferationNUAK family SNF1-like kinase 1Homo sapiens (human)
regulation of signal transduction by p53 class mediatorNUAK family SNF1-like kinase 1Homo sapiens (human)
regulation of cellular senescenceNUAK family SNF1-like kinase 1Homo 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)
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)
protein phosphorylationNUAK family SNF1-like kinase 2Homo sapiens (human)
apoptotic processNUAK family SNF1-like kinase 2Homo sapiens (human)
actin cytoskeleton organizationNUAK family SNF1-like kinase 2Homo sapiens (human)
protein localization to nucleusNUAK family SNF1-like kinase 2Homo sapiens (human)
regulation of hippo signalingNUAK family SNF1-like kinase 2Homo sapiens (human)
cellular response to glucose starvationNUAK family SNF1-like kinase 2Homo sapiens (human)
negative regulation of apoptotic processNUAK family SNF1-like kinase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
p53 bindingNUAK family SNF1-like kinase 1Homo sapiens (human)
protein serine/threonine kinase activityNUAK family SNF1-like kinase 1Homo sapiens (human)
protein bindingNUAK family SNF1-like kinase 1Homo sapiens (human)
ATP bindingNUAK family SNF1-like kinase 1Homo sapiens (human)
metal ion bindingNUAK family SNF1-like kinase 1Homo sapiens (human)
protein serine kinase activityNUAK family SNF1-like kinase 1Homo 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)
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)
magnesium ion bindingNUAK family SNF1-like kinase 2Homo sapiens (human)
protein serine/threonine kinase activityNUAK family SNF1-like kinase 2Homo sapiens (human)
protein bindingNUAK family SNF1-like kinase 2Homo sapiens (human)
ATP bindingNUAK family SNF1-like kinase 2Homo sapiens (human)
protein serine kinase activityNUAK family SNF1-like kinase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
fibrillar centerNUAK family SNF1-like kinase 1Homo sapiens (human)
nucleusNUAK family SNF1-like kinase 1Homo sapiens (human)
nucleoplasmNUAK family SNF1-like kinase 1Homo sapiens (human)
cytoplasmNUAK family SNF1-like kinase 1Homo sapiens (human)
microtubule cytoskeletonNUAK family SNF1-like kinase 1Homo 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)
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
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.
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.
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.
AID1755886Antiproliferative activity against human U2OS cells assessed as reduction in cell viability at 10 uM measured after 1 to 5 days by MTT assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755907Induction of apoptosis in human U2OS cells assessed as viable cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 95.5%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755910Induction of apoptosis in human U2OS cells assessed as necrotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 0.4%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755894Antiproliferative activity against human SW480 cells at 2.5 to 10 uM measured after 48 hrs by EdU staining based assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755908Induction of apoptosis in human U2OS cells assessed as early apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 2.8%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755913Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 1.6%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755918Induction of apoptosis in human SW480 cells assessed as necrotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 1.4%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1845553Inhibition of N-terminal GST-tagged wild type human NUAK1 expressed in Escherichia coli DH5alpha incubated for 30 mins in presence of gamma-[32P]ATP by cerenkov counting analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Development and Therapeutic Potential of NUAKs Inhibitors.
AID1755909Induction of apoptosis in human U2OS cells assessed as late apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 1.3%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755892Antiproliferative activity against human U2OS cells at 2.5 to 10 uM measured after 48 hrs by EdU staining based assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755884Inhibition of NUAK1 (unknown origin) at 10 uM using CHKtide as substrate in presence of ATP measured after 60 mins by ADP-Glo assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755917Induction of apoptosis in human SW480 cells assessed as late apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 2.8%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755911Induction of apoptosis in human HCT-116 cells assessed as viable cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 95.4%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755914Induction of apoptosis in human HCT-116 cells assessed as necrotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 2.2%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755885Inhibition of NUAK2 (unknown origin) at 10 uM using CHKtide as substrate in presence of ATP measured after 60 mins by ADP-Glo assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755888Antiproliferative activity against human SW480 cells assessed as reduction in cell viability at 10 uM measured after 1 to 5 days by MTT assay relative to control2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755915Induction of apoptosis in human SW480 cells assessed as viable cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 93.2%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755912Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 0.8%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755916Induction of apoptosis in human SW480 cells assessed as early apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 2.6%)2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1755893Antiproliferative activity against human HCT-116 cells at 2.5 to 10 uM measured after 48 hrs by EdU staining based assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
AID1845578Inhibition of N-terminal GST-tagged human NUAK2 expressed in Escherichia coli DH5alpha incubated for 30 mins in presence of gamma-[32P]ATP by cerenkov counting analysis2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Development and Therapeutic Potential of NUAKs Inhibitors.
AID1755887Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability at 10 uM measured after 1 to 5 days by MTT assay relative to control2021European journal of medicinal chemistry, Jan-15, Volume: 210Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer.
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.
AID1347013Human NUAK family, SNF1-like kinase, 2 (NuaK subfamily)2014The Biochemical journal, Jan-01, Volume: 457, Issue:1
Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.
AID1345741Human NUAK family kinase 1 (NuaK subfamily)2014The Biochemical journal, Jan-01, Volume: 457, Issue:1
Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (37.50)24.3611
2020's5 (62.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.06

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 Index24.06 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
sb 225002
[no description available]		2.1510nitrophenol
su 11248
[no description available]		3.4110monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
bx795
BX795: structure in first source		3.4110ureas
gsk 461364
GSK 461364: an antineoplastic agent that inhibits polo-like kinase 1		3.4110(trifluoromethyl)benzenes
nvp-tae684
[no description available]		3.4110piperidines
fedratinib
fedratinib: a selective small-molecule inhibitor of JAK2		3.4110sulfonamide
interleukin-8
Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.		2.1510
mrt67307
MRT67307: IKK (IκB(inhibitor of NF-κB (nuclear factor κB)) kinase) family inhibitor; structure in first source		3.4110aromatic amine
4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide
4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide: a protein kinase inhibitor; structure in first source		3.4110
thiopental sodium
[no description available]		3.4110organochlorine compound;
piperazines;
pyrimidines		antineoplastic agent;
tyrosine kinase inhibitor
bay 1000394
roniciclib: an antineoplastic agent that inhibits cyclin-dependent kinases; structure in first source		3.4110
on123300
ON123300: a protein kinase inhibitor; structure in first source		3.4110
hth-01-015
[no description available]		8.9930
ConditionIndicatedRelationship StrengthStudiesTrials
Benign Neoplasms
[description not available]		02.110
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.		02.110
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
Experimental Neoplasms
[description not available]		02.3110
Colorectal Cancer
[description not available]		07.3110
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		02.3110
Disease Exacerbation
[description not available]		03.2310