Compounds > unc569
Page last updated: 2024-11-13

unc569

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Description

UNC569: an antineoplastic agent that inhibits Mer protein; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID53355503
CHEMBL ID2036808
SCHEMBL ID12185720
SCHEMBL ID14755115
SCHEMBL ID17173901
SCHEMBL ID17178092
MeSH IDM000595258

Synonyms (29)

Synonym
SCHEMBL12185720
bdbm50384576
ckj ,
1-[(trans-4-aminocyclohexyl)methyl]-n-butyl-3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidin-6-amine
chembl2036808 ,
SCHEMBL14755115
1350547-65-7
1-((4-aminocyclohexyl)methyl)-n-butyl-3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidin-6-amine
unc569
SCHEMBL17173901
SCHEMBL17178092
NCGC00386692-01
1-(((1r,4r)-4-aminocyclohexyl)methyl)-n-butyl-3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidin-6-amine
1-((trans-4-aminocyclohexyl)methyl)-n-butyl-3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidin-6-amine
Q27458844
EX-A2464
rel-1-(((1r,4r)-4-aminocyclohexyl)methyl)-n-butyl-3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidin-6-amine
AS-35154
AC-36081
bdbm336260
us9744172, compound unc00000569a
unc-569;unc 569
BCP27883
1-[(4-aminocyclohexyl)methyl]-n-butyl-3-(4-fluorophenyl)pyrazolo[3,4-d]pyrimidin-6-amine
unc 569
unc-569
AKOS037643757
HY-117596
CS-0066589

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Treatment with UNC569 reduced proliferation/survival in liquid culture, decreased colony formation in methylcellulose/soft agar, and increased sensitivity to cytotoxic chemotherapies."( UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo.
Batchelor, LA; Christoph, S; Cummings, CT; Deryckere, D; Earp, HS; Frazer, JK; Frye, SV; Graham, DK; Hull-Ryde, EA; Hunter, DM; Janzen, WP; Johnson, GL; Kireev, D; Liu, J; Norris-Drouin, J; Sather, S; Schlegel, J; Simpson, C; Trakhimets, AY; Wang, X; Yang, C, 2013)		2.17

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

Dosage Studied

ExcerptRelevanceReference
" To investigate the influence of dosing time on MerTK inhibitor UNC569-induced retinal toxicity, UNC569 at 100 mg/kg was orally administered to male mice at 2 different Zeitgeber times (ZT5."( The Impact of the Timing of Dosing on the Severity of UNC569-Induced Ultrastructural Changes in the Mouse Retina.
Imaoka, M; Kai, K; Mori, K; Okado, K; Samata, N; Sayama, A; Yamaguchi, M, 2020)		1.05
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency8.06490.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency8.06490.00339.158239.8107AID1347411
[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)
Tyrosine-protein kinase receptor UFOHomo sapiens (human)IC50 (µMol)0.03700.00070.41169.1000AID1374833; AID663571; AID738487
Tyrosine-protein kinase receptor TYRO3Homo sapiens (human)IC50 (µMol)0.04800.00140.05730.3010AID663572; AID738486
Tyrosine-protein kinase MerHomo sapiens (human)IC50 (µMol)0.03740.00050.28634.9000AID1374834; AID663570; AID663580; AID738488
Tyrosine-protein kinase MerHomo sapiens (human)Ki0.00430.00030.01150.0300AID663575
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (88)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
neuron migrationTyrosine-protein kinase receptor UFOHomo sapiens (human)
positive regulation of cytokine-mediated signaling pathwayTyrosine-protein kinase receptor UFOHomo sapiens (human)
blood vessel remodelingTyrosine-protein kinase receptor UFOHomo sapiens (human)
phagocytosisTyrosine-protein kinase receptor UFOHomo sapiens (human)
inflammatory responseTyrosine-protein kinase receptor UFOHomo sapiens (human)
signal transductionTyrosine-protein kinase receptor UFOHomo sapiens (human)
spermatogenesisTyrosine-protein kinase receptor UFOHomo sapiens (human)
negative regulation of macrophage cytokine productionTyrosine-protein kinase receptor UFOHomo sapiens (human)
forebrain cell migrationTyrosine-protein kinase receptor UFOHomo sapiens (human)
animal organ regenerationTyrosine-protein kinase receptor UFOHomo sapiens (human)
negative regulation of type II interferon productionTyrosine-protein kinase receptor UFOHomo sapiens (human)
negative regulation of tumor necrosis factor productionTyrosine-protein kinase receptor UFOHomo sapiens (human)
positive regulation of natural killer cell differentiationTyrosine-protein kinase receptor UFOHomo sapiens (human)
secretion by cellTyrosine-protein kinase receptor UFOHomo sapiens (human)
erythrocyte homeostasisTyrosine-protein kinase receptor UFOHomo sapiens (human)
substrate adhesion-dependent cell spreadingTyrosine-protein kinase receptor UFOHomo sapiens (human)
cellular response to interferon-alphaTyrosine-protein kinase receptor UFOHomo sapiens (human)
ovulation cycleTyrosine-protein kinase receptor UFOHomo sapiens (human)
negative regulation of neuron apoptotic processTyrosine-protein kinase receptor UFOHomo sapiens (human)
innate immune responseTyrosine-protein kinase receptor UFOHomo sapiens (human)
symbiont entry into host cellTyrosine-protein kinase receptor UFOHomo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayTyrosine-protein kinase receptor UFOHomo sapiens (human)
cell maturationTyrosine-protein kinase receptor UFOHomo sapiens (human)
positive regulation of pinocytosisTyrosine-protein kinase receptor UFOHomo sapiens (human)
response to axon injuryTyrosine-protein kinase receptor UFOHomo sapiens (human)
negative regulation of lymphocyte activationTyrosine-protein kinase receptor UFOHomo sapiens (human)
neuron apoptotic processTyrosine-protein kinase receptor UFOHomo sapiens (human)
establishment of localization in cellTyrosine-protein kinase receptor UFOHomo sapiens (human)
vagina developmentTyrosine-protein kinase receptor UFOHomo sapiens (human)
cellular response to hydrogen peroxideTyrosine-protein kinase receptor UFOHomo sapiens (human)
cellular response to lipopolysaccharideTyrosine-protein kinase receptor UFOHomo sapiens (human)
dendritic cell differentiationTyrosine-protein kinase receptor UFOHomo sapiens (human)
neutrophil clearanceTyrosine-protein kinase receptor UFOHomo sapiens (human)
positive regulation of viral life cycleTyrosine-protein kinase receptor UFOHomo sapiens (human)
negative regulation of dendritic cell apoptotic processTyrosine-protein kinase receptor UFOHomo sapiens (human)
platelet activationTyrosine-protein kinase receptor UFOHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTyrosine-protein kinase receptor UFOHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase receptor UFOHomo sapiens (human)
natural killer cell differentiationTyrosine-protein kinase receptor UFOHomo sapiens (human)
cell migrationTyrosine-protein kinase receptor UFOHomo sapiens (human)
positive regulation of kinase activityTyrosine-protein kinase receptor UFOHomo sapiens (human)
nervous system developmentTyrosine-protein kinase receptor UFOHomo sapiens (human)
multicellular organism developmentTyrosine-protein kinase receptor UFOHomo sapiens (human)
negative regulation of apoptotic processTyrosine-protein kinase receptor UFOHomo sapiens (human)
neuron migrationTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
natural killer cell differentiationTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
cell adhesionTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
signal transductionTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
neuropeptide signaling pathwayTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
spermatogenesisTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
forebrain cell migrationTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
platelet activationTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
secretion by cellTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
negative regulation of toll-like receptor signaling pathwayTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
substrate adhesion-dependent cell spreadingTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
ovulation cycleTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
apoptotic cell clearanceTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
negative regulation of neuron apoptotic processTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
negative regulation of innate immune responseTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
symbiont entry into host cellTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
protein autophosphorylationTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
negative regulation of inflammatory responseTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
negative regulation of lymphocyte activationTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
neuron apoptotic processTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
establishment of localization in cellTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
vagina developmentTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
neuron cellular homeostasisTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
platelet aggregationTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
positive regulation of viral life cycleTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
nervous system developmentTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
phagocytosisTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
multicellular organism developmentTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
positive regulation of kinase activityTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
cell migrationTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
natural killer cell differentiationTyrosine-protein kinase MerHomo sapiens (human)
negative regulation of cytokine productionTyrosine-protein kinase MerHomo sapiens (human)
protein phosphorylationTyrosine-protein kinase MerHomo sapiens (human)
phagocytosisTyrosine-protein kinase MerHomo sapiens (human)
cell surface receptor signaling pathwayTyrosine-protein kinase MerHomo sapiens (human)
cell-cell signalingTyrosine-protein kinase MerHomo sapiens (human)
spermatogenesisTyrosine-protein kinase MerHomo sapiens (human)
platelet activationTyrosine-protein kinase MerHomo sapiens (human)
secretion by cellTyrosine-protein kinase MerHomo sapiens (human)
substrate adhesion-dependent cell spreadingTyrosine-protein kinase MerHomo sapiens (human)
positive regulation of phagocytosisTyrosine-protein kinase MerHomo sapiens (human)
negative regulation of lymphocyte activationTyrosine-protein kinase MerHomo sapiens (human)
establishment of localization in cellTyrosine-protein kinase MerHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTyrosine-protein kinase MerHomo sapiens (human)
retina development in camera-type eyeTyrosine-protein kinase MerHomo sapiens (human)
vagina developmentTyrosine-protein kinase MerHomo sapiens (human)
neutrophil clearanceTyrosine-protein kinase MerHomo sapiens (human)
negative regulation of leukocyte apoptotic processTyrosine-protein kinase MerHomo sapiens (human)
nervous system developmentTyrosine-protein kinase MerHomo sapiens (human)
positive regulation of kinase activityTyrosine-protein kinase MerHomo sapiens (human)
cell migrationTyrosine-protein kinase MerHomo sapiens (human)
multicellular organism developmentTyrosine-protein kinase MerHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase MerHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
virus receptor activityTyrosine-protein kinase receptor UFOHomo sapiens (human)
phosphatidylserine bindingTyrosine-protein kinase receptor UFOHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase receptor UFOHomo sapiens (human)
protein bindingTyrosine-protein kinase receptor UFOHomo sapiens (human)
ATP bindingTyrosine-protein kinase receptor UFOHomo sapiens (human)
myosin heavy chain bindingTyrosine-protein kinase receptor UFOHomo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase receptor UFOHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityTyrosine-protein kinase receptor UFOHomo sapiens (human)
virus receptor activityTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
protein bindingTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
ATP bindingTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
protein bindingTyrosine-protein kinase MerHomo sapiens (human)
ATP bindingTyrosine-protein kinase MerHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityTyrosine-protein kinase MerHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
extracellular spaceTyrosine-protein kinase receptor UFOHomo sapiens (human)
plasma membraneTyrosine-protein kinase receptor UFOHomo sapiens (human)
cell surfaceTyrosine-protein kinase receptor UFOHomo sapiens (human)
actin cytoskeletonTyrosine-protein kinase receptor UFOHomo sapiens (human)
intracellular membrane-bounded organelleTyrosine-protein kinase receptor UFOHomo sapiens (human)
extracellular exosomeTyrosine-protein kinase receptor UFOHomo sapiens (human)
plasma membraneTyrosine-protein kinase receptor UFOHomo sapiens (human)
receptor complexTyrosine-protein kinase receptor UFOHomo sapiens (human)
nucleusTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
nuclear envelopeTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
endoplasmic reticulum membraneTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
plasma membraneTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
cell surfaceTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
plasma membraneTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
receptor complexTyrosine-protein kinase receptor TYRO3Homo sapiens (human)
photoreceptor outer segmentTyrosine-protein kinase MerHomo sapiens (human)
extracellular spaceTyrosine-protein kinase MerHomo sapiens (human)
cytoplasmTyrosine-protein kinase MerHomo sapiens (human)
plasma membraneTyrosine-protein kinase MerHomo sapiens (human)
plasma membraneTyrosine-protein kinase MerHomo sapiens (human)
receptor complexTyrosine-protein kinase MerHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (23)

Assay IDTitleYearJournalArticle
AID663581Clearance in Swiss mouse at 3 mg/kg, iv2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID1374833Inhibition of AXL (unknown origin)2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.
AID663572Inhibition of Tyro3 using EFPIYDFLPAKKK-CONH2 as substrate after 180 mins by microfluid capillary electrophoresis assay2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID663582Volume of distribution at steady state in Swiss mouse at 3 mg/kg, iv2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID738486Inhibition of TYRO3 (unknown origin)2013European journal of medicinal chemistry, Mar, Volume: 61Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation.
AID663571Inhibition of Axl using KKKKEEIYFFF-CONH2 as substrate after 180 mins by microfluid capillary electrophoresis assay2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID663577Inhibition of MAPKAPK2 at 10 times IC50 concentration after 90 mins in presence of ATP2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID738488Inhibition of MER (unknown origin)2013European journal of medicinal chemistry, Mar, Volume: 61Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation.
AID738487Inhibition of AXL (unknown origin)2013European journal of medicinal chemistry, Mar, Volume: 61Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation.
AID663579Inhibition of Ret Y791F mutant at 10 times IC50 concentration after 90 mins in presence of ATP2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID663576Inhibition of FLT3 at 10 times IC50 concentration after 90 mins in presence of ATP2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID663580Inhibition of Mer autophosphorylation in human 697 cells pretreated for 1 hr before addition of phosphatase inhibitor measured by Western blot analysis2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID663575Inhibition of Mer using EFPIYDFLPAKKK-CONH2 as substrate by Michaelis-Menten equation2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID663578Inhibition of Ret at 10 times IC50 concentration after 90 mins in presence of ATP2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID1374834Inhibition of MER (unknown origin)2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Development of Potent Inhibitors of Receptor Tyrosine Kinases by Ligand-Based Drug Design and Target-Biased Phenotypic Screening.
AID663570Inhibition of Mer expressed in Escherichia coli BL21 (DE3) cells using EFPIYDFLPAKKK-CONH2 as substrate after 180 mins by microfluid capillary electrophoresis assay2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
AID663583Oral bioavailability in Swiss mouse at 3 mg/kg2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
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.
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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's10 (71.43)24.3611
2020's4 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.43

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 Index19.43 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.43)

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%
Other14 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
galactose
galactopyranose : The pyranose form of galactose.		2.1510D-galactose;
galactopyranose		Escherichia coli metabolite;
mouse metabolite
oseltamivir
Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.. oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza.		2.1510acetamides;
amino acid ester;
cyclohexenecarboxylate ester;
primary amino compound		antiviral drug;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
environmental contaminant;
prodrug;
xenobiotic
methotrexate
[no description available]		2.1110dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
zd 6474
CH 331: structure in first source		2.0810aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine		antineoplastic agent;
tyrosine kinase inhibitor
su 11248
[no description available]		2.0810monocarboxylic 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
unc1062
UNC1062: structure in first source		7.1710
ConditionIndicatedRelationship StrengthStudiesTrials
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
Acute Myelogenous Leukemia
[description not available]		02.1710
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.1710
Acute Lymphoid Leukemia
[description not available]		02.520
Experimental Neoplasms
[description not available]		02.0810
Dysembryoma
[description not available]		02.0810
Teratoma
A true neoplasm composed of a number of different types of tissue, none of which is native to the area in which it occurs. It is composed of tissues that are derived from three germinal layers, the endoderm, mesoderm, and ectoderm. They are classified histologically as mature (benign) or immature (malignant). (From DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1642)		02.0810
Rhabdoid Tumor
A rare but highly lethal childhood tumor found almost exclusively in infants. Histopathologically, it resembles RHABDOMYOSARCOMA but the tumor cells are not of myogenic origin. Although it arises primarily in the kidney, it may be found in other parts of the body. The rhabdoid cytomorphology is believed to be the expression of a very primitive malignant cell. (From Holland et al., Cancer Medicine, 3d ed, p2210)		02.0810
Precursor Cell Lymphoblastic Leukemia-Lymphoma
A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.		02.520
Glial Cell Tumors
[description not available]		02.1110
Chromosomal Translocation
[description not available]		02.1110
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		02.1110
Chronic Liver Failure
[description not available]		02.1110
Acute-On-Chronic Liver Failure (ACLF)
[description not available]		02.1110
Cirrhosis, Liver
[description not available]		02.1110
Acute Hepatic Failure
[description not available]		02.1110
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		02.1110
Liver Failure, Acute
A form of rapid-onset LIVER FAILURE, also known as fulminant hepatic failure, caused by severe liver injury or massive loss of HEPATOCYTES. It is characterized by sudden development of liver dysfunction and JAUNDICE. Acute liver failure may progress to exhibit cerebral dysfunction even HEPATIC COMA depending on the etiology that includes hepatic ISCHEMIA, drug toxicity, malignant infiltration, and viral hepatitis such as post-transfusion HEPATITIS B and HEPATITIS C.		02.1110
End Stage Liver Disease
Final stage of a liver disease when the liver failure is irreversible and LIVER TRANSPLANTATION is needed.		02.1110
Acute-On-Chronic Liver Failure
Sudden liver failure in the presence of underlying compensated chronic LIVER DISEASE (e.g., LIVER CIRRHOSIS; HEPATITIS; and liver injury and failure) due to a precipitating acute hepatic insult.		02.1110