Page last updated: 2024-12-10

3,3-dimethyl-5-oxo-5-[(3-phenyl-1H-pyrazol-5-yl)amino]pentanoic acid

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID2814387
CHEMBL ID1704021
CHEBI ID183433

Synonyms (14)

Synonym
IDI1_014148
smr000456421
MLS000850403
3,3-dimethyl-5-oxo-5-[(3-phenyl-1h-pyrazol-5-yl)amino]pentanoic acid
MAYBRIDGE3_002761 ,
SR-01000639212-1
OPREA1_838653
HMS1438N11
3,3-dimethyl-5-oxo-5-[(5-phenyl-1h-pyrazol-3-yl)amino]pentanoic acid
CHEBI:183433
CCG-49781
HMS2811J09
CHEMBL1704021 ,
bdbm50462226
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
ring assemblyTwo or more cyclic systems (single rings or fused systems) which are directly joined to each other by double or single bonds are named ring assemblies when the number of such direct ring junctions is one less than the number of cyclic systems involved.
pyrazoles
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency23.93410.007215.758889.3584AID588342
TDP1 proteinHomo sapiens (human)Potency0.73080.000811.382244.6684AID686979
Glycoprotein hormones alpha chainHomo sapiens (human)Potency28.18384.46688.344810.0000AID624291
Guanine nucleotide-binding protein GHomo sapiens (human)Potency0.89131.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)IC50 (µMol)82.60000.00010.34843.5970AID1394718
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC50 (µMol)47.00000.00000.48308.8000AID1394724
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (113)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of cell population proliferationGlycoprotein hormones alpha chainHomo sapiens (human)
hormone-mediated signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
regulation of signaling receptor activityGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of steroid biosynthetic processGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of cell migrationGlycoprotein hormones alpha chainHomo sapiens (human)
thyroid gland developmentGlycoprotein hormones alpha chainHomo sapiens (human)
luteinizing hormone secretionGlycoprotein hormones alpha chainHomo sapiens (human)
organ growthGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone signaling pathwayGlycoprotein hormones alpha chainHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlycoprotein hormones alpha chainHomo sapiens (human)
negative regulation of organ growthGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone secretionGlycoprotein hormones alpha chainHomo sapiens (human)
thyroid hormone generationGlycoprotein hormones alpha chainHomo sapiens (human)
MAPK cascadeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
ureteric bud developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
neural crest cell migrationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
embryonic epithelial tube formationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
protein phosphorylationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
homophilic cell adhesion via plasma membrane adhesion moleculesProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
neuron cell-cell adhesionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
signal transductionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
axon guidanceProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
posterior midgut developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
response to xenobiotic stimulusProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of gene expressionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of neuron projection developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of neuron maturationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
regulation of cell adhesionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of cell migrationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
membrane protein proteolysisProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of cell adhesion mediated by integrinProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
ureter maturationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
glial cell-derived neurotrophic factor receptor signaling pathwayProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
neuron maturationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of MAPK cascadeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of cell sizeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of DNA-templated transcriptionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
response to painProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
enteric nervous system developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
regulation of axonogenesisProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
retina development in camera-type eyeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
innervationProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
Peyer's patch morphogenesisProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
cellular response to retinoic acidProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of metanephric glomerulus developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
lymphocyte migration into lymphoid organsProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
GDF15-GFRAL signaling pathwayProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathway in absence of ligandProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
positive regulation of kinase activityProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
multicellular organism developmentProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
branching involved in blood vessel morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of macroautophagyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial depolarizationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial fissionVascular endothelial growth factor receptor 2Homo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
ovarian follicle developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of protein phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
lymph vessel developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell maturationVascular endothelial growth factor receptor 2Homo sapiens (human)
endocardium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of cell shapeVascular endothelial growth factor receptor 2Homo sapiens (human)
mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of gene expressionVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of BMP signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
embryonic hemopoiesisVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor-2 signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
surfactant homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of neuron apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
cell fate commitmentVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
lung alveolus developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
post-embryonic camera-type eye morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of positive chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of focal adhesion assemblyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionVascular endothelial growth factor receptor 2Homo sapiens (human)
calcium ion homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
blood vessel endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular wound healingVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
semaphorin-plexin signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of hematopoietic progenitor cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of bone developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to hydrogen sulfideVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of endothelial cell apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
hormone activityGlycoprotein hormones alpha chainHomo sapiens (human)
protein bindingGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone activityGlycoprotein hormones alpha chainHomo sapiens (human)
protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
calcium ion bindingProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
protein bindingProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
ATP bindingProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
signaling receptor activityProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
integrin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
coreceptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
identical protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
cadherin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
Hsp90 protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular regionGlycoprotein hormones alpha chainHomo sapiens (human)
extracellular spaceGlycoprotein hormones alpha chainHomo sapiens (human)
Golgi lumenGlycoprotein hormones alpha chainHomo sapiens (human)
follicle-stimulating hormone complexGlycoprotein hormones alpha chainHomo sapiens (human)
pituitary gonadotropin complexGlycoprotein hormones alpha chainHomo sapiens (human)
extracellular spaceGlycoprotein hormones alpha chainHomo sapiens (human)
plasma membraneProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
early endosomeProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
plasma membraneProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
endosome membraneProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
dendriteProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
neuronal cell bodyProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
receptor complexProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
plasma membrane protein complexProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
axonProto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)
extracellular regionVascular endothelial growth factor receptor 2Homo sapiens (human)
nucleusVascular endothelial growth factor receptor 2Homo sapiens (human)
endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
early endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
endoplasmic reticulumVascular endothelial growth factor receptor 2Homo sapiens (human)
Golgi apparatusVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
external side of plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
cell junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
membrane raftVascular endothelial growth factor receptor 2Homo sapiens (human)
anchoring junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
sorting endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1394724Inhibition of recombinant human VEGFR2 using peptide as substrate by fluorimetric analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.
AID1394718Inhibition of wild type recombinant human RET using peptide as substrate by fluorimetric analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.
AID1394727Inhibition of recombinant human EGFR up to 100 uM using peptide as substrate by fluorimetric analysis2018European journal of medicinal chemistry, Apr-25, Volume: 150Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[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's3 (60.00)24.3611
2020's2 (40.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.94

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.94 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.94)

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]