Page last updated: 2024-11-13

vel-0230

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

Description

VEL-0230: a cathepsin K antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25102841
CHEMBL ID1085282
SCHEMBL ID913738
MeSH IDM000608120

Synonyms (18)

Synonym
vel-0230
CHEMBL1085282 ,
z118i66gl4 ,
oxiranecarboxylic acid, 3-((((1s)-3-methyl-1-((2-methylpropoxy)methyl)butyl)amino)carbonyl)-, monosodium salt, (2s,3s)-
2-oxiranecarboxylic acid, 3-((((1s)-3-methyl-1-((2-methylpropoxy)methyl)butyl)amino)carbonyl)-, sodium salt (1:1), (2s,3s)-
221144-20-3
nc-2300
vel 0230
nc 2300
unii-z118i66gl4
sodium (2s,3s)-3[[(1s)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate
SGAKODIXAHVUKL-LFELFHSZSA-M ,
sodium (2s,3s)-3-[[(1s)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate
SCHEMBL913738
DTXSID80176631
sodium (2s,3s)-3-(((s)-1-isobutoxy-4-methylpentan-2-yl)carbamoyl)oxirane-2-carboxylate
sodium;(2s,3s)-3-[[(2s)-4-methyl-1-(2-methylpropoxy)pentan-2-yl]carbamoyl]oxirane-2-carboxylate
Q27294851

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"Plasma pharmacokinetic (PK) and bone resorption biomarker [carboxy-terminal cross-linking telopeptide of type I collagen (CTX-1)] analyses were performed following single and multiple oral dose protocols of a Cathepsin K inhibitor (VEL-0230) in horses."( Pharmacokinetics and bone resorption evaluation of a novel Cathepsin K inhibitor (VEL-0230) in healthy adult horses.
Bertone, A; Hussein, H; Ishihara, A; Menendez, M, 2014
)
0.81
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cathepsin KHomo sapiens (human)IC50 (µMol)0.03450.00010.848210.0000AID482895
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
collagen catabolic processCathepsin KHomo sapiens (human)
mitophagyCathepsin KHomo sapiens (human)
intramembranous ossificationCathepsin KHomo sapiens (human)
proteolysisCathepsin KHomo sapiens (human)
thyroid hormone generationCathepsin KHomo sapiens (human)
apoptotic processCathepsin KHomo sapiens (human)
response to organic cyclic compoundCathepsin KHomo sapiens (human)
extracellular matrix disassemblyCathepsin KHomo sapiens (human)
collagen catabolic processCathepsin KHomo sapiens (human)
response to insulinCathepsin KHomo sapiens (human)
cellular response to zinc ion starvationCathepsin KHomo sapiens (human)
bone resorptionCathepsin KHomo sapiens (human)
response to ethanolCathepsin KHomo sapiens (human)
proteolysis involved in protein catabolic processCathepsin KHomo sapiens (human)
negative regulation of cartilage developmentCathepsin KHomo sapiens (human)
cellular response to tumor necrosis factorCathepsin KHomo sapiens (human)
cellular response to transforming growth factor beta stimulusCathepsin KHomo sapiens (human)
mononuclear cell differentiationCathepsin KHomo sapiens (human)
positive regulation of apoptotic signaling pathwayCathepsin KHomo sapiens (human)
positive regulation of peptidase activityCathepsin KHomo sapiens (human)
immune responseCathepsin KHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
fibronectin bindingCathepsin KHomo sapiens (human)
cysteine-type endopeptidase activityCathepsin KHomo sapiens (human)
serine-type endopeptidase activityCathepsin KHomo sapiens (human)
protein bindingCathepsin KHomo sapiens (human)
collagen bindingCathepsin KHomo sapiens (human)
cysteine-type peptidase activityCathepsin KHomo sapiens (human)
proteoglycan bindingCathepsin KHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processCathepsin KHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
extracellular regionCathepsin KHomo sapiens (human)
extracellular spaceCathepsin KHomo sapiens (human)
nucleoplasmCathepsin KHomo sapiens (human)
lysosomeCathepsin KHomo sapiens (human)
external side of plasma membraneCathepsin KHomo sapiens (human)
apical plasma membraneCathepsin KHomo sapiens (human)
endolysosome lumenCathepsin KHomo sapiens (human)
lysosomal lumenCathepsin KHomo sapiens (human)
intracellular membrane-bounded organelleCathepsin KHomo sapiens (human)
extracellular spaceCathepsin KHomo sapiens (human)
lysosomeCathepsin KHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID482898Selectivity for cathepsin K over cathepsin B2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Emerging targets in osteoporosis disease modification.
AID482895Inhibition of cathepsin K2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Emerging targets in osteoporosis disease modification.
AID482900Selectivity for cathepsin K over cathepsin S2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Emerging targets in osteoporosis disease modification.
AID482899Selectivity for cathepsin K over cathepsin L2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Emerging targets in osteoporosis disease modification.
[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's1 (20.00)29.6817
2010's4 (80.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.84

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 Index12.84 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.84)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]