Page last updated: 2024-11-12

l-873724

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Description

L-873724: a selective inhibitor of cathepsin K; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9913088
CHEMBL ID437501
SCHEMBL ID2157182
MeSH IDM0519174

Synonyms (22)

Synonym
l-873724
bdbm19489
(2s)-n-(cyanomethyl)-4-methyl-2-[[(1s)-2,2,2-trifluoro-1-[4-(4-methylsulfon
(2s)-n-(cyanomethyl)-4-methyl-2-{[(1s)-2,2,2-trifluoro-1-[4-(4-methanesulfonylphenyl)phenyl]ethyl]amino}pentanamide
chembl437501 ,
SCHEMBL2157182
(+)-l-873724
pentanamide, n-(cyanomethyl)-4-methyl-2-(((1s)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)(1,1'-biphenyl)-4-yl)ethyl)amino)-, (2s)-
29250PP3ON ,
603139-12-4
(2s)-n-(cyanomethyl)-4-methyl-2-[[(1s)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]pentanamide
(2s)-n-(cyanomethyl)-4-methyl-2-[[(1s)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide
l873724
gtpl7860
n1(cyanomethyl)-n2{(1s)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)-1,1'-biphenyl-4-yl]ethyl}-l-leucinamide
unii-29250pp3on
HY-50887
CS-6814
Q27078443
(s)-n-(cyanomethyl)-4-methyl-2-(((s)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)ethyl)amino)pentanamide
MS-28951
AKOS040742150

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" This translated into an improved oral bioavailability in pre-clinical species."( Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
Black, WC; Boyd, MJ; Chauret, N; Deschênes, D; Desmarais, S; Falgueyret, JP; Gauthier, JY; Isabel, E; Khougaz, K; Lau, CK; Léger, S; Levorse, DA; Li, CS; Massé, F; Mellon, C; Percival, MD; Roy, B; Scheigetz, J; Thérien, M; Truong, VL; Wesolowski, G; Young, RN; Zamboni, R, 2011
)
0.37

Dosage Studied

ExcerptRelevanceReference
" To determine the correlation between the in vitro and ex vivo assays, a reversible cathepsin S inhibitor was dosed intravenously to a rhesus monkey."( Probing cathepsin S activity in whole blood by the activity-based probe BIL-DMK: cellular distribution in human leukocyte populations and evidence of diurnal modulation.
Black, WC; Falgueyret, JP; Gauthier, JY; Mellon, C; Percival, MD; Tawa, P; Veilleux, A, 2011
)
0.37
" Significant increases in DFBMD in animals dosed with the CatK inhibitors compared to vehicle were seen."( Cathepsin K inhibitors increase distal femoral bone mineral density in rapidly growing rabbits.
Duong, LT; Kimmel, DB; Levesque, S; Oballa, RM; Pennypacker, BL, 2013
)
0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cathepsin SMus musculus (house mouse)IC50 (µMol)0.25400.00032.45556.3500AID308695
Cathepsin BRattus norvegicus (Norway rat)IC50 (µMol)0.92500.92500.92500.9250AID308699
Procathepsin LMus musculus (house mouse)IC50 (µMol)0.25400.25401.33802.9800AID308700
Procathepsin LRattus norvegicus (Norway rat)IC50 (µMol)0.09000.09000.09000.0900AID308701
Procathepsin LHomo sapiens (human)IC50 (µMol)1.12280.00021.66619.5100AID1797859; AID1797866; AID262988; AID262992; AID308694; AID314221; AID314232
Cathepsin BHomo sapiens (human)IC50 (µMol)2.82260.00021.845310.0000AID1797859; AID1797866; AID262987; AID262991; AID308693; AID314220; AID314231
Coagulation factor VIIHomo sapiens (human)IC50 (µMol)0.00020.00020.83363.3000AID262994
Cathepsin BMus musculus (house mouse)IC50 (µMol)0.54000.54001.43332.9800AID308697
Tissue factorHomo sapiens (human)IC50 (µMol)0.00020.00010.734410.0000AID262994
Cathepsin SHomo sapiens (human)IC50 (µMol)0.92970.00021.319110.0000AID1797859; AID1797866; AID262989; AID262993; AID308691; AID314222; AID314233
Cathepsin KHomo sapiens (human)IC50 (µMol)0.00020.00010.848210.0000AID262994; AID308310; AID308692; AID314219; AID314228; AID342300; AID569575
Cathepsin KOryctolagus cuniculus (rabbit)IC50 (µMol)1.13760.00021.10186.3500AID1797859; AID1797866; AID262990; AID314229
Cathepsin KMus musculus (house mouse)IC50 (µMol)0.04300.04300.04300.0430AID308696
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (73)

Processvia Protein(s)Taxonomy
adaptive immune responseProcathepsin LHomo sapiens (human)
proteolysisProcathepsin LHomo sapiens (human)
protein autoprocessingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host plasma membraneProcathepsin LHomo sapiens (human)
receptor-mediated endocytosis of virus by host cellProcathepsin LHomo sapiens (human)
antigen processing and presentationProcathepsin LHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IIProcathepsin LHomo sapiens (human)
collagen catabolic processProcathepsin LHomo sapiens (human)
zymogen activationProcathepsin LHomo sapiens (human)
enkephalin processingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host endosome membraneProcathepsin LHomo sapiens (human)
CD4-positive, alpha-beta T cell lineage commitmentProcathepsin LHomo sapiens (human)
symbiont entry into host cellProcathepsin LHomo sapiens (human)
antigen processing and presentation of peptide antigenProcathepsin LHomo sapiens (human)
proteolysis involved in protein catabolic processProcathepsin LHomo sapiens (human)
elastin catabolic processProcathepsin LHomo sapiens (human)
macrophage apoptotic processProcathepsin LHomo sapiens (human)
cellular response to thyroid hormone stimulusProcathepsin LHomo sapiens (human)
positive regulation of apoptotic signaling pathwayProcathepsin LHomo sapiens (human)
positive regulation of peptidase activityProcathepsin LHomo sapiens (human)
immune responseProcathepsin LHomo sapiens (human)
proteolysisCathepsin BHomo sapiens (human)
thyroid hormone generationCathepsin BHomo sapiens (human)
collagen catabolic processCathepsin BHomo sapiens (human)
epithelial cell differentiationCathepsin BHomo sapiens (human)
regulation of apoptotic processCathepsin BHomo sapiens (human)
decidualizationCathepsin BHomo sapiens (human)
symbiont entry into host cellCathepsin BHomo sapiens (human)
proteolysis involved in protein catabolic processCathepsin BHomo sapiens (human)
cellular response to thyroid hormone stimulusCathepsin BHomo sapiens (human)
response to hypoxiaCoagulation factor VIIHomo sapiens (human)
positive regulation of leukocyte chemotaxisCoagulation factor VIIHomo sapiens (human)
blood coagulationCoagulation factor VIIHomo sapiens (human)
circadian rhythmCoagulation factor VIIHomo sapiens (human)
response to carbon dioxideCoagulation factor VIIHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayCoagulation factor VIIHomo sapiens (human)
protein processingCoagulation factor VIIHomo sapiens (human)
positive regulation of blood coagulationCoagulation factor VIIHomo sapiens (human)
positive regulation of cell migrationCoagulation factor VIIHomo sapiens (human)
animal organ regenerationCoagulation factor VIIHomo sapiens (human)
positive regulation of TOR signalingCoagulation factor VIIHomo sapiens (human)
response to estradiolCoagulation factor VIIHomo sapiens (human)
response to vitamin KCoagulation factor VIIHomo sapiens (human)
response to genisteinCoagulation factor VIIHomo sapiens (human)
response to estrogenCoagulation factor VIIHomo sapiens (human)
positive regulation of positive chemotaxisCoagulation factor VIIHomo sapiens (human)
response to growth hormoneCoagulation factor VIIHomo sapiens (human)
response to cholesterolCoagulation factor VIIHomo sapiens (human)
response to thyroxineCoagulation factor VIIHomo sapiens (human)
response to Thyroid stimulating hormoneCoagulation factor VIIHomo sapiens (human)
response to 2,3,7,8-tetrachlorodibenzodioxineCoagulation factor VIIHomo sapiens (human)
response to astaxanthinCoagulation factor VIIHomo sapiens (human)
response to thyrotropin-releasing hormoneCoagulation factor VIIHomo sapiens (human)
positive regulation of gene expressionTissue factorHomo sapiens (human)
positive regulation of interleukin-8 productionTissue factorHomo sapiens (human)
positive regulation of endothelial cell proliferationTissue factorHomo sapiens (human)
activation of plasma proteins involved in acute inflammatory responseTissue factorHomo sapiens (human)
activation of blood coagulation via clotting cascadeTissue factorHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTissue factorHomo sapiens (human)
blood coagulationTissue factorHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayTissue factorHomo sapiens (human)
protein processingTissue factorHomo sapiens (human)
positive regulation of cell migrationTissue factorHomo sapiens (human)
positive regulation of TOR signalingTissue factorHomo sapiens (human)
positive regulation of angiogenesisTissue factorHomo sapiens (human)
positive regulation of positive chemotaxisTissue factorHomo sapiens (human)
cytokine-mediated signaling pathwayTissue factorHomo sapiens (human)
toll-like receptor signaling pathwayCathepsin SHomo sapiens (human)
adaptive immune responseCathepsin SHomo sapiens (human)
proteolysisCathepsin SHomo sapiens (human)
apoptotic processCathepsin SHomo sapiens (human)
response to acidic pHCathepsin SHomo sapiens (human)
protein processingCathepsin SHomo sapiens (human)
antigen processing and presentationCathepsin SHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IICathepsin SHomo sapiens (human)
extracellular matrix disassemblyCathepsin SHomo sapiens (human)
collagen catabolic processCathepsin SHomo sapiens (human)
basement membrane disassemblyCathepsin SHomo sapiens (human)
antigen processing and presentation of peptide antigenCathepsin SHomo sapiens (human)
proteolysis involved in protein catabolic processCathepsin SHomo sapiens (human)
cellular response to thyroid hormone stimulusCathepsin SHomo sapiens (human)
positive regulation of cation channel activityCathepsin SHomo sapiens (human)
positive regulation of peptidase activityCathepsin SHomo sapiens (human)
immune responseCathepsin SHomo sapiens (human)
positive regulation of apoptotic signaling pathwayCathepsin SHomo sapiens (human)
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 (18)

Processvia Protein(s)Taxonomy
cysteine-type endopeptidase activityCathepsin SMus musculus (house mouse)
fibronectin bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityProcathepsin LHomo sapiens (human)
protein bindingProcathepsin LHomo sapiens (human)
collagen bindingProcathepsin LHomo sapiens (human)
cysteine-type peptidase activityProcathepsin LHomo sapiens (human)
histone bindingProcathepsin LHomo sapiens (human)
proteoglycan bindingProcathepsin LHomo sapiens (human)
serpin family protein bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityCathepsin BHomo sapiens (human)
protein bindingCathepsin BHomo sapiens (human)
collagen bindingCathepsin BHomo sapiens (human)
peptidase activityCathepsin BHomo sapiens (human)
cysteine-type peptidase activityCathepsin BHomo sapiens (human)
proteoglycan bindingCathepsin BHomo sapiens (human)
serine-type endopeptidase activityCoagulation factor VIIHomo sapiens (human)
signaling receptor bindingCoagulation factor VIIHomo sapiens (human)
calcium ion bindingCoagulation factor VIIHomo sapiens (human)
protein bindingCoagulation factor VIIHomo sapiens (human)
serine-type peptidase activityCoagulation factor VIIHomo sapiens (human)
serine-type endopeptidase activityTissue factorHomo sapiens (human)
protease bindingTissue factorHomo sapiens (human)
protein bindingTissue factorHomo sapiens (human)
phospholipid bindingTissue factorHomo sapiens (human)
cytokine receptor activityTissue factorHomo sapiens (human)
fibronectin bindingCathepsin SHomo sapiens (human)
cysteine-type endopeptidase activityCathepsin SHomo sapiens (human)
serine-type endopeptidase activityCathepsin SHomo sapiens (human)
collagen bindingCathepsin SHomo sapiens (human)
laminin bindingCathepsin SHomo sapiens (human)
proteoglycan bindingCathepsin SHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processCathepsin SHomo sapiens (human)
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 (31)

Processvia Protein(s)Taxonomy
early endosome lumenCathepsin SMus musculus (house mouse)
extracellular regionProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
nucleusProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
multivesicular bodyProcathepsin LHomo sapiens (human)
Golgi apparatusProcathepsin LHomo sapiens (human)
plasma membraneProcathepsin LHomo sapiens (human)
apical plasma membraneProcathepsin LHomo sapiens (human)
endolysosome lumenProcathepsin LHomo sapiens (human)
chromaffin granuleProcathepsin LHomo sapiens (human)
lysosomal lumenProcathepsin LHomo sapiens (human)
intracellular membrane-bounded organelleProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixProcathepsin LHomo sapiens (human)
extracellular exosomeProcathepsin LHomo sapiens (human)
endocytic vesicle lumenProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular regionCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
external side of plasma membraneCathepsin BHomo sapiens (human)
apical plasma membraneCathepsin BHomo sapiens (human)
endolysosome lumenCathepsin BHomo sapiens (human)
melanosomeCathepsin BHomo sapiens (human)
perinuclear region of cytoplasmCathepsin BHomo sapiens (human)
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular exosomeCathepsin BHomo sapiens (human)
peptidase inhibitor complexCathepsin BHomo sapiens (human)
ficolin-1-rich granule lumenCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
extracellular regionCoagulation factor VIIHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor VIIHomo sapiens (human)
Golgi lumenCoagulation factor VIIHomo sapiens (human)
plasma membraneCoagulation factor VIIHomo sapiens (human)
vesicleCoagulation factor VIIHomo sapiens (human)
collagen-containing extracellular matrixCoagulation factor VIIHomo sapiens (human)
serine-type peptidase complexCoagulation factor VIIHomo sapiens (human)
extracellular spaceCoagulation factor VIIHomo sapiens (human)
extracellular spaceTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
external side of plasma membraneTissue factorHomo sapiens (human)
cell surfaceTissue factorHomo sapiens (human)
membraneTissue factorHomo sapiens (human)
collagen-containing extracellular matrixTissue factorHomo sapiens (human)
serine-type peptidase complexTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
extracellular regionCathepsin SHomo sapiens (human)
extracellular spaceCathepsin SHomo sapiens (human)
lysosomeCathepsin SHomo sapiens (human)
late endosomeCathepsin SHomo sapiens (human)
endolysosome lumenCathepsin SHomo sapiens (human)
lysosomal lumenCathepsin SHomo sapiens (human)
intracellular membrane-bounded organelleCathepsin SHomo sapiens (human)
phagocytic vesicleCathepsin SHomo sapiens (human)
collagen-containing extracellular matrixCathepsin SHomo sapiens (human)
tertiary granule lumenCathepsin SHomo sapiens (human)
ficolin-1-rich granule lumenCathepsin SHomo sapiens (human)
extracellular spaceCathepsin SHomo sapiens (human)
lysosomeCathepsin SHomo sapiens (human)
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 (57)

Assay IDTitleYearJournalArticle
AID569580Ratio of product of IC50 for rabbit bone resorption and IC50 for humanized rabbit cathepsin K to IC50 for rabbit cathepsin K2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
AID262988Potency against Cathepsin L in HepG2 cells by whole cell enzyme occupancy assay2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID308694Inhibition of human cathepsin L2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID314229Inhibition of rabbit cathepsin K2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID263000Cmax in rat at 10 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID263007Volume of distribution in dog at 10 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID308699Inhibition of rat liver lysosomal cathepsin B2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID262996Decrease in urinary uNTx/Cr in ovariectomized rhesus monkey after 6 days at 3 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID314220Inhibition of cathepsin B2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID263004Half life in dog at 10 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID314221Inhibition of cathepsin L2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID262991Inhibition of Cathepsin B2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID263008Volume of distribution in rhesus monkey at 5 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID314228Inhibition of human cathepsin K2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID308721Inhibition of antigen presentation in mouse B cells2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID262994Inhibition of humanized rabbit Cathepsin K2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID569577Selectivity ratio of IC50 for human cathepsin F to IC50 for human cathepsin K2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
AID262998Oral bioavailability in dog at 10 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID262993Inhibition of Cathepsin S2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID342300Inhibition of cathepsin K2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
The many roles for fluorine in medicinal chemistry.
AID569576Selectivity ratio of IC50 for human cathepsin B to IC50 for human cathepsin K2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
AID308697Inhibition of mouse recombinant cathepsin B2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID569575Inhibition of humanized rabbit cathepsin K2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
AID263003Half life in rat at 10 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID308691Inhibition of human cathepsin S2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID262999Oral bioavailability in rhesus monkey at 5 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID569578Selectivity ratio of IC50 for human cathepsin L to IC50 for human cathepsin K2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
AID262989Potency against Cathepsin S in Ramos cells by whole cell enzyme occupancy assay2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID262992Inhibition of Cathepsin L2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID308693Inhibition of human cathepsin B2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID308695Inhibition of mouse recombinant cathepsin S2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID314230Inhibition of bone resorption in rabbit osteoclast2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID314232Inhibition of cathepsin L in human HepG2 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID314233Inhibition of cathepsin S in human ramos cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID308692Inhibition of human cathepsin K2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID308310Inhibition of humanized rabbit cathepsin K2007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Primary amides as selective inhibitors of cathepsin K.
AID262997Oral bioavailability in rat at 10 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID308700Inhibition of mouse recombinant cathepsin L2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID314219Inhibition of humanized rabbit cathepsin K2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID314215Clearance in monkey2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID308696Inhibition of mouse recombinant cathepsin K2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID263006Volume of distribution in rat at 10 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID263002Cmax in rhesus monkey at 5 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID262990Potency against Cathepsin K in rabbit osteoclasts by bone resorption assay2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID314231Inhibition of cathepsin B in human HepG2 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID308698Inhibition of rat spleen cathepsin S2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID569579Selectivity ratio of IC50 for human cathepsin S to IC50 for human cathepsin K2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
AID314214Half life in monkey2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID262987Potency against Cathepsin B in HepG2 cells by whole cell enzyme occupancy assay2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID314222Inhibition of cathepsin S2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
AID263005Half life in rhesus monkey at 5 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID263001Cmax in dog at 10 mg/kg, po2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID262995Activity in rabbit osteoclasts by bone resorption assay2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
AID308701Inhibition of rat liver lysosomal cathepsin L2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID1345903Human cathepsin K (C1: Papain)2009Biological chemistry, Sep, Volume: 390, Issue:9
Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools.
AID1797859Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2007.06.023: \\The identification of potent, selective, and bioavailable cathepsin S inhibitors.\\2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
AID1797866Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2005.12.071: \\Identification of a potent and selective non-basic cathepsin K inhibitor.\\2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Identification of a potent and selective non-basic cathepsin K inhibitor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (63.64)29.6817
2010's4 (36.36)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: 11.91

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 Index11.91 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.39 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.91)

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%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]