Page last updated: 2024-11-12

l 006235

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 CID9912381
CHEMBL ID426819
SCHEMBL ID6183485
MeSH IDM0494816

Synonyms (29)

Synonym
L235 ,
n-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
cra-013783/l-006235
chembl426819 ,
bdbm19854
basic piperazine-containing compound, 1
n-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
L006235 ,
l-006235-1
l 006235
294623-49-7
SCHEMBL6183485
n-[1-[[(cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide
AKOS024457410
l-006235
DTXSID90432735
l-006,235
J-017526
l-235 ,
NCGC00371088-01
n-(1-((cyanomethyl)carbamoyl)cyclohexyl)-4-(2-(4-methylpiperazin-1-yl)thiazol-4-yl)benzamide
E76845
BCP28510
benzamide, n-[1-[[(cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]-
EX-A4494
MS-28607
HY-103352
CS-0027704
n-[1-[[(cyanomethyl)amino]carbonyl] cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazo lyl]benzamide

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" This combination of binding elements resulted in sub-250 pM, reversible, selective, and orally bioavailable cathepsin K inhibitors."( Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Bryant, C; Burrill, LC; Cheung, H; Chung, T; Davis, DE; Enriquez, P; Falgueyret, JP; Janc, JW; Johnson, C; Kimmel, DB; Liu, L; McCarter, J; McGrath, M; Mendonca, RV; Oballa, R; Palmer, JT; Percival, MD; Prasit, P; Riendeau, D; Rodan, G; Rodan, SB; Rydzewski, RM; Setti, EL; Somoza, JR; Springman, E; Strickley, RM; Tian, ZQ; Venkatraman, S; Venuti, MC; Wang, DX; Wesolowski, G; Young, RN; Yu, ZW, 2005
)
0.33
"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
" 39n was dosed orally in ovariectomized rhesus monkeys once per day for 7 days."( Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Bryant, C; Burrill, LC; Cheung, H; Chung, T; Davis, DE; Enriquez, P; Falgueyret, JP; Janc, JW; Johnson, C; Kimmel, DB; Liu, L; McCarter, J; McGrath, M; Mendonca, RV; Oballa, R; Palmer, JT; Percival, MD; Prasit, P; Riendeau, D; Rodan, G; Rodan, SB; Rydzewski, RM; Setti, EL; Somoza, JR; Springman, E; Strickley, RM; Tian, ZQ; Venkatraman, S; Venuti, MC; Wang, DX; Wesolowski, G; Young, RN; Yu, ZW, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency11.98770.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency11.98770.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cathepsin SMus musculus (house mouse)IC50 (µMol)2.77960.00032.45556.3500AID1797908; AID257094; AID257095
Sterol O-acyltransferase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.32900.00580.66266.0000AID257087; AID257095
Procathepsin LHomo sapiens (human)IC50 (µMol)3.58860.00021.66619.5100AID1797909; AID254761; AID257086; AID257087
Procathepsin LHomo sapiens (human)Ki6.00000.00001.10139.3000AID256977
Cathepsin BHomo sapiens (human)IC50 (µMol)1.91340.00021.845310.0000AID1797909; AID254760; AID257084; AID257085
Cathepsin BHomo sapiens (human)Ki1.00000.00001.21808.6000AID256976
Cathepsin SHomo sapiens (human)IC50 (µMol)13.03800.00021.319110.0000AID1797909; AID254762; AID257088; AID257089
Cathepsin SHomo sapiens (human)Ki47.00000.00000.41433.2900AID256978
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC50 (µMol)0.79000.00030.81978.4900AID257089
Cathepsin KHomo sapiens (human)IC50 (µMol)0.00040.00010.848210.0000AID254886; AID257083
Cathepsin KOryctolagus cuniculus (rabbit)IC50 (µMol)1.35030.00021.10186.3500AID1797908; AID1797910; AID257092
Cathepsin KOryctolagus cuniculus (rabbit)Ki0.00040.00020.00070.0014AID256975; AID256992
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Procathepsin LHomo sapiens (human)EC50 (µMol)0.79000.00304.48749.8200AID1797909
Cathepsin BHomo sapiens (human)EC50 (µMol)0.79000.79001.84502.9000AID1797909
Cathepsin SHomo sapiens (human)EC50 (µMol)0.79000.79001.84502.9000AID1797909
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (85)

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)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

Processvia Protein(s)Taxonomy
cysteine-type endopeptidase activityCathepsin SMus musculus (house mouse)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (39)

Processvia Protein(s)Taxonomy
early endosome lumenCathepsin SMus musculus (house mouse)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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 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)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (38)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID1797909Enzyme Inhibition Assay and Whole Cell Enzyme Occupancy Assay from Article 10.1021/jm0504961: \\Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.\\2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID1797910Enzyme Inhibition Assay and Bone Resorption Assay from Article 10.1021/jm0504961: \\Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.\\2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID1797908Enzyme Inhibition Assay from Article 10.1021/jm0504961: \\Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.\\2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID257094Inhibitory activity against mouse cathepsin S2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID256990Terminal half-life in rat2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID257085Inhibitory activity against human cathepsin B expressed in HepG2 cells2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID254762Inhibitory activity against cathepsin S from human2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
AID256977Inhibitory constant against human cathepsin L using Z-Phe-Arg-AMC substrate2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID257088Inhibitory activity against human cathepsin S2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID256976Inhibitory constant against human cathepsin B using Boc-Leu-Lys-Arg-AMC substrate2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID256992Inhibitory constant against rabbit cathepsin K using Z-Phe-Arg-AMC substrate2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID257100Effect of compound on antigen presentation in mouse A20 cells transfected with PC-specific mIgM by IL-2 secretion2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID256978Inhibitory constant against human cathepsin S using Z-Val-Val-Arg-AMC substrate2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID254886Inhibitory activity against cathepsin K using humanized rabbit enzyme2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
AID254760Inhibitory activity against cathepsin B from human2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
AID257084Inhibitory activity against human cathepsin B2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID257096Volume of distribution in rat administered with 10 mg/kg, po2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID256991Reduction of collagen breakdown products in ovariectomized rhesus monkey dosed at 15, 3 and 0.6 mg/kg, po2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID256985Oral bioavailability in rat2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID257086Inhibitory activity against human cathepsin L2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID257090Partition co-efficient, logP of the compound2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID257092Inhibitory activity against rabbit cathepsin K2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID254761Inhibitory activity against cathepsin L from human2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
AID256975Inhibitory constant against rabbit cathepsin K using Z-Phe-Arg-AMC substrate2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID257083Inhibitory activity against humanized rabbit cathepsin K2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID256979In vitro bone resorption in isolated rabbit osteoclasts2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID257095Inhibitory activity against mouse cathepsin S in mouse splenocytes2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID257087Inhibitory activity against human cathepsin L expressed in HepG2 cells2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID257091Dissociation constant, pKa of the compound2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID257098Plasma concentration in rat at 10 mg/kg, po2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID257093Effect of compound on degradation of collagen in osteoclast bone resorption assay2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
AID256989Maximum concentration in rat administered with 20 mg/kg, po2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
AID257089Inhibitory activity against human cathepsin S expressed in ramos cells2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (50.00)29.6817
2010's1 (16.67)24.3611
2020's2 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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 Index12.56 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]