Page last updated: 2024-12-10

rs-130830

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Description

RS-130830: orally-active broad-spectrum matrix metalloproteinase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3342298
CHEMBL ID440498
SCHEMBL ID2381112
MeSH IDM0502503

Synonyms (36)

Synonym
ro-1130830
rs-130830
HY-10398
4-[4-(4-chloro-phenoxy)-benzenesulfonylmethyl]-tetrahydro-pyran-4-carboxylic acid hydroxyamide
rs-130,830
chembl440498 ,
alpha-tetrahydropyran beta-sulfone 1b
830C
rs 130830
bdbm11863
4-({[4-(4-chlorophenoxy)benzene]sulfonyl}methyl)-n-hydroxyoxane-4-carboxamide
cts-1027
DB08490
4-[[4-(4-chlorophenoxy)phenyl]sulfonylmethyl]-n-hydroxyoxane-4-carboxamide
CS-0281
4-(((4-(4-chlorophenoxy)phenyl)sulfonyl)-methyl) tetrahydro-n-hydroxy-2h-pyran-4-carboxamide
4-(4-(4-chloro-phenoxy)-benzenesulfonylmethyl )-tetrahydro-pyran-4-carboxylic acid hydroxyamide
2qd3f58224 ,
4-(4-(4-chloro-phenoxy)-benzenesulfonylmethyl)-tetrahydro-pyran-4-carboxylic acid hydroxyamide
2h-pyran-4-carboxamide, 4-(((4-(4-chlorophenoxy)phenyl)sulfonyl)methyl)tetrahydro-n-hydroxy-
193022-04-7
unii-2qd3f58224
SCHEMBL2381112
DTXSID90172907
AKOS030526690
cts-1027 193022-04-7
4-({[4-(4-chlorophenoxy)phenyl]sulfonyl}methyl)-n-hydroxytetrahydro-2h-pyran-4-carboxamide
Q27097691
4-(((4-(4-chlorophenoxy)phenyl)sulfonyl)methyl)-n-hydroxytetrahydro-2h-pyran-4-carboxamide
BCP13018
cts 1027
ro 1130830;rs 130830
A911573
2h-pyran-4-carboxamide, 4-[[[4-(4-chlorophenoxy)phenyl]sulfonyl]methyl]tetrahydro-n-hydroxy-
F83499
MS-27506

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" In this article, we report the discovery of highly potent, selective, and orally bioavailable MMP-13 inhibitors as well as their detailed structure-activity data."( Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
Kanzaki, N; Kori, M; Kuno, H; Mototani, H; Naito, T; Nara, H; Oki, H; Santou, T; Sato, K; Terauchi, J; Uchikawa, O; Yamamoto, Y, 2014
)
0.4

Dosage Studied

ExcerptRelevanceReference
" The investigation of the beta-sulfones subsequently led to the discovery of hitherto unknown alpha-sulfone hydroxamates that are superior to the corresponding beta-sulfones in potency for target MMPs, selectivity vs MMP-1, and exposure when dosed orally."( Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.
Barta, TE; Becker, DP; Bedell, LJ; Boehm, TL; Carron, CP; Decrescenzo, GA; Freskos, JN; Funckes-Shippy, CL; Getman, DP; Heintz, R; Hockerman, S; Howard, SC; Li, MH; McDonald, JJ; Mehta, PP; Munie, GE; Swearingen, CA; Villamil, CI, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency18.55690.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency18.55690.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MMP-13Homo sapiens (human)Ki0.00050.00050.00050.0005AID977610
Chain A, MMP-13Homo sapiens (human)Ki0.00050.00050.00050.0005AID977610
Chain A, MMP-1Homo sapiens (human)Ki0.00050.00050.00050.0005AID977610
Collagenase 3Bos taurus (cattle)IC50 (µMol)0.00400.00030.01060.0439AID1162790; AID1162791; AID1162792; AID352544
Bile salt export pumpHomo sapiens (human)IC50 (µMol)23.36000.11007.190310.0000AID1449628
Interstitial collagenaseHomo sapiens (human)IC50 (µMol)0.20620.00020.850210.0000AID108766; AID109072; AID1162784; AID1166662; AID1433732; AID1799084; AID352546
Interstitial collagenaseHomo sapiens (human)Ki0.22240.00030.49487.0000AID108922; AID1796811; AID1799084; AID238384
72 kDa type IV collagenaseHomo sapiens (human)IC50 (µMol)0.00010.00001.284810.0000AID107168; AID1162785; AID1166663; AID1328776; AID1433727; AID352553
72 kDa type IV collagenaseHomo sapiens (human)Ki0.10270.00000.34663.0000AID107316; AID1796811; AID238385
Stromelysin-1Homo sapiens (human)IC50 (µMol)0.05330.00001.148410.0000AID1162786; AID1166664; AID1433733; AID1799084; AID352554
Stromelysin-1Homo sapiens (human)Ki0.09340.00030.54258.0000AID107532; AID1796811; AID1799084; AID238386
MatrilysinHomo sapiens (human)IC50 (µMol)0.93250.00142.085910.0000AID1162787; AID1166665; AID1433734; AID352555
MatrilysinHomo sapiens (human)Ki1.20000.05401.50527.0000AID107834
Stromelysin-2Homo sapiens (human)IC50 (µMol)0.00050.00052.875410.0000AID1162790; AID1166668; AID1328781; AID1433729
Matrix metalloproteinase-9Homo sapiens (human)IC50 (µMol)0.04630.00000.705310.0000AID108297; AID1162789; AID1166667; AID1433735; AID1799084; AID352556
Matrix metalloproteinase-9Homo sapiens (human)Ki0.09140.00020.12810.8000AID108171; AID1796811; AID1799084; AID238387
Neutrophil collagenaseHomo sapiens (human)IC50 (µMol)0.00010.00000.927210.0000AID1162788; AID1166666; AID1328779; AID1433728
Neutrophil collagenaseHomo sapiens (human)Ki0.13690.00020.17972.1000AID1796811
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.01400.00070.97749.7000AID1162792
Collagenase 3Homo sapiens (human)IC50 (µMol)0.03670.00000.767510.0000AID109382; AID109410; AID1162780; AID1166661; AID1328774; AID1433726; AID1799084; AID352544; AID352545
Collagenase 3Homo sapiens (human)Ki0.08230.00000.47593.8000AID109390; AID1796811; AID1799084; AID238806; AID352935
Matrix metalloproteinase-14Homo sapiens (human)IC50 (µMol)0.00430.00030.718210.0000AID1162791; AID1166669; AID1433736; AID352557
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)IC50 (µMol)0.13160.00021.014010.0000AID1162792; AID1166670; AID1433737; AID215275; AID352558
TransporterRattus norvegicus (Norway rat)IC50 (µMol)0.01400.00081.95628.8000AID1162792
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Interstitial collagenaseHomo sapiens (human)Activity0.80000.00290.27550.8000AID108728
72 kDa type IV collagenaseHomo sapiens (human)Activity0.00040.00030.00050.0008AID109578
Collagenase 3Homo sapiens (human)Activity0.00060.00050.00100.0020AID109247
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (183)

Processvia Protein(s)Taxonomy
proteolysisCollagenase 3Bos taurus (cattle)
extracellular matrix disassemblyCollagenase 3Bos taurus (cattle)
collagen catabolic processCollagenase 3Bos taurus (cattle)
bone morphogenesisCollagenase 3Bos taurus (cattle)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
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)
proteolysisInterstitial collagenaseHomo sapiens (human)
protein metabolic processInterstitial collagenaseHomo sapiens (human)
extracellular matrix disassemblyInterstitial collagenaseHomo sapiens (human)
collagen catabolic processInterstitial collagenaseHomo sapiens (human)
positive regulation of protein-containing complex assemblyInterstitial collagenaseHomo sapiens (human)
cellular response to UV-AInterstitial collagenaseHomo sapiens (human)
extracellular matrix organizationInterstitial collagenaseHomo sapiens (human)
angiogenesis72 kDa type IV collagenaseHomo sapiens (human)
ovarian follicle development72 kDa type IV collagenaseHomo sapiens (human)
ovulation from ovarian follicle72 kDa type IV collagenaseHomo sapiens (human)
luteinization72 kDa type IV collagenaseHomo sapiens (human)
blood vessel maturation72 kDa type IV collagenaseHomo sapiens (human)
intramembranous ossification72 kDa type IV collagenaseHomo sapiens (human)
proteolysis72 kDa type IV collagenaseHomo sapiens (human)
negative regulation of cell adhesion72 kDa type IV collagenaseHomo sapiens (human)
heart development72 kDa type IV collagenaseHomo sapiens (human)
embryo implantation72 kDa type IV collagenaseHomo sapiens (human)
parturition72 kDa type IV collagenaseHomo sapiens (human)
response to xenobiotic stimulus72 kDa type IV collagenaseHomo sapiens (human)
response to mechanical stimulus72 kDa type IV collagenaseHomo sapiens (human)
peripheral nervous system axon regeneration72 kDa type IV collagenaseHomo sapiens (human)
response to activity72 kDa type IV collagenaseHomo sapiens (human)
protein metabolic process72 kDa type IV collagenaseHomo sapiens (human)
extracellular matrix disassembly72 kDa type IV collagenaseHomo sapiens (human)
protein catabolic process72 kDa type IV collagenaseHomo sapiens (human)
positive regulation of cell migration72 kDa type IV collagenaseHomo sapiens (human)
collagen catabolic process72 kDa type IV collagenaseHomo sapiens (human)
response to retinoic acid72 kDa type IV collagenaseHomo sapiens (human)
cellular response to reactive oxygen species72 kDa type IV collagenaseHomo sapiens (human)
response to nicotine72 kDa type IV collagenaseHomo sapiens (human)
endodermal cell differentiation72 kDa type IV collagenaseHomo sapiens (human)
response to hydrogen peroxide72 kDa type IV collagenaseHomo sapiens (human)
response to estrogen72 kDa type IV collagenaseHomo sapiens (human)
negative regulation of vasoconstriction72 kDa type IV collagenaseHomo sapiens (human)
ephrin receptor signaling pathway72 kDa type IV collagenaseHomo sapiens (human)
macrophage chemotaxis72 kDa type IV collagenaseHomo sapiens (human)
response to electrical stimulus72 kDa type IV collagenaseHomo sapiens (human)
response to hyperoxia72 kDa type IV collagenaseHomo sapiens (human)
face morphogenesis72 kDa type IV collagenaseHomo sapiens (human)
bone trabecula formation72 kDa type IV collagenaseHomo sapiens (human)
prostate gland epithelium morphogenesis72 kDa type IV collagenaseHomo sapiens (human)
cellular response to amino acid stimulus72 kDa type IV collagenaseHomo sapiens (human)
cellular response to interleukin-172 kDa type IV collagenaseHomo sapiens (human)
cellular response to estradiol stimulus72 kDa type IV collagenaseHomo sapiens (human)
cellular response to UV-A72 kDa type IV collagenaseHomo sapiens (human)
cellular response to fluid shear stress72 kDa type IV collagenaseHomo sapiens (human)
positive regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathway72 kDa type IV collagenaseHomo sapiens (human)
response to amyloid-beta72 kDa type IV collagenaseHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation72 kDa type IV collagenaseHomo sapiens (human)
extracellular matrix organization72 kDa type IV collagenaseHomo sapiens (human)
response to hypoxia72 kDa type IV collagenaseHomo sapiens (human)
tissue remodeling72 kDa type IV collagenaseHomo sapiens (human)
proteolysisStromelysin-1Homo sapiens (human)
extracellular matrix disassemblyStromelysin-1Homo sapiens (human)
protein catabolic processStromelysin-1Homo sapiens (human)
regulation of cell migrationStromelysin-1Homo sapiens (human)
collagen catabolic processStromelysin-1Homo sapiens (human)
positive regulation of protein-containing complex assemblyStromelysin-1Homo sapiens (human)
cellular response to reactive oxygen speciesStromelysin-1Homo sapiens (human)
innate immune responseStromelysin-1Homo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionStromelysin-1Homo sapiens (human)
cellular response to lipopolysaccharideStromelysin-1Homo sapiens (human)
cellular response to amino acid stimulusStromelysin-1Homo sapiens (human)
cellular response to UV-AStromelysin-1Homo sapiens (human)
cellular response to nitric oxideStromelysin-1Homo sapiens (human)
regulation of neuroinflammatory responseStromelysin-1Homo sapiens (human)
response to amyloid-betaStromelysin-1Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processStromelysin-1Homo sapiens (human)
extracellular matrix organizationStromelysin-1Homo sapiens (human)
membrane protein ectodomain proteolysisMatrilysinHomo sapiens (human)
membrane protein intracellular domain proteolysisMatrilysinHomo sapiens (human)
antibacterial peptide secretionMatrilysinHomo sapiens (human)
antibacterial peptide biosynthetic processMatrilysinHomo sapiens (human)
proteolysisMatrilysinHomo sapiens (human)
response to xenobiotic stimulusMatrilysinHomo sapiens (human)
extracellular matrix disassemblyMatrilysinHomo sapiens (human)
positive regulation of cell migrationMatrilysinHomo sapiens (human)
collagen catabolic processMatrilysinHomo sapiens (human)
regulation of cell population proliferationMatrilysinHomo sapiens (human)
defense response to Gram-negative bacteriumMatrilysinHomo sapiens (human)
defense response to Gram-positive bacteriumMatrilysinHomo sapiens (human)
extracellular matrix organizationMatrilysinHomo sapiens (human)
proteolysisStromelysin-2Homo sapiens (human)
extracellular matrix disassemblyStromelysin-2Homo sapiens (human)
collagen catabolic processStromelysin-2Homo sapiens (human)
extracellular matrix organizationStromelysin-2Homo sapiens (human)
skeletal system developmentMatrix metalloproteinase-9Homo sapiens (human)
positive regulation of protein phosphorylationMatrix metalloproteinase-9Homo sapiens (human)
proteolysisMatrix metalloproteinase-9Homo sapiens (human)
apoptotic processMatrix metalloproteinase-9Homo sapiens (human)
embryo implantationMatrix metalloproteinase-9Homo sapiens (human)
cell migrationMatrix metalloproteinase-9Homo sapiens (human)
extracellular matrix disassemblyMatrix metalloproteinase-9Homo sapiens (human)
macrophage differentiationMatrix metalloproteinase-9Homo sapiens (human)
collagen catabolic processMatrix metalloproteinase-9Homo sapiens (human)
cellular response to reactive oxygen speciesMatrix metalloproteinase-9Homo sapiens (human)
endodermal cell differentiationMatrix metalloproteinase-9Homo sapiens (human)
positive regulation of apoptotic processMatrix metalloproteinase-9Homo sapiens (human)
negative regulation of apoptotic processMatrix metalloproteinase-9Homo sapiens (human)
positive regulation of DNA bindingMatrix metalloproteinase-9Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayMatrix metalloproteinase-9Homo sapiens (human)
ephrin receptor signaling pathwayMatrix metalloproteinase-9Homo sapiens (human)
positive regulation of keratinocyte migrationMatrix metalloproteinase-9Homo sapiens (human)
cellular response to lipopolysaccharideMatrix metalloproteinase-9Homo sapiens (human)
cellular response to cadmium ionMatrix metalloproteinase-9Homo sapiens (human)
cellular response to UV-AMatrix metalloproteinase-9Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaMatrix metalloproteinase-9Homo sapiens (human)
regulation of neuroinflammatory responseMatrix metalloproteinase-9Homo sapiens (human)
positive regulation of receptor bindingMatrix metalloproteinase-9Homo sapiens (human)
response to amyloid-betaMatrix metalloproteinase-9Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationMatrix metalloproteinase-9Homo sapiens (human)
negative regulation of epithelial cell differentiation involved in kidney developmentMatrix metalloproteinase-9Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayMatrix metalloproteinase-9Homo sapiens (human)
negative regulation of cation channel activityMatrix metalloproteinase-9Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayMatrix metalloproteinase-9Homo sapiens (human)
extracellular matrix organizationMatrix metalloproteinase-9Homo sapiens (human)
positive regulation of microglial cell activationNeutrophil collagenaseHomo sapiens (human)
proteolysisNeutrophil collagenaseHomo sapiens (human)
extracellular matrix disassemblyNeutrophil collagenaseHomo sapiens (human)
collagen catabolic processNeutrophil collagenaseHomo sapiens (human)
positive regulation of tumor necrosis factor productionNeutrophil collagenaseHomo sapiens (human)
endodermal cell differentiationNeutrophil collagenaseHomo sapiens (human)
cellular response to lipopolysaccharideNeutrophil collagenaseHomo sapiens (human)
positive regulation of neuroinflammatory responseNeutrophil collagenaseHomo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayNeutrophil collagenaseHomo sapiens (human)
extracellular matrix organizationNeutrophil collagenaseHomo sapiens (human)
endochondral ossificationCollagenase 3Homo sapiens (human)
growth plate cartilage developmentCollagenase 3Homo sapiens (human)
proteolysisCollagenase 3Homo sapiens (human)
extracellular matrix disassemblyCollagenase 3Homo sapiens (human)
bone mineralizationCollagenase 3Homo sapiens (human)
collagen catabolic processCollagenase 3Homo sapiens (human)
bone morphogenesisCollagenase 3Homo sapiens (human)
response to amyloid-betaCollagenase 3Homo sapiens (human)
extracellular matrix organizationCollagenase 3Homo sapiens (human)
angiogenesisMatrix metalloproteinase-14Homo sapiens (human)
ovarian follicle developmentMatrix metalloproteinase-14Homo sapiens (human)
response to hypoxiaMatrix metalloproteinase-14Homo sapiens (human)
endothelial cell proliferationMatrix metalloproteinase-14Homo sapiens (human)
endochondral ossificationMatrix metalloproteinase-14Homo sapiens (human)
proteolysisMatrix metalloproteinase-14Homo sapiens (human)
response to oxidative stressMatrix metalloproteinase-14Homo sapiens (human)
male gonad developmentMatrix metalloproteinase-14Homo sapiens (human)
response to mechanical stimulusMatrix metalloproteinase-14Homo sapiens (human)
positive regulation of myotube differentiationMatrix metalloproteinase-14Homo sapiens (human)
positive regulation of protein processingMatrix metalloproteinase-14Homo sapiens (human)
response to organic cyclic compoundMatrix metalloproteinase-14Homo sapiens (human)
protein processingMatrix metalloproteinase-14Homo sapiens (human)
extracellular matrix disassemblyMatrix metalloproteinase-14Homo sapiens (human)
protein catabolic processMatrix metalloproteinase-14Homo sapiens (human)
positive regulation of cell growthMatrix metalloproteinase-14Homo sapiens (human)
lung developmentMatrix metalloproteinase-14Homo sapiens (human)
positive regulation of cell migrationMatrix metalloproteinase-14Homo sapiens (human)
collagen catabolic processMatrix metalloproteinase-14Homo sapiens (human)
zymogen activationMatrix metalloproteinase-14Homo sapiens (human)
endodermal cell differentiationMatrix metalloproteinase-14Homo sapiens (human)
chondrocyte proliferationMatrix metalloproteinase-14Homo sapiens (human)
astrocyte cell migrationMatrix metalloproteinase-14Homo sapiens (human)
response to estrogenMatrix metalloproteinase-14Homo sapiens (human)
positive regulation of B cell differentiationMatrix metalloproteinase-14Homo sapiens (human)
negative regulation of Notch signaling pathwayMatrix metalloproteinase-14Homo sapiens (human)
embryonic cranial skeleton morphogenesisMatrix metalloproteinase-14Homo sapiens (human)
branching morphogenesis of an epithelial tubeMatrix metalloproteinase-14Homo sapiens (human)
tissue remodelingMatrix metalloproteinase-14Homo sapiens (human)
cell motilityMatrix metalloproteinase-14Homo sapiens (human)
negative regulation of focal adhesion assemblyMatrix metalloproteinase-14Homo sapiens (human)
head developmentMatrix metalloproteinase-14Homo sapiens (human)
craniofacial suture morphogenesisMatrix metalloproteinase-14Homo sapiens (human)
negative regulation of GDF15-GFRAL signaling pathwayMatrix metalloproteinase-14Homo sapiens (human)
regulation of protein localization to plasma membraneMatrix metalloproteinase-14Homo sapiens (human)
positive regulation of macrophage migrationMatrix metalloproteinase-14Homo sapiens (human)
response to odorantMatrix metalloproteinase-14Homo sapiens (human)
extracellular matrix organizationMatrix metalloproteinase-14Homo sapiens (human)
skeletal system developmentMatrix metalloproteinase-14Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (32)

Processvia Protein(s)Taxonomy
endopeptidase activityCollagenase 3Bos taurus (cattle)
metalloendopeptidase activityCollagenase 3Bos taurus (cattle)
calcium ion bindingCollagenase 3Bos taurus (cattle)
collagen bindingCollagenase 3Bos taurus (cattle)
zinc ion bindingCollagenase 3Bos taurus (cattle)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
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)
endopeptidase activityInterstitial collagenaseHomo sapiens (human)
metalloendopeptidase activityInterstitial collagenaseHomo sapiens (human)
serine-type endopeptidase activityInterstitial collagenaseHomo sapiens (human)
peptidase activityInterstitial collagenaseHomo sapiens (human)
zinc ion bindingInterstitial collagenaseHomo sapiens (human)
fibronectin binding72 kDa type IV collagenaseHomo sapiens (human)
endopeptidase activity72 kDa type IV collagenaseHomo sapiens (human)
metalloendopeptidase activity72 kDa type IV collagenaseHomo sapiens (human)
serine-type endopeptidase activity72 kDa type IV collagenaseHomo sapiens (human)
protein binding72 kDa type IV collagenaseHomo sapiens (human)
metallopeptidase activity72 kDa type IV collagenaseHomo sapiens (human)
zinc ion binding72 kDa type IV collagenaseHomo sapiens (human)
endopeptidase activityStromelysin-1Homo sapiens (human)
metalloendopeptidase activityStromelysin-1Homo sapiens (human)
serine-type endopeptidase activityStromelysin-1Homo sapiens (human)
protein bindingStromelysin-1Homo sapiens (human)
peptidase activityStromelysin-1Homo sapiens (human)
metallopeptidase activityStromelysin-1Homo sapiens (human)
zinc ion bindingStromelysin-1Homo sapiens (human)
endopeptidase activityMatrilysinHomo sapiens (human)
metalloendopeptidase activityMatrilysinHomo sapiens (human)
serine-type endopeptidase activityMatrilysinHomo sapiens (human)
protein bindingMatrilysinHomo sapiens (human)
metallopeptidase activityMatrilysinHomo sapiens (human)
zinc ion bindingMatrilysinHomo sapiens (human)
metalloendopeptidase activityStromelysin-2Homo sapiens (human)
serine-type endopeptidase activityStromelysin-2Homo sapiens (human)
zinc ion bindingStromelysin-2Homo sapiens (human)
endopeptidase activityMatrix metalloproteinase-9Homo sapiens (human)
metalloendopeptidase activityMatrix metalloproteinase-9Homo sapiens (human)
serine-type endopeptidase activityMatrix metalloproteinase-9Homo sapiens (human)
protein bindingMatrix metalloproteinase-9Homo sapiens (human)
collagen bindingMatrix metalloproteinase-9Homo sapiens (human)
peptidase activityMatrix metalloproteinase-9Homo sapiens (human)
metallopeptidase activityMatrix metalloproteinase-9Homo sapiens (human)
zinc ion bindingMatrix metalloproteinase-9Homo sapiens (human)
identical protein bindingMatrix metalloproteinase-9Homo sapiens (human)
endopeptidase activityNeutrophil collagenaseHomo sapiens (human)
metalloendopeptidase activityNeutrophil collagenaseHomo sapiens (human)
serine-type endopeptidase activityNeutrophil collagenaseHomo sapiens (human)
peptidase activityNeutrophil collagenaseHomo sapiens (human)
zinc ion bindingNeutrophil collagenaseHomo sapiens (human)
tumor necrosis factor bindingNeutrophil collagenaseHomo sapiens (human)
endopeptidase activityCollagenase 3Homo sapiens (human)
metalloendopeptidase activityCollagenase 3Homo sapiens (human)
serine-type endopeptidase activityCollagenase 3Homo sapiens (human)
calcium ion bindingCollagenase 3Homo sapiens (human)
collagen bindingCollagenase 3Homo sapiens (human)
zinc ion bindingCollagenase 3Homo sapiens (human)
endopeptidase activityMatrix metalloproteinase-14Homo sapiens (human)
metalloendopeptidase activityMatrix metalloproteinase-14Homo sapiens (human)
serine-type endopeptidase activityMatrix metalloproteinase-14Homo sapiens (human)
integrin bindingMatrix metalloproteinase-14Homo sapiens (human)
protein bindingMatrix metalloproteinase-14Homo sapiens (human)
zinc ion bindingMatrix metalloproteinase-14Homo sapiens (human)
metalloaminopeptidase activityMatrix metalloproteinase-14Homo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
extracellular matrixCollagenase 3Bos taurus (cattle)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
extracellular regionInterstitial collagenaseHomo sapiens (human)
extracellular matrixInterstitial collagenaseHomo sapiens (human)
extracellular spaceInterstitial collagenaseHomo sapiens (human)
collagen-containing extracellular matrix72 kDa type IV collagenaseHomo sapiens (human)
extracellular region72 kDa type IV collagenaseHomo sapiens (human)
extracellular space72 kDa type IV collagenaseHomo sapiens (human)
nucleus72 kDa type IV collagenaseHomo sapiens (human)
mitochondrion72 kDa type IV collagenaseHomo sapiens (human)
plasma membrane72 kDa type IV collagenaseHomo sapiens (human)
sarcomere72 kDa type IV collagenaseHomo sapiens (human)
collagen-containing extracellular matrix72 kDa type IV collagenaseHomo sapiens (human)
extracellular space72 kDa type IV collagenaseHomo sapiens (human)
extracellular regionStromelysin-1Homo sapiens (human)
nucleusStromelysin-1Homo sapiens (human)
mitochondrionStromelysin-1Homo sapiens (human)
cytosolStromelysin-1Homo sapiens (human)
extracellular matrixStromelysin-1Homo sapiens (human)
extracellular spaceStromelysin-1Homo sapiens (human)
extracellular regionMatrilysinHomo sapiens (human)
extracellular matrixMatrilysinHomo sapiens (human)
extracellular exosomeMatrilysinHomo sapiens (human)
extracellular spaceMatrilysinHomo sapiens (human)
extracellular regionStromelysin-2Homo sapiens (human)
extracellular matrixStromelysin-2Homo sapiens (human)
extracellular spaceStromelysin-2Homo sapiens (human)
extracellular regionMatrix metalloproteinase-9Homo sapiens (human)
extracellular spaceMatrix metalloproteinase-9Homo sapiens (human)
collagen-containing extracellular matrixMatrix metalloproteinase-9Homo sapiens (human)
extracellular exosomeMatrix metalloproteinase-9Homo sapiens (human)
tertiary granule lumenMatrix metalloproteinase-9Homo sapiens (human)
ficolin-1-rich granule lumenMatrix metalloproteinase-9Homo sapiens (human)
extracellular spaceMatrix metalloproteinase-9Homo sapiens (human)
extracellular regionNeutrophil collagenaseHomo sapiens (human)
extracellular spaceNeutrophil collagenaseHomo sapiens (human)
specific granule lumenNeutrophil collagenaseHomo sapiens (human)
collagen-containing extracellular matrixNeutrophil collagenaseHomo sapiens (human)
tertiary granule lumenNeutrophil collagenaseHomo sapiens (human)
extracellular spaceNeutrophil collagenaseHomo sapiens (human)
extracellular regionCollagenase 3Homo sapiens (human)
extracellular matrixCollagenase 3Homo sapiens (human)
extracellular spaceCollagenase 3Homo sapiens (human)
cytoplasmMatrix metalloproteinase-14Homo sapiens (human)
plasma membraneMatrix metalloproteinase-14Homo sapiens (human)
extracellular spaceMatrix metalloproteinase-14Homo sapiens (human)
nucleusMatrix metalloproteinase-14Homo sapiens (human)
Golgi lumenMatrix metalloproteinase-14Homo sapiens (human)
cytosolMatrix metalloproteinase-14Homo sapiens (human)
plasma membraneMatrix metalloproteinase-14Homo sapiens (human)
focal adhesionMatrix metalloproteinase-14Homo sapiens (human)
extracellular matrixMatrix metalloproteinase-14Homo sapiens (human)
cytoplasmic vesicleMatrix metalloproteinase-14Homo sapiens (human)
melanosomeMatrix metalloproteinase-14Homo sapiens (human)
macropinosomeMatrix metalloproteinase-14Homo sapiens (human)
intermediate filament cytoskeletonMatrix metalloproteinase-14Homo sapiens (human)
extracellular spaceMatrix metalloproteinase-14Homo sapiens (human)
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (90)

Assay IDTitleYearJournalArticle
AID1166662Inhibition of human recombinant MMP1 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID1166668Inhibition of human recombinant MMP10 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID352555Inhibition of MMP72009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID1166667Inhibition of human recombinant MMP9 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID352935Inhibition of MMP13 assessed as dissociation constant2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID1162788Inhibition of human recombinant MMP8 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID238387Inhibition of matrix metalloprotease-92005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
AID352548Selectivity ratio of IC50 for MMP13 to IC50 for MMP13 in presence of 1% bovine serum albumin2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID108728Inhibitory activity against human Matrix metalloprotease-12001Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
Selective, orally active MMP inhibitors with an aryl backbone.
AID1328776Inhibition of recombinant human AMPA-activated MMP2 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method2016Bioorganic & medicinal chemistry, 12-01, Volume: 24, Issue:23
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors.
AID1166723Inhibition of cartilage degradation in monoiodoacetate-induced osteoarthritis rat model assessed as reduction in collagen type 2 C-telopeptide at 10 mg/kg, po once on day 7 of monoiodoacetate administration measured 4 hrs post dose relative to control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID1162786Inhibition of human recombinant MMP3 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID10938250 percent inhibition of human Matrix metalloprotease-13 by the cleavage of fluorogenic peptide MCA-Pro-Leu-Gly-Leu-Dpa-ala-Arg-NH22000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Synthesis and activity of selective MMP inhibitors with an aryl backbone.
AID109390Inhibition of matrix metalloprotease-13 (MMP-13).2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID1433727Inhibition of APMA-activated recombinant human MMP-2 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID109247Inhibitory activity against human Matrix metalloprotease-132001Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
Selective, orally active MMP inhibitors with an aryl backbone.
AID1166670Inhibition of human recombinant TACE using Cy3-PLAQAV(Cy5Q-L-2,3-diaminopropionic acid)-RSSSRNH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID1162787Inhibition of human recombinant MMP7 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID1162813Inhibition of MMP13 in bovine nasal cartilage assessed as collagen degradation at 1 uM after 7 and 14 days2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID238385Inhibition of matrix metalloprotease-22005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
AID1433726Inhibition of APMA-activated recombinant human MMP-13 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID352554Inhibition of MMP32009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID1162812Inhibition of MMP13 in bovine nasal cartilage assessed as collagen degradation at 0.1 uM after 7 and 14 days2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID109072In vitro inhibitory activity against matrix metalloprotease-12003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.
AID11415Cmax after oral administration at 20 mpk in rats2001Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
Selective, orally active MMP inhibitors with an aryl backbone.
AID1433732Inhibition of APMA-activated recombinant human MMP-1 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID1433749Inhibition of MMP13-mediated collagen degradation in bovine nasal septum cartilage assessed as reduction in IL1beta/oncastatin M-stimulated hydroxyproline release at 1 uM measured after 2 weeks relative to control2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID1328779Inhibition of recombinant human AMPA-activated MMP8 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method2016Bioorganic & medicinal chemistry, 12-01, Volume: 24, Issue:23
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors.
AID1166661Inhibition of human recombinant MMP13 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID1433729Inhibition of APMA-activated recombinant human MMP-10 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID352556Inhibition of MMP92009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID107316Inhibition of matrix metalloprotease-2 (MMP-2).2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID238386Inhibition of matrix metalloprotease-32005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
AID352549Inhibition of MMP13-induced cartilage degradation in rat assessed as chondroitin sulfate release at 30 mg/kg, po administered 4 hrs before MMP13 challenge injected intra-articularly measured after 2 hrs by ELISA2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID1166665Inhibition of human recombinant MMP7 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID352546Inhibition of MMP12009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID1433734Inhibition of APMA-activated recombinant human MMP-7 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID109578Inhibitory concentration against Matrix metalloprotease-22001Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
Selective, orally active MMP inhibitors with an aryl backbone.
AID13123Oral bioavailability in rat2001Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
Selective, orally active MMP inhibitors with an aryl backbone.
AID352544Inhibition of MMP132009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID1433735Inhibition of APMA-activated recombinant human MMP-9 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID10876650 percent inhibition of human Matrix metalloprotease-1 by the cleavage of fluorogenic peptide MCA-Pro-Leu-Gly-Leu-Dpa-ala-Arg-NH22000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Synthesis and activity of selective MMP inhibitors with an aryl backbone.
AID1162784Inhibition of human recombinant MMP1 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID1162792Inhibition of human recombinant TACE using Cy3-PLAQAV(Cy5QL-2,3-diaminopropionic acid)-RSSSR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID12487Half life period after intravenous administration at 20 mpk in rats2001Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18
Selective, orally active MMP inhibitors with an aryl backbone.
AID1433736Inhibition of APMA-activated recombinant human GST-tagged MMP-14 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID108922Inhibition of matrix metalloprotease-1 (MMP-1).2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID352547Selectivity ratio of IC50 for MMP1 to IC50 for MMP132009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID352553Inhibition of MMP22009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID604470Ex vivo inhibition of IL-1 and oncostatin M-induced bovine nasal cartilage degradation assessed as release of hydroxproline measured up to 16 days by mass spectrometry2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID1433747Inhibition of MMP13-mediated collagen degradation in bovine nasal septum cartilage assessed as reduction in IL1beta/oncastatin M-stimulated hydroxyproline release at 0.01 uM measured after 2 weeks relative to control2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID1433733Inhibition of APMA-activated recombinant human MMP-3 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID1166663Inhibition of human recombinant MMP2 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID1162790Inhibition of human recombinant MMP10 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID352552Inhibition of MMP13-induced cartilage degradation in rat assessed as chondroitin sulfate release at 10 mg/kg, po administered 4 hrs before MMP13 challenge injected intra-articularly measured after 2 hrs by ELISA2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID182044In vivo inhibition of by Matrix metalloprotease enzyme Sponge-wrapped cartilage assay at 5 mg/kg. po. bid2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.
AID1166669Inhibition of human recombinant GST-tagged MMP14 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID107834Inhibition of matrix metalloprotease-7 (MMP-7).2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID1162785Inhibition of human recombinant MMP2 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID1166664Inhibition of human recombinant MMP3 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID1328774Inhibition of recombinant human AMPA-activated MMP13 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method2016Bioorganic & medicinal chemistry, 12-01, Volume: 24, Issue:23
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors.
AID352545Inhibition of MMP13 in presence of 1% bovine serum albumin2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID1162811Inhibition of MMP13 in bovine nasal cartilage assessed as collagen degradation at 0.01 uM after 7 and 14 days2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID108297In vitro inhibitory activity against matrix metalloprotease-9.2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.
AID215275In vitro inhibitory activity against tumor necrosis factor alpha converting enzyme (TACE).2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.
AID107532Inhibition of matrix metalloprotease-3 (MMP-3).2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID1166666Inhibition of human recombinant MMP8 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
AID1433737Inhibition of TACE (unknown origin) using Cy3-PLAQAV(Cy5Q-L-2,3-diaminopropionic acid)-RSSSR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID1433748Inhibition of MMP13-mediated collagen degradation in bovine nasal septum cartilage assessed as reduction in IL1beta/oncastatin M-stimulated hydroxyproline release at 0.1 uM measured after 2 weeks relative to control2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID10716850 percent inhibition of human Matrix metalloprotease-2 by the cleavage of fluorogenic peptide MCA-Pro-Leu-Gly-Leu-Dpa-ala-Arg-NH22000Bioorganic & medicinal chemistry letters, Dec-18, Volume: 10, Issue:24
Synthesis and activity of selective MMP inhibitors with an aryl backbone.
AID440472Half life in rat at 20 mg/kg, iv2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Hydroxamates: relationships between structure and plasma stability.
AID238384Inhibition of matrix metalloprotease-12005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
AID109410In vitro inhibitory activity against matrix metalloprotease-13.2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.
AID1328781Inhibition of recombinant human AMPA-activated MMP10 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method2016Bioorganic & medicinal chemistry, 12-01, Volume: 24, Issue:23
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors.
AID1433728Inhibition of APMA-activated recombinant human MMP-8 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
AID238806Binding affinity for matrix metalloprotease 132005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
AID1162780Inhibition of human recombinant MMP13 catalytic domain using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID166471Effect of compound on cartilage in surgically induced osteoarthritis (OA) model in rabbit at 25 mg/kg2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID108171Inhibition of matrix metalloprotease-9 (MMP-9).2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID1162789Inhibition of human recombinant MMP9 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID352557Inhibition of MMP142009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID352558Inhibition of TACE2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID1162791Inhibition of human recombinant MMP14 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
AID1796811Enzyme Inhibition Assay from Article 10.1021/jm0500875: \\Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.\\2005Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.
AID1799084Determination of MMP-13 Activity from Article 10.1021/jm801394m: \\Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.\\2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB1999Nature structural biology, Mar, Volume: 6, Issue:3
Crystal structures of MMP-1 and -13 reveal the structural basis for selectivity of collagenase inhibitors.
AID1811Experimentally measured binding affinity data derived from PDB1999Nature structural biology, Mar, Volume: 6, Issue:3
Crystal structures of MMP-1 and -13 reveal the structural basis for selectivity of collagenase inhibitors.
AID493017Wombat Data for BeliefDocking2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (5.26)18.2507
2000's9 (47.37)29.6817
2010's7 (36.84)24.3611
2020's2 (10.53)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.77

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 Index11.77 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.77 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.77)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (94.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]