Page last updated: 2024-12-11

ik 682

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Description

IK 682: inhibits TNF-alpha converting enzyme; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6914621
CHEMBL ID148169
CHEBI ID40083
SCHEMBL ID5966106
MeSH IDM0443074

Synonyms (19)

Synonym
(2r)-n-hydroxy-2-[(3s)-3-methyl-3-{4-[(2-methylquinolin-4-yl)methoxy]phenyl}-2-oxopyrrolidin-1-yl]propanamide
2FV5
CHEBI:40083 ,
chembl148169 ,
bdbm26526
ik682
bmcl181958 compound 1
cid 6914621
ik-682
DB07145
(2r)-n-hydroxy-2-[(3s)-3-methyl-3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2-oxopyrrolidin-1-yl]propanamide
SCHEMBL5966106
ik862
ik-862
gtpl8680
478911-60-3
ik 682
Q27078037
AKOS040748566

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Further optimization led to the discovery of IK682 as a selective and orally bioavailable TACE inhibitor."( Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
Chen, L; Christ, DD; Covington, MB; Decicco, CP; Duan, JJ; Hardman, KD; Liu, RQ; Lu, Z; Magolda, RL; Newton, RC; Qian, M; Wasserman, ZR; Wexler, RR, 2002
)
0.31
" Since the discovery of anti-TNF-alpha biologicals, much efforts have gone into developing an orally bioavailable small size TNF-alpha antagonist."( Current perspective of TACE inhibitors: a review.
DasGupta, S; Giridhar, R; Murumkar, PR; Yadav, MR, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (3)

ClassDescription
hydroxamic acidA compound, RkE(=O)lNHOH, derived from an oxoacid RkE(=O)l(OH) (l =/= 0) by replacing -OH with -NHOH, and derivatives thereof. Specific examples of hydroxamic acids are preferably named as N-hydroxy amides.
quinolinesA class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
pyrrolidin-2-onesA pyrrolidinone in which the oxo group is at position 2 of the pyrrolidine ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (21)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Disintegrin and metalloproteinase domain-containing protein 17Sus scrofa (pig)IC50 (µMol)0.00100.00101.33658.0000AID215267
Disintegrin and metalloproteinase domain-containing protein 17Sus scrofa (pig)Ki0.00060.00060.00060.0006AID1895846; AID215269; AID344653
Interstitial collagenaseHomo sapiens (human)IC50 (µMol)30.00000.00020.850210.0000AID292734
Interstitial collagenaseHomo sapiens (human)Ki30.00000.00030.49487.0000AID108910; AID349373
72 kDa type IV collagenaseHomo sapiens (human)IC50 (µMol)2.05000.00001.284810.0000AID292735
72 kDa type IV collagenaseHomo sapiens (human)Ki2.05000.00000.34663.0000AID107179; AID290502; AID349374
Stromelysin-1Homo sapiens (human)IC50 (µMol)0.14100.00001.148410.0000AID292736
Stromelysin-1Homo sapiens (human)Ki0.14100.00030.54258.0000AID107519; AID290503; AID349375
MatrilysinHomo sapiens (human)Ki0.25900.05401.50527.0000AID107831; AID290504; AID349378
Matrix metalloproteinase-9Homo sapiens (human)IC50 (µMol)10.34000.00000.705310.0000AID292737
Matrix metalloproteinase-9Homo sapiens (human)Ki10.34000.00020.12810.8000AID108156; AID349379
Neutrophil collagenaseHomo sapiens (human)Ki0.25700.00020.17972.1000AID107857; AID349376
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)10.34000.00071.600310.0000AID292737
Collagenase 3Homo sapiens (human)IC50 (µMol)1.41700.00000.767510.0000AID292738
Collagenase 3Homo sapiens (human)Ki1.41700.00000.47593.8000AID109386; AID290506; AID349377
Matrix metalloproteinase-14Homo sapiens (human)Ki15.87200.01400.06770.1100AID109557; AID349381
Matrix metalloproteinase-15Homo sapiens (human)Ki3.99703.99703.99703.9970AID109568; AID349415
Matrix metalloproteinase-16Homo sapiens (human)Ki1.59901.59901.59901.5990AID109572; AID349413
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)IC50 (µMol)0.02890.00021.014010.0000AID290501; AID292733; AID292736; AID347023
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Ki0.00010.00010.50303.7000AID1798700; AID411501
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)10.34000.00071.630610.0000AID292737
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)10.34000.00061.525710.0000AID292737
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)10.34000.00071.747210.0000AID292737
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)10.34000.00071.741110.0000AID292737
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)10.34000.00071.741110.0000AID292737
Disintegrin and metalloproteinase domain-containing protein 33Homo sapiens (human)Ki0.01500.01500.01500.0150AID344620
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)10.34000.00071.741110.0000AID292737
[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)
Chain A, Adam 17Homo sapiens (human)Kd0.00000.00000.00000.0000AID977611
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (138)

Processvia Protein(s)Taxonomy
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)
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)
proteolysisMatrix metalloproteinase-15Homo sapiens (human)
extracellular matrix disassemblyMatrix metalloproteinase-15Homo sapiens (human)
collagen catabolic processMatrix metalloproteinase-15Homo sapiens (human)
response to estradiolMatrix metalloproteinase-15Homo sapiens (human)
endodermal cell differentiationMatrix metalloproteinase-15Homo sapiens (human)
protein modification processMatrix metalloproteinase-15Homo sapiens (human)
extracellular matrix organizationMatrix metalloproteinase-15Homo sapiens (human)
endochondral ossificationMatrix metalloproteinase-16Homo sapiens (human)
proteolysisMatrix metalloproteinase-16Homo sapiens (human)
protein processingMatrix metalloproteinase-16Homo sapiens (human)
chondrocyte proliferationMatrix metalloproteinase-16Homo sapiens (human)
embryonic cranial skeleton morphogenesisMatrix metalloproteinase-16Homo sapiens (human)
craniofacial suture morphogenesisMatrix metalloproteinase-16Homo sapiens (human)
skeletal system developmentMatrix metalloproteinase-16Homo sapiens (human)
extracellular matrix organizationMatrix metalloproteinase-16Homo sapiens (human)
collagen catabolic processMatrix metalloproteinase-16Homo 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)
proteolysisDisintegrin and metalloproteinase domain-containing protein 33Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
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)
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)
metalloendopeptidase activityMatrix metalloproteinase-15Homo sapiens (human)
protein bindingMatrix metalloproteinase-15Homo sapiens (human)
enzyme activator activityMatrix metalloproteinase-15Homo sapiens (human)
zinc ion bindingMatrix metalloproteinase-15Homo sapiens (human)
metalloaminopeptidase activityMatrix metalloproteinase-15Homo sapiens (human)
metalloendopeptidase activityMatrix metalloproteinase-16Homo sapiens (human)
enzyme activator activityMatrix metalloproteinase-16Homo sapiens (human)
zinc ion bindingMatrix metalloproteinase-16Homo sapiens (human)
metalloaminopeptidase activityMatrix metalloproteinase-16Homo 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)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 33Homo sapiens (human)
zinc ion bindingDisintegrin and metalloproteinase domain-containing protein 33Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

Processvia Protein(s)Taxonomy
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 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)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
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)
plasma membraneMatrix metalloproteinase-15Homo sapiens (human)
extracellular matrixMatrix metalloproteinase-15Homo sapiens (human)
extracellular spaceMatrix metalloproteinase-15Homo sapiens (human)
Golgi lumenMatrix metalloproteinase-16Homo sapiens (human)
plasma membraneMatrix metalloproteinase-16Homo sapiens (human)
cell surfaceMatrix metalloproteinase-16Homo sapiens (human)
extracellular matrixMatrix metalloproteinase-16Homo sapiens (human)
plasma membraneMatrix metalloproteinase-16Homo sapiens (human)
extracellular spaceMatrix metalloproteinase-16Homo 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)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
membraneDisintegrin and metalloproteinase domain-containing protein 33Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (61)

Assay IDTitleYearJournalArticle
AID1811Experimentally measured binding affinity data derived from PDB2006Archives of biochemistry and biophysics, Jul-01, Volume: 451, Issue:1
IK682, a tight binding inhibitor of TACE.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2006Archives of biochemistry and biophysics, Jul-01, Volume: 451, Issue:1
IK682, a tight binding inhibitor of TACE.
AID57001The compound was administered intravenously at a dose of 4 mg/Kg for determination area under curve2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID215436Inhibition of Tumor necrosis factor alpha secretion in LPS-stimulated human whole blood assay2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID109557Affinity for Matrix metalloprotease-14 (MMP-14)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID349377Inhibition of MMP132008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID109572Affinity for Matrix metalloprotease-16 (MMP-16)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID344653Inhibition of pig TACE2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID107857Affinity for Matrix metalloprotease-8 (MMP-8)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID349378Inhibition of MMP72008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID290501Inhibition of pTACE2007Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
AID108156Affinity towards Matrix metalloprotease-9 (MMP-9)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID173090The compound was administered intravenously at a dose of 4 mg/Kg for determination of systemic clearance2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID347023Inhibition of TACE2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Current perspective of TACE inhibitors: a review.
AID292735Inhibition of MMP22007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Identification of potent and selective TACE inhibitors via the S1 pocket.
AID349415Inhibition of MMP152008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID63432The compound was administered intravenously at a dose of 4 mg/Kg for determination of volume of distribution at steady state2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID290503Binding affinity to MMP32007Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
AID60296The compound was administered intravenously at a dose of 4 mg/Kg for determination of systemic clearance2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID347194Fraction unbound in human serum2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Current perspective of TACE inhibitors: a review.
AID292734Inhibition of MMP12007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Identification of potent and selective TACE inhibitors via the S1 pocket.
AID347195Oral bioavailability in rat2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Current perspective of TACE inhibitors: a review.
AID344621Inhibition of LPS-stimulated TNFalpha production in whole blood2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID196512The compound was administered orally at a dose of 8 mg/Kg for determination of t max2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID292733Inhibition of TACE2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Identification of potent and selective TACE inhibitors via the S1 pocket.
AID349376Inhibition of MMP82008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID347036Oral bioavailability in dog2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Current perspective of TACE inhibitors: a review.
AID107831Affinity for Matrix metalloprotease-7 (MMP-7)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID107179Affinity for Matrix metalloprotease-2 (MMP-2)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID349374Inhibition of MMP22008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID63011The compound was administered intravenously at a dose of 4 mg/Kg for determination of terminal half life2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID215269Affinity for Tumor necrosis factor alpha converting enzyme (TACE)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID58035Bioavailability (dose 8 mg/kg p.o.)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID109386Affinity for Matrix metalloprotease-13 (MMP-13)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID109568Affinity for Matrix metalloprotease-15 (MMP-15)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID1895846Inhibition of porcine TACE2021European journal of medicinal chemistry, Dec-15, Volume: 226Zinc enzymes in medicinal chemistry.
AID349413Inhibition of MMP162008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID349375Inhibition of MMP32008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID292736Inhibition of MMP32007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Identification of potent and selective TACE inhibitors via the S1 pocket.
AID344620Inhibition of ADAM332008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID170078The compound was administered intravenously at a dose of 4 mg/Kg for determination area under curve2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID290502Binding affinity to MMP22007Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
AID411501Inhibition of TACE catalytic domain by FRET assay2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.
AID349373Inhibition of MMP12008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID292738Inhibition of MMP132007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Identification of potent and selective TACE inhibitors via the S1 pocket.
AID349379Inhibition of MMP92008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID108910Affinity towards Matrix metalloprotease-1 (MMP-1)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID192013The compound was administered intravenously at a dose of 4 mg/Kg for determination of volume of distribution at steady state2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID107519Affinity for Matrix metalloprotease-3 (MMP-3)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID172654Bioavailability (dose 8 mg/kg p.o.)2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID290506Binding affinity to MMP132007Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
AID349381Inhibition of MMP142008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID347193Inhibition of TNFalpha production in whole blood2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Current perspective of TACE inhibitors: a review.
AID63010The compound was administered orally at a dose of 8 mg/Kg for determination of t max2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID292737Inhibition of MMP92007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Identification of potent and selective TACE inhibitors via the S1 pocket.
AID290504Binding affinity to MMP72007Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
AID196522The compound was administered intravenously at a dose of 4 mg/Kg for determination of terminal half life2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID215267Inhibitory activity against porcine Tumor necrosis factor alpha converting enzyme.2002Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
AID1345418Human ADAM33 (M12: Astacin/Adamalysin)2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID1345458Human ADAM17 (M12: Astacin/Adamalysin)2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
AID1798700TACE Inhibition Assay from Article 10.1016/j.bmcl.2008.11.034: \\Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.\\2009Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's9 (90.00)29.6817
2010's0 (0.00)24.3611
2020's1 (10.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.96

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 Index11.96 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.96)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (30.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (70.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]