Page last updated: 2024-12-10

tmi-1

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

Cross-References

ID SourceID
PubMed CID5288615
CHEMBL ID207729
SCHEMBL ID2358255
MeSH IDM0472870

Synonyms (21)

Synonym
IH6 ,
(3s)-4-{[4-(but-2-ynyloxy)phenyl]sulfonyl}-n-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide
1ZXC
(3s)-4-{[4-(but-2-yn-1-yloxy)benzene]sulfonyl}-n-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide
chembl207729 ,
tmi-1
bdbm23498
DB07964
(3s)-4-(4-but-2-ynoxyphenyl)sulfonyl-n-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide
SCHEMBL2358255
tmi 1
287403-39-8
(3s)-4-[[4-(2-butyn-1-yloxy)phenyl]sulfonyl]-n-hydroxy-2,2-dimethyl-3-thiomorpholinecarboxamide
tmi-1, >=98% (hplc)
AKOS027470325
(3s)-4-{[4-(but-2-yn-1-yloxy)phenyl]sulfonyl}-n-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide
EX-A7089
Q27097194
MS-26741
CS-0021358
HY-101448

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" In summary, TMI-1, a dual TACE/MMP inhibitor, represents a unique class of orally bioavailable small molecule TNF inhibitors that may be effective and beneficial for treating RA."( Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheu
Barone, D; Black, R; Brennan, F; Clarke, D; Cummons, T; Feldmann, M; Frost, P; Gibbons, J; Hegen, M; Larsen, G; Levin, J; Li, G; Lin, LL; Mohler, K; Nickerson-Nutter, C; Robertshaw, H; Skotnicki, J; Vansell, N; Xu, J; Zhang, Y, 2004
)
0.9
" 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]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Adam 17Homo sapiens (human)IC50 (µMol)0.00800.00800.00800.0080AID977608
A disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)IC50 (µMol)0.10000.10003.526710.0000AID1798327
Interstitial collagenaseHomo sapiens (human)IC50 (µMol)0.01150.00020.850210.0000AID1798326; AID261911; AID347029
72 kDa type IV collagenaseHomo sapiens (human)IC50 (µMol)0.01030.00001.284810.0000AID1798326; AID1798329; AID300533; AID347020
MatrilysinHomo sapiens (human)IC50 (µMol)0.01310.00142.085910.0000AID1798326
Matrix metalloproteinase-9Homo sapiens (human)IC50 (µMol)0.01310.00000.705310.0000AID1798326
Collagenase 3Homo sapiens (human)IC50 (µMol)0.00880.00000.767510.0000AID1798326; AID1798328; AID261912; AID300534; AID347022
Matrix metalloproteinase-14Homo sapiens (human)IC50 (µMol)0.01110.00030.718210.0000AID1798326; AID1798328
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)IC50 (µMol)0.00680.00021.014010.0000AID1798325; AID1798328; AID261910; AID300532; AID300533; AID347023
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (129)

Processvia Protein(s)Taxonomy
skeletal system developmentA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
proteolysisA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
extracellular matrix disassemblyA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
extracellular matrix organizationA disintegrin and metalloproteinase with thrombospondin motifs 4Homo 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)
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)
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 (22)

Processvia Protein(s)Taxonomy
protease bindingA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
metalloendopeptidase activityA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
protein bindingA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
peptidase activityA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
metallopeptidase activityA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
zinc ion bindingA disintegrin and metalloproteinase with thrombospondin motifs 4Homo 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 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 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 (29)

Processvia Protein(s)Taxonomy
extracellular regionA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
extracellular spaceA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
nuclear speckA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
collagen-containing extracellular matrixA disintegrin and metalloproteinase with thrombospondin motifs 4Homo sapiens (human)
extracellular matrixA disintegrin and metalloproteinase with thrombospondin motifs 4Homo 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 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 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 (26)

Assay IDTitleYearJournalArticle
AID300533Inhibition of human recombinant MMP22007Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
AID261913Inhibition of LPS-stimulated TNF production in THP cells at 3 uM2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
AID281652Inhibition of LPS-stimulated TNFalpha production in mouse model at 10 mg/kg, po at 1 hrs2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors.
AID347022Inhibition of MMP132009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Current perspective of TACE inhibitors: a review.
AID300534Inhibition of human recombinant MMP132007Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
AID347020Inhibition of MMP22009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Current perspective of TACE inhibitors: a review.
AID281654Inhibition of LPS-stimulated TNFalpha production in mouse model at 10 mg/kg, po at 12 hrs2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors.
AID261920Bioavailability in rat at 10 mg/kg2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
AID261921Bioavailability in dog at 10 mg/kg2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
AID297910Inhibition of TNFalpha production in Sprague-Dawley rat at 10 mg/kg, po administered 1 hr prior to LPS challenge after 1.5 hrs2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.
AID261912Inhibition of MMP132006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
AID347029Inhibition of MMP12009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Current perspective of TACE inhibitors: a review.
AID261910Inhibition of TACE2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
AID261919Bioavailability in mouse at 10 mg/kg2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
AID300536Inhibition of human TACE in human whole blood2007Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
AID261911Inhibition of MMP12006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
AID347023Inhibition of TACE2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Current perspective of TACE inhibitors: a review.
AID300532Inhibition of human TACE expressed in CHO cells by FRET assay2007Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
AID261914Inhibition of LPS-stimulated TNF production in THP cells at 1 uM2006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
AID1798327Aggrecanase-1 Inhibition Assay from Article 10.1124/jpet.103.059675: \\Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-conver2004The Journal of pharmacology and experimental therapeutics, Apr, Volume: 309, Issue:1
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheu
AID1798326MMP Inhibition Assay from Article 10.1124/jpet.103.059675: \\Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzym2004The Journal of pharmacology and experimental therapeutics, Apr, Volume: 309, Issue:1
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheu
AID1798328TACE Inhibition Assay from Article 10.1016/j.bmc.2007.06.031: \\Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.\\2007Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
AID1798325TACE Inhibition Assay from Article 10.1124/jpet.103.059675: \\Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzy2004The Journal of pharmacology and experimental therapeutics, Apr, Volume: 309, Issue:1
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheu
AID1798329MMP Inhibition Assay from Article 10.1016/j.bmc.2007.06.031: \\Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.\\2007Bioorganic & medicinal chemistry, Sep-15, Volume: 15, Issue:18
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2005Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates.
AID1811Experimentally measured binding affinity data derived from PDB2005Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (100.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.99

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index32.99 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index36.91 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.99)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]