Information on EC 3.4.24.86 - ADAM 17 endopeptidase

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The expected taxonomic range for this enzyme is: Eutheria

EC NUMBER
COMMENTARY
3.4.24.86
-
RECOMMENDED NAME
GeneOntology No.
ADAM 17 endopeptidase
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
Narrow endopeptidase specificity. Cleaves Pro-Leu-Ala-Gln-Ala-/-Val-Arg-Ser-Ser-Ser in the membrane-bound, 26-kDa form of tumor necrosis factor alpha (TNFalpha). Similarly cleaves other membrane-anchored, cell-surface proteins to 'shed' the extracellular domains
show the reaction diagram
proTNF-alpha + H2O = soluble TNF-alpha. Cleavage of the precursor of tumor necrosis factor proTNFalpha to the mature tumor necrosis factor TNF-alpha, Swiss-Prot Acesssion Numbers: P78536(human), Q77636(pig), Q9Z1K9(rat), Q9Z0F8(mouse), Q923X3(chinese hamster). In peptidase family M12. In vivo, the cleavage of tumor necrosis factor alpha precursor releases the soluble, 17-kDa TNFa, which induces inflammation.
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SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
(TACE/ADAM17/CD156q)
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(TACE:ADAM17)
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a disintegrin and metalloprotease 17
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a disintegrin and metalloprotease 17
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ADAM-17
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ADAM17 proteinase
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ADAM17/tumor necrosis factor-alpha (TNF-A)converting enzyme
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ADAMTS-2
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CD156
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H-TACE
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human TACE B
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metalloprotease TACE
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metalloprotease-disintegrin tumour necrosis factor alpha convertase
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metalloproteinase ADAM17
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pro tumor necrosis factor cleavage enzyme
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pro-tumor necrosis factor-alpha-processing enzyme
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proteinase, pro-tumor necrosis factor (9CI)
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sheddase
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TACE
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TACE proteinase
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TACE/ADAM17
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TACE/ADAM17
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TNF-alpha convertase
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TNF-alpha converting enzyme
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TNF-alpha converting enzyme
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TNF-alpha converting enzyme
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TNF-alpha converting enzyme
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TNF-alpha processing protease
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tumor necrosis factor alpha convertase
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tumor necrosis factor alpha converting enzyme
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tumor necrosis factor alpha converting enzyme
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tumor necrosis factor alpha-converting enzyme
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tumor necrosis factor alpha-converting enzyme
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tumor necrosis factor alpha-converting enzyme
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tumor necrosis factor-alpha converting enzyme
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tumor necrosis factor-alpha converting enzyme
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tumor necrosis factor-alpha converting enzyme
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tumor necrosis factor-alpha converting enzyme
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tumor necrosis factor-alpha converting enzyme
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tumor necrosis factor-alpha-converting enzyme
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tumor necrosis factor-alpha-converting enzyme
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tumour necrosis factor alpha-converting enzyme
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tumour necrosis factor alpha-converting enzyme
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CAS REGISTRY NUMBER
COMMENTARY
151769-16-3
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
african green monkey, COS-7, an SV40 transformed kidney cell line
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-
Manually annotated by BRENDA team
chinese hamster, fragment
SwissProt
Manually annotated by BRENDA team
tumor necrosis factor-alpha-converting enzyme
SwissProt
Manually annotated by BRENDA team
tumor necrosis factor-alpha-converting enzyme mutant variant M1
SwissProt
Manually annotated by BRENDA team
tumor necrosis factor-alpha-converting enzyme mutant variant M2a; tumor necrosis factor-alpha-converting enzyme mutant variant M2b
SwissProt
Manually annotated by BRENDA team
accession number for cytoplasmic domain coding sequence
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-
Manually annotated by BRENDA team
HEK293 cells
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-
Manually annotated by BRENDA team
HEK293 cells; human monocytic cell line THP-1; SH-SY5Y
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-
Manually annotated by BRENDA team
HeLa cells; human
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Manually annotated by BRENDA team
HeLa cells; human; human monocytic cell line THP-1
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-
Manually annotated by BRENDA team
human monocytic cell line THP-1
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Manually annotated by BRENDA team
human; human monocytic cell line THP-1
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-
Manually annotated by BRENDA team
human; MonoMac 6 cells
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-
Manually annotated by BRENDA team
HUVECs
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-
Manually annotated by BRENDA team
MonoMac 6 cells
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-
Manually annotated by BRENDA team
MonoMac 6 cells; Ntera2/cl.D1, human embryonal carcinoma cell line
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Manually annotated by BRENDA team
recombinant
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-
Manually annotated by BRENDA team
BAC-1.2F5 immortalized by transfection with replication-deficient SV40 DNA; Dexter-ras-myc cell line
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Manually annotated by BRENDA team
EC-2, clonal Ras/Myc-immortalized fibroblast cell line; mouse
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Manually annotated by BRENDA team
mouse; strain 129, strain C57Bl/6 chimaera/ly9.l-
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-
Manually annotated by BRENDA team
mouse; strain AC2/G3
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Manually annotated by BRENDA team
mouse; strain C3H/HEN
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Manually annotated by BRENDA team
mouse; wild-type EC-4
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Manually annotated by BRENDA team
Mus musculus AC2/G3
strain AC2/G3
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Manually annotated by BRENDA team
Mus musculus C3H/HEN
strain C3H/HEN
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-
Manually annotated by BRENDA team
Mus musculus EC-4
wild-type EC-4
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Manually annotated by BRENDA team
female, Lewis
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Manually annotated by BRENDA team
immature Sprague Dawley
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Manually annotated by BRENDA team
rat; strain Lewis
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Manually annotated by BRENDA team
Rattus norvegicus Lewis
strain Lewis
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Manually annotated by BRENDA team
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SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
-
transient transfection with siRNAs targeting ADAM17, which ablates its expression by up to 90%, inhibits phenyl mercuric acetate-stimulated shedding activity by up to 70%, indicating that ADAM17 is the major sheddase
malfunction
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to determine the involvement of ADAM10 and ADAM17 in G protein coupled receptor P2Y2 nucleotide receptor-mediated EGFR activation, human salivary gland cells are transfected with small interfering RNA targeting either ADAM10 or ADAM17 mRNA. Transfection of human salivary gland cells with ADAM10 or ADAM17 siRNA partially suppress EGFR and ERK1/2 phosphorylation induced by UTP, whereas co-transfection with both ADAM10 and ADAM17 siRNA almost completely preventd UTP-induced EGFR and ERK1/2 phosphorylation
malfunction
-
inhibition of ADAM17 protects from lipopolysaccharide-induced sepsis
malfunction
-
ADAM17 knockdown leads to a dramatic cell growth suppression in NCI-H292 cells
malfunction
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ADAM17-deficient mice are not viable. Mice with dramatically reduced ADAM17 levels show substantially increased susceptibility to inflammation in dextran sulfate sodium colitis and develop eye, heart, and skin defects
malfunction
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inhibition of ADAM17 leads to the upregulation of transforming growth factor-beta signaling
malfunction
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ADAM17-deficient mice have defects in the mammary epithelium, vascular system, lung, eye, hair, heart and skin and as a result die between embryonic day 17.5 and the first few days after birth
physiological function
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a cell-based ADAM17 assay is used to show that thiol isomerases, specifically protein disulfide isomerase, could be responsible for maintaining ADAM17 in an inactive form. Down-regulation of thiol isomerases, by changes in the redox environment markedly enhances ADAM17 activation
physiological function
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knockdown of both endogenous ADAM10 and endogenous ADAM17 by siRNA inhibits FcalphaR, i.e. Fc receptor for immunoglobulin A, shedding
physiological function
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ADAM10 and ADAM17 are activated by G protein-coupled receptor P2Y2
physiological function
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Notch1 signaling independent of ligands requires ADAM17, while ADAM10 is absolutely required for Notch1 signaling induced by ligands. Both proteases participate in signaling intrinsic to Notch mutations associated with leukemia
physiological function
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knocking down ADAM-17 expression using lentivirus-delivered siRNA in HUVECs inhibits cell proliferation and the ability of cells to form close contact in two-dimensional cultures. Similarly, ADAM-17 depletion inhibits the ability of HUVECs to form capillary-like networks on top of three-dimensional Matrigel as well as in coculture with fibroblasts within a three dimensional scaffold. Both baseline and VEGF-induced MMP-2 activation and Matrigel invasion are inhibited by ADAM-17 depletion
physiological function
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granulocyte-macrophage colony-stimulating factor GM-CSF and interleukin-4 in combination potently up-regulate tumor necrosis factor-alpha coverting enzyme TACE and activity in monocytes, causing ectodomain shedding of macrophage colony-stimulating factor M-CSF receptor, resulting in the disruption of its phosphorylation by M-CSF as well as the induction of osteoclastogenesis from monocytes by M-CSF and receptor activator of nuclear factor-kappaB RANK ligand. TACE inhibition robustly causes the resumption of the surface expression of M-CSF receptor on monocytes, facilitating M-CSF-mediated phosphorylation of M-CSF receptor and macrophage/osteoclast differentiation while impairing GM-CSF- and IL-4-mediated dendritic cell differentiation from monocytes
physiological function
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addition of human recombinant TACE promotes gene expression of endothelial specific markers including vWF, CD31, VE-cadherin, Flk-1 and Flt-1 in differentiating rat marrow stromal cells. Inhibition of TACE with TAPI-2 or inhibition of TNF-alpha with Etanercept attenuates endothelial differentiation of marrow stromal cells in direct co-culture condition with rain microvascular endothelial cells
physiological function
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inhibition of TACE with TAPI-2 or inhibition of TNF-alpha with Etanercept attenuates endothelial differentiation of marrow stromal cells in the direct co-culture condition with rain microvascular endothelial cells
physiological function
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small interfering RNA-mediated silencing of ADAM17 in AGS cells inhibits the repression of wild-type HKalpha promoter, i.e. gastric H, K-adenosine triphosphatase alpha-subunit promoter, and reduces ADAM17 activity and heparin-binding epidermal growth factor production, compared to controls
physiological function
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anti-Ro/SSA autoantibodies determine TACE pro-domain shedding suggesting that TACE activity is necessary for the release of TNF-alpha observed in anti-Ro/SSA autoantibody-stimulated cells. Adalimumab appears to be significantly more efficacious than Etanercept in preventing TACE activation caused by anti-Ro/SSA autoantibodies. Regulation of TACE may participate in the pathogenic role of autoantibodies and the modulation of TACE expression by TNF-alpha antagonists might contribute to the beneficial effect of these drugs in inflammatory and autoimmune diseases
physiological function
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ADAM17 is physically associated with active extracellular signal-regulated kinases ERK1/2 and is phosphorylated at serine residues in an ERK-dependent manner in wounded cells
physiological function
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inhibition and knockdown of ADAM17/TACE blocks the shedding of MHC class I-related chain. The recruitment of both enzyme and substrate to detergent-resistant membrane microdomains is crucial for efficient proteolysis
physiological function
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shRNA-approach to knock down ADAM17 expression in Jurkat cells show that during early events of death receptor-mediated neutrophil apoptosis, L-selectin downregulation occurs primarily by ADAM17-mediated shedding. The downregulation of L-selectin occurs by ectodomain shedding
physiological function
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during early events of death receptor-mediated neutrophil apoptosis, L-selectin downregulation occurs primarily by ADAM17-mediated shedding. ADAM17 activity occurs during programmed cell death. The cleavage of particular ADAM17 substrates may be an additional component of the anti-inflammatory program initiated by apoptotic neutrophils. During later stages of induced leukocyte apoptosis, soluble L-selectin production occurs independent of ADAM17, as well as membrane events, such as blebbing and microparticle production
physiological function
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silencing of ADAM17 by siRNA leads to significant inhibition of cell proliferation compared to the control groups at 24, 48 and 72 hours, and apoptosis is significantly increased at 48 hours. Cells that received a combination of siRNA transfection and genistein treatment, show a further significant decrease of proliferation and increase in apoptosis compared with either treatment alone
physiological function
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in 1C11-derived neuronal cells, antibody-mediated prion protein ligation triggers TNF-alpha release, through recruitement of the metalloproteinase TNF-alpha converting enzyme TACE. TNF-alpha shed in response to prion protein acts as a second message signal, eliciting serotonin or norepinephrine degradation in 1C115-HT or 1C11NE cells, respectively
physiological function
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increased expression and shedding of fractalkine by endothelial cells under pro-inflammatory conditions is not regulated by an increased activity of ADAM-17
physiological function
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silencing of ADAM17, but not ADAM15, expression using small interfering RNA interferes with endothelial cell invasion, resulting in decreased density of invading cells and decreased invasion distance. Stable endothelial cell lines expressing short hairpin RNA directed to ADAM17 are similarly inhibited. Expression of ADAM17 dominant negative mutant, but not ADAM10 or ADAM15 dominant negative mutants, decreases invasion density and distance. ADAM17 dominant negative mutant cells exhibit far greater numbers of protruding sprouts compared to control, suggesting an inability of extended processes to retract properly. Data suggest a role for ADAM17 in modulating endothelial sprouting events during angiogenesis
physiological function
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Porphyromonas gingivalis challenge results in a concentration-dependent enhancement of TACE messenger RNA expression and protein release by Jurkat cells. The induction of TACE by T-cells in response to Porphyromonas gingivalis may in turn favour the shedding of host cell-bound cytokines into the local microenvironment, potentially amplifying the inflammatory response
physiological function
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vitamin B12 cellular deficiency produces a slower proliferation and a speedier differentiation of neuroblastoma cells through interacting signaling pathways that are related with increased expression of phophatase 2A, pro-nerve growth factor and TACE
physiological function
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ADAM17 has pro-inflammatory activity, protects from osteoporosis and is necessary for the growth of lung cancer cells
physiological function
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the enzyme increases receptor activator of nuclear factor-kappaB ligand secretion and decreases osteoprotegerin protein expression in osteoblasts
physiological function
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ADAM17 regulates epidermal growth factor receptor expression through the activation of Notch1 in non-small cell lung cancer. ADAM17 mediates cell growth, survival, and tumorigenicity by epidermal growth factor receptor-independent mechanisms
physiological function
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ADAM17is the main sheddase of interleukin-6 receptor to induce interleukin-6 trans-signaling
physiological function
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ADAM17 is needed for vital regenerative activities during the immune response. ADAM17 is not crucial for developmental Notch or Notch ligand function in vivo
physiological function
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through the cleavage of vasorin, ADAM17 controls transforming growth factor-beta-mediated epithelial-to-mesenchymal transition
physiological function
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ADAM17 plays an in vivo role in controlling inflammation and tissue regeneration. ADAM17 modulates inflammation by activation of TNFR- and IL-6R-mediated signal transduction. ADAM17 activity regulates both homeostatic and activation-induced changes in cell surface L-selectin density and, thus, might direct the migration patterns of activated lymphocytes and neutrophils in vivo. Apoptosis leads to activation of ADAM17. During ADAM17 maturation, the prodomain is removed by furin cleavage. ADAM17 protects hepatocytes from apoptosis
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(7-methoxycoumarin-4-yl)-acetyl-KSPLAQA-VRSSSRK(2,4-dinitrophenyl)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-Pro-Leu-Ala-Gln-Ala-Val-[N-3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl]-Arg-Ser-Ser-Ser-Arg-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-SPLAQAVRSSSRK-(2,4-dinitrophenyl)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
(7-methoxycoumarin-4-yl)acetyl-Ser-Pro-Leu-Ala-Gln-Ala-Val-Arg-Ser-Ser-Ser-Arg-Lys(Dnp)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
26 kDa proTNF-alpha + H2O
17 kDa soluble TNF-alpha + ?
show the reaction diagram
-
-
-
?
4',5'-dimethoxyfluoresceinyl-SPLAQAVRSSSR-cys(4-(3-succinimid-1-yl)fluorescein)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-(yl)acetyl-Pro-Leu-Ala-Gln-Ala-Val-Arg-Ser-Ser-Ser-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl-Arg-NH2 + H2O
?
show the reaction diagram
-
an internally quenched peptide substrate is used
-
-
?
7-methoxycoumarin-4-yl-acetyl-Lys-Pro-Leu-Gly-Pro-Leu-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl-Ala-Arg + H2O
?
show the reaction diagram
-
-
-
-
?
75kDaTNFR2 + H2O
?
show the reaction diagram
-
-
-
-
?
75kDaTNFR2 + H2O
?
show the reaction diagram
-
-
-
-
?
ACE2 + H2O
?
show the reaction diagram
-
-
-
-
?
acetyl-SPLAQAVRSSSR-COOH + H2O
acetyl-SPLAQA + VRSSSR-COOH
show the reaction diagram
-
-
-
?
ALCAM + H2O
?
show the reaction diagram
-
-
-
-
?
Alzheimer's disease amyloid precursor protein + H2O
?
show the reaction diagram
-
TACE is involved in shedding of Alzheimer's disease amyloid precursor protein
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-
?
amphiregulin + H2O
?
show the reaction diagram
-
-
-
-
?
amphiregulin + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid-protein precursor + H2O
?
show the reaction diagram
-
-
-
-
?
angiotensin-converting enzyme-2 + H2O
?
show the reaction diagram
-
ADAM-17 is responsible for the ACE2 shedding
-
-
?
AREG + H2O
?
show the reaction diagram
-
-
-
-
?
beta-amyloid precursor protein + H2O
?
show the reaction diagram
-
-
-
-
?
beta-amyloid precursor protein + H2O
?
show the reaction diagram
-
-
-
-
?
beta-amyloid precursor protein + H2O
?
show the reaction diagram
-
shedding
-
-
?
beta-amyloid precursor protein + H2O
?
show the reaction diagram
-
Alzheimer amyloid precursor protein
-
-
?
beta-amyloid precursor protein + H2O
?
show the reaction diagram
-
alpha-secretase processing
-
-
?
beta-amyloid precursor protein + H2O
?
show the reaction diagram
-
APP
-
-
?
BTC + H2O
?
show the reaction diagram
-
-
-
-
?
c-KLR + H2O
?
show the reaction diagram
-
-
-
-
?
CD163 + H2O
?
show the reaction diagram
-
-
-
-
?
CD26L + H2O
?
show the reaction diagram
-
-
-
-
?
CD30 + H2O
?
show the reaction diagram
-
-
-
-
?
CD30 + H2O
?
show the reaction diagram
-
-
-
-
?
CD30 + H2O
?
show the reaction diagram
-
shedding of CD30 upon inhibition of the proteasome is catalyzed by ADAM17
-
-
?
CD40 + H2O
?
show the reaction diagram
-
-
-
-
?
CD44 + H2O
?
show the reaction diagram
-
-
-
-
?
CD89 + H2O
?
show the reaction diagram
-
-
-
-
?
CD91 + H2O
?
show the reaction diagram
-
-
-
-
?
cellular prion protein PrPc + H2O
?
show the reaction diagram
-
-
-
-
?
collagen type XVII + H2O
?
show the reaction diagram
-
-
-
-
?
CSF-1 + H2O
?
show the reaction diagram
-
-
-
-
?
CSF1R + H2O
?
show the reaction diagram
-
-
-
-
?
DLL1 + H2O
?
show the reaction diagram
-
-
-
-
?
Dpa-SPLAQAVRSSSR-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
DSG2 + H2O
?
show the reaction diagram
-
-
-
-
?
endothelial protein C receptor + H2O
?
show the reaction diagram
-
-
-
-
?
EpCAM + H2O
?
show the reaction diagram
-
-
-
-
?
EPCR + H2O
?
show the reaction diagram
-
-
-
-
?
epidermal growth factor receptor + H2O
?
show the reaction diagram
-
-
-
-
?
epigen + H2O
?
show the reaction diagram
-
-
-
-
?
epiregulin + H2O
?
show the reaction diagram
-
-
-
-
?
EPR + H2O
?
show the reaction diagram
-
-
-
-
?
ErbB4 + H2O
?
show the reaction diagram
-
-
-
-
?
erbB4/HER4 + H2O
?
show the reaction diagram
Mus musculus, Mus musculus AC2/G3
-
epidermal growth factor, essential function in heart and neural development, TACE is essential for regulated shedding of the HER4 JM-a receptor
-
-
?
EREG + H2O
?
show the reaction diagram
-
-
-
-
?
FcalphaR + H2O
?
show the reaction diagram
-
i.e. Fc receptor for immunoglobulin A
-
-
?
FLT-3L + H2O
?
show the reaction diagram
-
-
-
-
?
fractalkine + H2O
?
show the reaction diagram
-
-
-
-
?
fractalkine + H2O
?
show the reaction diagram
-
-
-
-
?
fractalkine + H2O
?
show the reaction diagram
-
FK, CX3CL1
-
-
?
GHR + H2O
?
show the reaction diagram
-
-
-
-
?
glycoprotein Ibalpha + H2O
?
show the reaction diagram
-
-
-
-
?
glycoprotein Ibalpha + H2O
?
show the reaction diagram
-
-
-
-
?
glycoprotein Ibalpha + H2O
?
show the reaction diagram
-
ADAM17 is the key enzyme mediating shedding of glycoprotein Ibalpha
-
-
?
glycoprotein V + H2O
?
show the reaction diagram
-
-
-
-
?
GPIba + H2O
?
show the reaction diagram
-
-
-
-
?
growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
?
growth hormone binding protein + H2O
?
show the reaction diagram
-
shedding, TACE is critical for PMA-induced GH receptor proteolysis and GHBP generation
-
-
?
growth hormone receptor + H2O
?
show the reaction diagram
-
growth hormone receptor/TACE interaction precedes proteolysis and is transient
-
-
?
HB-EGF + H2O
?
show the reaction diagram
-
-
-
-
?
HB-EGF heparin binding epidermal growth factor + H2O
?
show the reaction diagram
-
-
-
-
?
heparin-binding EGF-like growth factor + H2O
?
show the reaction diagram
-
-
-
-
?
heparin-binding EGF-like growth factor + H2O
?
show the reaction diagram
-
ADAM17 may be involved in heparin-binding EGF-like growth factor cleavage in response to injury
-
-
?
heparin-binding epidermal growth factor-like growth factor + H2O
?
show the reaction diagram
-
-
-
-
?
HER-4 Jma + H2O
?
show the reaction diagram
-
-
-
-
?
heregulin + H2O
?
show the reaction diagram
-
-
-
-
?
ICAM-1 + H2O
?
show the reaction diagram
-
-
-
-
?
IGF-2 receptor + H2O
?
show the reaction diagram
-
-
-
-
?
intercellular adhesion molecule-1 + H2O
?
show the reaction diagram
-
ADAM-17 mediates shedding of intercellular adhesion molecule-1. The shedding of intercellular adhesion molecule-1 reduces the adhesive capacity of the cells. the cleavage site in the intercellular adhesion molecule-1 is not sequence-specific, but appears to be nonselective
-
-
?
intercellular cell adhesion molecule-1 + H2O
?
show the reaction diagram
-
-
-
-
?
interleukin (IL)-1R-II + H2O
?
show the reaction diagram
-
-
-
-
?
interleukin (IL)-1R-II + H2O
?
show the reaction diagram
-
-
-
?
interleukin (IL)-1R-II + H2O
?
show the reaction diagram
-
-
-
-
?
interleukin-1 receptor 2 + H2O
?
show the reaction diagram
-
-
-
-
?
interleukin-6 receptor + H2O
soluble interleukin-6 receptor + ?
show the reaction diagram
-
-
-
?
interleukin-6-receptor + H2O
?
show the reaction diagram
-
-
-
-
?
Jagged protein + H2O
?
show the reaction diagram
-
-
-
-
?
JAM-A + H2O
?
show the reaction diagram
-
-
-
-
?
KL-1 + H2O
?
show the reaction diagram
-
-
-
-
?
KL-1 + H2O
?
show the reaction diagram
-
-
-
-
?
KL-2 + H2O
?
show the reaction diagram
-
-
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
-
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
-
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
-
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
shedding
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
regulates plasma membrane composition and releases soluble signaling molecules and receptors from cells
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
during early events of death receptor-mediated neutrophil apoptosis, L-selectin downregulation occurs primarily by ADAM17-mediated shedding. During later stages of induced leukocyte apoptosis, soluble L-selectin production occurs independent of ADAM17
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
TACE is involved in cantharidin-induced shedding of L-selectin. Cantharidin induces sustained surface expression and cytoplasmic tail phosphorylation of TACE via p38 MAPK, while L-selectin is involved in promoting protein kinase C-dependent shedding
-
-
-
L-selectin + H2O
?
show the reaction diagram
-
ADAM17 is the main sheddase of the adhesion protein L-selectin
-
-
?
L1-CAM + H2O
?
show the reaction diagram
-
-
-
-
?
LAG-3 + H2O
?
show the reaction diagram
-
-
-
-
?
LAQAVRSSSR + H2O
?
show the reaction diagram
-
fluorimetric assay for TACE, fluorogenic substrate, a 10-amino-acid peptide capped with an o-aminobenzoyl group on the N-terminal end and with a 3-(2,4-dinitrophenyl)-L-2,3-diaminopropionic amide group on the C-terminal end, enzymatic conversion of the substrate results in a fluorescence enhancement of 11fold
-
-
?
lipoprotein-related protein I + H2O
?
show the reaction diagram
-
lipoprotein-related protein I shedding is significantly decreased in embryonic fibroblast cells lacking ADAM10 and/or ADAM17
-
-
?
LOX-1 + H2O
?
show the reaction diagram
-
-
-
-
?
LTA + H2O
?
show the reaction diagram
-
-
-
-
?
LYPD3 + H2O
?
show the reaction diagram
-
-
-
-
?
macrophage colony-stimulating factor receptor M-CSFR + H2O
?
show the reaction diagram
-
-
-
-
?
Mca-PLAQAV-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide-RSSSR-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
MHC class I-related chain + H2O
?
show the reaction diagram
-
i.e. transmembrane protein expressed in pathological conditions, ligands for the activating receptor NKG2D found on cytotoxic lymphocytes. The recruitment of both enzyme and substrate to detergent-resistant membrane microdomains is crucial for efficient proteolysis
-
-
?
MICA + H2O
?
show the reaction diagram
-
-
-
-
?
MUC-1 + H2O
?
show the reaction diagram
-
-
-
-
?
NCAM + H2O
?
show the reaction diagram
-
-
-
-
?
nectin-4 + H2O
?
show the reaction diagram
-
-
-
-
?
NH2-LAQAVRSSSR-OH + H2O
?
show the reaction diagram
-
uncapped counterpart of the fluorogenic substrate
-
-
?
Notch 1 + H2O
?
show the reaction diagram
-
ADAM17 is required for Notch1 receptor proteolysis in NSCLC cells in vitro and in vivo
-
-
?
notch 1 receptor + H2O
?
show the reaction diagram
-
-
-
-
?
Notch1 + H2O
?
show the reaction diagram
-
-
-
-
?
Notch1 + H2O
?
show the reaction diagram
-
Notch1 is a substrate for both ADAM10 and ADAM17
-
-
?
NPR + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-LAQAFRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
?
show the reaction diagram
-
enzymatic cleavage 22%
-
-
?
o-aminobenzoyl-LAQAIRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
?
show the reaction diagram
-
enzymatic cleavage 66%
-
-
?
o-aminobenzoyl-LAQALRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
?
show the reaction diagram
-
enzymatic cleavage 92%
-
-
?
o-aminobenzoyl-LAQAVRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
?
show the reaction diagram
-
enzymatic cleavage 90%
-
-
?
o-aminobenzoyl-LAQFVRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
?
show the reaction diagram
-
enzymatic cleavage 39%
-
-
?
o-aminobenzoyl-LAQGVRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
?
show the reaction diagram
-
enzymatic cleavage 11%
-
-
?
o-aminobenzoyl-LAQLVRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
?
show the reaction diagram
-
enzymatic cleavage 34%
-
-
?
o-aminobenzoyl-LAQVARSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
?
show the reaction diagram
-
enzymatic cleavage 19%
-
-
?
p55 TNF-alpha RI + H2O
?
show the reaction diagram
-
-
-
-
?
p55 TNFR1 + H2O
?
show the reaction diagram
-
-
-
-
?
p55 TNFR1 + H2O
?
show the reaction diagram
-
-
-
?
p55 TNFR1 + H2O
?
show the reaction diagram
-
-
-
-
?
p55 TNFR1 + H2O
?
show the reaction diagram
-
-
-
-
?
p55 TNFR1 + H2O
?
show the reaction diagram
Mus musculus EC-4
-
-
-
-
?
p75 neurotrophin receptor + H2O
?
show the reaction diagram
-
-
-
-
?
p75 neurotrophin receptor + H2O
?
show the reaction diagram
-
critical role of TACE in ectodomain shedding of the p75 neurotrophin receptor
-
-
?
p75 TNF-alpha RII + H2O
?
show the reaction diagram
-
-
-
-
?
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
-
-
-
-
?
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
-
-
-
-
?
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
-
-
-
-
?
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
-
-
-
-
?
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
-
-
-
-
?
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
-
shedding
-
-
?
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
-
shedding
-
-
?
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
shedding
-
-
?
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
Mus musculus EC-4
-
shedding
-
-
?
p75NTR + H2O
?
show the reaction diagram
-
-
-
-
?
PMEL17 + H2O
?
show the reaction diagram
-
-
-
-
?
pN-collagen I substrate + H2O
?
show the reaction diagram
-
-
-
-
?
preadipocyte factor 1 + H2O
?
show the reaction diagram
-
TACE is the major protease responsible for conversion of membrane-bound Pref-1 to the biologically active diffusible form
-
-
?
Pref1 + H2O
?
show the reaction diagram
-
-
-
-
?
pro amphiregulin + H2O
?
show the reaction diagram
-
TACE is capable of cleaving both N- and C-terminal sites in the pro-amphiregulin ectodomain
-
-
?
pro heparin-binding epidermal growth factor + H2O
?
show the reaction diagram
-
purified soluble TACE cleaves a single site in the juxtamembrane stalk of pro heparin-binding epidermal growth factor
-
-
?
pro-EGF receptor + H2O
EGF receptor + ?
show the reaction diagram
-
-
-
?
pro-interleukin-6 receptor + H2O
interleukin-6 receptor + ?
show the reaction diagram
-
-
-
?
pro-L-selectin + H2O
L-selectin + ?
show the reaction diagram
-
-
-
?
pro-Notch 1 + H2O
Notch 1 + ?
show the reaction diagram
-
-
-
?
pro-TGF-alpha + H2O
mature growth factor
show the reaction diagram
-
-
-
?
pro-TNF-alpha + H2O
soluble TNF-alpha + ?
show the reaction diagram
-
-
-
?
protein C receptor + H2O
?
show the reaction diagram
-
-
-
-
?
proTGF-alpha + H2O
soluble TGF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
release of proTNFalpha from cellular membranes
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
release of membrane-bound TNF-alpha
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
membrane-bound tumor necrosis factor alpha undergoes proteolysis
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
Mus musculus EC-4
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
Mus musculus C3H/HEN
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
Mus musculus AC2/G3
-
-
-
-
proTNF-alpha + H2O
soluble TNF-alpha + 9000 Da membrane-bound fragment of TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha + ?
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha + ?
show the reaction diagram
-
-
-
?
PrPc + H2O
?
show the reaction diagram
-
-
-
-
?
Prprz + H2O
?
show the reaction diagram
-
-
-
-
?
PTP-LAR + H2O
?
show the reaction diagram
-
-
-
-
?
RA175/SynCAM1 + H2O
?
show the reaction diagram
-
neuronal RA175/SynCAM1 isoforms, members of the immunoglobulin family 4, are processed by TACE
-
-
?
RANKL + ?
?
show the reaction diagram
-
-
-
-
?
receptor tyrosine kinase c-Kit + H2O
?
show the reaction diagram
-
ADAM-17 controls mast cell survival by regulating shedding and surface expression of c-Kit
-
-
?
SDC1 + H2O
?
show the reaction diagram
-
-
-
-
?
SDC4 + H2O
?
show the reaction diagram
-
-
-
-
?
SEMA4D + H2O
?
show the reaction diagram
-
-
-
-
?
soluble TNF + H2O
?
show the reaction diagram
-
-
-
-
?
soluble TNF receptor 1 + H2O
?
show the reaction diagram
-
-
-
-
?
soluble TNF receptor 2 + H2O
?
show the reaction diagram
-
-
-
-
?
soluble TNF-alpha receptor type 1 + H2O
?
show the reaction diagram
-
-
-
-
?
SORCS1 + H2O
?
show the reaction diagram
-
-
-
-
?
sorCS1c + H2O
?
show the reaction diagram
-
member of the vacuolar protein sorting 10p domain family of neuronal type-I receptors
-
-
?
sorCS2 + H2O
?
show the reaction diagram
-
member of the vacuolar protein sorting 10p domain family of neuronal type-I receptors, minor shedding
-
-
?
sorCS3 + H2O
?
show the reaction diagram
-
-
-
-
?
sorCS3 + H2O
?
show the reaction diagram
-
member of the vacuolar protein sorting 10p domain family of neuronal type-I receptors
-
-
?
SORL1 + H2O
?
show the reaction diagram
-
-
-
-
?
sorLA + H2O
?
show the reaction diagram
-
member of the vacuolar protein sorting 10p domain family of neuronal type-I receptors
-
-
?
SORT1 + H2O
?
show the reaction diagram
-
-
-
-
?
sortilin + H2O
?
show the reaction diagram
-
member of the vacuolar protein sorting 10p domain family of neuronal type-I receptors, minor shedding
-
-
?
TMEF2 + H2O
?
show the reaction diagram
-
-
-
-
?
TNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
TNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
TNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
membrane-bound tumor necrosis factor alpha undergoes proteolysis
-
-
TNF-alpha + H2O
?
show the reaction diagram
-
-
-
-
?
TNF-alpha + H2O
?
show the reaction diagram
-
ranitidine enhances TNF-alpha production after lipopolysaccharide treatment through augmented p38 activation, and this seems to occur through TACE
-
-
?
TRANCE + H2O
?
show the reaction diagram
-
-
-
-
?
TRANCE/RANKL + H2O
?
show the reaction diagram
-
-
-
-
?
transforming growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
-
transforming growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
?
transforming growth factor alpha + H2O
?
show the reaction diagram
-
-
-
?
transforming growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
?
transforming growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
-
transforming growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
-
transforming growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
-
transforming growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
?
transforming growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
-
transforming growth factor alpha + H2O
?
show the reaction diagram
-
TGF alpha shedding
-
-
?
transforming growth factor alpha + H2O
?
show the reaction diagram
Rattus norvegicus Lewis
-
-
-
-
-
transforming growth factor alpha + H2O
?
show the reaction diagram
Mus musculus EC-4
-
-
-
-
-
transforming growth factor alpha + H2O
?
show the reaction diagram
Mus musculus C3H/HEN
-
-
-
-
-
transforming growth factor alpha + H2O
?
show the reaction diagram
Mus musculus AC2/G3
-
-
-
-
-
transforming growth factor-alpha + H2O
?
show the reaction diagram
-
-
-
-
?
TrkA + H2O
?
show the reaction diagram
-
-
-
-
?
tumour necrosis factor receptor-1 + H2O
?
show the reaction diagram
-
-
-
-
?
tumour necrosis factor receptor-2 + H2O
?
show the reaction diagram
-
-
-
-
?
vascular cellular adhesion molecule-1 + H2O
?
show the reaction diagram
-
-
-
-
?
vasorin + H2O
soluble vasorin + ?
show the reaction diagram
-
-
-
?
vasorin + H2O
?
show the reaction diagram
-
-
-
-
?
VCAM-1 + H2O
?
show the reaction diagram
-
-
-
-
?
VEGFR2 + H2O
?
show the reaction diagram
-
-
-
-
?
MICB + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
-
-
-
-
-
additional information
?
-
-
-
-
-
-
additional information
?
-
TACE is a multidomain, type I transmembrane protein, contains a pro-domain which is removed by proteolysis to generate the active enzyme and a zinc-dependent metalloprotease catalytic domain, TACE cleaves peptides containing the sequence of the processing site at the physiolocically relevant peptide bond
-
-
-
additional information
?
-
-
o-aminobenzoyl-LAQVARSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl diaminopropionic amide is no substrate
-
-
-
additional information
?
-
-
4-dinitrophenyl)-L-2,3-diaminopropionyl diaminopropionic amide-PChaGC(Me)HK(NMA)-NH2 is not cleaved at all by TACE
-
-
-
additional information
?
-
-
amphiregulin is no substrate
-
-
-
additional information
?
-
-
angiotensin converting enzyme is not cleaved by TACE
-
-
-
additional information
?
-
-
TACE is the only enzyme confirmed to process TNF-alpha in vitro and in vivo
-
-
-
additional information
?
-
-
ectodomain shedding of the hypoxia-induced carbonic anhydrase IX is a metalloprotease-dependent process regulated by TACE/ADAM17
-
-
-
additional information
?
-
-
TACE is not involved in shedding of angiotensin converting enzyme
-
-
-
additional information
?
-
-
TACE may have a role in phorbol myristate acetate-induced shedding of epiregulin
-
-
-
additional information
?
-
-
TACE-mediated ectodomain shedding of erbB ligands, epitomized by TGFalpha is a key component of the neuron-to-glia signaling mechanism used by excitatory amino acids to facilitate the advent of female puberty
-
-
-
additional information
?
-
-
a comparison of the binding sites of matrix metalloproteinases and tumor necrosis factor-alpha converting enzyme
-
-
-
additional information
?
-
-
protein in the absence of salt or inhibitor shows a rapid and specific autocleavage between residues Y352-V353 which resides within the surrounding sequence TLGLAYVGSPRN
-
-
-
additional information
?
-
-
affinity for TACE is measured by an internally quenched peptide substrate with its sequence derived from the pro-TNF-alpha cleavage site using a catalytic domain of recombinant human TACE enzyme
-
-
-
additional information
?
-
-
compounds are assessed in two cellular assays, the human peripheral blood mononuclear cell assay (PBMC) and the human whole blood assay (WBA), for their ability to suppress the formation of TNF-alpha brought about by lipopolysaccharide (LPS) stimulation. Success in the PBMC assay relies on the ability of the inhibitor to penetrate into the cells, thus enabling it to inhibit TACE and thereby to suppress the release of intracellular, soluble TNF-alpha. In the WBA, compounds must also have the ability to penetrate cells
-
-
-
additional information
?
-
-
in mice, the interleukin-6 receptor is not a target of ADAM17
-
-
-
additional information
?
-
Mus musculus EC-4
-
-
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
Alzheimer's disease amyloid precursor protein + H2O
?
show the reaction diagram
-
TACE is involved in shedding of Alzheimer's disease amyloid precursor protein
-
-
?
amphiregulin + H2O
?
show the reaction diagram
-
-
-
-
?
angiotensin-converting enzyme-2 + H2O
?
show the reaction diagram
-
ADAM-17 is responsible for the ACE2 shedding
-
-
?
AREG + H2O
?
show the reaction diagram
-
-
-
-
?
CD26L + H2O
?
show the reaction diagram
-
-
-
-
?
epidermal growth factor receptor + H2O
?
show the reaction diagram
-
-
-
-
?
epiregulin + H2O
?
show the reaction diagram
-
-
-
-
?
FLT-3L + H2O
?
show the reaction diagram
-
-
-
-
?
glycoprotein Ibalpha + H2O
?
show the reaction diagram
-
ADAM17 is the key enzyme mediating shedding of glycoprotein Ibalpha
-
-
?
GPIba + H2O
?
show the reaction diagram
-
-
-
-
?
growth factor alpha + H2O
?
show the reaction diagram
-
-
-
-
?
HB-EGF + H2O
?
show the reaction diagram
-
-
-
-
?
heparin-binding EGF-like growth factor + H2O
?
show the reaction diagram
-
-
-
-
?
ICAM-1 + H2O
?
show the reaction diagram
-
-
-
-
?
intercellular adhesion molecule-1 + H2O
?
show the reaction diagram
-
ADAM-17 mediates shedding of intercellular adhesion molecule-1. The shedding of intercellular adhesion molecule-1 reduces the adhesive capacity of the cells. the cleavage site in the intercellular adhesion molecule-1 is not sequence-specific, but appears to be nonselective
-
-
?
interleukin-6 receptor + H2O
soluble interleukin-6 receptor + ?
show the reaction diagram
-
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
-
-
-
?
Notch 1 + H2O
?
show the reaction diagram
-
ADAM17 is required for Notch1 receptor proteolysis in NSCLC cells in vitro and in vivo
-
-
?
Notch1 + H2O
?
show the reaction diagram
-
-
-
-
?
p55 TNF-alpha RI + H2O
?
show the reaction diagram
-
-
-
-
?
p75 neurotrophin receptor + H2O
?
show the reaction diagram
-
critical role of TACE in ectodomain shedding of the p75 neurotrophin receptor
-
-
?
p75 TNF-alpha RII + H2O
?
show the reaction diagram
-
-
-
-
?
preadipocyte factor 1 + H2O
?
show the reaction diagram
-
TACE is the major protease responsible for conversion of membrane-bound Pref-1 to the biologically active diffusible form
-
-
?
pro-EGF receptor + H2O
EGF receptor + ?
show the reaction diagram
-
-
-
?
pro-interleukin-6 receptor + H2O
interleukin-6 receptor + ?
show the reaction diagram
-
-
-
?
pro-L-selectin + H2O
L-selectin + ?
show the reaction diagram
-
-
-
?
pro-Notch 1 + H2O
Notch 1 + ?
show the reaction diagram
-
-
-
?
pro-TNF-alpha + H2O
soluble TNF-alpha + ?
show the reaction diagram
-
-
-
?
proTGF-alpha + H2O
soluble TGF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha + 9000 Da membrane-bound fragment of TNF-alpha
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha + ?
show the reaction diagram
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha + ?
show the reaction diagram
-
-
-
?
RA175/SynCAM1 + H2O
?
show the reaction diagram
-
neuronal RA175/SynCAM1 isoforms, members of the immunoglobulin family 4, are processed by TACE
-
-
?
receptor tyrosine kinase c-Kit + H2O
?
show the reaction diagram
-
ADAM-17 controls mast cell survival by regulating shedding and surface expression of c-Kit
-
-
?
TNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
TNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
-
-
-
TNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
-
membrane-bound tumor necrosis factor alpha undergoes proteolysis
-
-
TNF-alpha + H2O
?
show the reaction diagram
-
ranitidine enhances TNF-alpha production after lipopolysaccharide treatment through augmented p38 activation, and this seems to occur through TACE
-
-
?
vasorin + H2O
soluble vasorin + ?
show the reaction diagram
-
-
-
?
L-selectin + H2O
?
show the reaction diagram
-
ADAM17 is the main sheddase of the adhesion protein L-selectin
-
-
?
additional information
?
-
-
ectodomain shedding of the hypoxia-induced carbonic anhydrase IX is a metalloprotease-dependent process regulated by TACE/ADAM17
-
-
-
additional information
?
-
-
TACE is not involved in shedding of angiotensin converting enzyme
-
-
-
additional information
?
-
-
TACE may have a role in phorbol myristate acetate-induced shedding of epiregulin
-
-
-
additional information
?
-
-
TACE-mediated ectodomain shedding of erbB ligands, epitomized by TGFalpha is a key component of the neuron-to-glia signaling mechanism used by excitatory amino acids to facilitate the advent of female puberty
-
-
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Zinc
-
pronounced diversity in electronic and chemical properties between the catalytic zinc sites of tumor necrosis factor-alpha-converting enzyme and matrix metalloproteinases despite their high structural similarity
Zn2+
-
zinc metalloprotease
Zn2+
-
zinc-dependent catalytic domain
Zn2+
-
zinc metalloprotease
Zn2+
-
-
Zn2+
-
contains a catalytic zinc complex
Zn2+
-
contains a catalytic zinc ion
Zn2+
-
a zinc metalloprotease
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1R,2R)-2-(3-phenoxylphenyl)-2-trans-carbomethoxylcyclopropane hydroxamic acid
-
-
(1R,2R)-2-trans-carboisopropoxyl-2-[3-(2-methylquinolin-4-yl)methoxylphenyl]cyclopropane hydroxyamic acid
-
-
(1R,2R)-2-trans-N-benzylaminocarbonyl-2-[3-(2-methylquinolin-4-yl)methoxylphenyl]cyclopropane hydroxyamic acid
-
-
(1R,2R)-2-[3-(3,4-dichlorobenzyloxy)phenyl]-2-trans-carbomethoxylcyclopropane hydroxamic acid
-
-
(1R,2R)-N-hydroxy-2-[(4-methylpiperazin-1-yl)carbonyl]-2-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropanecarboxamide
-
-
(1R,2R)-N1-benzyl-N2-hydroxy-N1-methyl-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2R)-N1-cyclohexyl-N2-hydroxy-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2R)-N2-hydroxy-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]-N1-phenylcyclopropane-1,2-dicarboxamide
-
-
(1R,2R)-N2-hydroxy-N1,N1-dimethyl-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2R)-N2-hydroxy-N1-methyl-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-(3-fluoro-4-[[2-(1-methyl-1H-pyrazol-5-yl)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-(3-fluoro-4-[[2-(methylamino)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-morpholin-4-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxy-N1,N1-dimethylcyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-pyrrolidin-1-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[4-(benzyloxy)benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[4-(but-2-yn-1-yloxy)benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N1-(piperidin-4-ylmethyl)cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-N1,N1-dimethyl-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-N1,N1-dimethyl-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-N1-methyl-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1S,2R)-2-[[(3R)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
(1S,2R)-2-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
(1S,2R)-N-hydroxy-2-[[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
(1S,2R)-N-hydroxy-2-[[(3S)-3-hydroxypyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
(1S,2R)-N-hydroxy-2-{4-[(2-imino-1,2-dihydroquinolin-4-yl)methoxy]benzyl}-2-(methoxycarbonyl)cyclopropanecarboximidic acid
-
-
(1S,2S)-2-((S)-cyano(4-((2-phenylquinolin-4-yl)methoxy)phenyl)methyl)-N-hydroxycyclopropanecarboxamide
-
-
(2R)-5-nitroguanyl-2-([(2R,3S)-2-(cyclohexylmethyl)-3-cyclopropyl-3-[formyl(hydroxy)amino]propanoyl]-amino)-N-(1,3-thiazol-2-yl)pentanamide
-
-
(2R)-N-hydroxy-2-(7-methoxy-1,1-dioxido-4,5-dihydro-1,2,5-benzothiadiazepin-2(3H)-yl)-3-methylbutanamide
-
-
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[(4-methylcyclohexyl)-methyl]hexanamide
-
-
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[(5-methyl-2-thienyl)methyl]hexanamide
-
-
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutyl-4-methylpentanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl-(hydroxy)amino]-2-isobutyl-4-methylpentanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl-(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-6,6,6-trifluoro-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-(cyclohexylmethyl)-3-[formyl(hydroxy)amino]hexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-(cyclohexylmethyl)-6,6,6-trifluoro-3-[formyl(hydroxy)amino]hexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-[(1S)-1-[formyl(hydroxy)amino]-2-phenylethyl]-4-methylpentanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[5-methyl-2-thienylmethyl]hexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]hexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
-
(2R,3S)-N-[(1S,2R)-4-nitroguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-{(1R)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl}-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2S)-2-amino-5-({(E)-amino[(methylsulfonyl)imino]-methyl}amino)-N-(1,3-thiazol-2-yl)pentanamide hydrochloride
-
-
(2S)-2-[(tert-butoxycarbonyl)amino]-5-({(Z)-(methyl-sulfanyl)[(methylsulfonyl)imino]methyl}amino)pentanoic acid
-
-
(2S,3R)-2-[(tert-butoxycarbonyl)amino]-5-{[imino(2-oxido-2-oxohydrazino)methyl]amino}-3-methylpentanoic acid (3R) Nalpha-boc-Ngamma-nitro-3-methyl L-arginine
-
-
(2S,3R)-2-{[(benzyloxy)carbonyl]amino}-3-methyl-5-({(Z)-(methylsulfanyl)[(methylsulfonyl)imino]methyl}-amino)pentanoic acid
-
-
(2S,3R)-5-methanesulfonylguanyl-2-[((2R)-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-4-methylpentanoyl)amino]-3-methyl-N-(1,3-thiazol-2-yl)pentanamide
-
-
(2S,3R)-5-nitroguanyl-2-[((2R)-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-4-methylpentanoyl)amino]-3-methyl-N-(1,3-thiazol-2-yl)pentanamide
-
-
(3R,4R)-4-([[4-(1,3-dihydrofuro[3,4-b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-4-([[4-(2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-4-([[4-(2,3-dihydrofuro[2,3-b]quinolin-4-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-4-[([4-[(2,3-dimethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-4-[([4-[(2-cyclopropylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-4-[([4-[(2-ethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-4-[([4-[(3-ethyl-2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-4-[[(4-[[2-(dimethylamino)quinolin-4-yl]methyl]phenyl)carbonyl]amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-N-hydroxy-4-[([4-[(2-morpholin-4-ylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-N-hydroxy-4-[([4-[(3-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-N-hydroxy-4-[[(4-[[2-(1-methylethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4R)-N-hydroxy-4-[[(4-[[2-(trifluoromethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-3-carboxamide
-
-
(3R,4S)-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-4-carboxamide
-
-
(3R,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydrofuran-3-carboxamide
-
-
(3S)-1-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]pyrrolidine-3-thiol
-
-
(3S)-4-[[4-(but-2-ynylamino)phenyl]sulfonyl]-N-hydroxy-2,2-dimethylthio-morpholine-3-carboxamide
-
-
(3S,4R)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-3-carboxamide
-
-
(3S,4S)-1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-1-(2,2-dimethylpropyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-1-(butylsulfonyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-1-(furan-2-ylmethyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-1-acetyl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-1-but-2-yn-1-yl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-1-cyclobutyl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-1-tert-butyl-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-4-carboxamide
-
-
(3S,4S)-1-[2-(dimethylamino)ethyl]-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-4-carboxamide
-
-
(3S,4S)-3-[([4-[(2-cyclopropylimidazo[1,2-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-3-[([4-[(2-ethyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-3-[([4-[(2-ethylpyrazolo[1,5-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-3-[([4-[(2-tert-butylpyrazolo[1,5-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-N-hydroxy-1-(1-methylethyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-1-(2-methylprop-2-en-1-yl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-1-(2-methylpropanoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[([4-[(2-methyl-1-benzofuran-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[([4-[(2-methylimidazo[1,2-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-4-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)-1-benzofuran-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)imidazo[1,2-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
-
(3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
substance exhibits excellent oral bioavailability in pharmacokinetic studies
(3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1-benzofuran-3-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-phenylpyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-prop-2-en-1-ylpyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
(3S,4S)-N-hydroxy-4-[[(4-[[2-(1-methylethyl)-1-benzofuran-3-yl]methyl]phenyl)carbonyl]amino]pyrrolidine-3-carboxamide
-
-
(4-bromobut-2-enyloxymethyl)benzene
-
-
(4-methoxyphenyl)acetic acid 4-benzyloxybut-2-enyl ester
-
-
(5R)-5-(2',4'-difluorobiphenyl-4-yl)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5R)-5-(4'-chlorobiphenyl-4-yl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[2'-(1-methyl-1H-tetrazol-5-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(trifluoromethyl)biphenyl-4-yl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(6-oxo-1,6-dihydropyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(quinolin-6-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[3'-(2-methyl-1,3-thiazol-4-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(1H-pyrazol-3-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1,3-thiazol-2-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-5-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methyl-2H-indazol-6-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methylpyridin-4-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(3-phenyl-1,2-oxazol-5-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(4-methyl-2,5-dioxoimidazolidin-4-yl)phenyl]imidazolidine-2,4-dione (non-preferred name)
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrazin-2-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-2-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrimidin-5-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[4-(2-aminopyridin-4-yl)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5R)-5-[4-(3,5-dimethyl-1,2-oxazol-4-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5R)-5-[4-(5-chloro-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5R,6R)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,4-dioxo-1,3-diazaspiro[4.4]nonane-6-carboxamide
-
-
(5R,6S)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,4-dioxo-1,3-diazaspiro[4.4]nonane-6-carboxamide
-
-
(5R,7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-oxaspiro[4.4]nonane-7-carboxamide
-
-
(5S)-5-(4-fluorophenyl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5S,6R)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,4-dioxo-1,3-diazaspiro[4.5]decane-6-carboxamide
-
-
(5S,6S)-N-hydroxy-5-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-2,3,5,6-tetrahydro-4aH-cyclopenta[b][1,4]dioxine-6-carboxamide
-
-
(5S,7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-oxaspiro[4.4]nonane-7-carboxamide
-
-
(7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1,4-dioxaspiro[4.4]nonane-7-carboxamide
-
-
1,10-phenanthroline
-
-
1,25-dihydroxyvitamin D
-
1,25-dihydroxyvitamin D inhibition of TACE is a potential common mechanism underlying the efficacy of therapy with 1,25-dihydroxyvitamin D or its analogs to improve outcomes in chronic kidney disease. 1,25-dihydroxyvitamin D prevents/moderates not only the onset and progression of parathyroid TACE/TGFalpha-driven secondary hyperparathyroidism, but renal TACE/TGFalpha-driven fibrotic and inflammatory lesions to the renal parenchyma, and TACE/TNFalpha-driven systemic inflammation
1-(1,3-benzoxazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
-
-
1-(1H-benzimidazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
-
-
1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]piperidine-4-carboxamide
-
-
1-(2,2-dimethylpropyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
1-(butylsulfonyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
1-but-2-yn-1-yl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
1-ethylpropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
1-methyl-2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
1-methylethyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropanecarboxylate
-
-
1-methylethyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
-
1-methylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
1-[(4-acetylpiperazin-1-yl)sulfonyl]-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
-
-
1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]-1,3,5-triazinane-2,4,6-trione
-
IC50: 0.0073 mM
13-[(4R)-2,5-dioxoimidazolidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]tridecanamide
-
-
2(R)-benzyloxymethyl-N-(2,2-dimethyl-1(S)-methyl-carbamoylpropyl)-3-(S)-(4-methoxyphenyl)succinamic acid
-
-
2,6-anhydro-3,4,5-trideoxy-1-(hydroxyamino)-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-D-threo-hexose
-
-
2-(3-benzyloxyphenyl)-2-trans-carbomethoxylcyclopropane hydroxyamic acid
-
-
2-(6-methyl-2-oxo-2H-chromen-3-ylmethyl)-pent-4-enoic acid hydroxyamide
-
-
2-(N-benzoxycarbonyl)aminoethyl-N-(4-hydroxyamino-4-oxo-2-(isopropylthio)butanoyl)-L-3-(2'-naphthyl)-L-alanyl amide
-
peptidomimetic inhibitor, 54.5% inhibition in in vitro lipopolysaccharide cytotoxicity tests, inhibitory activity in vivo by measuring the expression of mTNFalpha
2-(N-benzoxycarbonyl)aminoethyl-N-(4-hydroxyamino-4-oxo-2-(isopropylthio)butanoyl)-L-3-phenylalanyl-L-alanyl amide
-
peptidomimetic inhibitor, 27.3% inhibition in in vitro lipopolysaccharide cytotoxicity tests, molecular docking studies
2-(N-benzoxycarbonyl)aminoethyl-N-(4-hydroxyamino-4-oxo-2-(phenylthio)butanoyl)-L-3-phenylalanyl-L-alanyl amide
-
peptidomimetic inhibitor, 54.5% inhibition in in vitro lipopolysaccharide cytotoxicity tests
2-benzyl-N-hydroxy-3-(6-methyl-2-oxo-2H-chromen-3-yl)-propionamide
-
-
2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
2-[(5R,6R)-2,4-dioxo-1,3-diazaspiro[4.4]non-6-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]acetamide
-
-
2-[(5R,6S)-2,4-dioxo-1,3-diazaspiro[4.4]non-6-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]acetamide
-
-
2-[3-(2-methylquinolin-4-yl)methoxylphenyl]-2-trans-carboxamidocyclopropane hydroxyamic acid
-
-
2-[3-(2-methylquinolin-4-yl)methoxyphenyl]-2-trans-carbomethoxylcyclopropane hydroxyamic acid
-
-
2-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-N-[(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)methyl]acetamide
-
; IC50: above 0.1 mM
2-[[4-(but-2-yn-1-ylamino)phenyl]sulfonyl]ethanethiol
-
-
2-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]ethanethiol
-
-
2-[[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl](methyl)amino]-N-hydroxyacetamide
-
-
3(R)-benzyloxymethyl-2-(S)-(4-methoxyphenyl)pent-4-enoic acid
-
-
3(R)-benzyloxymethyl-2-(S)-(4-methoxyphenyl)pent-4-enoic acid (2,2-dimethyl-1-(S)-methylcarbamoylpropyl)amide
-
-
3-(6-bromo-2-oxo-2H-chromen-3-yl)-N-hydroxy-propanamide
-
-
3-(6-chloro-2-oxo-2H-chromen-3-yl)-N-hydroxy-propanamide
-
-
3-(6-tert-butyl-2-oxo-2H-chromen-3-yl)-N-hydroxypropanamide
-
-
3-([[4-(1,3-dihydrofuro[3,4-b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-([[4-(2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-([[4-(2,3-dihydrofuro[2,3-b]quinolin-4-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[([4-[(2,3-dimethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[([4-[(2-cyclopropylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[([4-[(2-ethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[([4-[(3-ethyl-2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[4-[2-(hydroxyamino)-2-oxoethyl]-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidin-1-yl]propanoic acid
-
-
3-[[(4-[[2-(dimethylamino)quinolin-4-yl]methyl]phenyl)carbonyl]amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[[4-(but-2-yn-1-ylamino)phenyl]sulfonyl]cyclohexanethiol
-
-
3-[[4-(but-2-yn-1-ylamino)phenyl]sulfonyl]propane-1-thiol
-
-
3-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]cyclohexanethiol
-
-
3-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]cyclopentanethiol
-
-
3-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]propane-1-thiol
-
-
4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-benzoyl)-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-butyryl)-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(propane-2-sulfonyl)-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-isobutyryl-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-pyridin-4-ylmethyl-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-1,4-dicarboxylic acid 1-diethylamide 4-hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-4-carboxylic acid hydroxyamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-(dimethylsulfamoyl)-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dichlorothiophen-3-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dimethyl-1,3-thiazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)carbonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)methyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethyl-1H-pyrazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethylisoxazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(5-chlorothiophen-2-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(morpholin-4-ylsulfonyl)piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(piperidin-1-ylsulfonyl)piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(pyrrolidin-1-ylsulfonyl)piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-2-ylpiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-4-ylpiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[(2-methyl-1H-imidazol-4-yl)sulfonyl]piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
-
-
4-[(2-methylquinolin-4-yl)methoxy]-N-(1,3,5-trioxo-2,4-diazaspiro[5.5]undec-7-yl)benzamide
-
; IC50: 0.000138 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)benzamide
-
; IC50: above 0.1 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-(6,8,10-trioxo-2-oxa-7,9-diazaspiro[4.5]dec-4-yl)benzamide
-
; IC50: 0.000044 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-(6,8,10-trioxo-7,9-diazaspiro[4.5]dec-1-yl)benzamide
-
; IC50: 0.000024 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-([2,4,6-trioxo-5-[1-(tetrahydro-2H-pyran-2-yl)piperidin-4-yl]hexahydropyrimidin-5-yl]methyl)benzamide
-
-
4-[(2-methylquinolin-4-yl)methoxy]-N-([2,4,6-trioxo-5-[1-(tetrahydro-2H-pyran-4-yl)piperidin-4-yl]hexahydropyrimidin-5-yl]methyl)benzamide
-
IC50: 0.000031 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-([2,4,6-trioxo-5-[4-(pyridin-3-ylcarbonyl)piperazin-1-yl]hexahydropyrimidin-5-yl]methyl)benzamide
-
IC50: 0.00001 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-([5-[1-(methylsulfonyl)piperidin-4-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)benzamide
-
IC50: 0.000029 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-([5-[4-(methylsulfonyl)piperazin-1-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)benzamide
-
IC50: 0.000002 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-[(2,4,6-trioxo-5-phenylhexahydropyrimidin-5-yl)methyl]benzamide
-
-
4-[(2-methylquinolin-4-yl)methoxy]-N-[(2,4,6-trioxo-5-piperidin-4-ylhexahydropyrimidin-5-yl)methyl]benzamide
-
; IC50: 0.000055 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-[(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)(pyridin-4-yl)methyl]benzamide
-
; IC50: 0.00236 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-[(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)methyl]benzamide
-
; IC50: 0.000026 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-[2-(methylsulfonyl)-6,8,10-trioxo-2,7,9-triazaspiro[4.5]dec-4-yl]benzamide
-
IC50: 0.000036 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-[6,8,10-trioxo-2-(pyridin-3-ylcarbonyl)-2,7,9-triazaspiro[4.5]dec-4-yl]benzamide
-
IC50: 0.000029 mM
4-[(2-methylquinolin-4-yl)methoxy]-N-[[2,4,6-trioxo-5-(4-phenylpiperazin-1-yl)hexahydropyrimidin-5-yl]methyl]benzamide
-
-
4-[([4-[(1,1-dimethylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)methyl]-N-hydroxy-1-(isopropylsulfonyl)piperidine-4-carboxamide
-
-
4-[2-(hydroxyamino)-2-oxoethyl]-N,N-dimethyl-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-1-carboxamide
-
-
4-[4-(4-hydroxy-but-2-ynylamino)-benzenesulfonylmethyl]-4-hydroxycarbamoyl-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)-thiomorpholinecarboxamide
-
IC50: 0.009 mM
4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)-thiomorpholinecarboxamide
-
IC50: 0.05 mM
5-(4-acetylpiperazin-1-yl)-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.00062 mM
5-(4-benzylpiperazin-1-yl)-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.000195 mM
5-(4-hexylpiperazin-1-yl)-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.000081 mM
5-(4-methylpiperazin-1-yl)-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.000091 mM
5-methyl-5-(2-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]ethyl)pyrimidine-2,4,6(1H,3H,5H)-trione
-
; IC50: 0.049 mM
5-methyl-5-(3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-3-oxopropyl)pyrimidine-2,4,6(1H,3H,5H)-trione
-
; IC50: 0.0008 mM
5-methyl-5-(3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]prop-2-en-1-yl)pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.011 mM
5-methyl-5-(3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]propyl)pyrimidine-2,4,6(1H,3H,5H)-trione
-
; IC50: above 0.1 mM
5-methyl-5-[(2E)-3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]prop-2-en-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
; IC50: 0.0022 mM
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]phenoxy]pyrimidine-2,4,6(1H,3H,5H)-trione
-
; IC50: 0.0013 mM
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]dihydropyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0037 mM
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.00103 mM
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
; IC50: 0.00103 mM
5-[(5-methoxy-3-oxo-1,3-dihydro-2H-indazol-2-yl)methyl]-5-phenylimidazolidine-2,4-dione
-
-
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(2-phenoxyphenyl)imidazolidine-2,4-dione
-
-
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(3-phenoxyphenyl)imidazolidine-2,4-dione
-
-
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-oxopyrrolidin-1-yl)phenyl]imidazolidine-2,4-dione
-
-
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(morpholin-4-yl)phenyl]imidazolidine-2,4-dione
-
-
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yloxy)phenyl]imidazolidine-2,4-dione
-
-
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrrolidin-1-ylcarbonyl)phenyl]imidazolidine-2,4-dione
-
-
5-[4-(1-methylethyl)piperazin-1-yl]-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.000096 mM
5-[4-(2,2-dimethylpropanoyl)piperazin-1-yl]-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.00054 mM
5-[4-(2,2-dimethylpropyl)piperazin-1-yl]-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.00016 mM
5-[4-(cyclopentyloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
5-[4-(isoquinolin-7-yloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-(pyridin-3-ylcarbonyl)pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.000535 mM
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-piperazin-1-ylpyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.0011 mM
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-piperidin-1-ylpyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.000855 mM
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-[4-(2-phenylethyl)piperazin-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.000084 mM
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-[4-(3-phenylpropyl)piperazin-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.00011 mM
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-[4-(4-nitrophenyl)piperazin-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.0028 mM
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-[4-(methylsulfonyl)piperazin-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
-
IC50: 0.000275 mM
7-(1-methyl-2,5-dioxoimidazolidin-4-yl)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
-
-
7-(2,5-dioxoimidazolidin-4-yl)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
-
-
7-(3-methyl-2,5-dioxoimidazolidin-4-yl)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
-
-
7-[(4R)-2,5-dioxoimidazolidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
-
-
7-[(4S)-2,5-dioxoimidazolidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
-
-
APMA
-
inhibits TACE completely
BB 1101
-
-
BB 1433
-
-
BB 16
-
-
BB 2516
-
-
BB2275
-
-
-
BB2284
-
-
-
BB3103
-
-
-
BB3103
-
-
-
benzyl (1S,2R)-4-({(E)-amino[(methylsulfonyl)imino]-methyl}amino)-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butylcarbamate
-
-
BMS-561392
-
-
BMS-561392
-
TACE inhibitor also named DPC-333 is administered 15 min before ranitidine or its vehicle. Serum TNF-alpha concentration are measured 1 h afterwards. lipopolysaccharide/ranitidine treatment causes a significant increase in serum TNF-alpha concentration compared with lipopolysaccharide/vehicle treatment. Inhibitor does not affect serum TNF-alpha concentration after lipopolysaccharide/vehicle treatment. By contrast, it decreases serum TNF-alpha concentration after lipopolysaccharide/ranitidine treatment to the same level as lipopolysaccharide/vehicle treatment at both 1 h. In addition, TACE inhibitor decreases plasma active plasminogen activator inhibitor-1 concentration after lipopolysaccharide/ranitidine treatment to almost the same level as lipopolysaccharide/vehicle treatment
CGS 27023
-
-
CT 572
-
-
-
cyclohexyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
cyclohexylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
cyclopentyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
cyclopropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
dithiothreitol
-
-
DPH-067517
-
-
EDTA
-
1 mM, treatment of cells dramatically inhibits shedding of shedding of FcalphaR, i.e. Fc receptor for immunoglobulin A
EGTA
-
1 mM, treatment of cells dramatically inhibits shedding of shedding of FcalphaR, i.e. Fc receptor for immunoglobulin A
EndoH
-
full-length TACE is sensitive to EndoH, mature TACE is resistant
-
ethyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropanecarboxylate
-
-
ethyl (1R,2S)-1-[3-bromo-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-1-[3-chloro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-1-[3-fluoro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-phenoxybenzyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(2-methylpropyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(trifluoromethyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylpyridin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
gelastatin hydroxamate
-
-
GI 129471
-
-
GM 6001
-
-
GM6001
-
galardin
GM6001
-
broad-spectrum metalloproteinase inhibitor, treatment of cells dramatically inhibits shedding of shedding of FcalphaR, i.e. Fc receptor for immunoglobulin A
GM6001
-
poor inhibitive effectiveness on TACE
GW 3333
-
-
GW 3333
-
N-hydroxyformamide TACE inhibitor
GW1988
-
-
-
GW280264X
-
blocks ADAM10 and ADAM17 activity similarly
GW280264X
-
-
GW9471
-
hydroxamic acid competitive inhibitor that totally blocks TACE activity
-
IC-3
-
protects TACE from degradation by inhibiting either TACE itself or another metalloprotease
Immunex compound 3
-
-
JMV 390
-
-
KB-R7785
-
-
L-NG-(2-pyridylsulfonyl)arginine2-aminothiazole amide hydochloride
-
-
L-NG-nitroarginine 2-aminothiazole amide dihydrochloride
-
-
macrocyclic hydroxamic acid
-
-
-
macrocyclic hydroxamic acid
-
-
-
methyl (1R,2R)-1-[3-(2-[3-[(1Z)-buta-1,3-dien-1-yl]phenyl]ethoxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-1-[3-(benzyloxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-1-[3-(but-2-yn-1-yloxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-1-[3-(cyclohexylmethoxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-1-[3-[(4-chlorobenzyl)oxy]phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-(3-methoxyphenyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-(3-[[3-(trifluoromethyl)benzyl]oxy]phenyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-(3-[[4-(trifluoromethyl)benzyl]oxy]phenyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(2-methylphenoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(2-naphthalen-2-ylethoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(2-phenylethoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(4-methylphenoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(naphthalen-2-ylmethoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(naphthalen-2-yloxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(3-methoxybenzyl)oxy]phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-(benzyloxy)benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-(but-2-yn-1-yloxy)benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-(cyclohexylmethoxy)benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-[(2-chlorobenzyl)oxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-[(3,4-dichlorobenzyl)oxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-(2-naphthalen-1-ylethoxy)benzyl]cyclopropanecarboxylate
-
-
methyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-(2-naphthalen-2-ylethoxy)benzyl]cyclopropanecarboxylate
-
-
methyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
-
methyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
-
methyl (5R)-5-{7-[(3,5-diethoxybenzyl)oxy]-1,1-dioxido-4,5-dihydro-1,2,5-benzothiadiazepin-2(3H)-yl}-6-(hydroxyamino)-6-oxohexanoate
-
-
methyl (5R)-5-{7-[(3,5-dimethoxybenzyl)oxy]-1,1-dioxido-4,5-dihydro-1,2,5-benzothiadiazepin-2(3H)-yl}-6-(hydroxyamino)-6-oxohexanoate
-
human whole blood assay: 31% inhibition
methyl 3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
-
methyl 4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxylate
-
-
methyl 4-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,5-dioxoimidazolidine-4-carboxylate
-
IC50: 0.0047 mM
MMP-1
-
-
-
N(R)-[2-(hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-alanine amide
-
IC50: about 0.11 mM
N(R)-[2-(hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-alanine amide
-
IC50: about 0.7 mM
N-(2-acetyl-6,8,10-trioxo-2,7,9-triazaspiro[4.5]dec-4-yl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
IC50: 0.000055 mM
N-(8-acetyl-1,3,5-trioxo-2,4,8-triazaspiro[5.5]undec-11-yl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-([5-[1-(1-methylethyl)piperidin-4-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
; IC50: 0.000052 mM
N-([5-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
IC50: 0.000013 mM
N-([5-[4-(1-methylethyl)piperazin-1-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
; IC50: 0.000007 mM
N-([5-[4-(2,2-dimethylpropanoyl)piperazin-1-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
IC50: 0.000029 mM
N-([5-[4-(5-amino-8-carbamimidamido-4-oxooctyl)piperazin-1-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
N-hydroxy-2(R)-(6-methoxy-1,1-dioxo-3,4-dihydro-1H-1-benzo[1,2,4]thiadiazin-2-yl)propionamide
-
-
N-hydroxy-2(R)-[2,3,4,5-tetrahydrobenzo[1,2,5-f]-thiadiazepine-1,1-dioxide]propanamide
-
-
N-hydroxy-2(R)-[7-(2,6-methylpyridyl-4-methyleneoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-propanamide
-
human whole blood assay: 37% inhibition
N-hydroxy-2(R)-[7-(2-trifluromethylphenyl)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propylamide
-
-
N-hydroxy-2(R)-[7-(3,5-dichlorobenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
human whole blood assay: 12% inhibition
N-hydroxy-2(R)-[7-(3,5-diethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-3-methylbutanamide
-
human whole blood assay: 17% inhibition
N-hydroxy-2(R)-[7-(3,5-diethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methoxycarbonylbutanamide
-
human whole blood assay: 0% inhibition
N-hydroxy-2(R)-[7-(3,5-diethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
human whole blood assay: 26% inhibition
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine 1,1-dioxide]-6-N-(methanesulfonyl)hexylamide
-
-
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-3-methylbutanamide
-
human whole blood assay: 11% inhibition
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methoxycarbonylbutanamide
-
human whole blood assay: 0% inhibition
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentanamide
-
human whole blood assay: 16% inhibition
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-6-aminohexylamidetrifluoroacetic acid salt
-
human whole blood assay: 3% inhibition
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-6-N-[(1,1-dimethylethoxy)carbonyl]hexylamide
-
human whole blood assay: 3% inhibition
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
N-hydroxy-2(R)-[7-(3,5-dimethylbenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
human whole blood assay: 2% inhibition
N-hydroxy-2(R)-[7-(3-nitrophenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
N-hydroxy-2(R)-[7-(4,5-dimethylthiazolyl-2-methyleneoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-3-methylbutanamide
-
human whole blood assay: 0% inhibition
N-hydroxy-2(R)-[7-(4-methoxyphenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
N-hydroxy-2(R)-[7-(4-nitrophenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
N-hydroxy-2(R)-[7-(4-phenylphenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
N-hydroxy-2(R)-[7-(4-trifluoromethylphenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
human whole blood assay: 58% inhibition
N-hydroxy-2(R)-[7-(N-3,5-dimethylbenzoylamino)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-propylamide
-
-
N-hydroxy-2(R)-[7-benzyloxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentanamide
-
human whole blood assay: 39% inhibition
N-hydroxy-2(R)-[7-benzyloxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
human whole blood assay: 30% inhibition
N-hydroxy-2(R)-[7-hydroxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentamide
-
human whole blood assay: 20% inhibition
N-hydroxy-2(R)-[7-hydroxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
human whole blood assay: 21% inhibition
N-hydroxy-2(R)-[7-methoxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
N-hydroxy-2(R)-[7-N-(3,5-dimethoxymethyleneamino)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentamide
-
human whole blood assay: 3% inhibition
N-hydroxy-2(R)-[7-phenoxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
N-hydroxy-2(R)-[7-phenyl-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propylamide
-
-
N-hydroxy-2-((6-methoxy-2H-chromen-3-yl)methyl)propanamide
-
-
N-hydroxy-2-(2-oxo-2H-chromen-3-yl)acetamide
-
-
N-hydroxy-2-methyl-3-(6-methyl-2-oxo-2H-chromen-3-yl)-propionamide
-
-
N-hydroxy-2-[2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]ethanamide
-
-
N-hydroxy-2-[7-methoxy-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]ethanamide
-
-
N-hydroxy-3-(2-oxo-2H-chromen-3-yl)propanamide
-
-
N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl)propanamide
-
-
N-hydroxy-3-(6-methyl-2-oxo-2H-chromen-3-yl)propanamide
-
-
N-hydroxy-3-[([4-[(2-morpholin-4-ylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-2-carboxamide
-
-
N-hydroxy-3-[([4-[(3-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-2-carboxamide
-
-
N-hydroxy-3-[[(4-[[2-(trifluoromethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-2-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydrofuran-3-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-1-(methylsulfonyl)piperidine-4-carboxamide
-
-
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-1-propylpiperidine-4-carboxamide
-
-
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]piperidine-4-carboxamide
-
-
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-[(1R,2S)-2-(hydroxycarbamoyl)-4-oxocyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(1R,2S)-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(1R,2S)-4,4-difluoro-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(1R,2S)-4-aziridin-1-yl-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(1R,2S)-4-hydroxy-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(1S,2R)-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(4-methyl-2,5-dioxoimidazolidin-4-yl)methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]methylcarbamoyl-5-hydroxy-2-methyloct-4-yl]-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]isophthalamide
-
-
N-[(5-benzyl-2,4,6-trioxohexahydropyrimidin-5-yl)methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
IC50: 0.000018 mM
N-[(5-ethyl-2,4,6-trioxohexahydropyrimidin-5-yl)methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
; IC50: 0.000016 mM
N-[(5R,6R)-2,4-dioxo-1,3-diazaspiro[4.4]non-6-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(5R,6R)-2,4-dioxo-1,3-diazaspiro[4.5]dec-6-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(5R,6S)-2,4-dioxo-1,3-diazaspiro[4.4]non-6-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(5R,9R)-2,4-dioxo-1,3,7-triazaspiro[4.4]non-9-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[(5R,9R)-7-(2-methylpropanoyl)-2,4-dioxo-1,3,7-triazaspiro[4.4]non-9-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(1,1-dimethylprop-2-yn-1-yl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(2,2-dimethylpropanoyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(2,2-dimethylpropyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(2,5-dioxoimidazolidin-4-yl)ethyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(2-fluoroethyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(3,3-dimethylbutanoyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(4,5-dihydro-1,3-thiazol-2-yl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-acetyl-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-ethyl-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-tert-butyl-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-[2-(ethylsulfonyl)ethyl]-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-[2-(hydroxyamino)-2-oxoethyl]cyclohexyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-[2-(hydroxyamino)-2-oxoethyl]cyclohexyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
-
N-[2-(2,2-dimethylpropanoyl)-6,8,10-trioxo-2,7,9-triazaspiro[4.5]dec-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
IC50: 0.000111 mM
N-[2-(hydroxycarbamoyl)cyclobutyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
-
N-[2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
-
N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2-(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)acetamide
-
IC50: 0.012 mM
N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-3-(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)propanamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-(2-methylpropanoyl)piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-(3-methylbutanoyl)piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-(methylsulfonyl)piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-methylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-phenylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-propanoylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-propylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-[2-(methylsulfonyl)ethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydro-2H-pyran-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydro-2H-pyran-4-yl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydrofuran-3-yl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
-
N-[DL-[2-(hydroxyamino-carbonyl)methyl]-4-methylpentanoyl]-L-3-(tert-butyl)glycyl-L-alanine,2-aminoethylamide
-
-
N-[[(4R)-2,5-dioxoimidazolidin-4-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[[1-(hydroxycarbamoyl)cyclohexyl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[[5-(1-methylethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
; IC50: 0.000019 mM
N-[[5-(1-methylpiperidin-4-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
; IC50: 0.000057 mM
N-[[5-(4-acetylpiperazin-1-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
; IC50: 0.000005 mM
N-[[5-(4-benzylpiperazin-1-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
IC50: 0.000014 mM
N-[[5-(4-ethynylpiperazin-1-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
IC50: 0.000062 mM
N-[[5-(4-methylpiperazin-1-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
; IC50: 0.000058 mM
N1-benzyloxy-2(R)-benzyloxymethyl-N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-3(S)-(4-methoxyphenyl)-succinamide
-
-
N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-N1-hydroxy-2(R)-hydroxymethyl-3(R)-(isobutyl)succinamide
-
-
N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-N1-hydroxy-2(R)-hydroxymethyl-3(S)-(4-methoxyphenyl)succinamide
-
-
N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-N1-hydroxy-2(R)-hydroxymethyl-3(S)-p-tolylsuccinamide
-
-
N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-N1-hydroxy-2(R)-hydroxymethyl-3(S)-phenylsuccinamide
-
-
NaCl
-
dramatic inhibitory effect on the activity of TACE
peptide hydroxamate
-
-
-
peptidomimetic hydroxamate
-
-
-
PKF241-466
-
maximum inhibition at 10 mg/kg
PKF242-484
-
-
PKF242-484
-
maximum inhibition at 10 mg/kg
pyridin-4-ylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
Ro 31-9790
-
-
Ro 32-7315
-
-
Ro32-7315
-
inhibitor specific for ADAM17, blocks shedding of CD30 antigen from cell membrane and a simultaneous release of soluble CD30
SC 903
-
-
-
SE 205
-
-
succinate
-
-
succinyl hydroxamate
-
-
sulfonamide hydroxamate
-
-
TACE-pro domain
-
pro domain is an inhibitor of the catalytic domain
-
TACE-pro domain
-
-
-
TAPI
-
hydroxamic acid-based broad-spectrum inhibitor of zinc metalloproteinases
TAPI
-
selective inhibitor
TAPI-1
-
TAPI-1 blocks the processing of RA175/SynCAM1, a member of the immunoglobulin family 4. Furthermore, TAPI-1 increases the number of synaptophysin and RA175/SynCAM1 colocalization on the dendrites of neurons
TAPI-1
-
-
TAPI-2
-
hydroxamate-based inhibitor of matrix metalloproteases that has high activity against TACE
TAPI-2
-
-
tert-butyl (1S,2R)-4-{[imino(2-oxido-2-oxohydrazino)-methyl]amino}-2-methyl-1-[1,3-thiazol-2-ylaminocarbonyl]butylcarbamate
-
-
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-3-methyl-4-pentenoate
-
-
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-amino-3-methylpentanoate
-
-
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-azido-3-methylpentanoate
-
-
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-hydroxy-3-methylpentanoate
-
-
tert-butyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
-
tert-butyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
-
tert-butyl (5-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-2,4,6-trioxohexahydropyrimidin-5-yl)carbamate
-
; IC50: 0.000013 mM
tert-butyl (5R,9R)-9-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-2,4-dioxo-1,3,7-triazaspiro[4.4]nonane-7-carboxylate
-
-
tert-butyl 11-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1,3,5-trioxo-2,4,8-triazaspiro[5.5]undecane-8-carboxylate
-
-
tert-butyl 3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
-
tert-butyl 3-[4-[2-(hydroxyamino)-2-oxoethyl]-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidin-1-yl]propanoate
-
-
tert-butyl 4-(5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,4,6-trioxohexahydropyrimidin-5-yl)piperazine-1-carboxylate
-
IC50: 0.00016 mM
tert-butyl 4-(5-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-2,4,6-trioxohexahydropyrimidin-5-yl)piperidine-1-carboxylate
-
; IC50: 0.000047 mM
tert-butyl 4-(hydroxycarbamoyl)-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]piperidine-1-carboxylate
-
-
tert-butyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
tert-butyl 4-([[4-(but-2-ynylamino)phenyl]sulfonyl]methyl)-4-[(hydroxyamino)-carbonyl]piperidine-1-carboxylate
-
-
tert-butyl 4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-6,8,10-trioxo-2,7,9-triazaspiro[4.5]decane-2-carboxylate
-
IC50: 0.000128 mM
tert-butyl 4-[([4-[but-2-ynyl(methyl)amino]phenyl]sulfonyl)methyl]-4-[(hydroxyamino)carbonyl]piperidine-1-carboxylate
-
-
tert-butyl(1S)-4-({(Z)-(methylsulfanyl)[(methylsulfonyl)-imino]methyl}amino)-1-[(1,3-thiazol-2-ylamino)carbonyl]butylcarbamate
-
-
TIMP-3
-
tissue inhibitor of metalloproteases-3, CAS: 147783-68-4, 171039-15-9, 13037-60-4
-
TIMP-3
-
85% inhibition at 10 nM
-
TIMP-3
-
presence of TIMP-3 inhibits shedding of lipoprotein-related protein I
-
tissue inhibitor of metalloproteinase-3
-
-
-
tissue inhibitor of metalloproteinases-3
-
natural inhibitor of ADAM17
-
TMI-1
-
-
TMI-2
-
complete inhibition at 50 nM
TNF-alpha proteinase inhibitor
-
0.00005 mM
-
tumor necrosis factor-alpha protease inhibitor
-
-
-
tumor necrosis factor-alpha-converting enzyme pro domain
-
inhibition of the tumor necrosis factor-alpha-converting enzyme by its isolated pro domain, IC50: 70 nM
-
[((3R,4S)-4-{[(benzyloxy)carbonyl]}-4-carboxy-3-methylbutyl)amino](imino)methanaminium nitrate (3R) 3-methyl L-arginine nitric acid salt
-
-
[N-hydroxy-1-(isopropylsulfonyl)-4-[(4-[(1-methylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)-methyl]piperidine-4-carboxamide
-
-
MMP-2
-
-
-
additional information
-
not inhibited by FN-439
-
additional information
-
endothelial protein C receptor shedding is not influenced by DMSO, TIMP-1 or TIMP-2
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
12-HPETE
-
i.e. 12-hydroperoxy-5Z,8Z,10E,14Z-eicosatetraenoic acid, a peroxide synthesized in the platelet lipoxygenase pathway, induces TACE-mediated receptor cleavage
anti-Ro/SSA autoantibody
-
i.e. antinuclear autoantibodies in the blood directed against Ro/Sjögren's syndrome ribonucleoprotein A antigen. Adalimumab appears to be significantly more efficacious than Etanercept in preventing TACE activation caused by anti-Ro/SSA autoantibodies
-
bortezomib
-
stimulates ADAM17-catalyzed shedding of CD30, blocks bortezomib-stimulated sCD30 release from L540 cells with an IC50 of approximately 230 nM
four and half LIM domain 2 protein
-
four and half LIM domain 2 protein binds both ADAM-17 and the actin-based cytoskeletonand is involved in the regulation of ADAM-17 cellular localization and activity
-
furin
-
activates ADAM-17
-
glucose oxidase
-
oxidative damage via glucose oxidase or hydrogen peroxide activates TACE and induces shedding of its targets, glycoprotein Ibalpha and glycoprotein V, in murine and human platelets. The TACE activation is independent of platelet activation. TACE activation induced by hydrogen peroxide is dependent on p38 mitogen-activated protein kinase signalling, whereas protein kinase C, phosphoinositide 3-kinase, and caspases are not involved. Inhibition of p38 cytoplasmic targets, phospholipase A2 and heat shock protein 27, does not prevent shedding, whereas blocking 12-lipoxygenase or Src kinase slightly inhibits TACE activation
-
granulocyte-macrophage colony-stimulating factor
-
granulocyte-macrophage colony-stimulating factor GM-CSF and interleukin-4 in combination potently up-regulate tumor necrosis factor-alpha coverting enzyme TACE and activity in monocytes, causing ectodomain shedding of M-CSF receptor
-
heparan sulfate
-
removal of cell surface heparan sulfate increases TACE activity and TACE-dependent formation of ErbB4 80 kDa intracellular domain
hydrogen peroxide
-
-
interleukin-4
-
granulocyte-macrophage colony-stimulating factor GM-CSF and interleukin-4 in combination potently up-regulate tumor necrosis factor-alpha coverting enzyme TACE and activity in monocytes, causing ectodomain shedding of M-CSF receptor
-
lipopolysaccharide
-
-
N-formyl-L-methionyl-phenylalanine
-
ADAM17 substrates undergo efficient turnover during extended neutrophil activation by N-formyl-L-methionyl-phenylalanine
oxygen
-
low oxygen concentrations enhance TACE mRNA levels in synovial cells through direct binding of hypoxia-inducible factor-1 to the 5' promoter region
p38 mitogen-activated protein kinase
-
increased and sustained cell surface levels of TACE, and phosphorylation of its cytoplasmic tail, a hallmark of TACE activation, occur in lymphocytes and monocytes following p38 MAPK activation
-
phorbol 12-myristate 13-acetate
-
potent activator of ADAM17
phorbol 12-myristate-13-acetate
-
PMA
phorbol 12-myristate-13-acetate
-
-
phorbol ester
-
stimulates the TACE-mediated release of TNF-alpha from cells
phorbol-12-myristate 13-acetate
-
-
Tumor necrosis factor alpha
-
20 ng/ml tumor necrosis factor alpha enhances TACE mRNA levels in synovial cells through direct binding of hypoxia-inducible factor-1 to the 5' promoter region
-
lipopolysaccharide
-
lipopolysaccharide-vehicle or lipopolysaccharide-ranitidine treatments of rats causes a significant increase in hepatic TACE activity
additional information
-
no apparent change in mRNA contents of TACE upon stimulation with IFN alpha, IFN beta and IFN gamma
-
additional information
-
no effect: removal of chondroitin sulfate
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1.3
NH2-LAQAVRSSSR-OH
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0011
(1R,2R)-2-(3-phenoxylphenyl)-2-trans-carbomethoxylcyclopropane hydroxamic acid
-
-
0.000008
(1R,2R)-2-trans-carboisopropoxyl-2-[3-(2-methylquinolin-4-yl)methoxylphenyl]cyclopropane hydroxyamic acid
-
-
0.00014
(1R,2R)-2-trans-N-benzylaminocarbonyl-2-[3-(2-methylquinolin-4-yl)methoxylphenyl]cyclopropane hydroxyamic acid
-
-
0.000011
(1R,2R)-2-[3-(3,4-dichlorobenzyloxy)phenyl]-2-trans-carbomethoxylcyclopropane hydroxamic acid
-
-
0.005
(1R,2R)-N-hydroxy-2-[(4-methylpiperazin-1-yl)carbonyl]-2-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropanecarboxamide
-
-
0.003
(1R,2R)-N1-benzyl-N2-hydroxy-N1-methyl-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
0.000009
(1R,2R)-N1-cyclohexyl-N2-hydroxy-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
0.000011
(1R,2R)-N2-hydroxy-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]-N1-phenylcyclopropane-1,2-dicarboxamide
-
-
0.0027
(1R,2R)-N2-hydroxy-N1,N1-dimethyl-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
0.0001
(1R,2R)-N2-hydroxy-N1-methyl-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
0.00000015
(1R,2S)-1-(3-fluoro-4-[[2-(1-methyl-1H-pyrazol-5-yl)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
0.00000076
(1R,2S)-1-(3-fluoro-4-[[2-(methylamino)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
0.00000021
(1R,2S)-1-[3-fluoro-4-[(2-morpholin-4-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
0.00000036
(1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxy-N1,N1-dimethylcyclopropane-1,2-dicarboxamide
-
-
0.00000014
(1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
0.00000014
(1R,2S)-1-[3-fluoro-4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
0.00000015
(1R,2S)-1-[3-fluoro-4-[(2-pyrrolidin-1-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
0.00036
(1R,2S)-1-[4-(benzyloxy)benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
0.00008
(1R,2S)-1-[4-(but-2-yn-1-yloxy)benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
0.000001
(1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
0.000003
(1R,2S)-N2-hydroxy-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
0.00000063
(1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N1-(piperidin-4-ylmethyl)cyclopropane-1,2-dicarboxamide
-
-
0.00000018
(1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
0.000001
(1R,2S)-N2-hydroxy-N1,N1-dimethyl-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
0.00000028
(1R,2S)-N2-hydroxy-N1,N1-dimethyl-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
0.000014
(1R,2S)-N2-hydroxy-N1-methyl-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
0.00000038
(1S,2R)-2-[[(3R)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
0.00000054
(1S,2R)-2-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
0.0000003
(1S,2R)-N-hydroxy-2-[[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
0.00000025
(1S,2R)-N-hydroxy-2-[[(3S)-3-hydroxypyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
0.000012
(1S,2R)-N-hydroxy-2-{4-[(2-imino-1,2-dihydroquinolin-4-yl)methoxy]benzyl}-2-(methoxycarbonyl)cyclopropanecarboximidic acid
-
-
0.000004
(1S,2S)-2-((S)-cyano(4-((2-phenylquinolin-4-yl)methoxy)phenyl)methyl)-N-hydroxycyclopropanecarboxamide
-
-
0.000071
(2R)-N-hydroxy-2-(7-methoxy-1,1-dioxido-4,5-dihydro-1,2,5-benzothiadiazepin-2(3H)-yl)-3-methylbutanamide
-
-
0.000028
(3S)-1-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]pyrrolidine-3-thiol
-
-
0.000001
(3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
-
0.000002
(5R)-5-(2',4'-difluorobiphenyl-4-yl)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000002
(5R)-5-(4'-chlorobiphenyl-4-yl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.00001
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[2'-(1-methyl-1H-tetrazol-5-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000018
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(trifluoromethyl)biphenyl-4-yl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000002
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(6-oxo-1,6-dihydropyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000001
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000008
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(quinolin-6-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000031
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[3'-(2-methyl-1,3-thiazol-4-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000002
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(1H-pyrazol-3-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000006
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1,3-thiazol-2-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000002
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000003
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-5-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000002
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methyl-2H-indazol-6-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000005
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methylpyridin-4-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000028
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(3-phenyl-1,2-oxazol-5-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000026
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(4-methyl-2,5-dioxoimidazolidin-4-yl)phenyl]imidazolidine-2,4-dione (non-preferred name)
-
pH and temperature not specified in the publication
0.0000012
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrazin-2-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000005
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-2-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000008
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000006
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000009
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrimidin-5-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000014
(5R)-5-[4-(2-aminopyridin-4-yl)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000005
(5R)-5-[4-(3,5-dimethyl-1,2-oxazol-4-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000001
(5R)-5-[4-(5-chloro-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000008
(5S)-5-(4-fluorophenyl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000005
1-methylethyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropanecarboxylate
-
-
0.00019
2-(3-benzyloxyphenyl)-2-trans-carbomethoxylcyclopropane hydroxyamic acid
-
-
0.0007
2-[3-(2-methylquinolin-4-yl)methoxylphenyl]-2-trans-carboxamidocyclopropane hydroxyamic acid
-
-
0.000008
2-[3-(2-methylquinolin-4-yl)methoxyphenyl]-2-trans-carbomethoxylcyclopropane hydroxyamic acid
-
-
0.000002
2-[[4-(but-2-yn-1-ylamino)phenyl]sulfonyl]ethanethiol
-
-
0.000008
2-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]ethanethiol
-
-
0.00001
2-[[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl](methyl)amino]-N-hydroxyacetamide
-
-
0.000017
3-[[4-(but-2-yn-1-ylamino)phenyl]sulfonyl]cyclohexanethiol
-
-
0.0000045
3-[[4-(but-2-yn-1-ylamino)phenyl]sulfonyl]propane-1-thiol
-
-
0.00003
3-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]cyclohexanethiol
-
-
0.00005
3-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]cyclopentanethiol
-
-
0.00001
3-[[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]propane-1-thiol
-
-
0.000003
4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxamide
-
pH and temperature not specified in the publication
0.000006
5-[(5-methoxy-3-oxo-1,3-dihydro-2H-indazol-2-yl)methyl]-5-phenylimidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000029
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(2-phenoxyphenyl)imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000027
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(3-phenoxyphenyl)imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000008
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-oxopyrrolidin-1-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000006
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(morpholin-4-yl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000007
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yloxy)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000006
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrrolidin-1-ylcarbonyl)phenyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000003
5-[4-(cyclopentyloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.000008
5-[4-(isoquinolin-7-yloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
pH and temperature not specified in the publication
0.0000028
DPH-067517
-
-
0.000016
ethyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropanecarboxylate
-
-
0.000381
ethyl (1R,2S)-1-[3-bromo-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.000158
ethyl (1R,2S)-1-[3-chloro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.000005
ethyl (1R,2S)-1-[3-fluoro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.000002
ethyl (1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.0031
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-phenoxybenzyl)cyclopropanecarboxylate
-
-
0.000018
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(2-methylpropyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
-
0.000003
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(trifluoromethyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
-
0.000006
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
0.000037
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylpyridin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
0.000012
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
0.000022
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
0.00005
methyl (1R,2R)-1-[3-(2-[3-[(1Z)-buta-1,3-dien-1-yl]phenyl]ethoxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.0012
methyl (1R,2R)-1-[3-(benzyloxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.0016
methyl (1R,2R)-1-[3-(but-2-yn-1-yloxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.0009
methyl (1R,2R)-1-[3-(cyclohexylmethoxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.00005
methyl (1R,2R)-1-[3-[(4-chlorobenzyl)oxy]phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.003
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-(3-methoxyphenyl)cyclopropanecarboxylate
-
-
0.00007
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-(3-[[3-(trifluoromethyl)benzyl]oxy]phenyl)cyclopropanecarboxylate
-
-
0.000018
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-(3-[[4-(trifluoromethyl)benzyl]oxy]phenyl)cyclopropanecarboxylate
-
-
0.00024
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(2-methylphenoxy)phenyl]cyclopropanecarboxylate
-
-
0.00006
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(2-naphthalen-2-ylethoxy)phenyl]cyclopropanecarboxylate
-
-
0.00029
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(2-phenylethoxy)phenyl]cyclopropanecarboxylate
-
-
0.00014
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(4-methylphenoxy)phenyl]cyclopropanecarboxylate
-
-
0.003
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(naphthalen-2-ylmethoxy)phenyl]cyclopropanecarboxylate
-
-
0.00007
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(naphthalen-2-yloxy)phenyl]cyclopropanecarboxylate
-
-
0.00011
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(3-methoxybenzyl)oxy]phenyl]cyclopropanecarboxylate
-
-
0.0008
methyl (1R,2S)-1-[4-(benzyloxy)benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.00042
methyl (1R,2S)-1-[4-(but-2-yn-1-yloxy)benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.026
methyl (1R,2S)-1-[4-(cyclohexylmethoxy)benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.00026
methyl (1R,2S)-1-[4-[(2-chlorobenzyl)oxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.00013
methyl (1R,2S)-1-[4-[(3,4-dichlorobenzyl)oxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
0.1
methyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-(2-naphthalen-1-ylethoxy)benzyl]cyclopropanecarboxylate
-
-
0.1
methyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-(2-naphthalen-2-ylethoxy)benzyl]cyclopropanecarboxylate
-
-
0.000013
methyl (5R)-5-{7-[(3,5-diethoxybenzyl)oxy]-1,1-dioxido-4,5-dihydro-1,2,5-benzothiadiazepin-2(3H)-yl}-6-(hydroxyamino)-6-oxohexanoate
-
-
0.00001
methyl (5R)-5-{7-[(3,5-dimethoxybenzyl)oxy]-1,1-dioxido-4,5-dihydro-1,2,5-benzothiadiazepin-2(3H)-yl}-6-(hydroxyamino)-6-oxohexanoate
-
-
0.000009
methyl 4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxylate
-
pH and temperature not specified in the publication
0.0031
N-hydroxy-2(R)-(6-methoxy-1,1-dioxo-3,4-dihydro-1H-1-benzo[1,2,4]thiadiazin-2-yl)propionamide
-
-
0.000484
N-hydroxy-2(R)-[2,3,4,5-tetrahydrobenzo[1,2,5-f]-thiadiazepine-1,1-dioxide]propanamide
-
-
0.000544
N-hydroxy-2(R)-[7-(2,6-methylpyridyl-4-methyleneoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-propanamide
-
-
0.001
N-hydroxy-2(R)-[7-(2-trifluromethylphenyl)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propylamide
-
value above
0.000153
N-hydroxy-2(R)-[7-(3,5-dichlorobenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.000051
N-hydroxy-2(R)-[7-(3,5-diethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-3-methylbutanamide
-
-
0.000242
N-hydroxy-2(R)-[7-(3,5-diethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methoxycarbonylbutanamide
-
-
0.000081
N-hydroxy-2(R)-[7-(3,5-diethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.000005
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine 1,1-dioxide]-6-N-(methanesulfonyl)hexylamide
-
-
0.00001
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-3-methylbutanamide
-
-
0.000177
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methoxycarbonylbutanamide
-
-
0.000017
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentanamide
-
-
0.000031
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-6-aminohexylamidetrifluoroacetic acid salt
-
-
0.000077
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-6-N-[(1,1-dimethylethoxy)carbonyl]hexylamide
-
-
0.000027
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.000229
N-hydroxy-2(R)-[7-(3,5-dimethylbenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.000129
N-hydroxy-2(R)-[7-(3-nitrophenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.00029
N-hydroxy-2(R)-[7-(4,5-dimethylthiazolyl-2-methyleneoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-3-methylbutanamide
-
-
0.000621
N-hydroxy-2(R)-[7-(4-methoxyphenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.000011
N-hydroxy-2(R)-[7-(4-nitrophenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.001
N-hydroxy-2(R)-[7-(4-phenylphenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
value above
0.000758
N-hydroxy-2(R)-[7-(4-trifluoromethylphenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.001
N-hydroxy-2(R)-[7-(N-3,5-dimethylbenzoylamino)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-propylamide
-
value above
0.000177
N-hydroxy-2(R)-[7-benzyloxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentanamide
-
-
0.000705
N-hydroxy-2(R)-[7-benzyloxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.000089
N-hydroxy-2(R)-[7-hydroxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentamide
-
-
0.000391
N-hydroxy-2(R)-[7-hydroxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.000274
N-hydroxy-2(R)-[7-methoxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.000056
N-hydroxy-2(R)-[7-N-(3,5-dimethoxymethyleneamino)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentamide
-
-
0.000734
N-hydroxy-2(R)-[7-phenoxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
-
-
0.001
N-hydroxy-2(R)-[7-phenyl-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propylamide
-
value above
0.001
N-hydroxy-2-[2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]ethanamide
-
-
0.001
N-hydroxy-2-[7-methoxy-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]ethanamide
-
-
0.00008
N-[(4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]methylcarbamoyl-5-hydroxy-2-methyloct-4-yl]-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]isophthalamide
-
-
5
NaCl
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000026
(3R,4R)-4-([[4-(1,3-dihydrofuro[3,4-b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.000001
(3R,4R)-4-([[4-(2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.0000013
(3R,4R)-4-([[4-(2,3-dihydrofuro[2,3-b]quinolin-4-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.0000012
(3R,4R)-4-[([4-[(2,3-dimethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.0000013
(3R,4R)-4-[([4-[(2-cyclopropylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.0000017
(3R,4R)-4-[([4-[(2-ethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.0000078
(3R,4R)-4-[([4-[(3-ethyl-2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.0000012
(3R,4R)-4-[[(4-[[2-(dimethylamino)quinolin-4-yl]methyl]phenyl)carbonyl]amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.000001
(3R,4R)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.0000016
(3R,4R)-N-hydroxy-4-[([4-[(2-morpholin-4-ylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.0000015
(3R,4R)-N-hydroxy-4-[([4-[(3-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.000001
(3R,4R)-N-hydroxy-4-[[(4-[[2-(1-methylethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
IC50 below 0.000001 mM
0.0000022
(3R,4R)-N-hydroxy-4-[[(4-[[2-(trifluoromethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.000001
(3R,4S)-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-4-carboxamide
Sus scrofa
-
IC50 below 0.000001 mM
0.000001
(3R,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydrofuran-3-carboxamide
Sus scrofa
-
-
0.0000023
(3R,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydrofuran-3-carboxamide
Sus scrofa
-
-
0.0000023
(3S)-4-[[4-(but-2-ynylamino)phenyl]sulfonyl]-N-hydroxy-2,2-dimethylthio-morpholine-3-carboxamide
Homo sapiens
-
-
0.000024
(3S,4R)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-3-carboxamide
Sus scrofa
-
-
0.0000015
(3S,4S)-1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000016
(3S,4S)-1-(2,2-dimethylpropyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000011
(3S,4S)-1-(butylsulfonyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.000002
(3S,4S)-1-(furan-2-ylmethyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000013
(3S,4S)-1-acetyl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-1-but-2-yn-1-yl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-1-cyclobutyl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.000002
(3S,4S)-1-tert-butyl-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-4-carboxamide
Sus scrofa
-
-
0.000002
(3S,4S)-1-[2-(dimethylamino)ethyl]-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-4-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-3-[([4-[(2-cyclopropylimidazo[1,2-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-3-[([4-[(2-ethyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.000002
(3S,4S)-3-[([4-[(2-ethylpyrazolo[1,5-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.0000028
(3S,4S)-3-[([4-[(2-tert-butylpyrazolo[1,5-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.0000004
(3S,4S)-N-hydroxy-1-(1-methylethyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000015
(3S,4S)-N-hydroxy-1-(2-methylprop-2-en-1-yl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000021
(3S,4S)-N-hydroxy-1-(2-methylpropanoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000011
(3S,4S)-N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000016
(3S,4S)-N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000016
(3S,4S)-N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000025
(3S,4S)-N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000016
(3S,4S)-N-hydroxy-3-[([4-[(2-methyl-1-benzofuran-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.000006
(3S,4S)-N-hydroxy-3-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-N-hydroxy-3-[([4-[(2-methylimidazo[1,2-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-4-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-N-hydroxy-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
IC50 below 0.000001 mM
0.0000021
(3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)-1-benzofuran-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.0000032
(3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)imidazo[1,2-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.0000017
(3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.0000015
(3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1-benzofuran-3-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000022
(3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000016
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-phenylpyrrolidine-3-carboxamide
Sus scrofa
-
-
0.00000094
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-prop-2-en-1-ylpyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000063
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000043
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
Sus scrofa
-
-
0.000001
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000035
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.0000018
(3S,4S)-N-hydroxy-4-[[(4-[[2-(1-methylethyl)-1-benzofuran-3-yl]methyl]phenyl)carbonyl]amino]pyrrolidine-3-carboxamide
Sus scrofa
-
-
0.00023
(5R,6R)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,4-dioxo-1,3-diazaspiro[4.4]nonane-6-carboxamide
Sus scrofa
-
-
0.000064
(5R,6S)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,4-dioxo-1,3-diazaspiro[4.4]nonane-6-carboxamide
Sus scrofa
-
-
0.000001
(5R,7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-oxaspiro[4.4]nonane-7-carboxamide
Sus scrofa
-
-
0.000011
(5S,6R)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,4-dioxo-1,3-diazaspiro[4.5]decane-6-carboxamide
Sus scrofa
-
-
0.000001
(5S,6S)-N-hydroxy-5-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-2,3,5,6-tetrahydro-4aH-cyclopenta[b][1,4]dioxine-6-carboxamide
Sus scrofa
-
-
0.000001
(5S,7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-oxaspiro[4.4]nonane-7-carboxamide
Sus scrofa
-
-
0.000001
(7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1,4-dioxaspiro[4.4]nonane-7-carboxamide
Sus scrofa
-
-
0.0000011
1-(1,3-benzoxazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
-
0.000001
1-(1H-benzimidazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
IC50 above 0.000001 mM
0.0000015
1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000023
1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]piperidine-4-carboxamide
Homo sapiens
-
-
0.0000016
1-(2,2-dimethylpropyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000011
1-(butylsulfonyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.000001
1-but-2-yn-1-yl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000012
1-ethylpropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
-
0.0000014
1-methyl-2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
-
0.0000015
1-methylethyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
Sus scrofa
-
-
0.0000015
1-methylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
-
0.0000015
1-[(4-acetylpiperazin-1-yl)sulfonyl]-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
-
0.0073
1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]-1,3,5-triazinane-2,4,6-trione
Sus scrofa
-
IC50: 0.0073 mM
0.00015
13-[(4R)-2,5-dioxoimidazolidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]tridecanamide
Sus scrofa
-
-
0.000003
2,6-anhydro-3,4,5-trideoxy-1-(hydroxyamino)-3-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-D-threo-hexose
Sus scrofa
-
-
0.00003
2-(6-methyl-2-oxo-2H-chromen-3-ylmethyl)-pent-4-enoic acid hydroxyamide
Homo sapiens
-
at 25°C
0.000005
2-benzyl-N-hydroxy-3-(6-methyl-2-oxo-2H-chromen-3-yl)-propionamide
Homo sapiens
-
at 25°C
0.0000022
2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
-
0.0074
2-[(5R,6R)-2,4-dioxo-1,3-diazaspiro[4.4]non-6-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]acetamide
Sus scrofa
-
-
0.000017
2-[(5R,6S)-2,4-dioxo-1,3-diazaspiro[4.4]non-6-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]acetamide
Sus scrofa
-
-
0.1
2-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-N-[(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)methyl]acetamide
Sus scrofa
-
IC50 above 0.1 mM; IC50: above 0.1 mM
0.00084
3-(6-bromo-2-oxo-2H-chromen-3-yl)-N-hydroxy-propanamide
Homo sapiens
-
at 25°C
0.00055
3-(6-chloro-2-oxo-2H-chromen-3-yl)-N-hydroxy-propanamide
Homo sapiens
-
at 25°C
0.0124
3-(6-tert-butyl-2-oxo-2H-chromen-3-yl)-N-hydroxypropanamide
Homo sapiens
-
at 25°C
0.0000026
3-([[4-(1,3-dihydrofuro[3,4-b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.000001
3-([[4-(2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000013
3-([[4-(2,3-dihydrofuro[2,3-b]quinolin-4-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000012
3-[([4-[(2,3-dimethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000013
3-[([4-[(2-cyclopropylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000017
3-[([4-[(2-ethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000078
3-[([4-[(3-ethyl-2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000032
3-[4-[2-(hydroxyamino)-2-oxoethyl]-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidin-1-yl]propanoic acid
Homo sapiens
-
-
0.0000012
3-[[(4-[[2-(dimethylamino)quinolin-4-yl]methyl]phenyl)carbonyl]amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000025
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-benzoyl)-piperidine-4-carboxylic acid hydroxyamide
Homo sapiens
-
-
0.0000035
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-butyryl)-piperidine-4-carboxylic acid hydroxyamide
Homo sapiens
-
-
0.000002
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(propane-2-sulfonyl)-piperidine-4-carboxylic acid hydroxyamide
Homo sapiens
-
-
0.0000023
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-isobutyryl-piperidine-4-carboxylic acid hydroxyamide
Homo sapiens
-
-
0.0000064
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-pyridin-4-ylmethyl-piperidine-4-carboxylic acid hydroxyamide
Homo sapiens
-
-
0.000001
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-1,4-dicarboxylic acid 1-diethylamide 4-hydroxyamide
Homo sapiens
-
IC50 below 0.000001 mM
0.000064
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-4-carboxylic acid hydroxyamide
Homo sapiens
-
-
0.0000018
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-(dimethylsulfamoyl)-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
-
0.000001
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dichlorothiophen-3-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
IC50 below 0.000001 mM
0.000001
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dimethyl-1,3-thiazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
IC50 below 0.000001 mM
0.0000017
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)carbonyl]-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
-
0.0000016
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)methyl]-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
-
0.000001
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethyl-1H-pyrazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
IC50 below 0.000001 mM
0.0000022
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethylisoxazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
-
0.000007
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(5-chlorothiophen-2-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
Homo sapiens
-
-
0.000001
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(morpholin-4-ylsulfonyl)piperidine-4-carboxamide
Homo sapiens
-
-
0.0000012
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(piperidin-1-ylsulfonyl)piperidine-4-carboxamide
Homo sapiens
-
-
0.000001
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(pyrrolidin-1-ylsulfonyl)piperidine-4-carboxamide
Homo sapiens
-
-
0.00000133
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-2-ylpiperidine-4-carboxamide
Homo sapiens
-
-
0.0000056
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-4-ylpiperidine-4-carboxamide
Homo sapiens
-
-
0.000003
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[(2-methyl-1H-imidazol-4-yl)sulfonyl]piperidine-4-carboxamide
Homo sapiens
-
-
0.0000014
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
Homo sapiens
-
-
0.0000015
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
Homo sapiens
-
-
0.000138
4-[(2-methylquinolin-4-yl)methoxy]-N-(1,3,5-trioxo-2,4-diazaspiro[5.5]undec-7-yl)benzamide
Sus scrofa
-
; IC50: 0.000138 mM
0.1
4-[(2-methylquinolin-4-yl)methoxy]-N-(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)benzamide
Sus scrofa
-
IC50 above 0.1 mM; IC50: above 0.1 mM
0.000044
4-[(2-methylquinolin-4-yl)methoxy]-N-(6,8,10-trioxo-2-oxa-7,9-diazaspiro[4.5]dec-4-yl)benzamide
Sus scrofa
-
; IC50: 0.000044 mM
0.000024
4-[(2-methylquinolin-4-yl)methoxy]-N-(6,8,10-trioxo-7,9-diazaspiro[4.5]dec-1-yl)benzamide
Sus scrofa
-
; IC50: 0.000024 mM
0.000031
4-[(2-methylquinolin-4-yl)methoxy]-N-([2,4,6-trioxo-5-[1-(tetrahydro-2H-pyran-2-yl)piperidin-4-yl]hexahydropyrimidin-5-yl]methyl)benzamide
Sus scrofa
-
-
0.000031
4-[(2-methylquinolin-4-yl)methoxy]-N-([2,4,6-trioxo-5-[1-(tetrahydro-2H-pyran-4-yl)piperidin-4-yl]hexahydropyrimidin-5-yl]methyl)benzamide
Sus scrofa
-
IC50: 0.000031 mM
0.00001
4-[(2-methylquinolin-4-yl)methoxy]-N-([2,4,6-trioxo-5-[4-(pyridin-3-ylcarbonyl)piperazin-1-yl]hexahydropyrimidin-5-yl]methyl)benzamide
Sus scrofa
-
IC50: 0.00001 mM
0.000029
4-[(2-methylquinolin-4-yl)methoxy]-N-([5-[1-(methylsulfonyl)piperidin-4-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)benzamide
Sus scrofa
-
IC50: 0.000029 mM
0.000002
4-[(2-methylquinolin-4-yl)methoxy]-N-([5-[4-(methylsulfonyl)piperazin-1-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)benzamide
Sus scrofa
-
IC50: 0.000002 mM
0.000018
4-[(2-methylquinolin-4-yl)methoxy]-N-[(2,4,6-trioxo-5-phenylhexahydropyrimidin-5-yl)methyl]benzamide
Sus scrofa
-
-
0.000055
4-[(2-methylquinolin-4-yl)methoxy]-N-[(2,4,6-trioxo-5-piperidin-4-ylhexahydropyrimidin-5-yl)methyl]benzamide
Sus scrofa
-
; IC50: 0.000055 mM
0.00236
4-[(2-methylquinolin-4-yl)methoxy]-N-[(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)(pyridin-4-yl)methyl]benzamide
Sus scrofa
-
; IC50: 0.00236 mM
0.000026
4-[(2-methylquinolin-4-yl)methoxy]-N-[(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)methyl]benzamide
Sus scrofa
-
; IC50: 0.000026 mM
0.000036
4-[(2-methylquinolin-4-yl)methoxy]-N-[2-(methylsulfonyl)-6,8,10-trioxo-2,7,9-triazaspiro[4.5]dec-4-yl]benzamide
Sus scrofa
-
IC50: 0.000036 mM
0.000029
4-[(2-methylquinolin-4-yl)methoxy]-N-[6,8,10-trioxo-2-(pyridin-3-ylcarbonyl)-2,7,9-triazaspiro[4.5]dec-4-yl]benzamide
Sus scrofa
-
IC50: 0.000029 mM
0.000014
4-[(2-methylquinolin-4-yl)methoxy]-N-[[2,4,6-trioxo-5-(4-phenylpiperazin-1-yl)hexahydropyrimidin-5-yl]methyl]benzamide
Sus scrofa
-
-
0.000027
4-[([4-[(1,1-dimethylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)methyl]-N-hydroxy-1-(isopropylsulfonyl)piperidine-4-carboxamide
Homo sapiens
-
-
0.0000028
4-[2-(hydroxyamino)-2-oxoethyl]-N,N-dimethyl-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-1-carboxamide
Homo sapiens
-
-
0.00001
4-[4-(4-hydroxy-but-2-ynylamino)-benzenesulfonylmethyl]-4-hydroxycarbamoyl-piperidine-1-carboxylic acid tert-butyl ester
Homo sapiens
-
-
0.009
4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)-thiomorpholinecarboxamide
Homo sapiens
-
IC50: 0.009 mM
0.05
4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)-thiomorpholinecarboxamide
Mus musculus
-
IC50: 0.05 mM
0.00062
5-(4-acetylpiperazin-1-yl)-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.00062 mM
0.000195
5-(4-benzylpiperazin-1-yl)-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.000195 mM
0.000081
5-(4-hexylpiperazin-1-yl)-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.000081 mM
0.000091
5-(4-methylpiperazin-1-yl)-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.000091 mM
0.049
5-methyl-5-(2-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]ethyl)pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
; IC50: 0.049 mM
0.0008
5-methyl-5-(3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-3-oxopropyl)pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
; IC50: 0.0008 mM
0.011
5-methyl-5-(3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]prop-2-en-1-yl)pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.011 mM
0.1
5-methyl-5-(3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]propyl)pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50 above 0.1 mM; IC50: above 0.1 mM
0.011
5-methyl-5-[(2E)-3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]prop-2-en-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
-
0.0022
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
; IC50: 0.0022 mM
0.0013
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]phenoxy]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
; IC50: 0.0013 mM
0.0037
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]dihydropyrimidine-2,4(1H,3H)-dione
Sus scrofa
-
IC50: 0.0037 mM
0.00103
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.00103 mM
0.00103
5-methyl-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
; IC50: 0.00103 mM
0.000096
5-[4-(1-methylethyl)piperazin-1-yl]-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.000096 mM
0.00054
5-[4-(2,2-dimethylpropanoyl)piperazin-1-yl]-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.00054 mM
0.00016
5-[4-(2,2-dimethylpropyl)piperazin-1-yl]-5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.00016 mM
0.000535
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-(pyridin-3-ylcarbonyl)pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.000535 mM
0.0011
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-piperazin-1-ylpyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.0011 mM
0.000855
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-piperidin-1-ylpyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.000855 mM
0.000084
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-[4-(2-phenylethyl)piperazin-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.000084 mM
0.00011
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-[4-(3-phenylpropyl)piperazin-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.00011 mM
0.0028
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-[4-(4-nitrophenyl)piperazin-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.0028 mM
0.000275
5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-5-[4-(methylsulfonyl)piperazin-1-yl]pyrimidine-2,4,6(1H,3H,5H)-trione
Sus scrofa
-
IC50: 0.000275 mM
1
7-(1-methyl-2,5-dioxoimidazolidin-4-yl)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
Sus scrofa
-
-
0.00021
7-(2,5-dioxoimidazolidin-4-yl)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
Sus scrofa
-
-
1
7-(3-methyl-2,5-dioxoimidazolidin-4-yl)-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
Sus scrofa
-
-
0.00017
7-[(4R)-2,5-dioxoimidazolidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
Sus scrofa
-
-
0.0037
7-[(4S)-2,5-dioxoimidazolidin-4-yl]-N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]heptanamide
Sus scrofa
-
-
0.0000028
cyclohexyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
-
0.000001
cyclohexylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
IC50 above 0.000001 mM
0.0000013
cyclopentyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
-
0.0000016
cyclopropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
-
0.000028
gelastatin hydroxamate
Homo sapiens
-
at 25°C
0.000317
GM6001
Homo sapiens
-
in 25 mM Tris-HCl buffer, pH 9, 0.0025 mM ZnCl2 and 0.005% (v/v) Brij-35, at 37°C
0.00006
JMV 390
Homo sapiens
-
mutant enzyme V353G
0.000065
JMV 390
Homo sapiens
-
wild type enzyme
0.000001
methyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
Sus scrofa
-
-
0.0000033
methyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
Sus scrofa
-
-
0.0011
methyl (5R)-5-{7-[(3,5-diethoxybenzyl)oxy]-1,1-dioxido-4,5-dihydro-1,2,5-benzothiadiazepin-2(3H)-yl}-6-(hydroxyamino)-6-oxohexanoate
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0009
methyl (5R)-5-{7-[(3,5-dimethoxybenzyl)oxy]-1,1-dioxido-4,5-dihydro-1,2,5-benzothiadiazepin-2(3H)-yl}-6-(hydroxyamino)-6-oxohexanoate
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0000033
methyl 3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
Homo sapiens
-
-
0.0047
methyl 4-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,5-dioxoimidazolidine-4-carboxylate
Sus scrofa
-
IC50: 0.0047 mM
0.11
N(R)-[2-(hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-alanine amide
Homo sapiens
-
IC50: about 0.11 mM
0.7
N(R)-[2-(hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-alanine amide
Mus musculus
-
IC50: about 0.7 mM
0.000055
N-(2-acetyl-6,8,10-trioxo-2,7,9-triazaspiro[4.5]dec-4-yl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
IC50: 0.000055 mM
0.000055
N-(8-acetyl-1,3,5-trioxo-2,4,8-triazaspiro[5.5]undec-11-yl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.000052
N-([5-[1-(1-methylethyl)piperidin-4-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
; IC50: 0.000052 mM
0.000013
N-([5-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
IC50: 0.000013 mM
0.000007
N-([5-[4-(1-methylethyl)piperazin-1-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
; IC50: 0.000007 mM
0.000029
N-([5-[4-(2,2-dimethylpropanoyl)piperazin-1-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
IC50: 0.000029 mM
0.000062
N-([5-[4-(5-amino-8-carbamimidamido-4-oxooctyl)piperazin-1-yl]-2,4,6-trioxohexahydropyrimidin-5-yl]methyl)-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.0000016
N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000025
N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0029
N-hydroxy-2(R)-[7-(2,6-methylpyridyl-4-methyleneoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-propanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.00094
N-hydroxy-2(R)-[7-(3,5-dichlorobenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0082
N-hydroxy-2(R)-[7-(3,5-diethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-3-methylbutanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0062
N-hydroxy-2(R)-[7-(3,5-diethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methoxycarbonylbutanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0045
N-hydroxy-2(R)-[7-(3,5-diethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0019
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine 1,1-dioxide]-6-N-(methanesulfonyl)hexylamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.004
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-3-methylbutanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0072
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methoxycarbonylbutanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0054
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.00077
N-hydroxy-2(R)-[7-(3,5-dimethoxybenzyloxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.00047
N-hydroxy-2(R)-[7-(3-nitrophenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0245
N-hydroxy-2(R)-[7-(4,5-dimethylthiazolyl-2-methyleneoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]-3-methylbutanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0012
N-hydroxy-2(R)-[7-(4-nitrophenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.00084
N-hydroxy-2(R)-[7-(4-trifluoromethylphenoxy)-2,3,4,5-tetrahydrobenzo[1,2,5-f]thiadiazepine-1,1-dioxide]propanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.00035
N-hydroxy-2(R)-[7-benzyloxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentanamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.0095
N-hydroxy-2(R)-[7-hydroxy-2,3,4,5-tetrahydrobenzo-[1,2,5-f]thiadiazepine-1,1-dioxide]-4-methylpentamide
Sus scrofa
-
human peripheral blood mononuclear cell assay (PBMC)
0.000036
N-hydroxy-2-((6-methoxy-2H-chromen-3-yl)methyl)propanamide
Homo sapiens
-
at 25°C
0.000175
N-hydroxy-2-(2-oxo-2H-chromen-3-yl)acetamide
Homo sapiens
-
in 25 mM Tris-HCl buffer, pH 9.0, 0.0025 mM ZnCl2 and 0.005% (v/v) Brij-35, at 37°C
0.000003
N-hydroxy-2-methyl-3-(6-methyl-2-oxo-2H-chromen-3-yl)-propionamide
Homo sapiens
-
at 25°C
0.00015
N-hydroxy-3-(2-oxo-2H-chromen-3-yl)propanamide
Homo sapiens
-
at 25°C
0.00011
N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl)propanamide
Homo sapiens
-
at 25°C
0.00006
N-hydroxy-3-(6-methyl-2-oxo-2H-chromen-3-yl)propanamide
Homo sapiens
-
at 25°C
0.0000016
N-hydroxy-3-[([4-[(2-morpholin-4-ylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000015
N-hydroxy-3-[([4-[(3-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000022
N-hydroxy-3-[[(4-[[2-(trifluoromethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-2-carboxamide
Homo sapiens
-
-
0.0000063
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000043
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
Homo sapiens
-
-
0.000001
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
Sus scrofa
-
-
0.000001
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
Homo sapiens
-
-
0.000002
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydrofuran-3-carboxamide
Homo sapiens
-
-
0.0000035
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000019
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-1-(methylsulfonyl)piperidine-4-carboxamide
Homo sapiens
-
-
0.000011
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-1-propylpiperidine-4-carboxamide
Homo sapiens
-
-
0.0000049
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]piperidine-4-carboxamide
Homo sapiens
-
-
0.0000023
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]tetrahydro-2H-pyran-4-carboxamide
Homo sapiens
-
-
0.0000018
N-[(1R,2S)-2-(hydroxycarbamoyl)-4-oxocyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.0002
N-[(1R,2S)-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.00000063
N-[(1R,2S)-4,4-difluoro-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.000001
N-[(1R,2S)-4-aziridin-1-yl-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
IC50 below 0.000001 mM
0.0000046
N-[(1R,2S)-4-hydroxy-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.000001
N-[(1S,2R)-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.000029
N-[(4-methyl-2,5-dioxoimidazolidin-4-yl)methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.000018
N-[(5-benzyl-2,4,6-trioxohexahydropyrimidin-5-yl)methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
IC50: 0.000018 mM
0.000016
N-[(5-ethyl-2,4,6-trioxohexahydropyrimidin-5-yl)methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
; IC50: 0.000016 mM
0.0009
N-[(5R,6R)-2,4-dioxo-1,3-diazaspiro[4.4]non-6-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.000024
N-[(5R,6R)-2,4-dioxo-1,3-diazaspiro[4.5]dec-6-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.0055
N-[(5R,6S)-2,4-dioxo-1,3-diazaspiro[4.4]non-6-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.000025
N-[(5R,9R)-2,4-dioxo-1,3,7-triazaspiro[4.4]non-9-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.000024
N-[(5R,9R)-7-(2-methylpropanoyl)-2,4-dioxo-1,3,7-triazaspiro[4.4]non-9-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.0000023
N-[1-(1,1-dimethylprop-2-yn-1-yl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000021
N-[1-(2,2-dimethylpropanoyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000026
N-[1-(2,2-dimethylpropyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.000028
N-[1-(2,5-dioxoimidazolidin-4-yl)ethyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.0000026
N-[1-(2-fluoroethyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000019
N-[1-(3,3-dimethylbutanoyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000012
N-[1-(4,5-dihydro-1,3-thiazol-2-yl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000019
N-[1-acetyl-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000022
N-[1-ethyl-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000037
N-[1-tert-butyl-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000014
N-[1-[2-(ethylsulfonyl)ethyl]-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000077
N-[1-[2-(hydroxyamino)-2-oxoethyl]cyclohexyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.000097
N-[1-[2-(hydroxyamino)-2-oxoethyl]cyclohexyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
Sus scrofa
-
-
0.000111
N-[2-(2,2-dimethylpropanoyl)-6,8,10-trioxo-2,7,9-triazaspiro[4.5]dec-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
IC50: 0.000111 mM
0.000001
N-[2-(hydroxycarbamoyl)cyclobutyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.0000018
N-[2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
Sus scrofa
-
-
0.0000018
N-[2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
Homo sapiens
-
-
0.012
N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2-(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)acetamide
Sus scrofa
-
IC50: 0.012 mM
0.012
N-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-3-(5-methyl-2,4,6-trioxohexahydropyrimidin-5-yl)propanamide
Sus scrofa
-
-
0.0000012
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-(2-methylpropanoyl)piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000022
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-(3-methylbutanoyl)piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.000001
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-(methylsulfonyl)piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000031
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-methylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000019
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-phenylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000027
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-propanoylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.000002
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-propylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000012
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-[2-(methylsulfonyl)ethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.0000014
N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydro-2H-pyran-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.000097
N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydro-2H-pyran-4-yl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
Homo sapiens
-
-
0.000002
N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydrofuran-3-yl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
Sus scrofa
-
-
0.000098
N-[[(4R)-2,5-dioxoimidazolidin-4-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
-
0.0000086
N-[[1-(hydroxycarbamoyl)cyclohexyl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Homo sapiens
-
-
0.000019
N-[[5-(1-methylethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
; IC50: 0.000019 mM
0.000057
N-[[5-(1-methylpiperidin-4-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
; IC50: 0.000057 mM
0.000005
N-[[5-(4-acetylpiperazin-1-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
; IC50: 0.000005 mM
0.000014
N-[[5-(4-benzylpiperazin-1-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
IC50: 0.000014 mM
0.000062
N-[[5-(4-ethynylpiperazin-1-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
IC50: 0.000062 mM
0.000058
N-[[5-(4-methylpiperazin-1-yl)-2,4,6-trioxohexahydropyrimidin-5-yl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
Sus scrofa
-
; IC50: 0.000058 mM
0.000002
pyridin-4-ylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
-
0.000041
TAPI-2
Homo sapiens
-
mutant enzyme V353G
0.000043
TAPI-2
Homo sapiens
-
wild type enzyme
0.000001
tert-butyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
Sus scrofa
-
-
0.0000013
tert-butyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
Sus scrofa
-
-
0.000013
tert-butyl (5-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-2,4,6-trioxohexahydropyrimidin-5-yl)carbamate
Sus scrofa
-
; IC50: 0.000013 mM
0.000013
tert-butyl (5R,9R)-9-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-2,4-dioxo-1,3,7-triazaspiro[4.4]nonane-7-carboxylate
Sus scrofa
-
-
0.000128
tert-butyl 11-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1,3,5-trioxo-2,4,8-triazaspiro[5.5]undecane-8-carboxylate
Sus scrofa
-
-
0.0000013
tert-butyl 3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
Homo sapiens
-
-
0.0000019
tert-butyl 3-[4-[2-(hydroxyamino)-2-oxoethyl]-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidin-1-yl]propanoate
Homo sapiens
-
-
0.00016
tert-butyl 4-(5-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2,4,6-trioxohexahydropyrimidin-5-yl)piperazine-1-carboxylate
Sus scrofa
-
IC50: 0.00016 mM
0.000047
tert-butyl 4-(5-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-2,4,6-trioxohexahydropyrimidin-5-yl)piperidine-1-carboxylate
Sus scrofa
-
; IC50: 0.000047 mM
0.0000024
tert-butyl 4-(hydroxycarbamoyl)-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]piperidine-1-carboxylate
Homo sapiens
-
-
0.000001
tert-butyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
Homo sapiens
-
IC50 above 0.000001 mM
0.0000016
tert-butyl 4-([[4-(but-2-ynylamino)phenyl]sulfonyl]methyl)-4-[(hydroxyamino)-carbonyl]piperidine-1-carboxylate
Homo sapiens
-
-
0.000128
tert-butyl 4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-6,8,10-trioxo-2,7,9-triazaspiro[4.5]decane-2-carboxylate
Sus scrofa
-
IC50: 0.000128 mM
0.0000033
tert-butyl 4-[([4-[but-2-ynyl(methyl)amino]phenyl]sulfonyl)methyl]-4 [(hydroxyamino)carbonyl]piperidine-1-carboxylate
Homo sapiens
-
-
0.000008
TMI-1
Homo sapiens
-
-
0.00007
tumor necrosis factor-alpha-converting enzyme pro domain
Homo sapiens
-
inhibition of the tumor necrosis factor-alpha-converting enzyme by its isolated pro domain, IC50: 70 nM
-
0.000004
[N-hydroxy-1-(isopropylsulfonyl)-4-[(4-[(1-methylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)-methyl]piperidine-4-carboxamide
Homo sapiens
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.4
-
assay at
7.5
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
26
-
assay at
37
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
adipose tissue
Manually annotated by BRENDA team
-
atherosclerotic lesions of apolipoprotein E-deficient mice
Manually annotated by BRENDA team
-
metalloproteases ADAM-9, ADAM-15, and ADAM-17 are upregulated in advanced human atherosclerotic lesions in samples from carotid, abdominal aortic, and femoral territories compared to samples from internal thoracic artery free of atherosclerotic plaques. ADAM-9, ADAM-15, and ADAM-17-expressing cells colocalize with CD68-positive cells of monocytic origin in the atherosclerotic plaques
Manually annotated by BRENDA team
-
atherosclerotic plaque
Manually annotated by BRENDA team
-
peripheral blood T-cells
Manually annotated by BRENDA team
-
cellular suppression of TNF-alpha is measured using human whole blood (WBA) stimulated with lipopolysaccharide (LPS)
Manually annotated by BRENDA team
-
fetal brain
Manually annotated by BRENDA team
-
neocortex, cerebellum, pyramidal neurons of the cerebral cortex and granular cell layer neurons in the hippocampus
Manually annotated by BRENDA team
-
the expression of TACE is increased in intermittent and prolonged hyperoxia
Manually annotated by BRENDA team
-
TACE expression measured by immunohistochemical analysis is observed in 183 of 383 breast carcinomas. TACE expression is predominantly seen in tumors with high levels of released human epidermal growth factor-4 receptor intracellular domain (4ICD) and membranous human epidermal growth factor-4 receptor
Manually annotated by BRENDA team
-
metalloproteases ADAM-9, ADAM-15, and ADAM-17 are upregulated in advanced human atherosclerotic lesions in samples from carotid, aortic, and femoral territories compared to samples from internal thoracic artery free of atherosclerotic plaques. ADAM-9, ADAM-15, and ADAM-17-expressing cells colocalize with CD68-positive cells of monocytic origin in the atherosclerotic plaques, in the carotid territory, cells expressing the ADAMs codistribute also with smooth muscle cells
Manually annotated by BRENDA team
mutated sublines M1 and M2. M1 contains only one expressible TACE allele encoding an M435I point mutation in the catalytic center of the protease, and M2 cells produce two TACE variants with distinct point mutations in the catalytic domain (C22Y) and the cysteine-rich/disintegrin domain (C600Y); mutated sublines M1 and M2. M1 contains only one expressible TACE allele encoding an M435I point mutation in the catalytic center of the protease, and M2 cells produce two TACE variants with distinct point mutations in the catalytic domain (C22Y) and the cysteine-rich/disintegrin domain (C600Y); mutated sublines M1 and M2. M1 contains only one expressible TACE allele encoding an M435I point mutation in the catalytic center of the protease, and M2 cells produce two TACE variants with distinct point mutations in the catalytic domain (C22Y) and the cysteine-rich/disintegrin domain (C600Y)
Manually annotated by BRENDA team
Mus musculus AC2/G3
-
-
-
Manually annotated by BRENDA team
-
marrow stromal cell-brain microvascular endothelial cell contact coculture and indirect co-culture of marrow stromal cell and brain microvascular endothelial cell
Manually annotated by BRENDA team
-
salivary gland epithelial cell
Manually annotated by BRENDA team
-
non-neoplastic salivary gland epithelial cells
Manually annotated by BRENDA team
-
corneal epithelial cell
Manually annotated by BRENDA team
-
glandular epithelial cells
Manually annotated by BRENDA team
-
metalloproteases ADAM-9, ADAM-15, and ADAM-17 are upregulated in advanced human atherosclerotic lesions in samples from carotid, aortic, and femoral territories compared to samples from internal thoracic artery free of atherosclerotic plaques. ADAM-9, ADAM-15, and ADAM-17-expressing cells colocalize with CD68-positive cells of monocytic origin in the atherosclerotic plaques, in the femoral territory, cells expressing the ADAMs codistribute also with CD31-positive endothelial cells
Manually annotated by BRENDA team
-
dermal fibroblasts
Manually annotated by BRENDA team
-
embryonic fibroblast
Manually annotated by BRENDA team
Mus musculus AC2/G3, Mus musculus EC-4
-
-
-
Manually annotated by BRENDA team
-
TACE amounts in gingival crevicular fluid are higher in persons with chronic and aggressive periodontitis than in those with gingivitis or in healthy persons. TACE concentrations in gingival crevicular fluid are higher in persons with chronic and aggressive periodontitis than in those with gingivitis, although not significantly higher than in healthy persons. Persons with chronic periodontitis receiving immunosuppressive treatment exhibit over 10fold lower TACE levels than the other periodontitis groups. TACE is positively correlated with probing pocket depth, clinical attachment levels, and receptor activator of NF-kappaB ligand concentrations in gingival crevicular fluid
Manually annotated by BRENDA team
-
ADAM-17, TIMP-3 and fractalkine are constitutively expressed
Manually annotated by BRENDA team
-
within the hypothalamus, TACE is most abundantly expressed in astrocytes of the median eminence, specific changes in TACE activity are required for the normal timimg of puberty. TACE is a component of the neuron-to-glia signaling process used by glutamatergic neurons to control female sexual development
Manually annotated by BRENDA team
-
large cell anaplastic lymphoma cell line
Manually annotated by BRENDA team
-
CD30-positive Hodgkin’s lymphoma cell line
Manually annotated by BRENDA team
-
CD30-positive Hodgkin’s lymphoma cell line
Manually annotated by BRENDA team
-
expression of TACE in liver and spleen tissues after 70% partial hepatectomy is a time-dependent alteration, reaching a maximal level between 24 and 48 h and remaining elevated for more than 168 h
Manually annotated by BRENDA team
-
adenocarcinoma cells
Manually annotated by BRENDA team
Mus musculus C3H/HEN
-
-
-
Manually annotated by BRENDA team
-
TACE protein is localized to mononuclear cells (MNC), which infiltrate the liver from the spleen after hepatectomy. The kinetics of TACE expression is in accordance with the number of TACE-staining mononuclear cells and synchronizes with those of transforming growth factor-alpha. TACE-staining mononuclear cells partially overlapp with CD3+ T lymphocytes
Manually annotated by BRENDA team
-
skeletal muscle, smooth muscle cells
Manually annotated by BRENDA team
-
neuroblastoma cell line
Manually annotated by BRENDA team
-
sural nerve biopsies from Guillain-Barre syndrome patients. ADAM-17-expressing T cells can be localized primarily within the epi- and perineurium, whereas in control sections from patients with non-inflammatory neuropathies, no axpression can be depected. The enzyme may contribute to the pathogenesis of inflammatory demyelination of the peripheral nervous system
Manually annotated by BRENDA team
-
TACE expression measured by immunohistochemical analysis is observed in 39 of 217 ovarian carcinomas.TACE expression is predominantly seen in tumors with high levels of released human epidermal growth factor-4 receptor intracellular domain (4ICD) and membranous human epidermal growth factor-4 receptor
Manually annotated by BRENDA team
-
ADAM17/TACE mRNA is expressed in 3 of 10 normal pancreatic tissues, 6 of 8 samples from patients with chronic pancreatitis
Manually annotated by BRENDA team
-
ADAM17/TACE mRNA is expressed in 10 of 10 PDAC tissues. ADAM17/TACE mRNA expression is down-regulated in pancreatic cancer cells arrested in G2 -M phase. Critical involvement of ADAM17/TACE in the invasion behavior of pancreatic cancer cells
Manually annotated by BRENDA team
-
ADAM17/TACE mRNA is expressed in 10 of 10 PDAC tissues. ADAM17/TACE expression is a later event in progression of pancreatic intraepithelial neoplasia to pancreatic ductal adenocarcinoma
Manually annotated by BRENDA team
-
by analyzing villous samples representing different gestational ages, it is shown that TACE is continuously expressed in the placentas throughout gestation and that the levels of TACE are positively correlated with the levels of TGF-alpha, heparin-binding epidermal growth factor-like growth factor, and amphiregulin
Manually annotated by BRENDA team
-
Villous explant cultures or cytotrophoblastic cells are used. Preadministration of TACE inhibitor in villous explant cultures or transfection of cytotrophoblastic cells with TACE-specific small interference RNA decreases the shedding of heparin-binding epidermal growth factor-like growth factor and amphiregulin. Hypoxia (2% O2) causes an increase in the levels of TACE mRNA and protein in villous explants and primary cytotrophoblastic cells in vitro
Manually annotated by BRENDA team
-
TACE expression measured by immunohistochemical analysis is observed in 16 of 24 and 17 of 24 hormone-sensitive and hormone-insensitive prostate carcinomas. TACE expression is predominantly seen in tumors with high levels of released human epidermal growth factor-4 receptor intracellular domain (4ICD) and membranous human epidermal growth factor-4 receptor
Manually annotated by BRENDA team
-
CD30-negative acute lymphoblastic leukemia cell line
Manually annotated by BRENDA team
-
human salivary gland cells are used
Manually annotated by BRENDA team
-
non-neoplastic salivary gland epithelial cells
Manually annotated by BRENDA team
Mus musculus C3H/HEN
-
-
-
Manually annotated by BRENDA team
-
marrow stromal cell-brain microvascular endothelial cell contact coculture and indirect co-culture of marrow stromal cell and brain microvascular endothelial cell
Manually annotated by BRENDA team
-
primary cellular source of ADAM-17 in inflamed peripheral nervous system (experimental autoimmune neuritis). Not all T lymphocytes within the inflamed peripheral nervous system express ADAM-17. No ADAM-17 expressing cells are found in nerves from control animals
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
TACE is located in the cytoplasm of IFN gamma-treated cells
Manually annotated by BRENDA team
-
ADAM-17 is located diffusely within the cell cytoplasm, and treatment with TNF-alpha does not alter the level of expression or the cytoplasmic distribution of ADAM-17
Manually annotated by BRENDA team
Mus musculus C3H/HEN
-
cytoplasmic tail
-
Manually annotated by BRENDA team
Mus musculus EC-4
-
-
-
Manually annotated by BRENDA team
-
only the mature form of ADAM-17 associates with the cytoskeleton
Manually annotated by BRENDA team
-
cytosolic tail of TACE precedes TACE activation
Manually annotated by BRENDA team
-
disintegrin and protease regions
-
Manually annotated by BRENDA team
-
microsomal membrane, transmembrane domain
Manually annotated by BRENDA team
-
detergent-resistant membrane microdomain, i.e. regions of the membrane enriched in cholesterol and sphingolipids
Manually annotated by BRENDA team
Mus musculus C3H/HEN
-
-
-
Manually annotated by BRENDA team
Mus musculus EC-4
-
membrane-bound
-
Manually annotated by BRENDA team
additional information
-
ADAM17 localizes to bifurcations in invading sprouts
-
Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
UNIPROT
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
16060
-
mature enzyme, estimated from amino acid sequence
682629
17000
-
mature enzyme, SDS-PAGE
681016
26000
-
pro-enzyme, SDS-PAGE
681016
80000
-
migrates as a 80 kDa protein under non-reducing conditions, immunoprecipitation
638994
80000 - 100000
-
sucrose density gradient centrifugation
638984
85000
-
SDS-PAGE
638981
85000
-
glycerol gradient, gel filtration
638984
85000
-
proteolytically mature TACE, immunoblotting
639002
100000
-
100 kDa reduced form represents mature TACE lacking the prodomain, immunoprecipitation
638994
110000
-
pro TACE, immunoblotting
639002
120000
-
full length form of TACE migrates as a 120 kDa protein under reducing conditions, immunoprecipitation
638994
160000
-
identified with prodomain antibody in COS-7 membrane preparations
638994
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
-
-
phosphoprotein
-
in wounded cells, ADAM17 is phosphorylated at serine residues in an extracellular signal-regulated kinases ERK1/2-dependent manner
proteolytic modification
-
TACE cleaves proTNF-alpha in its active form
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
hanging drop vapour diffusion method with 15% polyethylene glycol 4000, 10% 2-propanol, 100 mM sodium citrate (pH 5.6)
-
molecular docking studies of inhibitor 2-(N-benzoxycarbonyl)aminoethyl-N-(4-hydroxyamino-4-oxo-2-(isopropylthio)butanoyl)-L-3-phenylalanyl-L-alanyl amide
-
TACE mutant V353G is crystallized with the respective inhibitors with a resolution of 1.7 A using the hanging drop method
-
X-ray crystal structure of the catalytic domain of TACE
-
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
extreme salt sensitivity
-
in absence of cell activators the enzyme is long-lived, with a half-life of more than 8h
-
surface-biotinylated TACE is stable in Jurkat cells with a half-life of at least 8h
-
TACE appears quite stable in untreated cells
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-70°C, TACE stored in small aliquots prevents self-degradation
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
Ni-NTA column chromatography and Superdex-75 gel filtration
-
recombinant enzyme
-
Sepharose column chromatography
-
Sephacryl HR300 column chromatography
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cDNA clones coding for various segments of the TACE cytotail
-
cDNA encoding TACE, full-length human TACE, inefficiently expressed in insect cells, baculovirus particles in Sf9 cell line from Spodoptera frugiperda
-
cDNA fragment coding for the prodomain of human TACE, expressed and purified from a baculoviral expression system
-
cloned with retroviral expression plasmids
-
expressed in Trichoplusia Ni cells (High-5 cells9)
-
expressed using the baculovirus expression system; recombinantly expressed
-
expression in MCF-7 cell
-
human embryonic kidney 293 transfectants overexpressing TACE
-
PCR used or quantification of TACE-mRNA in fresh tissue
-
recombinantly expressed human TACE in plasmid transfected chinese hamster ovary cells
-
the catalytic domain of recombinant human TNF-converting enzyme (residues 215-477 with two mutations S266A and N452Q) and a His-tagged tail is purified from the baculovirus/Hi5 cells expression system using affinity chromatography
-
expressed in CHO cells
-
expressed in the M1 cell line
-
bone marrow cultures infected with a retrovirus expressing murine TACE cDNA
-
cDNA encoding mouse TACE, transfection of COS-7 cells
-
expression in Escherichia coli
-
isolation of cDNA clones encoding TACE by PCR
-
mouse TACE complete cDNA cloned
-
reconstitution of TNF shedding in TACE-deficient cells by TACE cDNA transfection
-
TACE transfected CHO cells
-
transfection of TACE into TACE deficient cells
-
recombinant TACE expressed in insect cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
increased TACE mRNA expression in anti-Ro/SSA antibodies-treated salivary gland epithelial cells is restored to normal levels by Adalimumab treatment
-
ADAM-17 mRNA remains at control levels when treated with IL-1beta and IFN-gamma
-
metalloproteases ADAM-9, ADAM-15, and ADAM-17 are upregulated in advanced human atherosclerotic lesions in samples from carotid, aortic, and femoral territories compared to samples from internal thoracic artery free of atherosclerotic plaques
-
granulocyte-macrophage colony-stimulating factor GM-CSF and interleukin-4 in combination potently up-regulate tumor necrosis factor-alpha coverting enzyme TACE and activity in monocytes, causing ectodomain shedding of M-CSF receptor
-
infection of AGS cells with wild-type H pylori or an H pylori cagL-deficient isogenic mutant that also contains a wild-type version of cagL, P12DeltacagL/cagL, represses HKalpha promoter-Luc reporter activity and stimulates ADAM17 activity. Both responses are inhibited by point mutations in the nuclear factor-kappaB binding site of HKalpha or by infection with P12DeltacagL
-
dose-dependent increase of TACE mRNA expression in anti-Ro/SSA antibodies-treated salivary land epithelial cells, followed by internalization, pro-domain shedding and activation of TACE protein, suggesting that increased TACE activity is necessary for the release of TNF-alpha observed in anti-Ro/SSA antibodies-stimulated salivary gland epithelial cells. Adalimumab treatment brings TACE mRNA and surface TACE expression to levels similar to those observed in untreated salivary gland epithelial cells
-
transcription factor Sp1 binds to the ADAM17 promoter, and Sp1 regulates ADAM17 expression under hypoxia. Suppression of Sp1 decreases invasiveness and migration in U87 tumor cells
-
ADAM-17 mRNA increases, but not significantly upon treatment with TNF -alpha and TGF-beta1
-
expression of ADAM-17 is significantly increased in gallbladder carcinoma with high histological grade and pT stage compared with low histological grade and pT stage tumors and is not associated with patients’ gender, age, histological type, and resection margin involvement
-
Porphyromonas gingivalis challenge results in a concentration-dependent enhancement of TACE messenger RNA expression and protein release by Jurkat cells. TLCK treatment or heat treatment of Porphyromonas gingivalis culture supernatants decreases TACE release to control levels
-
in proliferating cells which are stably transfected to impose the anchorage of a chimeric B12-binding protein, transcobalamin-oleosin TO, to the intracellular membrane, a 2-fold increase of p75NTR-regulated intramembraneous proteolysis is observed that is associated with an increased expression of enzymes Adam-10 and Adam-17
-
ADAM17 expression is increased in chronically inflamed tissue
-
ADAM17 is expressed in most tissues and is up-regulated during inflammation and cancer
-
ADAM17 is upregulated in most tumor cells
-
transcript levels of TACE and TNF-alpha as well as TACE protein expression are significantly upregulated in direct, but not in indirect coculture condition of marrow stromal cell and brain microvascular endothelial cell
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
C225Y
overexpression of C225 and C600Y TACE by transient transfection largely compensates for maturation defects in the variants but fails to restore TNF-alpha and TGF-alpha release in the shedding-defective CHO cell lines and fibroblasts derived from TACE-null mouse embryos; overexpression of C225 and C600Y TACE by transient transfection largely compensates for maturation defects in the variants but fails to restore TNF-alpha and TGF-alpha release in the shedding-defective CHO cell lines and fibroblasts derived from TACE-null mouse embryos; overexpression of C225 and C600Y TACE by transient transfection largely compensates for maturation defects in the variants but fails to restore TNF-alpha and TGF-alpha release in the shedding-defective CHO cell lines and fibroblasts derived from TACE-null mouse embryos
S266A/N452Q
-
the catalytic domain of recombinant human TNF-converting enzyme (residues 215-477) with two mutations S266A and N452Q is used
V353G
-
highly resistant to autoproteolysis, shows similar kinetic properties to wild type TACE
V353G
-
TACE mutant V353G is crystallized with the respective inhibitors with a resolution of 1.7 A using the hanging drop method
V353S
-
highly resistant to autoproteolysis
M435I
-
mutation inactivates ectodomain shedding activity
M435L
-
mutation inactivates ectodomain shedding activity
M435S
-
mutation inactivates ectodomain shedding activity
T735A
-
the mutant has a basal TGF-alpha shedding activity lower than that of wild type cells and shedding is not induced by p38 MAPK
C600Y
overexpression of C225 and C600Y TACE by transient transfection largely compensates for maturation defects in the variants but fails to restore TNF-alpha and TGF-alpha release in the shedding-defective CHO cell lines and fibroblasts derived from TACE-null mouse embryos; overexpression of C225 and C600Y TACE by transient transfection largely compensates for maturation defects in the variants but fails to restore TNF-alpha and TGF-alpha release in the shedding-defective CHO cell lines and fibroblasts derived from TACE-null mouse embryos; overexpression of C225 and C600Y TACE by transient transfection largely compensates for maturation defects in the variants but fails to restore TNF-alpha and TGF-alpha release in the shedding-defective CHO cell lines and fibroblasts derived from TACE-null mouse embryos
additional information
-
study on the association of ADAM-17 single nucleotide polymorphisms with insulin-resistance phenotypes and obesity risk. G allele carriers at the ADAM17_m1254A > G polymorphism exhibit significantly higher risk of obesity, are shorter, have higher insulin, and lower HDL-C concentrations than AA subjects. For the ADAM17_i33708A > G single nucleotide polymorphism, homozygotes for the A allele display higher risk of obesity, are heavier, have higher body-mass-index and higher waist measurements than GG subjects. There is a significant gene-diet interaction, in which the deleterious association of the i33708A allele with obesity is observed in subjects with low intakes from n-6 polyunsaturated fatty acids, whereas no differences in obesity risk are seen among subjects with high n-6 polyunsaturated fatty acid intake
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
-
isolation of TACE facilitates the development of therapeutically useful inhibitors of TNF-alpha release
medicine
-
implicated in the pathogenesis of dilated cardiomyopathy
medicine
-
TNF-alpha thought to be a selective anti-tumor agent and a contributor to cachexia in cancer patients, clinical trials for cancer
medicine
-
tumor necrosis factor alpha converting enzyme is involved in regulated alpha-secretase cleavage of the Alzheimer amyloid protein precursor, activating TACE by pharmacological manipulation might prove beneficial in Alzheimer's disease
medicine
-
TACE plays a role in the pathogenesis of endometriosis, a benign gynecologic disorder
medicine
-
TACE has implications in the pathogenesis of myocarditis and may have influence on advanced cardiac dysfunction in myocarditis
medicine
-
over-expression of TNF-alpha has been implicated in diseases such as rheumatoid arthritis, Crohn's disease, septic shock, AIDS, insulin resistance, cachexia and cancer
medicine
-
TACE as target for drug discovery, potential therapeutic target in the areas of arthritis, cancer, diabetes and HIV cachexia
medicine
-
putative cellular targets of a therapeutic strategy in neurodegenerative prion diseases
medicine
-
therapeutic potential of TACE inhibitors benefit in treating autoimmune diseases like Crohn's disease or rheumatoid arthritis
medicine