Application | Comment | Organism |
---|---|---|
medicine | design and development for potent and selective inhibitors of ADAMTS-4 and ADAMTS-5, which will be required for chronic osteoarthritis therapy | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expressed in Sf9 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide | - |
Homo sapiens | |
(3R)-N2-(cyclopropylmethyl)-N1-hydroxy-3-(3-hydroxybenzyl)-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide | - |
Homo sapiens | |
marimastat | - |
Homo sapiens | |
additional information | design and development for potent and selective inhibitors of ADAMTS-4 and ADAMTS-5 | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
aggrecan + H2O | Homo sapiens | ADAMTS-4 and ADAMTS-5 are the proteases responsible for the endogenous aggrecanase activity observed in IL-1beta stimulated bovine cartilage | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
aggrecan + H2O | ADAMTS-4 and ADAMTS-5 are the proteases responsible for the endogenous aggrecanase activity observed in IL-1beta stimulated bovine cartilage | Homo sapiens | ? | - |
? | |
aggrecan + H2O | cleavage at the Glu373-Ala374 site of aggrecan is measured | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
ADAMTS-4 | - |
Homo sapiens |
aggrecanase-1 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000003 | - |
pH 7.5, 37°C | Homo sapiens | (3R)-N2-(cyclopropylmethyl)-N1-hydroxy-3-(3-hydroxybenzyl)-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide | |
0.000065 | - |
pH 7.5, 37°C | Homo sapiens | (2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide | |
0.000079 | - |
pH 7.5, 37°C | Homo sapiens | marimastat |