Protein Variants | Comment | Organism |
---|---|---|
S295F | affects minimally catalytic activity, significantly reduces the potency of inhibitors derived from 7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
((2-bromo-4-((((2E)-3-phenylprop-2-en-1-yl)sulfanyl)methyl)phenyl)carbonyl)phosphonate | 50% inhibition at 810 nM for wild-type, at 1290 nM for mutant S295F | Homo sapiens | |
((2-bromo-4-(((4-chlorobenzyl)thio)methyl)phenyl)(difluoro)methyl)phosphonate | 50% inhibition at 285 nM for wild-type, at 1644 nM for mutant S295F | Homo sapiens | |
((2-phenyl-2-(phenylcarbonyl)propane-1,3-diyl)bis(benzene-4,1-diyl(difluoromethanediyl)))bis(phosphonate) | 50% inhibition at 82 nM for wild-type, at 399 nM for mutant S295F | Homo sapiens | |
((4-((((3'-(acetylsulfamoyl)biphenyl-4-yl)methyl)sulfanyl)methyl)-2-bromophenyl)(difluoro)methyl)phosphonate | 50% inhibition at 2.2 nM for wild-type, at 11 nM for mutant S295F | Homo sapiens | |
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonate | 50% inhibition at 47 nM for wild-type, at 260 nM for mutant S295F | Homo sapiens | |
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(fluoro)methyl)phosphonate | 50% inhibition at 570 nM for wild-type, at 830 nM for mutant S295F | Homo sapiens | |
(4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)benzyl)phosphonate | 50% inhibition at 3260 nM for wild-type, at 5030 nM for mutant S295F | Homo sapiens | |
7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile | 50% inhibition at 230 nM for wild-type, at 886 nM for mutant S295F | Homo sapiens | |
BzN-EJJ-amide | 50% inhibition at 3.7 nM for wild-type, at 18 nM for mutant S295F | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.38 | - |
4-nitrophenyl phosphate | wild-type, pH 6.3 | Homo sapiens | |
1.1 | - |
4-nitrophenyl phosphate | mutant S295F, pH 6.3 | Homo sapiens | |
5.2 | - |
difluoromethylumbelliferyl phosphate | wild-type, pH 6.3 | Homo sapiens | |
11.1 | - |
difluoromethylumbelliferyl phosphate | mutant S295F, pH 6.3 | Homo sapiens | |
15 | - |
3,6-fluorescein diphosphate | mutant S295F, pH 6.3 | Homo sapiens | |
19 | - |
3,6-fluorescein diphosphate | wild-type, pH 6.3 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P18031 | isoform PTP1B, amino acids 1-400, catalytic domain plus 80-amino acid C-terminal tail | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
3,6-fluorescein diphosphate + H2O | - |
Homo sapiens | ? + phosphate | - |
? | |
4-nitrophenyl phosphate + H2O | - |
Homo sapiens | 4-nitrophenol + phosphate | - |
? | |
difluoromethylumbelliferyl phosphate + H2O | - |
Homo sapiens | difluoromethylumbelliferone + phosphate | - |
? |