Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid | - |
Homo sapiens | |
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid | - |
Homo sapiens | |
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenoxyphenyl)methylidene]thiazolidin-3-yl) methyl)benzoic acid | - |
Homo sapiens | |
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid | - |
Homo sapiens | |
4-(((5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid | - |
Homo sapiens | |
4-(((5Z)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid | - |
Homo sapiens | |
4-(((5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid | - |
Homo sapiens | |
4-(((5Z)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid | - |
Homo sapiens | |
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(5Z)-2,4-dioxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([3-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([4-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid | - |
Homo sapiens | |
4-([(5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-([(5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(5Z)-2,4-dioxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(5Z)-2,4-dioxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
4-[[(5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid | - |
Homo sapiens | |
additional information | 4-[(5-arylidene-4-oxothiazolidin-3-yl)methyl]benzoic acid derivatives determined as active potent allosteric inhibitors of protein tyrosine phosphatase 1B, in silico studies and in vitro evaluation as insulinomimetic and anti-inflammatory agents, binding modes and inhibitory mechanism, docking studies, detailed overview | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
intracellular | - |
Homo sapiens | 5622 | - |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P18031 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
C2C12 cell | - |
Homo sapiens | - |
Hep-G2 cell | - |
Homo sapiens | - |
myotube | - |
Homo sapiens | - |
Synonyms | Comment | Organism |
---|---|---|
protein tyrosine phosphatase 1B | - |
Homo sapiens |
PTP1B | - |
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 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0011 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(2E,5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.0011 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.0011 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.0014 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid | |
0.0015 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([4-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid | |
0.0015 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(2E,5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.0016 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.0019 | - |
pH 7.0, 37°C | Homo sapiens | 4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid | |
0.0019 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid | |
0.0019 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(2E,5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.0022 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | |
0.0025 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | |
0.0026 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(5Z)-2,4-dioxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.0028 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | |
0.003 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid | |
0.0035 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid | |
0.0038 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.0042 | - |
pH 7.0, 37°C | Homo sapiens | 4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid | |
0.0046 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(2E,5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.005 | - |
pH 7.0, 37°C | Homo sapiens | 4-(((5Z)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid | |
0.0051 | - |
pH 7.0, 37°C | Homo sapiens | 4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenoxyphenyl)methylidene]thiazolidin-3-yl) methyl)benzoic acid | |
0.0051 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid | |
0.0056 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid | |
0.0057 | - |
pH 7.0, 37°C | Homo sapiens | 4-(((5Z)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid | |
0.0071 | - |
pH 7.0, 37°C | Homo sapiens | 4-(((5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid | |
0.0095 | - |
pH 7.0, 37°C | Homo sapiens | 4-[[(5Z)-2,4-dioxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid | |
0.01 | - |
pH 7.0, 37°C | Homo sapiens | 4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid | |
0.0104 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | |
0.0106 | - |
pH 7.0, 37°C | Homo sapiens | 4-(((5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid | |
0.0109 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid | |
0.0145 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([3-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid | |
0.018 | - |
pH 7.0, 37°C | Homo sapiens | 4-([(5Z)-2,4-dioxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid |
General Information | Comment | Organism |
---|---|---|
evolution | protein tyrosine phosphatase 1B (PTP1B) belongs to class I of the cysteine-based protein tyrosine phosphatases | Homo sapiens |