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Literature summary for 3.1.3.48 extracted from

  • Zhang, L.; Ge, Y.; Song, H.M.; Wang, Q.M.; Zhou, C.H.
    Design, synthesis of novel azolyl flavonoids and their protein tyrosine Phosphatase-1B inhibitory activities (2018), Bioorg. Chem., 80, 195-203 .
    View publication on PubMed
Search for more literature for 3.1.3.48

Inhibitors

Inhibitors Comment Organism Structure
7-(2-((1H-imidazol-2-yl)thio)ethoxy)-2-phenyl-4H-chromen-4-one
-
 Homo sapiens
7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one the inhibitor is significantly selective for enzyme protein tyrosine phosphatase 1B (PTP1B) versus other phosphatases, i.e. T-cell protein tyrosine phosphatase (TCPTP), megakaryocyte protein tyrosine phosphatase (PTP-MEG2), and src homology phosphatase 2 Homo sapiens
7-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
 Homo sapiens
7-(2-(4-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
 Homo sapiens
7-(2-(5-methyl-1H-tetrazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
 Homo sapiens
7-(2-bromoethoxy)-2-phenyl-4H-1-benzopyran-4-one
-
 Homo sapiens
7-(3-(4-nitro-1H-imidazol-1-yl)propoxy)-2-phenyl-4H-chromen-4-one
-
 Homo sapiens
7-(4-((1H-imidazol-2-yl)thio)butoxy)-2-phenyl-4H-chromen-4-one
-
 Homo sapiens
7-(4-(1H-1,2,4-triazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
 Homo sapiens
7-(4-(2-methyl-5-nitro-1H-imidazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
 Homo sapiens
7-(4-(5-methyl-1H-tetrazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
 Homo sapiens
7-(4-bromobutoxy)-2-phenyl-4H-1-benzopyran-4-one
-
 Homo sapiens
additional information design and synthesis of azolyl flavonoids as enzyme inhibitors of protein tyrosine phosphatase 1B, molecular modeling and dynamics studies, using the crystal structure of PTP1B (PDB ID 1G1H) reveals the selectivity of triazolyl flavonoid inhibitor 7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one for PTP1B over the closely related T-cell protein tyrosine phosphatase (TCPTP), detailed overview. The inhibitory effects and kinetics analysis of the azoyl flavonoids against PTPs are measured, using 4-nitrophenol phosphate as the substrate Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
[a protein]-tyrosine phosphate + H2O Homo sapiens
-
 [a protein]-tyrosine + phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P18031
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl phosphate + H2O
-
 Homo sapiens 4-nitrophenol + phosphate
-
 ?
[a protein]-tyrosine phosphate + H2O
-
 Homo sapiens [a protein]-tyrosine + phosphate
-
 ?

Synonyms

Synonyms Comment Organism
Protein phosphatase 1B
-
 Homo sapiens
protein tyrosine phosphatase
-
 Homo sapiens
PTP1B
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0016
-
 pH 7.2, 37°C Homo sapiens 7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
0.003
-
 pH 7.2, 37°C Homo sapiens 7-(2-((1H-imidazol-2-yl)thio)ethoxy)-2-phenyl-4H-chromen-4-one
0.0036
-
 pH 7.2, 37°C Homo sapiens 7-(4-(1H-1,2,4-triazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
0.0039
-
 pH 7.2, 37°C Homo sapiens 7-(4-((1H-imidazol-2-yl)thio)butoxy)-2-phenyl-4H-chromen-4-one
0.004
-
 pH 7.2, 37°C Homo sapiens 7-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
0.005
-
 pH 7.2, 37°C Homo sapiens 7-(2-(4-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
0.0069
-
 pH 7.2, 37°C Homo sapiens 7-(4-(2-methyl-5-nitro-1H-imidazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
0.007
-
 pH 7.2, 37°C Homo sapiens 7-(3-(4-nitro-1H-imidazol-1-yl)propoxy)-2-phenyl-4H-chromen-4-one
0.0079
-
 pH 7.2, 37°C Homo sapiens 7-(2-(5-methyl-1H-tetrazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
0.0151
-
 pH 7.2, 37°C Homo sapiens 7-(4-(5-methyl-1H-tetrazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one