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Literature summary for 3.1.3.48 extracted from

  • Ge, L.; Li, K.S.; Li, M.M.; Xiao, P.; Hou, X.B.; Chen, X.; Liu, H.D.; Lin, A.; Yu, X.; Ren, G.J.; Fang, H.; Sun, J.P.
    Identification of a benzo imidazole thiazole derivative as the specific irreversible inhibitor of protein tyrosine phosphatase (2016), Bioorg. Med. Chem. Lett., 26, 4795-4798 .
    View publication on PubMed
Search for more literature for 3.1.3.48

Inhibitors

Inhibitors Comment Organism Structure
(2Z)-2-([5-[4-(1H-tetrazol-1-yl)phenyl]furan-2-yl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
 Homo sapiens
(2Z)-2-[[5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
 Homo sapiens
3-([2-chloro-6-methoxy-4-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]phenoxy]methyl)benzoic acid
-
 Homo sapiens
3-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]benzoic acid
-
 Homo sapiens
3-[2,5-dimethyl-3-[(3-oxo-2,3-dihydro[1,3]thiazolo[3,2-a]benzimidazol-2-yl)methyl]-1H-pyrrol-1-yl]benzoic acid irreversible inhibition, detailed kinetic analysis of the interaction between E4 and the catalytic domain of enzyme STEP, overview. kinact is 0.068/s Homo sapiens
3-[3-(2,4-dichlorophenyl)propanoyl]-2-hydroxycyclohepta-2,4,6-trien-1-one
-
 Homo sapiens
4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-2-hydroxybenzoic acid
-
 Homo sapiens
4-[2-[(5-chloro-1,3-benzoxazol-2-yl)sulfanyl]acetamido]benzoic acid
-
 Homo sapiens
6-oxo-6H-cyclohepta[b]furan-5,7-dicarboxylic acid
-
 Homo sapiens
additional information identification of a benzo imidazole thiazole derivative as the specific irreversible inhibitor of protein tyrosine phosphatase, overview Homo sapiens
[2-bromo-4-[(E)-(7,8-dimethyl-3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]-6-ethoxyphenoxy]acetic acid irreversible inhibition Homo sapiens
[[1-(4-chlorophenyl)-2-methyl-1H-indol-5-yl]oxy]acetic acid
-
 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 P54829
-
-

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 tyrosine phosphatase
-
 Homo sapiens
PTP
-
 Homo sapiens
PTPN5
-
 Homo sapiens
selective striatal enriched protein phosphatase
-
 Homo sapiens
STEP
-
 Homo sapiens
tyrosine-protein phosphatase non-receptor type 5 UniProt Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0216
-
 3-[2,5-dimethyl-3-[(3-oxo-2,3-dihydro[1,3]thiazolo[3,2-a]benzimidazol-2-yl)methyl]-1H-pyrrol-1-yl]benzoic acid pH 7.0, 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0083
-
 pH 7.0, 25°C Homo sapiens 3-[2,5-dimethyl-3-[(3-oxo-2,3-dihydro[1,3]thiazolo[3,2-a]benzimidazol-2-yl)methyl]-1H-pyrrol-1-yl]benzoic acid
0.0158
-
 pH 7.0, 25°C Homo sapiens [2-bromo-4-[(E)-(7,8-dimethyl-3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]-6-ethoxyphenoxy]acetic acid
0.0329
-
 pH 7.0, 25°C Homo sapiens 3-[3-(2,4-dichlorophenyl)propanoyl]-2-hydroxycyclohepta-2,4,6-trien-1-one
0.0632
-
 pH 7.0, 25°C Homo sapiens (2Z)-2-([5-[4-(1H-tetrazol-1-yl)phenyl]furan-2-yl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
0.2732
-
 pH 7.0, 25°C Homo sapiens 4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-2-hydroxybenzoic acid
0.3
-
 above, pH 7.0, 25°C Homo sapiens (2Z)-2-[[5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
0.3
-
 above, pH 7.0, 25°C Homo sapiens 3-([2-chloro-6-methoxy-4-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]phenoxy]methyl)benzoic acid
0.3
-
 above, pH 7.0, 25°C Homo sapiens 3-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]benzoic acid
0.3
-
 above, pH 7.0, 25°C Homo sapiens 4-[2-[(5-chloro-1,3-benzoxazol-2-yl)sulfanyl]acetamido]benzoic acid
0.3
-
 above, pH 7.0, 25°C Homo sapiens 6-oxo-6H-cyclohepta[b]furan-5,7-dicarboxylic acid
0.3
-
 above, pH 7.0, 25°C Homo sapiens [[1-(4-chlorophenyl)-2-methyl-1H-indol-5-yl]oxy]acetic acid

General Information

General Information Comment Organism
evolution protein tyrosine phosphatases share a common catalytic mechanism that utilizes a highly reactive nucleophilic Cys residue Homo sapiens