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Literature summary for 3.1.3.48 extracted from

  • Shim, Y.S.; Kim, K.C.; Lee, K.A.; Shrestha, S.; Lee, K.H.; Kim, C.K.; Cho, H.
    Formylchromone derivatives as irreversible and selective inhibitors of human protein tyrosine phosphatase 1B. Kinetic and modeling studies (2005), Bioorg. Med. Chem., 13, 1325-1332.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.073 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
4-oxo-6,8-diphenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.0033 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM Homo sapiens
4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde 50% inhibition at 0.0062 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
4-oxo-6-phenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.014 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
4-oxo-8-phenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6,8-dibenzyl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.013 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-((2-benzyl-1-benzothien-3-yl)methyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0032 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM Homo sapiens
6-((E)-1,2-diphenylvinyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0097 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-(1-benzothien-2-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.006 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-(1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0077 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-(1-benzothien-3-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.06 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0025 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.57 mM Homo sapiens
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM Homo sapiens
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.001 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.52 mM Homo sapiens
6-(9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0071 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-benzyl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.036 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-biphenyl-4-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0043 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-biphenyl-4-yl-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.002 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM Homo sapiens
6-bromo-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.020 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0076 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
8-benzyl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.018 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
8-bromo-4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde 50% inhibition at 0.0078 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
8-bromo-6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
8-bromo-6-(2-bromo-1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0082 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
8-bromo-6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.010 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens
8-bromo-6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P18031
-
-

Synonyms

Synonyms Comment Organism
PTP1B
-
Homo sapiens