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Literature summary extracted from

  • Zhi, Y.; Gao, L.X.; Jin, Y.; Tang, C.L.; Li, J.Y.; Li, J.; Long, Y.Q.
    4-Quinolone-3-carboxylic acids as cell-permeable inhibitors of protein tyrosine phosphatase 1B (2014), Bioorg. Med. Chem., 22, 3670-3683.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.3.48 (Z)-1-(3-(3-carboxy-3-hydroxyacryloyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of 2.4 mg/ml Homo sapiens
3.1.3.48 (Z)-1-(3-(4-ethoxy-3-hydroxy-4-oxobut-2-enoyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of 3.1 mg/ml Homo sapiens
3.1.3.48 1,1'-(piperazine-1,4-diyl)bis(4-(3-(dibenzylamino)phenyl)butane-1,2,4-trione)
-
 Homo sapiens
3.1.3.48 1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 15.1% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 36.2% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 1-(4-hydroxy-3-(methoxycarbonyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of 8.1 mg/ml Homo sapiens
3.1.3.48 1-benzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 15.1% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 1-benzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 3.1% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 0.7% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 0.8% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 3.5% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 1-cyclopropyl-N-(4-fluorobenzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide 3.3% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 4-(3-(dibenzylamino)phenyl)-2,4-dioxobutanoic acid
-
 Homo sapiens
3.1.3.48 4-fluorobenzyl-1-cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylate 73% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 6-(4-(3-(3-(benzyloxy)-2-(methoxycarbonyl)phenoxy)propyl)piperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of 45.2 mg/ml Homo sapiens
3.1.3.48 6-(4-benzylpiperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 62.3% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 6-amino-1-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 12.4% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 6-benzyl-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 87.5% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 6-iodo-1-(4-methoxy-3-(methoxycarbonyl)benzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of more than 20 mg/ml Homo sapiens
3.1.3.48 benzyl 1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylate 0.1% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 benzyl 1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylate 80.5% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 71.1% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 methyl 2-(3-(1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate IC50 of 6.5 mg/ml Homo sapiens
3.1.3.48 methyl 2-(3-(1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate IC50 of 9.4 mg/ml Homo sapiens
3.1.3.48 methyl-5-((3-(benzylcarbamoyl)-6-iodo-4-oxoquinolin-1(4H)-yl)methyl)-2-methoxybenzoate IC50 of more than 20 mg/ml Homo sapiens
3.1.3.48 N,1-dibenzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide 41.4% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 N,1-dibenzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide 61.8% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 N-benzyl-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide 0.2% inhibition at 0.02 mg/ml; 7.4% inhibition at 0.02 mg/ml Homo sapiens
3.1.3.48 N-benzyl-1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide 6.1% inhibition at 0.02 mg/ml Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
3.1.3.48 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.3.48 4-nitrophenyl phosphate + H2O
-
 Homo sapiens 4-nitrophenol + phosphate
-
 ?
3.1.3.48 [a protein]-tyrosine phosphate + H2O
-
 Homo sapiens [a protein]-tyrosine + phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.3.48 protein tyrosine phosphatase 1B
-
 Homo sapiens
3.1.3.48 PTP1B
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.3.48 0.0028
-
 in 50 mM MOPS, pH 6.5, at 30°C Homo sapiens 1,1'-(piperazine-1,4-diyl)bis(4-(3-(dibenzylamino)phenyl)butane-1,2,4-trione)
3.1.3.48 0.02
-
 in 50 mM MOPS, pH 6.5, at 30°C Homo sapiens 4-(3-(dibenzylamino)phenyl)-2,4-dioxobutanoic acid