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Literature summary extracted from

  • Kloeck, C.; Jin, X.; Choi, K.; Khosla, C.; Madrid, P.B.; Spencer, A.; Raimundo, B.C.; Boardman, P.; Lanza, G.; Griffin, J.H.
    Acylideneoxoindoles: a new class of reversible inhibitors of human transglutaminase 2 (2011), Bioorg. Med. Chem. Lett., 21, 2692-2696.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.2.13 (3E)-1-benzyl-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-3-(2-oxopropylidene)-6-(trifluoromethoxy)-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-3-[2-(3-aminophenyl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-3-[2-(4-aminophenyl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-3-[2-(5-bromopyridin-3-yl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-1-(2-methylpropyl)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-1-(cyclohexylmethyl)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-1-methyl-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-(2-oxo-2-phenylethylidene)-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-(2-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-(3-chlorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-(3-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-(4-chlorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-(4-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-(6-methoxypyridin-3-yl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-oxo-2-(pyridin-2-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(2-phenylethyl)-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(3-phenylpropyl)-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(propan-2-yl)-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-phenyl-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-4-chloro-3-[2-oxo-2-(pyridin-4-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-5-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-5-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-5-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-5-methyl-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-5-nitro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-6-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-6-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-6-fluoro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-7-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-7-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 (3E)-7-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
Homo sapiens
2.3.2.13 1,1'-methanediylbis(1H-indole-2,3-dione)
-
Homo sapiens
2.3.2.13 1,1'-[(2,5-dimethylbenzene-1,4-diyl)dimethanediyl]bis(1H-indole-2,3-dione)
-
Homo sapiens
2.3.2.13 1,1'-[(4,6-dimethylbenzene-1,3-diyl)dimethanediyl]bis(1H-indole-2,3-dione)
-
Homo sapiens
2.3.2.13 2-[(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]-N,N-dimethylacetamide
-
Homo sapiens
2.3.2.13 5,5'-methanediylbis(1H-indole-2,3-dione)
-
Homo sapiens
2.3.2.13 5,5'-oxybis(1H-indole-2,3-dione)
-
Homo sapiens
2.3.2.13 6,6'-oxybis(1H-indole-2,3-dione)
-
Homo sapiens
2.3.2.13 ethyl [(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]acetate
-
Homo sapiens
2.3.2.13 indirubin
-
Homo sapiens
2.3.2.13 isatin weak, reversible inhibitor Homo sapiens
2.3.2.13 isoindigotin
-
Homo sapiens
2.3.2.13 methyl 3-([(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]methyl)benzoate
-
Homo sapiens
2.3.2.13 methyl 4-([(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]methyl)benzoate
-
Homo sapiens
2.3.2.13 methyl ketone
-
Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.3.2.13 Ca2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.2.13 Cbz-L-Gln-Gly + alkylamine Homo sapiens
-
?
-
?

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.2.13 Cbz-L-Gln-Gly + alkylamine
-
Homo sapiens ?
-
?

Synonyms

EC Number Synonyms Comment Organism
2.3.2.13 TG2
-
Homo sapiens
2.3.2.13 transglutaminase 2
-
Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.2.13 0.0004
-
(3E)-4-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.00041
-
(3E)-1-benzyl-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.0007
-
(3E)-4-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.0009
-
(3E)-5-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.003
-
5,5'-oxybis(1H-indole-2,3-dione) pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.003
-
(3E)-5-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.0033
-
(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.004
-
(3E)-4-chloro-1-methyl-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.0053
-
(3E)-6-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.0054
-
(3E)-6-fluoro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.01
-
methyl ketone pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.01
-
1,1'-methanediylbis(1H-indole-2,3-dione) pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.011
-
1,1'-[(4,6-dimethylbenzene-1,3-diyl)dimethanediyl]bis(1H-indole-2,3-dione) pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.012
-
(3E)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.015
-
5,5'-methanediylbis(1H-indole-2,3-dione) pH and temperature not specified in the publication Homo sapiens
2.3.2.13 0.041
-
isoindigotin pH and temperature not specified in the publication Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.2.13 0.0007
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-(3-chlorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0008
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-(4-chlorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0008
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-phenyl-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0009
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0009
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0009
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-(2-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.001
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-(3-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.001
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-1-(2-methylpropyl)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0011
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-oxo-2-(pyridin-2-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0011
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-(4-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0011
-
pH and temperature not specified in the publication Homo sapiens (3E)-3-[2-(4-aminophenyl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0011
-
pH and temperature not specified in the publication Homo sapiens methyl 3-([(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]methyl)benzoate
2.3.2.13 0.0012
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-oxo-2-(pyridin-4-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0012
-
pH and temperature not specified in the publication Homo sapiens methyl 4-([(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]methyl)benzoate
2.3.2.13 0.0013
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(3-phenylpropyl)-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0014
-
pH and temperature not specified in the publication Homo sapiens (3E)-3-[2-(5-bromopyridin-3-yl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0014
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-(6-methoxypyridin-3-yl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0014
-
pH and temperature not specified in the publication Homo sapiens (3E)-3-[2-(3-aminophenyl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0014
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(propan-2-yl)-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0015
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0015
-
pH and temperature not specified in the publication Homo sapiens (3E)-1-benzyl-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0015
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(2-phenylethyl)-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0015
-
pH and temperature not specified in the publication Homo sapiens (3E)-6-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0018
-
pH and temperature not specified in the publication Homo sapiens ethyl [(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]acetate
2.3.2.13 0.0021
-
pH and temperature not specified in the publication Homo sapiens (3E)-6-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0021
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-1-(cyclohexylmethyl)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0028
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-3-(2-oxo-2-phenylethylidene)-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0029
-
pH and temperature not specified in the publication Homo sapiens (3E)-7-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0036
-
pH and temperature not specified in the publication Homo sapiens (3E)-3-(2-oxopropylidene)-6-(trifluoromethoxy)-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.004
-
pH and temperature not specified in the publication Homo sapiens (3E)-4-chloro-1-methyl-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0043
-
pH and temperature not specified in the publication Homo sapiens (3E)-5-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0047
-
pH and temperature not specified in the publication Homo sapiens (3E)-7-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0048
-
pH and temperature not specified in the publication Homo sapiens (3E)-5-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0055
-
pH and temperature not specified in the publication Homo sapiens 2-[(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]-N,N-dimethylacetamide
2.3.2.13 0.006
-
pH and temperature not specified in the publication Homo sapiens (3E)-5-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0063
-
pH and temperature not specified in the publication Homo sapiens (3E)-5-methyl-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0073
-
pH and temperature not specified in the publication Homo sapiens (3E)-7-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.0079
-
pH and temperature not specified in the publication Homo sapiens (3E)-5-nitro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.008
-
pH and temperature not specified in the publication Homo sapiens isoindigotin
2.3.2.13 0.011
-
pH and temperature not specified in the publication Homo sapiens methyl ketone
2.3.2.13 0.011
-
pH and temperature not specified in the publication Homo sapiens (3E)-6-fluoro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.018
-
pH and temperature not specified in the publication Homo sapiens 1,1'-methanediylbis(1H-indole-2,3-dione)
2.3.2.13 0.022
-
pH and temperature not specified in the publication Homo sapiens (3E)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
2.3.2.13 0.025
-
pH and temperature not specified in the publication Homo sapiens 5,5'-oxybis(1H-indole-2,3-dione)
2.3.2.13 0.03
-
pH and temperature not specified in the publication Homo sapiens 5,5'-methanediylbis(1H-indole-2,3-dione)
2.3.2.13 0.03 0.04 pH and temperature not specified in the publication Homo sapiens 6,6'-oxybis(1H-indole-2,3-dione)
2.3.2.13 0.04
-
pH and temperature not specified in the publication Homo sapiens 1,1'-[(4,6-dimethylbenzene-1,3-diyl)dimethanediyl]bis(1H-indole-2,3-dione)
2.3.2.13 0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens indirubin
2.3.2.13 0.25
-
IC50 above 0.25 mM, pH and temperature not specified in the publication Homo sapiens 1,1'-[(2,5-dimethylbenzene-1,4-diyl)dimethanediyl]bis(1H-indole-2,3-dione)