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Literature summary for 1.14.11.65 extracted from

  • Upadhyay, A.K.; Rotili, D.; Han, J.W.; Hu, R.; Chang, Y.; Labella, D.; Zhang, X.; Yoon, Y.S.; Mai, A.; Cheng, X.
    An analog of BIX-01294 selectively inhibits a family of histone H3 lysine 9 Jumonji demethylases (2012), J. Mol. Biol., 416, 319-327 .
    View publication on PubMedView publication on EuropePMC
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Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor E67 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
7-[(5-aminopentyl)oxy]-6-methoxy-N2,N2,N4,N4-tetramethylquinazoline-2,4-diamine
-
 Homo sapiens
7-[(5-aminopentyl)oxy]-N2-[3-(dimethylamino)propyl]-6-methoxy-N4,N4-dimethylquinazoline-2,4-diamine
-
 Homo sapiens
7-[(5-aminopentyl)oxy]-N4-(1-benzylpiperidin-4-yl)-N2-[3-(dimethylamino)propyl]-6-methoxyquinazoline-2,4-diamine
-
 Homo sapiens
N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
-
 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ni2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
[histone H3]-N6,N6-dimethyl-L-lysine27 + 2-oxoglutarate + O2 Homo sapiens
-
 [histone H3]-N6-methyl-L-lysine27 + succinate + formaldehyde + CO2
-
 ?
[histone H3]-N6,N6-dimethyl-L-lysine9 + 2-oxoglutarate + O2 Homo sapiens
-
 [histone H3]-N6-methyl-L-lysine9 + succinate + formaldehyde + CO2
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q6ZMT4
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
[histone H3]-N6,N6-dimethyl-L-lysine27 + 2-oxoglutarate + O2
-
 Homo sapiens [histone H3]-N6-methyl-L-lysine27 + succinate + formaldehyde + CO2
-
 ?
[histone H3]-N6,N6-dimethyl-L-lysine9 + 2-oxoglutarate + O2
-
 Homo sapiens [histone H3]-N6-methyl-L-lysine9 + succinate + formaldehyde + CO2
-
 ?

Synonyms

Synonyms Comment Organism
H3K9 Jumonji demethylase
-
 Homo sapiens
histone H3 lysine 9 Jumonji demethylase
-
 Homo sapiens
KIAA1718
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0021
-
 7-[(5-aminopentyl)oxy]-N2-[3-(dimethylamino)propyl]-6-methoxy-N4,N4-dimethylquinazoline-2,4-diamine pH and temperature not specified in the publication Homo sapiens
0.0025
-
 7-[(5-aminopentyl)oxy]-N4-(1-benzylpiperidin-4-yl)-N2-[3-(dimethylamino)propyl]-6-methoxyquinazoline-2,4-diamine pH and temperature not specified in the publication Homo sapiens
0.0153
-
 N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine pH and temperature not specified in the publication Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0034
-
 pH and temperature not specified in the publication Homo sapiens 7-[(5-aminopentyl)oxy]-N2-[3-(dimethylamino)propyl]-6-methoxy-N4,N4-dimethylquinazoline-2,4-diamine
0.0037
-
 pH and temperature not specified in the publication Homo sapiens 7-[(5-aminopentyl)oxy]-N4-(1-benzylpiperidin-4-yl)-N2-[3-(dimethylamino)propyl]-6-methoxyquinazoline-2,4-diamine
0.0165
-
 pH and temperature not specified in the publication Homo sapiens N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
0.019
-
 pH and temperature not specified in the publication Homo sapiens 7-[(5-aminopentyl)oxy]-6-methoxy-N2,N2,N4,N4-tetramethylquinazoline-2,4-diamine