Cloned (Comment) | Organism |
---|---|
- |
Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
N-terminal fragments of the enzyme in complex with inhibitors, sitting drop vapor diffusion method, using 1.2-1.35 M (NH4)2SO4, 0.1 M Tris-HCl (pH 8.6-9.2), 0-20% (v/v) glycerol and 25 mM (Na/K) dibasic/monobasic phosphate | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(E)-2-((3-(4-(dimethylamino)but-2-enamido)-phenyl)(2-(piperidin-1-yl)ethoxy)methyl)thieno[3,2-b]pyridine-7-carboxylic acid | - |
Homo sapiens | |
2-((2-chlorophenyl)(2-(1-methylpyrrolidin-2-yl)-ethoxy)methyl)thieno[3,2-b]pyridine-7-carboxylic acid | - |
Homo sapiens | |
2-((3-aminophenyl)(2-(piperidin-1-yl)ethoxy)methyl)thieno[3,2-b]-pyridine-7-carboxylic acid | 2-oxoglutarate-competitive inhibition | Homo sapiens | |
3-((2-(pyridin-2-yl)-6-(4-(vinylsulfonyl)-1,4-diazepan-1-yl)pyrimidin-4-yl)amino)propanoic acid | - |
Homo sapiens | |
3-((6-(4-acryloyl-1,4-diazepan-1-yl)-2-(pyridin-2-yl)-pyrimidin-4-yl)amino)propanoic acid | - |
Homo sapiens | |
CPI-455 | - |
Homo sapiens | |
ethyl 2-([(2-([2-(dimethylamino)ethyl](ethyl)amino)-2-oxoethyl)amino]methyl)pyridine-4-carboxylate | KDM5-C70 | Homo sapiens | |
KDOAM-25 | - |
Homo sapiens | |
N-[2-(pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)pyrimidin-4-yl]-beta-alanine | GSK-J1 | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
[histone H3]-N6,N6,N6-trimethyl-L-lysine4 + 2-oxoglutarate + O2 | Homo sapiens | - |
[histone H3]-N6,N6-dimethyl-L-lysine4 + succinate + formaldehyde + CO2 | - |
? | |
[histone H3]-N6,N6,N6-trimethyl-L-lysine4 + 3 2-oxoglutarate + 3 O2 | Homo sapiens | overall reaction | [histone H3]-L-lysine4 + 3 succinate + 3 formaldehyde + 3 CO2 | - |
? | |
[histone H3]-N6,N6-dimethyl-L-lysine4 + 2-oxoglutarate + O2 | Homo sapiens | - |
[histone H3]-N6-methyl-L-lysine4 + succinate + formaldehyde + CO2 | - |
? | |
[histone H3]-N6-methyl-L-lysine4 + 2-oxoglutarate + O2 | Homo sapiens | - |
[histone H3]-L-lysine4 + succinate + formaldehyde + CO2 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
affinity column chromatography, anion exchange column chromatography, and gel filtration | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
BT-474 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
[histone H3]-N6,N6,N6-trimethyl-L-lysine4 + 2-oxoglutarate + O2 | - |
Homo sapiens | [histone H3]-N6,N6-dimethyl-L-lysine4 + succinate + formaldehyde + CO2 | - |
? | |
[histone H3]-N6,N6,N6-trimethyl-L-lysine4 + 3 2-oxoglutarate + 3 O2 | overall reaction | Homo sapiens | [histone H3]-L-lysine4 + 3 succinate + 3 formaldehyde + 3 CO2 | - |
? | |
[histone H3]-N6,N6-dimethyl-L-lysine4 + 2-oxoglutarate + O2 | - |
Homo sapiens | [histone H3]-N6-methyl-L-lysine4 + succinate + formaldehyde + CO2 | - |
? | |
[histone H3]-N6-methyl-L-lysine4 + 2-oxoglutarate + O2 | - |
Homo sapiens | [histone H3]-L-lysine4 + succinate + formaldehyde + CO2 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
KDM5A | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00022 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-2-((3-(4-(dimethylamino)but-2-enamido)-phenyl)(2-(piperidin-1-yl)ethoxy)methyl)thieno[3,2-b]pyridine-7-carboxylic acid | |
0.00032 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-((2-chlorophenyl)(2-(1-methylpyrrolidin-2-yl)-ethoxy)methyl)thieno[3,2-b]pyridine-7-carboxylic acid | |
0.00049 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-((3-aminophenyl)(2-(piperidin-1-yl)ethoxy)methyl)thieno[3,2-b]-pyridine-7-carboxylic acid | |
0.071 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-((6-(4-acryloyl-1,4-diazepan-1-yl)-2-(pyridin-2-yl)-pyrimidin-4-yl)amino)propanoic acid | |
0.083 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-((2-(pyridin-2-yl)-6-(4-(vinylsulfonyl)-1,4-diazepan-1-yl)pyrimidin-4-yl)amino)propanoic acid | |
0.11 | - |
pH and temperature not specified in the publication | Homo sapiens | N-[2-(pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)pyrimidin-4-yl]-beta-alanine |