Cloned (Comment) | Organism |
---|---|
mutant enzymes are expressed in Escherichia coli BL21-DE3 pLysS-Rosetta cells | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
T217E | the mutant has very similar activity as the wild type enzyme | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-chloro-N-(4-(5-fluoro-2-(4-hydroxyphenylamino)pyrimidin-4-ylamino)phenyl)benzamide | - |
Homo sapiens | |
4-(2-(4-(2-(4-acetylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)-N-(2-chlorophenyl)benzamide | - |
Homo sapiens | |
5-fluoro-N2,N4-bis(4-methoxyphenyl)pyrimidine-2,4-diamine | - |
Homo sapiens | |
5-fluoro-N2,N4-di(m-tolyl)pyrimidine-2,4-diamine | - |
Homo sapiens | |
MLN8054 | Aurora A-selective inhibitor | Homo sapiens | |
N-(2-chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide | - |
Homo sapiens | |
N-(2-chlorophenyl)-4-(5-fluoro-2-(4-hydroxyphenylamino)pyrimidin-4-ylamino)benzamide | - |
Homo sapiens | |
N-cyclopropyl-4-(5-fluoro-2-(4-hydroxyphenylamino)pyrimidin-4-ylamino)benzamide | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + protein | Homo sapiens | - |
ADP + phosphoprotein | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O14965 | - |
- |
Purification (Comment) | Organism |
---|---|
mutant enzymes are purified by anti-Flag M2 agarose column chromatography and Superdex S-200 gel filtration | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + protein | - |
Homo sapiens | ADP + phosphoprotein | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Aurora A | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000001 | - |
wild type Aurora A kinase | Homo sapiens | MLN8054 | |
0.000006 | - |
wild type Aurora A kinase | Homo sapiens | 2-chloro-N-(4-(5-fluoro-2-(4-hydroxyphenylamino)pyrimidin-4-ylamino)phenyl)benzamide | |
0.00001 | - |
wild type Aurora A kinase | Homo sapiens | N-(2-chlorophenyl)-4-(5-fluoro-2-(4-hydroxyphenylamino)pyrimidin-4-ylamino)benzamide | |
0.000026 | - |
wild type Aurora A kinase | Homo sapiens | N-(2-chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide | |
0.000044 | - |
wild type Aurora A kinase | Homo sapiens | 4-(2-(4-(2-(4-acetylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)-N-(2-chlorophenyl)benzamide | |
0.000054 | - |
wild type Aurora A kinase | Homo sapiens | N-cyclopropyl-4-(5-fluoro-2-(4-hydroxyphenylamino)pyrimidin-4-ylamino)benzamide | |
0.00013 | - |
wild type Aurora A kinase | Homo sapiens | 5-fluoro-N2,N4-bis(4-methoxyphenyl)pyrimidine-2,4-diamine | |
0.00068 | - |
wild type Aurora A kinase | Homo sapiens | 5-fluoro-N2,N4-di(m-tolyl)pyrimidine-2,4-diamine | |
0.002 | - |
mutant Aurora A kinase T217E | Homo sapiens | N-(2-chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide | |
0.0028 | - |
mutant Aurora A kinase T217E | Homo sapiens | 4-(2-(4-(2-(4-acetylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)-N-(2-chlorophenyl)benzamide |