Literature summary for 2.7.11.1 extracted from

Aliagas-Martin, I.; Burdick, D.; Corson, L.; Dotson, J.; Drummond, J.; Fields, C.; Huang, O.W.; Hunsaker, T.; Kleinheinz, T.; Krueger, E.; Liang, J.; Moffat, J.; Phillips, G.; Pulk, R.; Rawson, T.E.; Ultsch, M.; Walker, L.; Wiesmann, C.; Zhang, B.; Zhu, B.Y.; Cochran, A.G.
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B (2009), J. Med. Chem., 52, 3300-3307.

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Cloned(Commentary)

Cloned (Comment)	Organism
mutant enzymes are expressed in Escherichia coli BL21-DE3 pLysS-Rosetta cells	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
T217E	the mutant has very similar activity as the wild type enzyme	Homo sapiens

Inhibitors

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/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + protein	Homo sapiens	-	ADP + phosphoprotein	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	O14965	-	-

Purification (Commentary)

Purification (Comment)	Organism
mutant enzymes are purified by anti-Flag M2 agarose column chromatography and Superdex S-200 gel filtration	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + protein	-	Homo sapiens	ADP + phosphoprotein	-	?

Synonyms

Synonyms	Comment	Organism
Aurora A	-	Homo sapiens

IC50 Value

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

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Release 2023.1 (January 2023)