Reaction Details
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RAC-alpha serine/threonine-protein kinase [E49C,C296S,C310S,C344S]
Ligand
BDBM153706
Substrate
n/a
Meas. Tech.
iFLik Assay
pH
7.4±n/a
Kd
7.2e+3± 9e+2 nM
Comments
extracted
Citation
Fang, Z; Simard, JR; Plenker, D; Nguyen, HD; Phan, T; Wolle, P; Baumeister, S; Rauh, D Discovery of inter-domain stabilizers-a novel assay system for allosteric akt inhibitors. ACS Chem Biol 10:279-88 (2015) [PubMed] Article More Info.:
Target
Name:
RAC-alpha serine/threonine-protein kinase [E49C,C296S,C310S,C344S]
Synonyms:
AKT1 | AKT1_HUMAN | PKB | Protein kinase B (Akt1 E49C, C296S, C310S and C344S ) | RAC
Type:
Protein
Mol. Mass.:
55608.09
Organism:
Homo sapiens (Human)
Description:
Human Akt1 containing mutations E49C, C296S, C310S and C344S
Residue:
480
Sequence:
MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQRCAPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDFRSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLSKEGIKDGATMKTFSGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMSGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
Inhibitor
Name:
BDBM153706
Synonyms:
2-(4-((4-(4-Methoxyphenyl)piperazin-1-yl)methyl)phenyl)-3-phenyl-1,6-naphthyridin-5(6H)-one (7e)
Type:
Small organic molecule
Emp. Form.:
C32H30N4O2
Mol. Mass.:
502.6062
SMILES:
COc1ccc(cc1)N1CCN(Cc2ccc(cc2)-c2nc3cc[nH]c(=O)c3cc2-c2ccccc2)CC1
Structure:
