Reaction Details
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RAC-alpha serine/threonine-protein kinase [E49C,C296S,C310S,C344S]
Ligand
BDBM50313650
Substrate
n/a
Meas. Tech.
iFLik Assay
pH
7.4±n/a
Kd
9e+1± 1e+1 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:
BDBM50313650
Synonyms:
8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one | CHEMBL1079175 | MK-2206 | US10550114, Compound MK-2206
Type:
Small organic molecule
Emp. Form.:
C25H21N5O
Mol. Mass.:
407.4671
SMILES:
NC1(CCC1)c1ccc(cc1)-c1nc2ccn3c(n[nH]c3=O)c2cc1-c1ccccc1
Structure:
