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Target
RAC-alpha serine/threonine-protein kinase [E49C,C296S,C310S,C344S]
Ligand
BDBM153709
Substrate
n/a
Meas. Tech.
iFLik Assay
pH
7.4±n/a
Kd
2.2e+3± 5e+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 
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:
BDBM153709
Synonyms:
7-(4-methylphenyl)-5-phenyl-N-(thiophen-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (8a)
Type:
Small organic molecule
Emp. Form.:
C24H20N4S
Mol. Mass.:
396.507
SMILES:
Cc1ccc(cc1)-n1cc(-c2ccccc2)c2c(NCc3cccs3)ncnc12
Structure:
Search PDB for entries with ligand similarity: