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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM24881
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
18±n/a nM
Citation
 Wu, Z; Hartnett, JC; Neilson, LA; Robinson, RG; Fu, S; Barnett, SF; Defeo-Jones, D; Jones, RE; Kral, AM; Huber, HE; Hartman, GD; Bilodeau, MT Development of pyridopyrimidines as potent Akt1/2 inhibitors. Bioorg Med Chem Lett 18:1274-9 (2008) [PubMed]  Article 
Target
Name:
RAC-alpha serine/threonine-protein kinase
Synonyms:
AKT phosphorylation (p-AKT) | AKT1 | AKT1/PPP1CA | AKT1_HUMAN | C-AKT | PKB | PKB alpha | Protein kinase Akt-1 | Protein kinase B | Protein kinase B (AKT1) | Protein kinase B (Akt 1) | Protein kinase B (Akt) | Protein kinase B alpha | Protein kinase B alpha (AKT1) | Proto-oncogene Akt (Akt1) | Proto-oncogene c-Akt (AKT) | Proto-oncogene c-Akt (AKT1) | RAC | RAC-PK-alpha | RAC-alpha serine/threonine-protein kinase (AKT) | RAC-alpha serine/threonine-protein kinase (AKT1) | RAC-alpha serine/threonine-protein kinase (pAKT)
Type:
Enzyme
Mol. Mass.:
55681.25
Organism:
Homo sapiens (Human)
Description:
P31749
Residue:
480
Sequence:
MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQREAPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDFRSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
  
Inhibitor
Name:
BDBM24881
Synonyms:
7-(4-{[4-(6-fluoro-1H-1,3-benzodiazol-2-yl)piperidin-1-yl]methyl}phenyl)-6-phenylpyrido[2,3-d]pyrimidin-4-amine | Pyridopyrimidine, 1
Type:
Small organic molecule
Emp. Form.:
C32H28FN7
Mol. Mass.:
529.61
SMILES:
Nc1ncnc2nc(-c3ccc(CN4CCC(CC4)c4nc5ccc(F)cc5[nH]4)cc3)c(cc12)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated Akt peptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1734.89
Organism:
n/a
Description:
n/a
Residue:
17
Sequence:
ITINGGRARTSSFAEPG