Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM24867
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
15±3 nM
Citation
 Wu, ZHartnett, JCNeilson, LARobinson, RGFu, SBarnett, SFDefeo-Jones, DJones, REKral, AMHuber, HEHartman, GDBilodeau, 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:
BDBM24867
Synonyms:
1-(2-aminophenyl)-3-[({4-[2-(methylsulfanyl)-6-phenylpyrido[2,3-d]pyrimidin-7-yl]phenyl}methyl)amino]propan-1-one | CHEMBL252456 | Pyridopyrimidine, 12l
Type:
Small organic molecule
Emp. Form.:
C30H27N5OS
Mol. Mass.:
505.633
SMILES:
CSc1ncc2cc(-c3ccccc3)c(nc2n1)-c1ccc(CNCCC(=O)c2ccccc2N)cc1
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