Target
RAC-beta serine/threonine-protein kinase
Ligand
BDBM24874
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Inhibition Assay
IC50
1304±n/a 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-beta serine/threonine-protein kinase
Synonyms:
AKT2 | AKT2_HUMAN | PKB beta | Protein kinase Akt-2 | Protein kinase B (Akt 2) | Protein kinase B beta (AKT2) | Protein kinase B, beta | RAC-PK-beta | RAC-alpha serine/threonine-protein kinase (AKT2) | RAC-beta serine/threonine-protein kinase | RAC-beta serine/threonine-protein kinase (AKT2) | Serine/threonine-protein kinase AKT | Serine/threonine-protein kinase AKT2 | Serine/threonine-protein kinase Rac alpha/beta
Type:
Enzyme
Mol. Mass.:
55766.64
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
481
Sequence:
MNEVSVIKEGWLHKRGEYIKTWRPRYFLLKSDGSFIGYKERPEAPDQTLPPLNNFSVAECQLMKTERPRPNTFVIRCLQWTTVIERTFHVDSPDEREEWMRAIQMVANSLKQRAPGEDPMDYKCGSPSDSSTTEEMEVAVSKARAKVTMNDFDYLKLLGKGTFGKVILVREKATGRYYAMKILRKEVIIAKDEVAHTVTESRVLQNTRHPFLTALKYAFQTHDRLCFVMEYANGGELFFHLSRERVFTEERARFYGAEIVSALEYLHSRDVVYRDIKLENLMLDKDGHIKITDFGLCKEGISDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHERLFELILMEEIRFPRTLSPEAKSLLAGLLKKDPKQRLGGGPSDAKEVMEHRFFLSINWQDVVQKKLLPPFKPQVTSEVDTRYFDDEFTAQSITITPPDRYDSLGLLELDQRTHFPQFSYSASIRE
  
Inhibitor
Name:
BDBM24874
Synonyms:
5-[1-({4-[2-(methylsulfanyl)-6-phenylpyrido[2,3-d]pyrimidin-7-yl]phenyl}methyl)piperidin-4-yl]-3-(pyridin-3-yl)-1,2,4-oxadiazole | Pyridopyrimidine, 13g
Type:
Small organic molecule
Emp. Form.:
C33H29N7OS
Mol. Mass.:
571.695
SMILES:
CSc1ncc2cc(-c3ccccc3)c(nc2n1)-c1ccc(CN2CCC(CC2)c2nc(no2)-c2cccnc2)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