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Target
RAC-beta serine/threonine-protein kinase
Ligand
BDBM24887
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
22±n/a nM
Citation
 Hartnett, JC; Barnett, SF; Bilodeau, MT; Defeo-Jones, D; Hartman, GD; Huber, HE; Jones, RE; Kral, AM; Robinson, RG; Wu, Z Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors. Bioorg Med Chem Lett 18:2194-7 (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:
BDBM24887
Synonyms:
2,3,5-trisubstituted pyridine, 10c | 5-{5-phenyl-6-[4-({4-[5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl]piperidin-1-yl}methyl)phenyl]pyridin-3-yl}-1,3,4-thiadiazol-2-amine
Type:
Small organic molecule
Emp. Form.:
C32H29N9S
Mol. Mass.:
571.698
SMILES:
Nc1nnc(s1)-c1cnc(-c2ccc(CN3CCC(CC3)c3nnc([nH]3)-c3ccccn3)cc2)c(c1)-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