Target
RAC-alpha serine/threonine-protein kinase [139-480,S378A,S381A,T450D,S473D]
Ligand
BDBM16933
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Kinase Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
24.6±n/a nM
Citation
 Zhu, GDGandhi, VBGong, JLuo, YLiu, XShi, YGuan, RMagnone, SRKlinghofer, VJohnson, EFBouska, JShoemaker, AOleksijew, AJarvis, KPark, CJong, RDOltersdorf, TLi, QRosenberg, SHGiranda, VL Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers. Bioorg Med Chem Lett 16:3424-9 (2006) [PubMed]  Article 
Target
Name:
RAC-alpha serine/threonine-protein kinase [139-480,S378A,S381A,T450D,S473D]
Synonyms:
AKT1 | AKT1_HUMAN | C-AKT | PKB | Protein kinase B (Akt 1) | Protein kinase B alpha | RAC | RAC-PK-alpha
Type:
Enzyme
Mol. Mass.:
39513.28
Organism:
Homo sapiens (Human)
Description:
Recombinant His-tagged Akt1 (S378A, S381A, T450D, S473D; 139-480)
Residue:
342
Sequence:
AKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKALLAGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITIDPPDQDDSMECVDSERRPHFPQFDYSASGTA
  
Inhibitor
Name:
BDBM16933
Synonyms:
5-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]pyridin-3-yl}-3,3-dimethyl-2,3-dihydro-1H-indol-2-one | oxindole pyridine, 9o
Type:
Small organic molecule
Emp. Form.:
C26H26N4O2
Mol. Mass.:
426.5102
SMILES:
CC1(C)C(=O)Nc2ccc(cc12)-c1cncc(OC[C@@H](N)Cc2c[nH]c3ccccc23)c1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated Akt peptide substrate
Synonyms:
n/a
Type:
Biotinylated Peptide
Mol. Mass.:
3178.04
Organism:
n/a
Description:
Km=15 uM
Residue:
28
Sequence:
ITINAHEELSPFRGRSRSAPPNLWAAQR