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Target
RAC-gamma serine/threonine-protein kinase
Ligand
BDBM16958
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Kinase Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
39±n/a nM
Citation
 Zhu, GD; Gong, J; Claiborne, A; Woods, KW; Gandhi, VB; Thomas, S; Luo, Y; Liu, X; Shi, Y; Guan, R; Magnone, SR; Klinghofer, V; Johnson, EF; Bouska, J; Shoemaker, A; Oleksijew, A; Stoll, VS; De Jong, R; Oltersdorf, T; Li, Q; Rosenberg, SH; Giranda, VL Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity. Bioorg Med Chem Lett 16:3150-5 (2006) [PubMed]  Article 
Target
Name:
RAC-gamma serine/threonine-protein kinase
Synonyms:
AKT3 | AKT3_HUMAN | PKB gamma | PKBG | Protein kinase Akt-3 | Protein kinase B (Akt 3) | Protein kinase B, gamma | RAC-PK-gamma | RAC-gamma serine/threonine-protein kinase | STK-2 | Serine/threonine-protein kinase AKT | Serine/threonine-protein kinase AKT3
Type:
Enzyme
Mol. Mass.:
55769.36
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
479
Sequence:
MSDVTIVKEGWVQKRGEYIKNWRPRYFLLKTDGSFIGYKEKPQDVDLPYPLNNFSVAKCQLMKTERPKPNTFIIRCLQWTTVIERTFHVDTPEEREEWTEAIQAVADRLQRQEEERMNCSPTSQIDNIGEEEMDASTTHHKRKTMNDFDYLKLLGKGTFGKVILVREKASGKYYAMKILKKEVIIAKDEVAHTLTESRVLKNTRHPFLTSLKYSFQTKDRLCFVMEYVNGGELFFHLSRERVFSEDRTRFYGAEIVSALDYLHSGKIVYRDLKLENLMLDKDGHIKITDFGLCKEGITDAATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEDIKFPRTLSSDAKSLLSGLLIKDPNKRLGGGPDDAKEIMRHSFFSGVNWQDVYDKKLVPPFKPQVTSETDTRYFDEEFTAQTITITPPEKYDEDGMDCMDNERRPHFPQFSYSASGRE
  
Inhibitor
Name:
BDBM16958
Synonyms:
6-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]-2-ethynylpyridin-3-yl}isoquinoline | Isoquinoline-pyridine, 10e
Type:
Small organic molecule
Emp. Form.:
C27H22N4O
Mol. Mass.:
418.4898
SMILES:
N[C@H](COc1cnc(C#C)c(c1)-c1ccc2cnccc2c1)Cc1c[nH]c2ccccc12 |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