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Target
RAC-alpha serine/threonine-protein kinase [139-480,S378A,S381A,T450D,S473D]
Ligand
BDBM16919
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Kinase Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
5.4±n/a nM
Citation
 Zhu, GD; Gandhi, VB; Gong, J; Luo, Y; Liu, X; Shi, Y; Guan, R; Magnone, SR; Klinghofer, V; Johnson, EF; Bouska, J; Shoemaker, A; Oleksijew, A; Jarvis, K; Park, C; Jong, RD; Oltersdorf, T; Li, Q; Rosenberg, SH; Giranda, 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:
BDBM16919
Synonyms:
3-[(2S)-2-amino-3-[(5-{thieno[2,3-c]pyridin-2-yl}pyridin-3-yl)oxy]propyl]-1H-indole | Biochemistry 469551 Compound 12 | CHEMBL516429 | thieno[2,3-c]pyridine, 9a
Type:
Small organic molecule
Emp. Form.:
C23H20N4OS
Mol. Mass.:
400.496
SMILES:
N[C@H](COc1cncc(c1)-c1cc2ccncc2s1)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