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Target
RAC-alpha serine/threonine-protein kinase [139-480,S378A,S381A,T450D,S473D]
Ligand
BDBM15146
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Kinase Assay
pH
7.5±n/a
Temperature
295.15±n/a K
Ki
244±n/a nM
Citation
 Thomas, SA; Li, T; Woods, KW; Song, X; Packard, G; Fischer, JP; Diebold, RB; Liu, X; Shi, Y; Klinghofer, V; Johnson, EF; Bouska, JJ; Olson, A; Guan, R; Magnone, SR; Marsh, K; Luo, Y; Rosenberg, SH; Giranda, VL; Li, Q Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase. Bioorg Med Chem Lett 16:3740-4 (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:
BDBM15146
Synonyms:
5-(5-{[(2S)-2-amino-3-(1H-indol-3-yl)propyl]sulfanyl}pyridin-3-yl)-3-methyl-1H-indazole | 5-indazolyl pyridine 23
Type:
Small organic molecule
Emp. Form.:
C24H23N5S
Mol. Mass.:
413.538
SMILES:
Cc1n[nH]c2ccc(cc12)-c1cncc(SC[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