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Target
RAC-alpha serine/threonine-protein kinase [139-480,S378A,S381A,T450D,S473D]
Ligand
BDBM16537
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Kinase Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
8.5±n/a nM
Citation
 Zhu, GD; Gandhi, VB; Gong, J; Thomas, S; Woods, KW; Song, X; Li, T; Diebold, RB; Luo, Y; Liu, X; Guan, R; Klinghofer, V; Johnson, EF; Bouska, J; Olson, A; Marsh, KC; Stoll, VS; Mamo, M; Polakowski, J; Campbell, TJ; Martin, RL; Gintant, GA; Penning, TD; Li, Q; Rosenberg, SH; Giranda, VL Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension. J Med Chem 50:2990-3003 (2007) [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:
BDBM16537
Synonyms:
(2S)-1-(2,3-difluorophenyl)-3-{[5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl]oxy}propan-2-amine | 5-{5-[(2S)-2-amino-3-(2,3-difluorophenyl)propoxy]pyridin-3-yl}-3-methyl-1H-indazole | indazole-pyridine, 13b
Type:
Small organic molecule
Emp. Form.:
C22H20F2N4O
Mol. Mass.:
394.4172
SMILES:
Cc1n[nH]c2ccc(cc12)-c1cncc(OC[C@@H](N)Cc2cccc(F)c2F)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