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Target
RAC-alpha serine/threonine-protein kinase [139-480,S378A,S381A,T450D,S473D]
Ligand
BDBM15022
Substrate
biotinylated Akt peptide substrate
Meas. Tech.
Akt Kinase Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
14±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
More Info.:
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:
BDBM15022
Synonyms:
3-[(2S)-2-amino-3-({5-[(E)-2-(pyridin-4-yl)ethenyl]pyridin-3-yl}oxy)propyl]-1H-indole | bispyridinylethylene, 2 | pyridine-base inhibitor 1b | trans-bispyridinylethylene analog 2q
Type:
Small organic molecule
Emp. Form.:
C23H22N4O
Mol. Mass.:
370.447
SMILES:
N[C@H](COc1cncc(\C=C\c2ccncc2)c1)Cc1c[nH]c2ccccc12 |r|
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