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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM25010
Substrate
AKT Substrate Peptide
Meas. Tech.
In Vitro Kinase Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
3±n/a nM
Citation
 Heerding, DA; Rhodes, N; Leber, JD; Clark, TJ; Keenan, RM; Lafrance, LV; Li, M; Safonov, IG; Takata, DT; Venslavsky, JW; Yamashita, DS; Choudhry, AE; Copeland, RA; Lai, Z; Schaber, MD; Tummino, PJ; Strum, SL; Wood, ER; Duckett, DR; Eberwein, D; Knick, VB; Lansing, TJ; McConnell, RT; Zhang, S; Minthorn, EA; Concha, NO; Warren, GL; Kumar, R Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. J Med Chem 51:5663-79 (2008) [PubMed]  Article 
Target
Name:
RAC-alpha serine/threonine-protein kinase
Synonyms:
AKT phosphorylation (p-AKT) | AKT1 | AKT1/PPP1CA | AKT1_HUMAN | C-AKT | PKB | PKB alpha | Protein kinase Akt-1 | Protein kinase B | Protein kinase B (AKT1) | Protein kinase B (Akt 1) | Protein kinase B (Akt) | Protein kinase B alpha | Protein kinase B alpha (AKT1) | Proto-oncogene Akt (Akt1) | Proto-oncogene c-Akt (AKT) | Proto-oncogene c-Akt (AKT1) | RAC | RAC-PK-alpha | RAC-alpha serine/threonine-protein kinase (AKT) | RAC-alpha serine/threonine-protein kinase (AKT1) | RAC-alpha serine/threonine-protein kinase (pAKT)
Type:
Enzyme
Mol. Mass.:
55681.25
Organism:
Homo sapiens (Human)
Description:
P31749
Residue:
480
Sequence:
MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQREAPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDFRSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
  
Inhibitor
Name:
BDBM25010
Synonyms:
4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-7-[(3S)-3-amino-4-phenylbutoxy]-1-ethyl-1H-imidazo[4,5-c]pyridin-4-yl]-2-methylbut-3-yn-2-ol | oxadiazole-containing compound, 3d
Type:
Small organic molecule
Emp. Form.:
C25H29N7O3
Mol. Mass.:
475.5429
SMILES:
CCn1c(nc2c(ncc(OCC[C@@H](N)Cc3ccccc3)c12)C#CC(C)(C)O)-c1nonc1N |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
AKT Substrate Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1689.88
Organism:
n/a
Description:
n/a
Residue:
14
Sequence:
ARKRERAYSFGHHA