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Target
RAC-gamma serine/threonine-protein kinase
Ligand
BDBM24992
Substrate
AKT Substrate Peptide
Meas. Tech.
In Vitro Kinase Inhibition Assay
IC50
1549±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
More Info.:
Target
Name:
RAC-gamma serine/threonine-protein kinase
Synonyms:
AKT3 | AKT3_HUMAN | PKB gamma | PKBG | Protein kinase Akt-3 | Protein kinase B (Akt 3) | Protein kinase B, gamma | RAC-PK-gamma | RAC-gamma serine/threonine-protein kinase | STK-2 | Serine/threonine-protein kinase AKT | Serine/threonine-protein kinase AKT3
Type:
Enzyme
Mol. Mass.:
55769.36
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
479
Sequence:
MSDVTIVKEGWVQKRGEYIKNWRPRYFLLKTDGSFIGYKEKPQDVDLPYPLNNFSVAKCQLMKTERPKPNTFIIRCLQWTTVIERTFHVDTPEEREEWTEAIQAVADRLQRQEEERMNCSPTSQIDNIGEEEMDASTTHHKRKTMNDFDYLKLLGKGTFGKVILVREKASGKYYAMKILKKEVIIAKDEVAHTLTESRVLKNTRHPFLTSLKYSFQTKDRLCFVMEYVNGGELFFHLSRERVFSEDRTRFYGAEIVSALDYLHSGKIVYRDLKLENLMLDKDGHIKITDFGLCKEGITDAATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEDIKFPRTLSSDAKSLLSGLLIKDPNKRLGGGPDDAKEIMRHSFFSGVNWQDVYDKKLVPPFKPQVTSETDTRYFDEEFTAQTITITPPEKYDEDGMDCMDNERRPHFPQFSYSASGRE
Inhibitor
Name:
BDBM24992
Synonyms:
4-[1-ethyl-7-(piperazin-1-ylcarbonyl)-1H-imidazo[4,5-c]pyridin-2-yl]-1,2,5-oxadiazol-3-amine | oxadiazole-containing compound, 5
Type:
Small organic molecule
Emp. Form.:
C15H18N8O2
Mol. Mass.:
342.3558
SMILES:
CCn1c(nc2cncc(C(=O)N3CCNCC3)c12)-c1nonc1N
Substrate
Name:
AKT Substrate Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1689.88
Organism:
n/a
Description:
n/a
Residue:
14
Sequence:
ARKRERAYSFGHHA