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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM50243283
Substrate
n/a
Meas. Tech.
ChEMBL_491925 (CHEMBL947433)
IC50
33±n/a nM
Citation
 Siu, T; Li, Y; Nagasawa, J; Liang, J; Tehrani, L; Chua, P; Jones, RE; Defeo-Jones, D; Barnett, SF; Robinson, RG The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity. Bioorg Med Chem Lett 18:4191-4 (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:
BDBM50243283
Synonyms:
CHEMBL455071 | Dimethyl-(2-{4-[7-(4-{4-[5-(1-oxy-pyridin-4-yl)-4H-[1,2,4]triazol-3-yl]-piperidin-1-ylmethyl}-phenyl)-6-phenyl-pyrido[2,3-d]pyrimidin-2-yl]-piperazin-1-yl}-ethyl)-amine
Type:
Small organic molecule
Emp. Form.:
C40H45N11O
Mol. Mass.:
695.8584
SMILES:
CN(C)CCN1CCN(CC1)c1ncc2cc(-c3ccccc3)c(nc2n1)-c1ccc(CN2CCC(CC2)c2nnc([nH]2)-c2cc[n+]([O-])cc2)cc1
Structure:
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