Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM50243276
Substrate
n/a
Meas. Tech.
ChEMBL_491925 (CHEMBL947433)
IC50
38±n/a nM
Citation
 Siu, TLi, YNagasawa, JLiang, JTehrani, LChua, PJones, REDefeo-Jones, DBarnett, SFRobinson, 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:
BDBM50243276
Synonyms:
2-(4-(7-(4-((4-(5-(6-aminopyridin-3-yl)-4H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-6-phenylpyrido[2,3-d]pyrimidin-2-yl)piperazin-1-yl)ethanol | CHEMBL503810
Type:
Small organic molecule
Emp. Form.:
C38H41N11O
Mol. Mass.:
667.8052
SMILES:
Nc1ccc(cn1)-c1nnc([nH]1)C1CCN(Cc2ccc(cc2)-c2nc3nc(ncc3cc2-c2ccccc2)N2CCN(CCO)CC2)CC1
Structure:
Search PDB for entries with ligand similarity: