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Target
RAC-alpha serine/threonine-protein kinase
Ligand
BDBM116477
Substrate
n/a
Meas. Tech.
ChEMBL_2122111 (CHEMBL4831258)
IC50
>10000±n/a nM
Citation
 DeSelm, L; Huck, B; Lan, R; Neagu, C; Potnick, J; Xiao, Y; Chen, X; Jones, R; Richardson, TE; Heasley, BH; Haxell, T; Moore, J; Tian, H; Georgi, K; Rohdich, F; Sutton, A; Johnson, T; Mochalkin, I; Jackson, J; Lin, J; Crowley, L; Machl, A; Clark, A; Wilker, E; Sherer, B; Goutopoulos, A Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers. J Med Chem 64:14603-14619 (2021) [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:
BDBM116477
Synonyms:
US8637532, 158
Type:
Small organic molecule
Emp. Form.:
C18H15N3O3
Mol. Mass.:
321.33
SMILES:
NC(=O)c1cccc2c(NCc3ccc4OCOc4c3)ccnc12
Structure:
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