Target
RAC-beta serine/threonine-protein kinase
Ligand
BDBM50593633
Substrate
n/a
Meas. Tech.
ChEMBL_2262234 (CHEMBL5217245)
IC50
1.4±n/a nM
Citation
 Yu, XXu, JCahuzac, KMXie, LShen, YChen, XLiu, JParsons, REJin, J Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells. J Med Chem 65:14237-14260 (2022) [PubMed]  Article
Target
Name:
RAC-beta serine/threonine-protein kinase
Synonyms:
AKT2 | AKT2_HUMAN | PKB beta | Protein kinase Akt-2 | Protein kinase B (Akt 2) | Protein kinase B beta (AKT2) | Protein kinase B, beta | RAC-PK-beta | RAC-alpha serine/threonine-protein kinase (AKT2) | RAC-beta serine/threonine-protein kinase | RAC-beta serine/threonine-protein kinase (AKT2) | Serine/threonine-protein kinase AKT | Serine/threonine-protein kinase AKT2 | Serine/threonine-protein kinase Rac alpha/beta
Type:
Enzyme
Mol. Mass.:
55766.64
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
481
Sequence:
MNEVSVIKEGWLHKRGEYIKTWRPRYFLLKSDGSFIGYKERPEAPDQTLPPLNNFSVAECQLMKTERPRPNTFVIRCLQWTTVIERTFHVDSPDEREEWMRAIQMVANSLKQRAPGEDPMDYKCGSPSDSSTTEEMEVAVSKARAKVTMNDFDYLKLLGKGTFGKVILVREKATGRYYAMKILRKEVIIAKDEVAHTVTESRVLQNTRHPFLTALKYAFQTHDRLCFVMEYANGGELFFHLSRERVFTEERARFYGAEIVSALEYLHSRDVVYRDIKLENLMLDKDGHIKITDFGLCKEGISDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHERLFELILMEEIRFPRTLSPEAKSLLAGLLKKDPKQRLGGGPSDAKEVMEHRFFLSINWQDVVQKKLLPPFKPQVTSEVDTRYFDDEFTAQSITITPPDRYDSLGLLELDQRTHFPQFSYSASIRE
  
Inhibitor
Name:
BDBM50593633
Synonyms:
ARQ 092 | ARQ 092 FREE BASE | ARQ-092 | Arq-092 | MIRANSERTIB | Miransertib
Type:
Small organic molecule
Emp. Form.:
C27H24N6
Mol. Mass.:
432.5197
SMILES:
Nc1ncccc1-c1nc2ccc(nc2n1-c1ccc(cc1)C1(N)CCC1)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity: