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Target
RAC-gamma serine/threonine-protein kinase
Ligand
BDBM27250
Substrate
AKTide-2T
Meas. Tech.
Fluorometric TLC Kinase Assay
IC50
43.1±n/a nM
Citation
 Lavogina, D; Lust, M; Viil, I; König, N; Raidaru, G; Rogozina, J; Enkvist, E; Uri, A; Bossemeyer, D Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhibitors of basophilic protein kinases. J Med Chem 52:308-21 (2009) [PubMed]  Article 
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:
BDBM27250
Synonyms:
6-{[(1S,3R,4R)-3-(6-amino-9H-purin-9-yl)-4-hydroxycyclopentyl]formamido}-N-[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-carbamoylbutyl]carbamoyl}butyl]carbamoyl}butyl]carbamoyl}butyl]carbamoyl}butyl]carbamoyl}butyl]hexanamide | ARC-659-1b
Type:
Small organic molecule
Emp. Form.:
C53H97N31O9
Mol. Mass.:
1312.5396
SMILES:
[#7]\[#6](-[#7])=[#7]\[#6]-[#6]-[#6]-[#6@@H](-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](/[#7])-[#7])-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](/[#7])-[#7])-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](/[#7])-[#7])-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](\[#7])-[#7])-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](\[#7])-[#7])-[#7]-[#6](=O)-[#6]-[#6]-[#6]-[#6]-[#6]-[#7]-[#6](=O)-[#6@@H]-1-[#6]-[#6@@H](-[#8])-[#6@@H](-[#6]-1)-n1cnc2c(-[#7])ncnc12)-[#6](-[#7])=O |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
AKTide-2T
Synonyms:
AKT/PKB/Rac Protein Kinase Substrate
Type:
Peptide
Mol. Mass.:
1719.90
Organism:
n/a
Description:
n/a
Residue:
14
Sequence:
ARKRERTYSFGHHA