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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM16231
Substrate
PKA-specific peptide substrate
Meas. Tech.
PKA In Vitro Enzyme Assay
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
15±n/a nM
Citation
 Donald, A; McHardy, T; Rowlands, MG; Hunter, LJ; Davies, TG; Berdini, V; Boyle, RG; Aherne, GW; Garrett, MD; Collins, I Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design. J Med Chem 50:2289-92 (2007) [PubMed]  Article 
Target
Name:
cAMP-dependent protein kinase catalytic subunit alpha
Synonyms:
KAPCA_BOVIN | PKA C-alpha | PKC | PRKACA | Protein Kinase C | Protein Kinase C, bovine brain | cAMP-Dependent Protein Kinase (PKA) | cAMP-dependent Protein Kinase, bovine heart | cAMP-dependent protein kinase A | cAMP-dependent protein kinase alpha-catalytic subunit | cAMP-dependent protein kinase, alpha-catalytic subunit
Type:
Enzyme Complex
Mol. Mass.:
40627.77
Organism:
Bos taurus (bovine)
Description:
The PKA holoenzyme purified from bovine heart, exists as an inactive tetrameric complex, which consists of a regulatory dimer associated with two catalytic subunits. It requires cAMP to activate the enzymatic reaction.
Residue:
351
Sequence:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWENPAQNTAHLDQFERIKTLGTGSFGRVMLVKHMETGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMVMEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGYIQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFFADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFATTDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFSEF
  
Inhibitor
Name:
BDBM16231
Synonyms:
2-(4-chlorophenyl)-N-methyl-2-[4-(9H-purin-6-yl)phenyl]ethanamine | 6-phenylpurine compound 18 | [2-(4-chlorophenyl)-2-[4-(9H-purin-6-yl)phenyl]ethyl](methyl)amine
Type:
Small organic molecule
Emp. Form.:
C20H18ClN5
Mol. Mass.:
363.843
SMILES:
CNCC(c1ccc(Cl)cc1)c1ccc(cc1)-c1ncnc2nc[nH]c12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PKA-specific peptide substrate
Synonyms:
PKAtide
Type:
Peptide
Mol. Mass.:
1019.14
Organism:
n/a
Description:
n/a
Residue:
9
Sequence:
GRTGRRNSI