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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM11826
Substrate
Peptide Substrate
Meas. Tech.
Fluorescence Polarization-based Assay
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
800±n/a nM
Citation
 Breitenlechner, CB; Wegge, T; Berillon, L; Graul, K; Marzenell, K; Friebe, WG; Thomas, U; Schumacher, R; Huber, R; Engh, RA; Masjost, B Structure-based optimization of novel azepane derivatives as PKB inhibitors. J Med Chem 47:1375-90 (2004) [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:
BDBM11826
Synonyms:
Azepane Derivative 7 | N-((3R,4R)-4-{[4-(2-fluoro-6-hydroxy-3-methoxybenzoyl)benzyl]amino}azepan-3-yl)isonicotinamide trihydrochloride | N-[(3R,4R)-4-[({4-[(2-fluoro-6-hydroxy-3-methoxyphenyl)carbonyl]phenyl}methyl)amino]azepan-3-yl]pyridine-4-carboxamide trihydrochloride
Type:
Small organic molecule
Emp. Form.:
C27H29FN4O4
Mol. Mass.:
492.542
SMILES:
COc1ccc(O)c(C(=O)c2ccc(CN[C@@H]3CCCNC[C@H]3NC(=O)c3ccncc3)cc2)c1F |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Peptide Substrate
Synonyms:
biotinylated tridecapeptide substrate
Type:
Peptide
Mol. Mass.:
1564.86
Organism:
n/a
Description:
n/a
Residue:
13
Sequence:
RFARKGSLRQKNV