Reaction Details Report a problem with these data
Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM11823
Substrate
Peptide Substrate
Meas. Tech.
Fluorescence Polarization-based Assay
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
2±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:
BDBM11823
Synonyms:
Azepane Derivative 4 | N-((3R,4R)-4-{[4-(2-fluoro-6-hydroxy-3-methoxybenzoyl)benzoyl]amino}azepan-3-yl)isonicotinamide dihydrochloride | N-[(3R,4R)-4-({4-[(2-fluoro-6-hydroxy-3-methoxyphenyl)carbonyl]benzene}amido)azepan-3-yl]pyridine-4-carboxamide dihydrochloride
Type:
Small organic molecule
Emp. Form.:
C27H27FN4O5
Mol. Mass.:
506.5255
SMILES:
COc1ccc(O)c(C(=O)c2ccc(cc2)C(=O)N[C@@H]2CCCNC[C@H]2NC(=O)c2ccncc2)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