Reaction Details Report a problem with these data
Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM16958
Substrate
biotinylated kemptide
Meas. Tech.
PKA/PKC Kinase Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
1±n/a nM
Citation
 Zhu, GD; Gong, J; Claiborne, A; Woods, KW; Gandhi, VB; Thomas, S; Luo, Y; Liu, X; Shi, Y; Guan, R; Magnone, SR; Klinghofer, V; Johnson, EF; Bouska, J; Shoemaker, A; Oleksijew, A; Stoll, VS; De Jong, R; Oltersdorf, T; Li, Q; Rosenberg, SH; Giranda, VL Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity. Bioorg Med Chem Lett 16:3150-5 (2006) [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:
BDBM16958
Synonyms:
6-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]-2-ethynylpyridin-3-yl}isoquinoline | Isoquinoline-pyridine, 10e
Type:
Small organic molecule
Emp. Form.:
C27H22N4O
Mol. Mass.:
418.4898
SMILES:
N[C@H](COc1cnc(C#C)c(c1)-c1ccc2cnccc2c1)Cc1c[nH]c2ccccc12 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated kemptide
Synonyms:
n/a
Type:
Biotinylated Peptide
Mol. Mass.:
1353.09
Organism:
n/a
Description:
n/a
Residue:
12
Sequence:
ITINHLRRASLG