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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM15067
Substrate
biotinylated kemptide
Meas. Tech.
PKA/PKC Kinase Assay
IC50
2.1±n/a nM
Citation
 Li, Q; Woods, KW; Thomas, S; Zhu, GD; Packard, G; Fisher, J; Li, T; Gong, J; Dinges, J; Song, X; Abrams, J; Luo, Y; Johnson, EF; Shi, Y; Liu, X; Klinghofer, V; Des Jong, R; Oltersdorf, T; Stoll, VS; Jakob, CG; Rosenberg, SH; Giranda, VL Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. Bioorg Med Chem Lett 16:2000-7 (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:
BDBM15067
Synonyms:
(2S)-1-(1H-indol-3-yl)-3-(5-isoquinolin-6-ylpyridin-3-yl)oxy-propan-2-amine | 13a (S-) | 5-isoquinolinyl pyridine 2 | 6-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]pyridin-3-yl}isoquinoline | isoquinoline-pyridine, 1 | isoquinoline-pyridine, 3 | pyridine-base inhibitor 13a
Type:
Small organic molecule
Emp. Form.:
C25H22N4O
Mol. Mass.:
394.4684
SMILES:
N[C@H](COc1cncc(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