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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM16532
Substrate
biotinylated kemptide
Meas. Tech.
Akt Kinase Assay
IC50
15±n/a nM
Citation
 Zhu, GD; Gong, J; Gandhi, VB; Woods, K; Luo, Y; Liu, X; Guan, R; Klinghofer, V; Johnson, EF; Stoll, VS; Mamo, M; Li, Q; Rosenberg, SH; Giranda, VL Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt. Bioorg Med Chem 15:2441-52 (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:
BDBM16532
Synonyms:
(2S)-1-(1H-indol-3-yl)-3-{[5-(3-methyl-1H-pyrazolo[3,4-c]pyridin-5-yl)pyridin-3-yl]oxy}propan-2-amine | 3-[(2S)-2-amino-3-[(5-{3-methyl-1H-pyrazolo[3,4-c]pyridin-5-yl}pyridin-3-yl)oxy]propyl]-1H-indole | pyrazolopyridine analog, 9g | pyrazolopyridine-pyridine, 6
Type:
Small organic molecule
Emp. Form.:
C23H22N6O
Mol. Mass.:
398.4604
SMILES:
Cc1n[nH]c2cnc(cc12)-c1cncc(OC[C@@H](N)Cc2c[nH]c3ccccc23)c1 |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