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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM16582
Substrate
biotinylated kemptide
Meas. Tech.
PKA/PKC Kinase Assay
IC50
>3000±n/a nM
Citation
 Zhu, GD; Gandhi, VB; Gong, J; Thomas, S; Woods, KW; Song, X; Li, T; Diebold, RB; Luo, Y; Liu, X; Guan, R; Klinghofer, V; Johnson, EF; Bouska, J; Olson, A; Marsh, KC; Stoll, VS; Mamo, M; Polakowski, J; Campbell, TJ; Martin, RL; Gintant, GA; Penning, TD; Li, Q; Rosenberg, SH; Giranda, VL Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase b/akt inhibitors with reduced hypotension. J Med Chem 50:2990-3003 (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:
BDBM16582
Synonyms:
5-{5-[(2S)-2-amino-3-[3-(cyclohexylmethoxy)phenyl]propoxy]pyridin-3-yl}-3-methyl-1H-indazole | indazole-pyridine, 13au
Type:
Small organic molecule
Emp. Form.:
C29H34N4O2
Mol. Mass.:
470.6059
SMILES:
Cc1n[nH]c2ccc(cc12)-c1cncc(OC[C@@H](N)Cc2cccc(OCC3CCCCC3)c2)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