Reaction Details Report a problem with these data
Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM16588
Substrate
biotinylated kemptide
Meas. Tech.
PKA/PKC Kinase Assay
IC50
7±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:
PKC | Protein Kinase C, bovine brain | cAMP-dependent Protein Kinase, bovine heart | cAMP-dependent protein kinase alpha-catalytic subunit | cAMP-dependent protein kinase, alpha-catalytic subunit | PKA C-alpha | cAMP-dependent protein kinase A | Protein Kinase C | KAPCA_BOVIN | PRKACA | cAMP-Dependent Protein Kinase (PKA)
Type:
Enzyme Complex
Mol. Mass.:
40627.77
Organism:
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:
BDBM16588
Synonyms:
(2S)-1-(2,3-difluorophenyl)-3-{[5-(3-methyl-1H-pyrazolo[3,4-c]pyridin-5-yl)pyridin-3-yl]oxy}propan-2-amine | 3-[(2S)-2-amino-3-(2,3-difluorophenyl)propoxy]-5-{3-methyl-1H-pyrazolo[3,4-c]pyridin-5-yl}pyridine | pyrazolopyridine-pyridine, 37d
Type:
Small organic molecule
Emp. Form.:
C21H19F2N5O
Mol. Mass.:
395.16
SMILES:
Cc1n[nH]c2cnc(-c3cncc(OC[C@@H](N)Cc4cccc(F)c4F)c3)cc12
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