Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM15131
Substrate
PKA-specific peptide substrate
Meas. Tech.
PKA In Vitro Enzyme Assay
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
27±n/a nM
Citation
 Davies, TGVerdonk, MLGraham, BSaalau-Bethell, SHamlett, CCMcHardy, TCollins, IGarrett, MDWorkman, PWoodhead, SJJhoti, HBarford, D A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera. J Mol Biol 367:882-94 (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:
BDBM15131
Synonyms:
5-indazolyl pyridine 3 | 5-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]pyridin-3-yl}-3-methyl-1H-indazole | A-443654 | indazole-pyridine, 4
Type:
Small organic molecule
Emp. Form.:
C24H23N5O
Mol. Mass.:
397.4723
SMILES:
Cc1n[nH]c2ccc(cc12)-c1cncc(OC[C@@H](N)Cc2c[nH]c3ccccc23)c1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PKA-specific peptide substrate
Synonyms:
PKAtide
Type:
Peptide
Mol. Mass.:
1019.14
Organism:
n/a
Description:
n/a
Residue:
9
Sequence:
GRTGRRNSI