Reaction Details Report a problem with these data
Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM15210
Substrate
PKA-specific peptide substrate
Meas. Tech.
PKA In Vitro Enzyme Assay
IC50
5300±n/a nM
Citation
 Collins, I; Caldwell, J; Fonseca, T; Donald, A; Bavetsias, V; Hunter, LJ; Garrett, MD; Rowlands, MG; Aherne, GW; Davies, TG; Berdini, V; Woodhead, SJ; Davis, D; Seavers, LC; Wyatt, PG; Workman, P; McDonald, E Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B. Bioorg Med Chem 14:1255-73 (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:
BDBM15210
Synonyms:
CHEMBL148333 | H-8 | Lopac-M-9656 | N-(2-methylaminoethyl)isoquinoline-5-sulfonamide | N-[2-(methylamino)ethyl]isoquinoline-5-sulfonamide
Type:
Small organic molecule
Emp. Form.:
C12H15N3O2S
Mol. Mass.:
265.331
SMILES:
CNCCNS(=O)(=O)c1cccc2cnccc12
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