Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM27250
Substrate
Kemptide
Meas. Tech.
Fluorometric TLC Kinase Assay
IC50
2.41±n/a nM
Citation
 Lavogina, DLust, MViil, IKönig, NRaidaru, GRogozina, JEnkvist, EUri, ABossemeyer, D Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhibitors of basophilic protein kinases. J Med Chem 52:308-21 (2009) [PubMed]  Article 
Target
Name:
cAMP-dependent protein kinase catalytic subunit alpha
Synonyms:
KAPCA_MOUSE | PKA C-alpha | Pkaca | Prkaca | cAMP-Dependent Protein Kinase (PKA) | cAMP-dependent protein kinase catalytic subunit alpha | cAMP-dependent protein kinase, alpha-catalytic subunit
Type:
Enzyme Catalytic Unit
Mol. Mass.:
40579.18
Organism:
Mus musculus (mouse)
Description:
n/a
Residue:
351
Sequence:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWETPSQNTAQLDQFDRIKTLGTGSFGRVMLVKHKESGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMVMEYVAGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGYIQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFFADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFATTDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFTEF
  
Inhibitor
Name:
BDBM27250
Synonyms:
6-{[(1S,3R,4R)-3-(6-amino-9H-purin-9-yl)-4-hydroxycyclopentyl]formamido}-N-[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-carbamoylbutyl]carbamoyl}butyl]carbamoyl}butyl]carbamoyl}butyl]carbamoyl}butyl]carbamoyl}butyl]hexanamide | ARC-659-1b
Type:
Small organic molecule
Emp. Form.:
C53H97N31O9
Mol. Mass.:
1312.5396
SMILES:
[#7]\[#6](-[#7])=[#7]\[#6]-[#6]-[#6]-[#6@@H](-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](/[#7])-[#7])-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](/[#7])-[#7])-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](/[#7])-[#7])-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](\[#7])-[#7])-[#7]-[#6](=O)-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](\[#7])-[#7])-[#7]-[#6](=O)-[#6]-[#6]-[#6]-[#6]-[#6]-[#7]-[#6](=O)-[#6@@H]-1-[#6]-[#6@@H](-[#8])-[#6@@H](-[#6]-1)-n1cnc2c(-[#7])ncnc12)-[#6](-[#7])=O |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Kemptide
Synonyms:
Aurora Peptide Substrate
Type:
Peptide
Mol. Mass.:
773.92
Organism:
n/a
Description:
50 uM ATP as co-substrate.
Residue:
7
Sequence:
LRRASLG