Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetcAMP-Dependent Protein Kinase (PKA)
LigandBDBM11818
Substrate/CompetitorPeptide Substrate
Meas. Tech.Fluorescence Polarization-based Assay
pH7.2±n/a
Temperature295.15±n/a K
IC50 2400±1800 nM
Citation Breitenlechner, CBFriebe, WGBrunet, EWerner, GGraul, KThomas, UKunkele, KPSchafer, WGassel, MBossemeyer, DHuber, REngh, RAMasjost, B Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants. J Med Chem48:163-70 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
cAMP-Dependent Protein Kinase (PKA)
Name:cAMP-dependent protein kinase A
Synonyms:PKA C-alpha | PKC | Protein Kinase C | Protein Kinase C, bovine brain | 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:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWENPAQNTAHLDQFERIKTLGTGSFGRVML
VKHMETGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMV
MEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGY
IQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFF
ADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFAT
TDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFSEF
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM11818
NameBDBM11818
Synonyms:(3R,4R)-N-(4-{4-[3-(3,3-dimethylpiperidin-2-yl)-2-fluoro-6-hydroxybenzoyl]benzoylamino}azepan-3-yl)isonicotinamide hydrochloride | N-[(3R,4R)-4-[(4-{[3-(3,3-dimethylpiperidin-2-yl)-2-fluoro-6-hydroxyphenyl]carbonyl}benzene)amido]azepan-3-yl]pyridine-4-carboxamide hydrochloride | Protein Kinase B-Selective Inhibitor 2
TypeSmall organic molecule
Emp. Form.C33H38FN5O4
Mol. Mass.587.6843
SMILESCC1(C)CCCNC1c1ccc(O)c(C(=O)c2ccc(cc2)C(=O)N[C@@H]2CCCNC[C@H]2NC(=O)c2ccncc2)c1F |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
Peptide Substrate
Name:Peptide Substrate
Synonyms:biotinylated tridecapeptide substrate
Type:Peptide
Mol. Mass.:1564.86
Organism:n/a
Description:n/a
Residue:13
Sequence:
RFARKGSLRQKNV