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TargetcAMP-Dependent Protein Kinase (PKA)
LigandBDBM11823
Substrate/CompetitorPeptide Substrate
Meas. Tech.Fluorescence Polarization-based Assay
pH7.2±n/a
Temperature295.15±n/a K
IC50 2±n/a nM
Citation Breitenlechner, CBWegge, TBerillon, LGraul, KMarzenell, KFriebe, WGThomas, USchumacher, RHuber, REngh, RAMasjost, B Structure-based optimization of novel azepane derivatives as PKB inhibitors. J Med Chem47:1375-90 (2004) [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
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BDBM11823
NameBDBM11823
Synonyms:Azepane Derivative 4 | N-((3R,4R)-4-{[4-(2-fluoro-6-hydroxy-3-methoxybenzoyl)benzoyl]amino}azepan-3-yl)isonicotinamide dihydrochloride | N-[(3R,4R)-4-({4-[(2-fluoro-6-hydroxy-3-methoxyphenyl)carbonyl]benzene}amido)azepan-3-yl]pyridine-4-carboxamide dihydrochloride
TypeSmall organic molecule
Emp. Form.C27H27FN4O5
Mol. Mass.506.5255
SMILESCOc1ccc(O)c(C(=O)c2ccc(cc2)C(=O)N[C@@H]2CCCNC[C@H]2NC(=O)c2ccncc2)c1F |r|
Structure
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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