Reaction Details Report a problem with these data
Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM10838
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
Temperature
303.15±n/a K
IC50
11000±n/a nM
Comments
extracted
Citation
 Gompel, M; Leost, M; De Kier Joffe, EB; Puricelli, L; Franco, LH; Palermo, J; Meijer, L Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum. Bioorg Med Chem Lett 14:1703-7 (2004) [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:
BDBM10838
Synonyms:
3-(2-aminopyrimidin-4-yl)-1H-indol-4-ol | Meridianin A
Type:
Small organic molecule
Emp. Form.:
C12H10N4O
Mol. Mass.:
226.234
SMILES:
Nc1nccc(n1)-c1c[nH]c2cccc(O)c12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone H1
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
n/a
Residue:
3
Sequence:
NA