Reaction Details Report a problem with these data
Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM6717
Substrate
Lysine-rich histone
Meas. Tech.
CDK Kinase Inhibition Assay
Temperature
298.15±n/a K
IC50
40±n/a nM
Comments
extracted
Citation
 Al-awar, RS; Ray, JE; Hecker, KA; Joseph, S; Huang, J; Shih, C; Brooks, HB; Spencer, CD; Watkins, SA; Schultz, RM; Considine, EL; Faul, MM; Sullivan, KA; Kolis, SP; Carr, MA; Zhang, F Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors. Bioorg Med Chem Lett 14:3925-8 (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:
BDBM6717
Synonyms:
1,4,14,24-tetraazaheptacyclo[16.10.1.0^{2,17}.0^{3,11}.0^{5,10}.0^{12,16}.0^{22,29}]nonacosa-2(17),3(11),5(10),6,8,12(16),18(29),19,21-nonaene-13,15-dione hydrochloride | aza-1,7-annulated indole deriv. 28
Type:
Small organic molecule
Emp. Form.:
C25H20N4O2
Mol. Mass.:
408.4519
SMILES:
O=C1NC(=O)c2c1c1c3ccccc3[nH]c1c1n3CCCCNCc4cccc(c34)c21
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Lysine-rich histone
Synonyms:
ING Peptide | Lys-rich histone | histone type IIIS
Type:
Peptide
Mol. Mass.:
10508.21
Organism:
Bos taurus (bovine)
Description:
Purified as a lysine rich fraction of histone H1 from calf thymus.
Residue:
105
Sequence:
SETAPAAPAAAPPAEKTPVKKKAAKKPAGARRKASGPPVSELITKAVAASKERSGVSLAALKKALAAAGYDVEKNNSRIKLGLKSLVSKGTLVQTKGTGASGSFK