Reaction Details Report a problem with these data
Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM6751
Substrate
Lysine-rich histone
Meas. Tech.
CDK Kinase Inhibition Assay
Temperature
298.15±n/a K
IC50
>2000±n/a nM
Comments
extracted
Citation
 Zhu, G; Conner, SE; Zhou, X; Chan, HK; Shih, C; Engler, TA; Al-Awar, RS; Brooks, HB; Watkins, SA; Spencer, CD; Schultz, RM; Dempsey, JA; Considine, EL; Patel, BR; Ogg, CA; Vasudevan, V; Lytle, ML Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors. Bioorg Med Chem Lett 14:3057-61 (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:
BDBM6751
Synonyms:
1,7-Annulated indolocarbazole deriv. 13Af | 26-(hydroxymethyl)-1,15-diazaheptacyclo[17.7.1.0^{2,18}.0^{3,12}.0^{6,11}.0^{13,17}.0^{23,27}]heptacosa-2(18),3(12),4,6(11),7,9,13(17),19(27),20,22-decaene-14,16-dione
Type:
Small organic molecule
Emp. Form.:
C26H18N2O3
Mol. Mass.:
406.4327
SMILES:
OCC1CCc2cccc3c4c5C(=O)NC(=O)c5c5c(ccc6ccccc56)c4n1c23
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