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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM3232
Substrate
Histone type HL
Meas. Tech.
PKA assay
IC50
500±n/a nM
Citation
Lampe, JW; Biggers, CK; Defauw, JM; Foglesong, RJ; Hall, SE; Heerding, JM; Hollinshead, SP; Hu, H; Hughes, PF; Jagdmann, GE; Johnson, MG; Lai, YS; Lowden, CT; Lynch, MP; Mendoza, JS; Murphy, MM; Wilson, JW; Ballas, LM; Carter, K; Darges, JW; Davis, JE; Hubbard, FR; Stamper, ML Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits. J Med Chem 45:2624-43 (2002) [PubMed] Article
More Info.:
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:
BDBM3232
Synonyms:
(1R,2R)-2-[(4-hydroxybenzene)amido]cyclopentyl 4-[(2-cyano-6-hydroxyphenyl)carbonyl]-3,5-dihydroxybenzoate | Modified Benzophenone Carboxylic Acid, Balanol Analog 32 | trans-2-[4-(6-Hydroxy-2-nitrilobenzoyl)-3,5-dihydroxybenzoyloxy]-1-(4-hydroxybenzamido)cyclopentane
Type:
Small organic molecule
Emp. Form.:
C27H22N2O8
Mol. Mass.:
502.4722
SMILES:
Oc1ccc(cc1)C(=O)N[C@@H]1CCC[C@H]1OC(=O)c1cc(O)c(C(=O)c2c(O)cccc2C#N)c(O)c1 |r|
Substrate
Name:
Histone type HL
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
358.43
Organism:
n/a
Description:
unfractionated histone (Worthington)
30 uM [gamma-32P]ATP as co-substrate.
Residue:
3
Sequence:
NA