Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM25472
Substrate
Kemptide
Meas. Tech.
PKA Inhibition Assay
pH
7.3±n/a
Temperature
295.15±n/a K
IC50
186±16 nM
Citation
 Feng, YYin, YWeiser, AGriffin, ECameron, MDLin, LRuiz, CSchürer, SCInoue, TRao, PVSchröter, TLograsso, P Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem 51:6642-5 (2008) [PubMed]  Article 
Target
Name:
cAMP-dependent protein kinase catalytic subunit alpha
Synonyms:
KAPCA_HUMAN | PKA C-alpha | PKACA | PRKACA | cAMP-dependent protein kinase (PKA) | cAMP-dependent protein kinase catalytic (PKA) | cAMP-dependent protein kinase catalytic subunit alpha | cAMP-dependent protein kinase catalytic subunit alpha (PKA) | cAMP-dependent protein kinase catalytic subunit alpha (PKACA) | cAMP-dependent protein kinase catalytic subunit alpha (PKAc) | cAMP-dependent protein kinase catalytic subunit alpha isoform 1 | cAMP-dependent protein kinase, alpha-catalytic subunit
Type:
Enzyme Catalytic Subunit
Mol. Mass.:
40598.73
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
351
Sequence:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWESPAQNTAHLDQFERIKTLGTGSFGRVMLVKHKETGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMVMEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGYIQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFFADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFATTDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFSEF
  
Inhibitor
Name:
BDBM25472
Synonyms:
CHEMBL519123 | N-[4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-2-carboxamide | US11759530, Compound Table1.7 | pyrazole-phenyl, 3
Type:
Small organic molecule
Emp. Form.:
C18H15N3O3
Mol. Mass.:
321.33
SMILES:
O=C(Nc1ccc(cc1)-c1cn[nH]c1)C1COc2ccccc2O1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Kemptide
Synonyms:
Aurora Peptide Substrate
Type:
Peptide
Mol. Mass.:
773.92
Organism:
n/a
Description:
50 uM ATP as co-substrate.
Residue:
7
Sequence:
LRRASLG