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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM27232
Substrate
BDBM27221
Meas. Tech.
Fluorescence Polarization-Based Binding Displacement Kinase Assay
pH
7.5±n/a
Temperature
303.15±n/a K
Kd
52100±1300 nM
Citation
Lavogina, D; Lust, M; Viil, I; König, N; Raidaru, G; Rogozina, J; Enkvist, E; Uri, A; Bossemeyer, D Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhibitors of basophilic protein kinases. J Med Chem 52:308-21 (2009) [PubMed] Article
Target
Name:
cAMP-dependent protein kinase catalytic subunit alpha
Synonyms:
KAPCA_MOUSE | PKA C-alpha | Pkaca | Prkaca | cAMP-Dependent Protein Kinase (PKA) | cAMP-dependent protein kinase catalytic subunit alpha | cAMP-dependent protein kinase, alpha-catalytic subunit
Type:
Enzyme Catalytic Unit
Mol. Mass.:
40579.18
Organism:
Mus musculus (mouse)
Description:
n/a
Residue:
351
Sequence:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWETPSQNTAQLDQFDRIKTLGTGSFGRVMLVKHKESGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMVMEYVAGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGYIQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFFADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFATTDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFTEF
Inhibitor
Name:
BDBM27232
Synonyms:
ARC-1056, 5 | [(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl N-(5-carbamoylpentyl)carbamate
Type:
Small organic molecule
Emp. Form.:
C17H25N7O6
Mol. Mass.:
423.4237
SMILES:
NC(=O)CCCCCNC(=O)OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cnc2c(N)ncnc12 |r|