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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM16591
Substrate
Kemptide
Meas. Tech.
Kinase assays for IC50 determinations
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
190±n/a nM
Citation
 Foloppe, N; Fisher, LM; Francis, G; Howes, R; Kierstan, P; Potter, A Identification of a buried pocket for potent and selective inhibition of Chk1: prediction and verification. Bioorg Med Chem 14:1792-804 (2006) [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:
BDBM16591
Synonyms:
(4Z)-4-(2-amino-5-oxo-3,5-dihydro-4H-imidazol-4-ylidene)-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8(1H)-one | 2-amino-5-[(4Z)-8-oxo-1H,4H,5H,6H,7H,8H-pyrrolo[2,3-c]azepin-4-ylidene]-4,5-dihydro-1H-imidazol-4-one | B722657K110 | CHEMBL255465 | Debromohymenialdisine (DBH) | Hymenialdisine, 8 | NSC607174
Type:
Small organic molecule
Emp. Form.:
C11H11N5O2
Mol. Mass.:
245.2373
SMILES:
NC1=NC(=O)C(N1)=C1CCNC(=O)c2[nH]ccc12 |w:7.18,t:1|
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