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Target
cAMP-dependent protein kinase catalytic subunit alpha
Ligand
BDBM16589
Substrate
Kemptide
Meas. Tech.
Kinase assays for IC50 determinations
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
171719±38850 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:
BDBM16589
Synonyms:
4-[3-(1H-1,3-benzodiazol-2-yl)-1H-indazol-6-yl]-2-methoxyphenol | 4-[3-(1H-benzimidazol-2-yl)-1H-indazol-6-yl]-2-methoxyphenol | Indazole Compound 1
Type:
Small organic molecule
Emp. Form.:
C21H16N4O2
Mol. Mass.:
356.3773
SMILES:
COc1cc(ccc1O)-c1ccc2c(n[nH]c2c1)-c1nc2ccccc2[nH]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