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TargetcAMP-dependent protein kinase (PKA)
LigandBDBM50126732
Substrate/Competitorn/a
Meas. Tech.ChEMBL_161916
IC50>100000±n/a nM
Citation Goldberg DRButz TCardozo MGEckner RJHammach AHuang JJakes SKapadia SKashem MLukas SMorwick TMPanzenbeck MPatel UPav SPeet GWPeterson JDProkopowicz ASSnow RJSellati RTakahashi HTan JTschantz MAWang XJWang YWolak JXiong PMoss N Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase. J Med Chem 46:1337-49 (2003) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
cAMP-dependent protein kinase (PKA)
Name:cAMP-dependent protein kinase (PKA)
Synonyms:n/a
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 217489
Components:This complex has 3 components.
Component 1
Name:cAMP-dependent protein kinase (PKA)
Synonyms:PKA C-beta | PKAC-beta | cAMP-dependent protein kinase beta-1 catalytic subunit | cAMP-dependent protein kinase catalytic subunit beta
Type:PROTEIN
Mol. Mass.:40631.25
Organism:Homo sapiens (Human)
Description:ChEMBL_586348
Residue:351
Sequence:
MGNAATAKKGSEVESVKEFLAKAKEDFLKKWENPTQNNAGLEDFERKKTLGTGSFGRVML
VKHKATEQYYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVRLEYAFKDNSNLYMV
MEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDHQGY
IQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFF
ADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVSDIKTHKWFAT
TDWIAIYQRKVEAPFIPKFRGSGDTSNFDDYEEEDIRVSITEKCAKEFGEF
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Component 2
Name:cAMP-dependent protein kinase (PKA)
Synonyms:PKA C-alpha | 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:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWESPAQNTAHLDQFERIKTLGTGSFGRVML
VKHKETGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMV
MEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGY
IQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFF
ADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFAT
TDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFSEF
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Component 3
Name:cAMP-dependent protein kinase (PKA)
Synonyms:PKA C-gamma | PRKACG | cAMP-dependent protein kinase catalytic subunit gamma
Type:PROTEIN
Mol. Mass.:40442.03
Organism:Homo sapiens (Human)
Description:ChEMBL_104720
Residue:351
Sequence:
MGNAPAKKDTEQEESVNEFLAKARGDFLYRWGNPAQNTASSDQFERLRTLGMGSFGRVML
VRHQETGGHYAMKILNKQKVVKMKQVEHILNEKRILQAIDFPFLVKLQFSFKDNSYLYLV
MEYVPGGEMFSRLQRVGRFSEPHACFYAAQVVLAVQYLHSLDLIHRDLKPENLLIDQQGY
LQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAVGFPPFY
ADQPIQIYEKIVSGRVRFPSKLSSDLKHLLRSLLQVDLTKRFGNLRNGVGDIKNHKWFAT
TSWIAIYEKKVEAPFIPKYTGPGDASNFDDYEEEELRISINEKCAKEFSEF
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BDBM50126732
n/a
NameBDBM50126732
Synonyms:2-(2,6-Dichloro-phenylamino)-7-(3-diethylamino-propenyl)-1,6-dimethyl-1,8-dihydro-imidazo[4,5-h]isoquinolin-9-one | CHEMBL281957
TypeSmall organic molecule
Emp. Form.C25H27Cl2N5O
Mol. Mass.484.421
SMILESCCN(CC)CC=Cc1[nH]c(=O)c2c3n(C)c(Nc4c(Cl)cccc4Cl)nc3ccc2c1C |w:6.5|
Structure
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