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Target
cAMP-dependent protein kinase catalytic subunit alpha/beta/gamma
Ligand
BDBM50179207
Substrate
n/a
Meas. Tech.
ChEMBL_325234 (CHEMBL861595)
IC50
>100000±n/a nM
Citation
 Ho, CY; Ludovici, DW; Maharoof, US; Mei, J; Sechler, JL; Tuman, RW; Strobel, ED; Andraka, L; Yen, HK; Leo, G; Li, J; Almond, H; Lu, H; DeVine, A; Tominovich, RM; Baker, J; Emanuel, S; Gruninger, RH; Middleton, SA; Johnson, DL; Galemmo, RA (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. J Med Chem 48:8163-73 (2005) [PubMed]  Article 
Target
Name:
cAMP-dependent protein kinase catalytic subunit alpha/beta/gamma
Synonyms:
cAMP-dependent protein kinase (PKA)
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 catalytic subunit beta
Synonyms:
KAPCB_HUMAN | PKA C-beta | PKAC-beta | PRKACB | cAMP-dependent protein kinase (PKA) | 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:
MGNAATAKKGSEVESVKEFLAKAKEDFLKKWENPTQNNAGLEDFERKKTLGTGSFGRVMLVKHKATEQYYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVRLEYAFKDNSNLYMVMEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDHQGYIQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFFADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVSDIKTHKWFATTDWIAIYQRKVEAPFIPKFRGSGDTSNFDDYEEEDIRVSITEKCAKEFGEF
  
Component 2
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
  
Component 3
Name:
cAMP-dependent protein kinase catalytic subunit gamma
Synonyms:
KAPCG_HUMAN | PKA C-gamma | PRKACG | cAMP-dependent protein kinase (PKA) | cAMP-dependent protein kinase catalytic subunit gamma
Type:
PROTEIN
Mol. Mass.:
40442.03
Organism:
Homo sapiens (Human)
Description:
ChEMBL_104720
Residue:
351
Sequence:
MGNAPAKKDTEQEESVNEFLAKARGDFLYRWGNPAQNTASSDQFERLRTLGMGSFGRVMLVRHQETGGHYAMKILNKQKVVKMKQVEHILNEKRILQAIDFPFLVKLQFSFKDNSYLYLVMEYVPGGEMFSRLQRVGRFSEPHACFYAAQVVLAVQYLHSLDLIHRDLKPENLLIDQQGYLQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAVGFPPFYADQPIQIYEKIVSGRVRFPSKLSSDLKHLLRSLLQVDLTKRFGNLRNGVGDIKNHKWFATTSWIAIYEKKVEAPFIPKYTGPGDASNFDDYEEEELRISINEKCAKEFSEF
  
Inhibitor
Name:
BDBM50179207
Synonyms:
3-fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine | CHEMBL120077 | JNJ-10198409
Type:
Small organic molecule
Emp. Form.:
C18H16FN3O2
Mol. Mass.:
325.3369
SMILES:
COc1cc2Cc3c(Nc4cccc(F)c4)[nH]nc3-c2cc1OC
Structure:
Search PDB for entries with ligand similarity: