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TargetcAMP-dependent protein kinase catalytic subunit alpha/beta/gamma
LigandBDBM50204694
Substrate/Competitorn/a
Meas. Tech.ChEMBL_442106 (CHEMBL891244)
IC50>50000±n/a nM
Citation Tong, YClaiborne, AStewart, KDPark, CKovar, PChen, ZCredo, RBGu, WZGwaltney, SLJudge, RAZhang, HRosenberg, SHSham, HLSowin, TJLin, NH Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Bioorg Med Chem15:2759-67 (2007) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
cAMP-dependent protein kinase catalytic subunit alpha/beta/gamma
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:
MGNAATAKKGSEVESVKEFLAKAKEDFLKKWENPTQNNAGLEDFERKKTLGTGSFGRVML
VKHKATEQYYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVRLEYAFKDNSNLYMV
MEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDHQGY
IQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFF
ADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVSDIKTHKWFAT
TDWIAIYQRKVEAPFIPKFRGSGDTSNFDDYEEEDIRVSITEKCAKEFGEF
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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:
MGNAAAAKKGSEQESVKEFLAKAKEDFLKKWESPAQNTAHLDQFERIKTLGTGSFGRVML
VKHKETGNHYAMKILDKQKVVKLKQIEHTLNEKRILQAVNFPFLVKLEFSFKDNSNLYMV
MEYVPGGEMFSHLRRIGRFSEPHARFYAAQIVLTFEYLHSLDLIYRDLKPENLLIDQQGY
IQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAAGYPPFF
ADQPIQIYEKIVSGKVRFPSHFSSDLKDLLRNLLQVDLTKRFGNLKNGVNDIKNHKWFAT
TDWIAIYQRKVEAPFIPKFKGPGDTSNFDDYEEEEIRVSINEKCGKEFSEF
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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:
MGNAPAKKDTEQEESVNEFLAKARGDFLYRWGNPAQNTASSDQFERLRTLGMGSFGRVML
VRHQETGGHYAMKILNKQKVVKMKQVEHILNEKRILQAIDFPFLVKLQFSFKDNSYLYLV
MEYVPGGEMFSRLQRVGRFSEPHACFYAAQVVLAVQYLHSLDLIHRDLKPENLLIDQQGY
LQVTDFGFAKRVKGRTWTLCGTPEYLAPEIILSKGYNKAVDWWALGVLIYEMAVGFPPFY
ADQPIQIYEKIVSGRVRFPSKLSSDLKHLLRSLLQVDLTKRFGNLRNGVGDIKNHKWFAT
TSWIAIYEKKVEAPFIPKYTGPGDASNFDDYEEEELRISINEKCAKEFSEF
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BDBM50204694
n/a
NameBDBM50204694
Synonyms:3-(4'-HYDROXYBIPHENYL-4-YL)-N-(4-HYDROXYCYCLOHEXYL)-1,4-DIHYDROINDENO[1,2-C]PYRAZOLE-6-CARBOXAMIDE | 3-(4'-hydroxy-biphenyl-4-yl)-1,4-dihydro-indeno[1,2-c]pyrazole-6-carboxylic acid (trans-4-hydroxycyclohexyl)-amide | 3-(4'-hydroxybiphenyl-4-yl)-N-((1r,4r)-4-hydroxycyclohexyl)-1,4-dihydroindeno[1,2-c]pyrazole-6-carboxamide | 3-(4'-hydroxybiphenyl-4-yl)-N-(trans-4-hydroxycyclohexyl)-2,4-dihydroindeno[1,2-c]pyrazole-6-carboxamide | CHEMBL438485
TypeSmall organic molecule
Emp. Form.C29H27N3O3
Mol. Mass.465.543
SMILESO[C@H]1CC[C@@H](CC1)NC(=O)c1ccc-2c(Cc3c(n[nH]c-23)-c2ccc(cc2)-c2ccc(O)cc2)c1 |wU:4.7,wD:1.0,(19.77,-1.9,;21.02,-1.01,;22.42,-1.66,;23.69,-.77,;23.53,.76,;22.14,1.41,;20.89,.52,;24.79,1.65,;26.19,1.01,;26.33,-.53,;27.44,1.9,;27.3,3.44,;28.55,4.33,;29.95,3.7,;30.1,2.15,;31.61,1.81,;32.4,3.14,;33.83,3.77,;33.68,5.31,;32.16,5.65,;31.37,4.31,;35.16,2.99,;35.15,1.44,;36.46,.66,;37.81,1.42,;37.82,2.96,;36.49,3.74,;39.13,.64,;39.12,-.9,;40.44,-1.67,;41.78,-.91,;43.11,-1.69,;41.78,.63,;40.46,1.4,;28.85,1.26,)|
Structure
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