Compile Data Set for Download or QSAR
Report error Found 1291 Enz. Inhib. hit(s) with Target = 'cAMP-dependent protein kinase catalytic subunit alpha'
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50599148(CHEMBL5188777)
Affinity DataKd:  0.00500nMAssay Description:Displacement of ARC-1063 fluorescent probe from recombinant human PKAC-alpha assessed as dissociation equilibrium constant preincubated for 1 hr foll...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50599153(CHEMBL5196521)
Affinity DataKi:  0.00700nMAssay Description:Covalent inhibition of human recombinant PKAC-alpha assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50599147(CHEMBL5201435)
Affinity DataKd:  0.0190nMAssay Description:Displacement of ARC-1063 fluorescent probe from recombinant human PKAC-alpha assessed as dissociation equilibrium constant preincubated for 1 hr foll...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50599152(CHEMBL5179794)
Affinity DataKi:  0.0230nMAssay Description:Covalent inhibition of human recombinant PKAC-alpha assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50587772(CHEMBL5185265)
Affinity DataKd:  0.0420nMAssay Description:Displacement of mAb(D38C6)-BTN from human recombinant PKAc alpha incubated for 15 mins by microplate reader assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM258601(US9493490, Example 13 | US9493490, 6-(4-(aminometh...)
Affinity DataIC50: 0.0550nMT: 2°CAssay Description:Phosphorylation of activity of ROCK1 and ROCK2 and those of other kinases, AKT1, GRK2, PKA, PKCa and RSK1 were performed by Reaction Biology (Malvern...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2017
Entry Details
US Patent

LigandPNGBDBM50188913(N-((S)-1-amino-3-(2,4-dichlorophenyl)propan-2-yl)-...)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of PKAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM27226((2R)-6-amino-2-(6-{[(2S,3S,4R,5R)-5-(6-amino-9H-pu...)
Affinity DataKd:  0.5nMpH: 7.5 T: 2°CAssay Description:The assay is based on the kinase-bound labeled fluorescent probe can be displaced by competitive inhibitors, which can be registered by measurement o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2009
Entry Details Article
PubMed
LigandPNGBDBM27227((2R)-6-amino-2-(6-{[(2S,3S,4R,5R)-5-(6-amino-9H-pu...)
Affinity DataKd: <0.5nMpH: 7.5 T: 2°CAssay Description:The assay is based on the kinase-bound labeled fluorescent probe can be displaced by competitive inhibitors, which can be registered by measurement o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2009
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50599149(CHEMBL5174535)
Affinity DataKi:  0.630nMAssay Description:Covalent inhibition of human recombinant PKAC-alpha assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50599146(CHEMBL5189362)
Affinity DataKd:  0.630nMAssay Description:Displacement of ARC-1063 fluorescent probe from recombinant human PKAC-alpha assessed as dissociation equilibrium constant preincubated for 1 hr foll...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM139540(US8889696, Staurosporine | US9051313, Staurosporin...)
Affinity DataIC50: 0.678nMAssay Description:Compounds as a powder were dissolved in dimethyl sulfoxide to make a 10 mM stock. Compounds were tested in 10-dose IC50 triplicate mode with a 3-fold...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/7/2024
Entry Details
US Patent

LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of PKAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 0.935nMAssay Description:Inhibition of human PKA using LCGRTGRRNSI as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
LigandPNGBDBM50044004(CHEMBL3356433)
Affinity DataIC50: 1nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
LigandPNGBDBM16958(6-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]-2-eth...)
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:The kinase assay uses purified recombinant enzyme and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2007
Entry Details Article
PubMed
LigandPNGBDBM50117503(CHEMBL3613621)
Affinity DataIC50: 1nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
LigandPNGBDBM50117504(CHEMBL3613620)
Affinity DataIC50: 1nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
LigandPNGBDBM50117489(CHEMBL3613598)
Affinity DataIC50: 1nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
LigandPNGBDBM50117631(CHEMBL3613610)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 1.58nMAssay Description:Inhibition of human PKACA using LCGRTGRRNSI as substrate in presence of [gamma-32P]ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2020
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM258598(US9493490, Example 10 | US9493490, G)
Affinity DataIC50: 1.79nMT: 2°CAssay Description:Phosphorylation of activity of ROCK1 and ROCK2 and those of other kinases, AKT1, GRK2, PKA, PKCa and RSK1 were performed by Reaction Biology (Malvern...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2017
Entry Details
US Patent

LigandPNGBDBM27229(6-{[(1S,3R,4R)-3-(6-amino-9H-purin-9-yl)-4-hydroxy...)
Affinity DataKd:  1.80nMpH: 7.5 T: 2°CAssay Description:The assay is based on the kinase-bound labeled fluorescent probe can be displaced by competitive inhibitors, which can be registered by measurement o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2009
Entry Details Article
PubMed
LigandPNGBDBM11823(N-[(3R,4R)-4-({4-[(2-fluoro-6-hydroxy-3-methoxyphe...)
Affinity DataIC50: 2nMpH: 7.2 T: 2°CAssay Description:In this assay, a fluorescent phosphopeptide tracer and the nonfluorescent phosphopeptides generated during a PKA reaction compete for binding to an a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2006
Entry Details Article
PubMed
LigandPNGBDBM15067(13a (S-) | 6-{5-[(2S)-2-amino-3-(1H-indol-3-yl)pro...)
Affinity DataIC50: 2.10nMAssay Description:The kinase assay uses purified recombinant enzyme and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2007
Entry Details Article
PubMed
LigandPNGBDBM50117632(CHEMBL3613609)
Affinity DataIC50: 2.20nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 2.30nMAssay Description:Inhibition of PKACalpha (unknown origin) incubated for 1 hr by spectrophotometric analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/26/2017
Entry Details Article
PubMed
LigandPNGBDBM27250(6-{[(1S,3R,4R)-3-(6-amino-9H-purin-9-yl)-4-hydroxy...)
Affinity DataIC50: 2.41nMAssay Description:The IC50 values of the inhibitors corresponding to the concentration of the inhibitor decreasing the enzyme activity 50% were measured using fluoresc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50117370(CHEMBL3613599)
Affinity DataIC50: 2.60nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
LigandPNGBDBM50117299(CHEMBL3613605)
Affinity DataIC50: 2.70nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM258600(US9493490, Example 12 | US9493490, 6-(3-(aminometh...)
Affinity DataIC50: 3.38nMT: 2°CAssay Description:Phosphorylation of activity of ROCK1 and ROCK2 and those of other kinases, AKT1, GRK2, PKA, PKCa and RSK1 were performed by Reaction Biology (Malvern...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2017
Entry Details
US Patent

LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 3.60nMpH: 7.4 T: 2°CAssay Description:The kinase assay uses purified recombinant enzyme and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/30/2007
Entry Details Article
PubMed
LigandPNGBDBM50117629(CHEMBL3613612)
Affinity DataIC50: 3.80nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM3149(Acyclic Balanol Analog (-)-1 | 2-{[2,6-dihydroxy-4...)
Affinity DataIC50: 3.90nMAssay Description:Inhibition of human PKAC-alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM3149(Acyclic Balanol Analog (-)-1 | 2-{[2,6-dihydroxy-4...)
Affinity DataKd:  3.90nMAssay Description:Binding affinity to PKAalpha (unknown origin) using Lys-Arg-Thr-Leu-Arg-Arg as substrate after 8 mins in presence of [gamma-32P]ATP by liquid scintil...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2018
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM773718(D0157 | US20250299772, Compound 16)
Affinity DataIC50: 4nMAssay Description:Compounds were tested in biochemical protein-protein interaction assays to determine if they can specifically block the interaction between the extra...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
TBA
Entry Details
US Patent

LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 4nMAssay Description:Inhibition of Protein kinase AMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM258595(US9493490, Example 4 | US9493490, 6-(4-(aminomethy...)
Affinity DataIC50: 4.06nMT: 2°CAssay Description:Phosphorylation of activity of ROCK1 and ROCK2 and those of other kinases, AKT1, GRK2, PKA, PKCa and RSK1 were performed by Reaction Biology (Malvern...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/20/2017
Entry Details
US Patent

TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM224009(ARC-3430)
Affinity DataKd:  4.10nMpH: 7.5Assay Description:All measurements were performed in HEPES (50 mm, pH 7.5) containing NaCl (150 mm), Tween-20 (0.005%) and DTT (5 mm) according to a previously publish...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/7/2017
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50599151(CHEMBL5172486)
Affinity DataKi:  4.20nMAssay Description:Covalent inhibition of human recombinant PKAC-alpha assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50599145(CHEMBL5179913)
Affinity DataKd:  4.20nMAssay Description:Displacement of ARC-1063 fluorescent probe from recombinant human PKAC-alpha assessed as dissociation equilibrium constant preincubated for 1 hr foll...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50311410(N-((5S,8R,11R,14R,17R,20R,23R,33R)-1-amino-33-(4-a...)
Affinity DataIC50: 4.90nMAssay Description:Inhibition of PKACalpha in presence of 1000 uM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/17/2010
Entry Details Article
PubMed
LigandPNGBDBM16564((2S)-1-{[5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl]...)
Affinity DataIC50: 5nMAssay Description:The kinase assay uses purified recombinant enzyme and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/17/2007
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM2683(2-[1-(3-dimethylaminopropyl)-indol-3-yl]-3-(indol-...)
Affinity DataIC50: 5nMAssay Description:Inhibition of human PKAC-alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
LigandPNGBDBM11822((3R,4R)-3-(pyridine-4-amido)azepan-4-yl 4-[(2-fluo...)
Affinity DataIC50: 5nMpH: 7.2 T: 2°CAssay Description:In this assay, a fluorescent phosphopeptide tracer and the nonfluorescent phosphopeptides generated during a PKA reaction compete for binding to an a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2006
Entry Details Article
PubMed
LigandPNGBDBM16954(6-{5-[(2S)-2-amino-3-(1H-indol-3-yl)propoxy]-2-chl...)
Affinity DataIC50: 5nMpH: 7.5 T: 2°CAssay Description:The kinase assay uses purified recombinant enzyme and a biotinylated peptide as substrate. The biotinylated peptides were immobilized on streptavidi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2007
Entry Details Article
PubMed
LigandPNGBDBM2685(3-(1H-indol-3-yl)-4-{1-[2-(piperidin-2-yl)ethyl]-1...)
Affinity DataIC50: 5nMAssay Description:IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2004
Entry Details
PubMed
LigandPNGBDBM50117630(CHEMBL3613611)
Affinity DataIC50: 5.10nMAssay Description:Inhibition of PKA (unknown origin) by radiometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50199310(2S,3S,4R,5R)-5-6-amino-9H-purin-9-yl)-N-12R,15R,18...)
Affinity DataIC50: 5.30nMAssay Description:Inhibitory potency towards human cAPK C alpha in the presence of 100 uM ATP and 30 uM TAMRA-kemptideMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetcAMP-dependent protein kinase catalytic subunit alpha(Human)
University of Tartu

Curated by ChEMBL
LigandPNGBDBM50199310(2S,3S,4R,5R)-5-6-amino-9H-purin-9-yl)-N-12R,15R,18...)
Affinity DataIC50: 5.30nMAssay Description:Inhibitory potency towards human cAPK C alpha in the presence of 100 uM ATP and 30 uM TAMRA-kemptideMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
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