BDBM385079 US10287267, Compound 1086::US10287267, Compound 1087::US10287267, Compound 77::US10287267, Compound 972::US10508099, Compound 972::US10556885, Compound 1087::US10604514, Compound 6::US11174244, Compound 972::US11673881, Compound 77

SMILES CC(C)CN1CCC(CC1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1

InChI Key InChIKey=OGPJOAYIAOEJAM-UHFFFAOYSA-N

Data  15 IC50  3 Kd  50 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 68 hits for monomerid = 385079   

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataKd:  0.283nMAssay Description:Binding affinity to human DYRK1A assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetDual specificity protein kinase CLK1(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataKd:  0.968nMAssay Description:Binding affinity to human CLK1 assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  1.60nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  1.60nMAssay Description:The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies a Divis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2022
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  1.60nMAssay Description:The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions. This is a non-radioactive...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  1.60nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  1.60nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  2.5nMAssay Description:The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions. This is a non-radioactive...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  2.5nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  2.5nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  2.5nMAssay Description:The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies a Divis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2022
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  2.5nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3nMAssay Description:The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies a Divis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2022
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3nMAssay Description:Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1 Kinase buffer to final concentrations of 0.19 μg/mL, 30 μ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3nMAssay Description:The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions. This is a non-radioactive...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3.5nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3.5nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3.5nMAssay Description:Each compound was dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3.5nMAssay Description:The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies a Divis...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2022
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  3.5nMAssay Description:The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions. This is a non-radioactive...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataIC50: 6nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataKd:  6.20nMAssay Description:Binding affinity to human GSK-3beta assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataIC50: 8nMAssay Description:Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataIC50: 9.70nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetDual specificity protein kinase CLK1(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataIC50: 15nMAssay Description:Inhibition of recombinant human CLK1 expressed in Sf9 insect cells using myelin basic protein as substrate incubated for 110 mins in presence of ATP ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataIC50: 15nMAssay Description:Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  24nMAssay Description:Each compound is dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  24nMAssay Description:The GSK3B kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies-a Divisio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetDual specificity protein kinase CLK4(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataIC50: 24nMAssay Description:Inhibition of recombinant human CLK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scinti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  24nMAssay Description:GSK3B: This is a non-radioactive assay using fluorescence resonance energy transfer (FRET) between coumarin and fluorescein to detect kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  24nMAssay Description:The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies a Di...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2022
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  24nMAssay Description:Each compound is dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  28nMAssay Description:GSK3B: This is a non-radioactive assay using fluorescence resonance energy transfer (FRET) between coumarin and fluorescein to detect kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  28nMAssay Description:Each compound is dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  28nMAssay Description:The GSK3B kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies-a Divisio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  28nMAssay Description:The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies a Di...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2022
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  28nMAssay Description:Each compound is dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  37nMAssay Description:GSK3B: This is a non-radioactive assay using fluorescence resonance energy transfer (FRET) between coumarin and fluorescein to detect kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/13/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  37nMAssay Description:Each compound is dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  37nMAssay Description:The GSK3B kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies-a Divisio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  37nMAssay Description:Each compound is dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  37nMAssay Description:The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies a Di...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2022
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataIC50: 46nMAssay Description:Inhibition of recombinant human GSK-3beta expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric s...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  51nMAssay Description:Briefly, recombinant GSK3β kinase, ATP and Ser/Thr peptide 09 are prepared in 1 Kinase buffer to final concentrations of 0.04 μg/mL, 46 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  64nMAssay Description:Each compound is dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  64nMAssay Description:Each compound is dissolved in DMSO as a 10 mM stock and used to prepare compound source plates. Serial dilution (1:3, 11-point dose-response curves f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2020
Entry Details
US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385079(US10287267, Compound 77 | US10287267, Compound 108...)
Affinity DataEC50:  64nMAssay Description:The GSK3B kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologies-a Divisio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/16/2023
Entry Details
US Patent

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