BDBM385170 US10287267, Compound 330::US10508099, Compound 330::US10556885, Compound 330::US11174244, Compound 330::US11673881, Compound 330

SMILES Cn1cc(cn1)-c1ccc2cnc(NC(=O)C3CCN(CC3)S(C)(=O)=O)cc2c1

InChI Key InChIKey=GXCOUFPTCZUTEE-UHFFFAOYSA-N

Data  15 IC50  3 Kd  12 EC50

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

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 30 hits for monomerid = 385170   

TargetDual specificity protein kinase CLK2(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 90nMAssay Description:Inhibition of recombinant human CLK2 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
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataKd:  3.70nMAssay 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 protein kinase CLK1(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataKd:  0.620nMAssay 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
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataKd:  0.101nMAssay 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 tyrosine-phosphorylation-regulated kinase 1B(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 4.80nMAssay 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 tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 1.80nMAssay 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 protein kinase CLK1(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 21nMAssay 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
TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 197nMAssay 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
TargetDual specificity tyrosine-phosphorylation-regulated kinase 4(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 612nMAssay Description:Inhibition of recombinant human DYRK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scint...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 3(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 209nMAssay Description:Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scint...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 37nMAssay Description:Inhibition of recombinant human DYRK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scint...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
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 10nMAssay 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
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 4.70nMAssay 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
TargetDual specificity protein kinase CLK4(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 14nMAssay 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
TargetDual specificity protein kinase CLK3(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 681nMAssay Description:Inhibition of recombinant human CLK3 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
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataEC50:  15nMAssay 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
Go to US Patent

TargetDual specificity protein kinase CLK1(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 38nMAssay Description:Inhibition of recombinant human CLK1 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
TargetCasein kinase I isoform epsilon(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of recombinant human CK1epsilon expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataIC50: 1.79E+3nMAssay Description:Inhibition of recombinant human CDK5/p25 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric sc...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
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataEC50:  15nMAssay 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
Go to US Patent

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

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
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
Go to US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataEC50:  15nMAssay 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
Go to US Patent

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

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
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
Go to US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataEC50:  15nMAssay 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
Go to US Patent

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

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
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
Go to US Patent

TargetGlycogen synthase kinase-3 beta(Human)
Perha Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataEC50:  15nMAssay 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
Go to US Patent

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

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
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
Go to US Patent

TargetProto-oncogene Wnt-1(Human)
Samumed

US Patent
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataEC50:  449nMAssay Description:SW480 colon carcinoma cells were transduced with a lentiviral vector expressing luciferase with a human Sp5 promoter consisting of a sequence of eigh...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2020
Entry Details
Go to US Patent

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

Curated by ChEMBL
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
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
Go to US Patent

TargetProto-oncogene Wnt-1(Human)
Samumed

US Patent
LigandPNGBDBM385170(US10287267, Compound 330 | US10556885, Compound 33...)
Affinity DataEC50:  449nMAssay Description:The screening assay for Wnt activity is described as follows. Reporter cell lines can be generated by stably transducing cancer cell lines (e.g., col...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2020
Entry Details
Go to US Patent