BDBM50466133 CHEMBL4292847::US11547712, Compound 3-1

SMILES O=c1[nH]c2ccc(cc2[nH]1)C1=NN=C(NCc2ccccc2)SC1

InChI Key InChIKey=PNJQHHXWPZEHTA-UHFFFAOYSA-N

Data  1 IC50  8 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 9 hits for monomerid = 50466133   

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50466133(CHEMBL4292847 | US11547712, Compound 3-1)
Affinity DataKd:  4.32E+3nMAssay Description:Inhibition of DYRK1A (unknown origin) using Alexa-Fluor tracer-647 by FRET-based LanthaScreen Eu kinase binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50466133(CHEMBL4292847 | US11547712, Compound 3-1)
Affinity DataKd:  4.50E+3nMAssay Description:Binding affinity to wild-type human partial length DYRK1A (H129 to S509 residues) expressed in mammalian expression system by Kinomescan methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50466133(CHEMBL4292847 | US11547712, Compound 3-1)
Affinity DataKd:  4.50E+3nMAssay Description:Compound 1, a 1,3,4-thiadiazine compound identified in a screening assay, was evaluated for testing of in vitro DYRK1A activity at 30 μM concent...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50466133(CHEMBL4292847 | US11547712, Compound 3-1)
Affinity DataKd:  7.30E+3nMAssay Description:Binding affinity to wild-type human partial length DYRK1A (H129 to S509 residues) expressed in mammalian expression system by Kinomescan methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50466133(CHEMBL4292847 | US11547712, Compound 3-1)
Affinity DataKd:  7.30E+3nMAssay Description:Binding affinity to DYRK1A (unknown origin) assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50466133(CHEMBL4292847 | US11547712, Compound 3-1)
Affinity DataKd:  7.30E+3nMAssay Description:Binding affinity to DYRK1A (unknown origin) assessed as dissociation constant by ADP hunter plus assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50466133(CHEMBL4292847 | US11547712, Compound 3-1)
Affinity DataKd:  7.30E+3nMAssay Description:Compound 1, a 1,3,4-thiadiazine compound identified in a screening assay, was evaluated for testing of in vitro DYRK1A activity at 30 μM concent...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details
US Patent

TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50466133(CHEMBL4292847 | US11547712, Compound 3-1)
Affinity DataIC50: 9.41E+3nMAssay Description:Inhibition of DYRK1A (unknown origin) at 1 uM by kinomescan methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50466133(CHEMBL4292847 | US11547712, Compound 3-1)
Affinity DataKd:  9.42E+3nMAssay Description:Inhibition of DYRK1A (unknown origin) using Alexa-Fluor tracer-647 by FRET-based LanthaScreen Eu kinase binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed