BDBM284001 E27::US10023564, Example 27

SMILES COc1ccccc1C(C)NC(=O)c1cc(ccc1F)C1NC(=O)NC(C)=C1C(=O)Nc1ccc2[nH]ncc2c1

InChI Key InChIKey=UWIYUJKCXJAORH-UHFFFAOYSA-N

Data  6 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 284001   

TargetRhodopsin kinase GRK1(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM284001(US10023564, Example 27 | E27)
Affinity DataIC50: 1.40E+4nMpH: 7.0Assay Description:GRK1, 2 and 5 kinetic assays were conducted in a buffer containing 20 mM HEPES pH 7.0, 5 μM ATP, 2 mM MgCl2, and 0.025% DDM with 50 nM GRK and e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/10/2019
Entry Details
Go to US Patent

TargetBeta-adrenergic receptor kinase 1(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM284001(US10023564, Example 27 | E27)
Affinity DataIC50: 320nMpH: 7.0Assay Description:GRK1, 2 and 5 kinetic assays were conducted in a buffer containing 20 mM HEPES pH 7.0, 5 μM ATP, 2 mM MgCl2, and 0.025% DDM with 50 nM GRK and e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/10/2019
Entry Details
Go to US Patent

TargetG protein-coupled receptor kinase 5(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM284001(US10023564, Example 27 | E27)
Affinity DataIC50: 2.40E+3nMpH: 7.0Assay Description:GRK1, 2 and 5 kinetic assays were conducted in a buffer containing 20 mM HEPES pH 7.0, 5 μM ATP, 2 mM MgCl2, and 0.025% DDM with 50 nM GRK and e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/10/2019
Entry Details
Go to US Patent

TargetG protein-coupled receptor kinase 5(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM284001(US10023564, Example 27 | E27)
Affinity DataIC50: 2.80E+3nMAssay Description:Inhibition of GRK5 (unknown origin) preincubated for 10 mins followed by peptide substrate and ATP addition measured after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetBeta-adrenergic receptor kinase 1(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM284001(US10023564, Example 27 | E27)
Affinity DataIC50: 400nMAssay Description:Inhibition of GRK2 (unknown origin) preincubated for 10 mins followed by peptide substrate and ATP addition measured after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetRhodopsin kinase GRK1(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM284001(US10023564, Example 27 | E27)
Affinity DataIC50: 1.60E+4nMAssay Description:Inhibition of GRK1 (unknown origin) preincubated for 10 mins followed by peptide substrate and ATP addition measured after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed