BDBM50173320 GSK-180736A::GSK180736A::US10023564, Compound GSK180736A

SMILES CC1=C(C(NC(=O)N1)c1ccc(F)cc1)C(=O)Nc1ccc2[nH]ncc2c1

InChI Key InChIKey=HEAIGWIZTYAQTC-UHFFFAOYSA-N

Data  16 IC50

  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 16 hits for monomerid = 50173320   

TargetG protein-coupled receptor kinase 5(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of GRK5 (unknown origin) using tubulin as substrate by SDS-PAGE methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/7/2017
Entry Details Article
PubMed
TargetRhodopsin kinase GRK1(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of GRK1 (unknown origin) using tubulin as substrate by SDS-PAGE methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/7/2017
Entry Details Article
PubMed
TargetRho-associated protein kinase 1(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 100nMAssay Description:Inhibition of ROCK1 (unknown origin) by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/7/2017
Entry Details Article
PubMed
TargetG protein-coupled receptor kinase 5(Bovine)
University of Messina

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of bovine GRK5 assessed as decrease in phosphorylation of tubulin after 5 mins by SDS-PAGE analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2018
Entry Details Article
PubMed
TargetRhodopsin kinase GRK1(Bovine)
University of Messina

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 1.00E+6nMAssay Description:Inhibition of bovine GRK1 (1 to 535 residues) assessed as decrease in phosphorylation of tubulin after 5 mins by SDS-PAGE analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2018
Entry Details Article
PubMed
TargetRhodopsin kinase GRK1(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 1.00E+5nMpH: 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
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 770nMpH: 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)
Temple University

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 1.00E+5nMpH: 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

TargetRho-associated protein kinase 1(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 78nMAssay Description:Rho-associated coiled-coil kinase (ROCK) assays were performed with the ADP-Glo system using 0.1 μg ROCK1 and 1 μg S6K substrate, and 100 &...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(Bovine)
University of Messina

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of bovine GRK5 after 5 mins after 5 mins in presence of ATP by phosphorimaging assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2020
Entry Details Article
PubMed
TargetBeta-adrenergic receptor kinase 1(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 770nMAssay Description:Inhibition of GRK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2020
Entry Details Article
PubMed
TargetRhodopsin kinase GRK1(Bovine)
University of Messina

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of bovine GRK1 (1 to 535 residues) after 5 mins after 5 mins in presence of ATP by phosphorimaging assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2020
Entry Details Article
PubMed
TargetBeta-adrenergic receptor kinase 1(Bovine)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 770nMAssay Description:Inhibition of bovine GRK2 S670A mutant after 5 mins in presence of ATP by phosphorimaging assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2020
Entry Details Article
PubMed
TargetBeta-adrenergic receptor kinase 1(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 770nMAssay Description:Inhibition of GRK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetBeta-adrenergic receptor kinase 1(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 770nMAssay Description:Inhibition of GRK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetBeta-adrenergic receptor kinase 1(Human)
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50173320(GSK-180736A | GSK180736A | US10023564, Compound GS...)
Affinity DataIC50: 390nMAssay Description:Inhibition of GRK2 (unknown origin) using CRRREEEEESAAA as substrate measured for 120 mins in presence of ATP by ADP-glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed