null
SMILES CCCn1c(CNc2cccc(c2)C(=O)NCc2c(F)cccc2F)nnc1-c1ccncn1
InChI Key InChIKey=VWBSMGFTNCQOMB-UHFFFAOYSA-N
PDB links: 1 PDB ID matches this monomer.
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 11 hits for monomerid = 50173313
Affinity DataIC50: 2.20E+3nMAssay Description:Inhibition of GRK5 (unknown origin) using tubulin as substrate by SDS-PAGE methodMore data for this Ligand-Target Pair
Affinity DataIC50: 9.00E+3nMAssay Description:Inhibition of GRK1 (unknown origin) using tubulin as substrate by SDS-PAGE methodMore data for this Ligand-Target Pair
TargetProtein kinase C alpha type(Homo sapiens (Human))
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Affinity DataIC50: 250nMAssay Description:Inhibition of human PKCalpha active using MBP as substrate after 60 mins in presence of [gamma-32]ATP by scintillation countingMore data for this Ligand-Target Pair
TargetBeta-adrenergic receptor kinase 1(Homo sapiens (Human))
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Affinity DataIC50: 1.20nMAssay Description:Inhibition of human GRK2 expressed in HEK-B2 cells assessed as isoproterenol-stimulated cAMP accumulation preincubation for 20 mins followed by isopr...More data for this Ligand-Target Pair
3D Structure (crystal)TargetRho-associated protein kinase 2(Homo sapiens (Human))
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Affinity DataIC50: 190nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ROCK2 catalytic domain (1 to 553 residues) expressed in baculovirus expression system using STK...More data for this Ligand-Target Pair
TargetBeta-adrenergic receptor kinase 1(Homo sapiens (Human))
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
TargetBeta-adrenergic receptor kinase 1(Homo sapiens (Human))
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Affinity DataIC50: 20nMAssay Description:Inhibition of GRK2 (unknown origin)More data for this Ligand-Target Pair
TargetG protein-coupled receptor kinase 5(Bos taurus)
Department of Medicinal Chemistry, College of Pharmacy,?Departments of Pharmacology and Biological Chemistry, Life Sciences Institute,§Ph.D. Program in Chemical Biology,?Vahlteich Medicinal Chemistry
Curated by ChEMBL
Department of Medicinal Chemistry, College of Pharmacy,?Departments of Pharmacology and Biological Chemistry, Life Sciences Institute,§Ph.D. Program in Chemical Biology,?Vahlteich Medicinal Chemistry
Curated by ChEMBL
Affinity DataIC50: 2.20E+3nMAssay Description:Binding affinity towards norepinephrine transporter determined using [3H]nisoxetine as radioligandMore data for this Ligand-Target Pair
TargetBeta-adrenergic receptor kinase 1(Bos taurus)
Department of Medicinal Chemistry, College of Pharmacy,?Departments of Pharmacology and Biological Chemistry, Life Sciences Institute,§Ph.D. Program in Chemical Biology,?Vahlteich Medicinal Chemistry
Curated by ChEMBL
Department of Medicinal Chemistry, College of Pharmacy,?Departments of Pharmacology and Biological Chemistry, Life Sciences Institute,§Ph.D. Program in Chemical Biology,?Vahlteich Medicinal Chemistry
Curated by ChEMBL
Affinity DataIC50: 20nMAssay Description:Inhibition of bovine GRK2 S670A mutant after 5 mins in presence of ATP by phosphorimaging assayMore data for this Ligand-Target Pair
TargetBeta-adrenergic receptor kinase 1(Homo sapiens (Human))
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Shonan Research Center, Pharmaceutical Research Division, Takeda Pharmaceutical Co., Ltd. , 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
Curated by ChEMBL
Affinity DataKd: 2nMAssay Description:Binding affinity to full length human GRK2 by Thermofluor thermal shift assayMore data for this Ligand-Target Pair
TargetRhodopsin kinase GRK1(Bos taurus)
Department of Medicinal Chemistry, College of Pharmacy,?Departments of Pharmacology and Biological Chemistry, Life Sciences Institute,§Ph.D. Program in Chemical Biology,?Vahlteich Medicinal Chemistry
Curated by ChEMBL
Department of Medicinal Chemistry, College of Pharmacy,?Departments of Pharmacology and Biological Chemistry, Life Sciences Institute,§Ph.D. Program in Chemical Biology,?Vahlteich Medicinal Chemistry
Curated by ChEMBL
Affinity DataIC50: 9.10E+3nMAssay 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