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Compile Data Set for Download or QSAR

Found 121 hits of ic50 for UniProtKB: P43250   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566950
PNG
(CHEMBL4852125)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(Cl)cn3)nc3cccc(OC)c23)n[nH]1 |r|
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n/an/a 3.5n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566949
PNG
(CHEMBL4877302)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(Cl)cc3OC)nc3cccc(OC)c23)n[nH]1
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n/an/a 3.80n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human GRK6 using casein as substrate in presence of [gamma33P]ATP by radiometric hotspot kinase assay


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566953
PNG
(CHEMBL4860332)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(Cl)cc3OC)nc3cccc(C)c23)n[nH]1
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566946
PNG
(CHEMBL4854871)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)nc3cccc(OC)c23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566949
PNG
(CHEMBL4877302)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(Cl)cc3OC)nc3cccc(OC)c23)n[nH]1
PDB
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566923
PNG
(CHEMBL4855000)
Show SMILES CCc1cc(Nc2nc(NCCc3ccccc3)nc3cccc(OC)c23)n[nH]1
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566951
PNG
(CHEMBL4875929)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)nc3cccc(C)c23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566948
PNG
(CHEMBL4874424)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(Cl)cc3)nc3cccc(OC)c23)n[nH]1
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566947
PNG
(CHEMBL4847703)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(F)cn3)nc3cccc(OC)c23)n[nH]1
PDB
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566946
PNG
(CHEMBL4854871)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)nc3cccc(OC)c23)n[nH]1 |r|
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n/an/a 18n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human GRK6 using casein as substrate in presence of [gamma33P]ATP by radiometric hotspot kinase assay


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566922
PNG
(CHEMBL4876072)
Show SMILES CCc1cc(Nc2nc(NCCc3ccccc3)nc3cccc(F)c23)n[nH]1
PDB
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n/an/a 20n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566939
PNG
(CHEMBL4871944)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(C)cc3)nc3cccc(F)c23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566952
PNG
(CHEMBL4872426)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(Cl)cc3)nc3cccc(C)c23)n[nH]1
PDB
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566940
PNG
(CHEMBL4870615)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)nc3cccc(F)c23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566949
PNG
(CHEMBL4877302)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(Cl)cc3OC)nc3cccc(OC)c23)n[nH]1
PDB
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n/an/a 30n/an/an/an/an/an/a


TBA

Assay Description
Binding affinity to FLAG-tagged GRK6 in human KMS11 cells incubated for 2.5 hrs by ITDR assay


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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TBA

Assay Description
Inhibition of human GRK6 using casein as substrate by [gamma-33P]-ATP assay


Citation and Details

Article DOI: 10.1016/j.bmc.2018.02.022
BindingDB Entry DOI: 10.7270/Q2DJ5KB8
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566947
PNG
(CHEMBL4847703)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(F)cn3)nc3cccc(OC)c23)n[nH]1
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TBA

Assay Description
Inhibition of human GRK6 using casein as substrate in presence of [gamma33P]ATP by radiometric hotspot kinase assay


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566943
PNG
(CHEMBL4846282)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(Cl)cc3OC)nc3ccccc23)n[nH]1
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566928
PNG
(CHEMBL4847311)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cc3)nc3cccc(F)c23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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University of Florida

Curated by ChEMBL


Assay Description
Inhibition of human GRK6 using casein as substrate by [gamma-33P]-ATP assay


Eur J Med Chem 161: 456-467 (2019)


Article DOI: 10.1016/j.ejmech.2018.10.052
BindingDB Entry DOI: 10.7270/Q2W380MT
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566937
PNG
(CHEMBL4850937)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(Cl)cc3)nc3ccccc23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566941
PNG
(CHEMBL4849245)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(cn3)C#N)nc3cccc(F)c23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566924
PNG
(CHEMBL4860927)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cc3)nc3cc(F)ccc23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566921
PNG
(CHEMBL4876138)
Show SMILES CCc1cc(Nc2nc(NCCc3ccc(F)cc3)nc3cccc(F)c23)n[nH]1
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566915
PNG
(CHEMBL4848826)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cc3)nc3ccccc23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566927
PNG
(CHEMBL4860406)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cc3)nc3ccc(OC)cc23)n[nH]1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566925
PNG
(CHEMBL4860226)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cc3)nc3ccc(F)cc23)n[nH]1 |r|
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n/an/a 160n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566953
PNG
(CHEMBL4860332)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(Cl)cc3OC)nc3cccc(C)c23)n[nH]1
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n/an/a 170n/an/an/an/an/an/a


TBA

Assay Description
Binding affinity to FLAG-tagged GRK6 in human KMS11 cells incubated for 2.5 hrs by ITDR assay


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566917
PNG
(CHEMBL4848792)
Show SMILES CCc1cc(Nc2nc(NCCc3ccc(F)cc3)nc3cc(F)ccc23)n[nH]1
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566916
PNG
(CHEMBL4858397)
Show SMILES CCc1cc(Nc2nc(NCCc3ccc(F)cc3)nc3ccccc23)n[nH]1
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n/an/a 190n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566942
PNG
(CHEMBL4875743)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ncc(F)cn3)nc3cccc(F)c23)n[nH]1 |r|
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n/an/a 230n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566933
PNG
(CHEMBL4856820)
Show SMILES CCc1cc(Nc2nc(NCc3ccc(F)cc3)nc3ccccc23)n[nH]1
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n/an/a 250n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566938
PNG
(CHEMBL4876835)
Show SMILES CCc1cc(Nc2nc(NC3(CC3)c3ccc(Cl)cc3)nc3ccccc23)n[nH]1
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n/an/a 280n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566931
PNG
(CHEMBL4857672)
Show SMILES CCn1cnc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)nc3cccc(F)c23)c1 |r|
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TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566936
PNG
(CHEMBL4865412)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(OC)cc3)nc3ccccc23)n[nH]1 |r|
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n/an/a 290n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566919
PNG
(CHEMBL4856240)
Show SMILES CCc1cc(Nc2nc(NCCc3ccc(F)cc3)nc3ccc(F)cc23)n[nH]1
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n/an/a 310n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566935
PNG
(CHEMBL4869975)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3cccc(F)c3)nc3ccccc23)n[nH]1 |r|
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n/an/a 340n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566926
PNG
(CHEMBL4865487)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cc3)nc3cc(Cl)ccc23)n[nH]1 |r|
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n/an/a 440n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566920
PNG
(CHEMBL4875677)
Show SMILES CCc1cc(Nc2nc(NCCc3ccc(F)cc3)nc3ccc(OC)cc23)n[nH]1
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n/an/a 460n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM3149
PNG
(2-{[2,6-dihydroxy-4-({[(3R,4R)-3-[(4-hydroxybenzen...)
Show SMILES OC(=O)c1cccc(O)c1C(=O)c1c(O)cc(cc1O)C(=O)O[C@@H]1CCCNC[C@H]1NC(=O)c1ccc(O)cc1 |r|
Show InChI InChI=1S/C28H26N2O10/c31-16-8-6-14(7-9-16)26(36)30-18-13-29-10-2-5-22(18)40-28(39)15-11-20(33)24(21(34)12-15)25(35)23-17(27(37)38)3-1-4-19(23)32/h1,3-4,6-9,11-12,18,22,29,31-34H,2,5,10,13H2,(H,30,36)(H,37,38)/t18-,22-/m1/s1
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Article
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n/an/a 490n/an/an/an/an/an/a



University of Michigan

Curated by ChEMBL


Assay Description
Inhibition of GRK6-mediated bovine tubulin phosphorylation by scintillation counting


J Med Chem 53: 1867-70 (2010)


Article DOI: 10.1021/jm9017515
BindingDB Entry DOI: 10.7270/Q2P26Z8Z
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50536679
PNG
(CHEMBL4568087)
Show SMILES Cn1cc(cn1)-c1cnc2c(cnn2c1)-c1csc(c1)C(=O)N[C@@H]1CCCC[C@@H]1N |r|
Show InChI InChI=1S/C21H23N7OS/c1-27-10-15(8-24-27)14-7-23-20-16(9-25-28(20)11-14)13-6-19(30-12-13)21(29)26-18-5-3-2-4-17(18)22/h6-12,17-18H,2-5,22H2,1H3,(H,26,29)/t17-,18+/m0/s1
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n/an/a 500n/an/an/an/an/an/a



Merck and Co.

Curated by ChEMBL


Assay Description
Inhibition of full-length recombinant human GST-tagged GRK6 expressed in baculovirus expression system by Z'-LYTE assay


Bioorg Med Chem Lett 26: 4362-6 (2016)


Article DOI: 10.1016/j.bmcl.2016.02.003
BindingDB Entry DOI: 10.7270/Q2NP27X5
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566951
PNG
(CHEMBL4875929)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)c3ccc(F)cn3)nc3cccc(C)c23)n[nH]1 |r|
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n/an/a 610n/an/an/an/an/an/a


TBA

Assay Description
Binding affinity to FLAG-tagged GRK6 in human KMS11 cells incubated for 2.5 hrs by ITDR assay


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566944
PNG
(CHEMBL4860741)
Show SMILES CCc1cc(Nc2nc(N[C@@H](C)C3CCCCC3)nc3ccccc23)n[nH]1 |r|
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n/an/a 960n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM375076
PNG
(US10252984, Table 2.37)
Show SMILES COC(=O)c1c(N)n(CC=C)c2nc3ccccc3nc12
Show InChI InChI=1S/C15H14N4O2/c1-3-8-19-13(16)11(15(20)21-2)12-14(19)18-10-7-5-4-6-9(10)17-12/h3-7H,1,8,16H2,2H3
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n/an/a 973n/an/an/an/an/an/a



Vrije Universiteit Amsterdam



Assay Description
TBD


J Pharmacol Exp Ther 314: 1310-21 (2005)


BindingDB Entry DOI: 10.7270/Q2BV7JXQ
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM375078
PNG
(US10252984, Table 2.39)
Show SMILES CCCCCn1c(N)c(C(=O)OC)c2nc3ccccc3nc12
Show InChI InChI=1S/C17H20N4O2/c1-3-4-7-10-21-15(18)13(17(22)23-2)14-16(21)20-12-9-6-5-8-11(12)19-14/h5-6,8-9H,3-4,7,10,18H2,1-2H3
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n/an/a 1.03E+3n/an/an/an/an/an/a



Vrije Universiteit Amsterdam



Assay Description
TBD


J Pharmacol Exp Ther 314: 1310-21 (2005)


BindingDB Entry DOI: 10.7270/Q2BV7JXQ
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566918
PNG
(CHEMBL4869307)
Show SMILES CCc1cc(Nc2nc(NCCc3ccc(F)cc3)nc3cc(Cl)ccc23)n[nH]1
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n/an/a 1.10E+3n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM375071
PNG
(US10252984, Table 2.32)
Show SMILES CN(C)[C@H]1C2CC3Cc4c(ccc(O)c4C(=O)C3=C(O)[C@]2(O)C(=O)C(C(N)=O)=C1O)N(C)C |r,c:30,t:19|
Show InChI InChI=1S/C23H27N3O7/c1-25(2)12-5-6-13(27)15-10(12)7-9-8-11-17(26(3)4)19(29)16(22(24)32)21(31)23(11,33)20(30)14(9)18(15)28/h5-6,9,11,17,27,29-30,33H,7-8H2,1-4H3,(H2,24,32)/t9?,11?,17-,23-/m0/s1
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n/an/a 1.37E+3n/an/an/an/an/an/a



Vrije Universiteit Amsterdam



Assay Description
TBD


J Pharmacol Exp Ther 314: 1310-21 (2005)


BindingDB Entry DOI: 10.7270/Q2BV7JXQ
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566945
PNG
(CHEMBL4868574)
Show SMILES CCc1cc(Nc2nc(NCCN3CCOCC3)nc3cccc(F)c23)n[nH]1
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n/an/a 1.40E+3n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM50566934
PNG
(CHEMBL4865763)
Show SMILES CCc1cc(Nc2nc(N[C@H](C)c3ccc(F)cc3)nc3ccccc23)n[nH]1 |r|
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n/an/a 1.40E+3n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant full-length human GRK6 using casein as substrate measured after 80 mins in presence of [gamma33P]ATP by radiometric scintil...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c00506
BindingDB Entry DOI: 10.7270/Q20K2D97
More data for this
Ligand-Target Pair
G protein-coupled receptor kinase 6


(Homo sapiens (Human))
BDBM375079
PNG
(US10252984, Table 2.40)
Show SMILES CCCCCCn1c(N)c(C(=O)OC)c2nc3ccccc3nc12
Show InChI InChI=1S/C18H22N4O2/c1-3-4-5-8-11-22-16(19)14(18(23)24-2)15-17(22)21-13-10-7-6-9-12(13)20-15/h6-7,9-10H,3-5,8,11,19H2,1-2H3
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n/an/a 1.43E+3n/an/an/an/an/an/a



Vrije Universiteit Amsterdam



Assay Description
TBD


J Pharmacol Exp Ther 314: 1310-21 (2005)


BindingDB Entry DOI: 10.7270/Q2BV7JXQ
More data for this
Ligand-Target Pair
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