Cloned (Comment) | Organism |
---|---|
expressed in High Five cells | Bos taurus |
Crystallization (Comment) | Organism |
---|---|
in complex with inhibitors, hanging drop vapor diffusion method, using 50 mM MES pH 6.0, 0.8-1.2 M NaCl, and 8-16% (w/v) PEG 3350 | Bos taurus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-(3-((2,6-bis(trifluoromethyl)benzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-((2,6-dichlorobenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-((2,6-difluorobenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-((2,6-dimethoxybenzyl)carbamoyl)-4-fluorophenyl)-N-(1Hindazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-((2,6-dimethylbenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5 carboxamide | - |
Bos taurus | |
4-(3-((2,6-dimethylbenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-N,6-dimethyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-((2,6-dimethylphenethyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-((3,5-bis(trifluoromethyl)benzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-(2-((2,6-bis(trifluoromethyl)benzyl)amino)-2-oxoethyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-(2-((2,6-dimethoxybenzyl)amino)-2-oxoethyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-(2-((2,6-dimethylbenzyl)amino)-2-oxoethyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(3-(benzylcarbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-(((3-methylpyridin-2-yl)methyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-((2-(pyridin-2-yl)ethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-((2-(pyridin-4-yl)ethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-((2-methoxybenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-((3-fluorobenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-((3-methoxybenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-((4-methoxybenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-((isoquinolin-1-ylmethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-((pyridin-2-ylmethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
4-(4-fluoro-3-(methylcarbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
5-(5-((1H-indazol-5-yl)carbamoyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidin-4-yl)-2-fluorobenzoic acid | - |
Bos taurus | |
balanol | - |
Bos taurus | |
CCG-224406 | - |
Bos taurus | |
GSK180736A | - |
Bos taurus | |
N-(benzo[d][1,3]dioxol-5-yl)-4-(4-fluoro-3-((pyridin-2-ylmethyl)-carbamoyl)phenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | - |
Bos taurus | |
paroxetine | - |
Bos taurus | |
Takeda103A | - |
Bos taurus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [beta-adrenergic receptor] | Bos taurus | - |
ADP + phospho-[beta-adrenergic receptor] | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Bos taurus | P21146 | - |
- |
Purification (Comment) | Organism |
---|---|
Ni-NTA column chromatography | Bos taurus |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [beta-adrenergic receptor] | - |
Bos taurus | ADP + phospho-[beta-adrenergic receptor] | - |
? |
Synonyms | Comment | Organism |
---|---|---|
G protein-coupled receptor kinase 2 | - |
Bos taurus |
GRK2 | - |
Bos taurus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00002 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | Takeda103A | |
0.00006 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-((2-methoxybenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00007 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-((2,6-dimethylbenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5 carboxamide | |
0.00013 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | CCG-224406 | |
0.00013 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-((2,6-dichlorobenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00013 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-((2,6-dimethoxybenzyl)carbamoyl)-4-fluorophenyl)-N-(1Hindazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00015 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-((pyridin-2-ylmethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.0002 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-((3-fluorobenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00022 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-((2,6-difluorobenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00023 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-((2,6-dimethylphenethyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00028 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-((2-(pyridin-2-yl)ethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00028 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-((isoquinolin-1-ylmethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00042 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-((3-methoxybenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00045 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-(2-((2,6-dimethoxybenzyl)amino)-2-oxoethyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00046 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-((4-methoxybenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00069 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-(benzylcarbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00077 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | GSK180736A | |
0.0012 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-((2,6-bis(trifluoromethyl)benzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.00138 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | paroxetine | |
0.0019 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-(((3-methylpyridin-2-yl)methyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.0027 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-((3,5-bis(trifluoromethyl)benzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.0043 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-(methylcarbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.0046 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-((2,6-dimethylbenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-N,6-dimethyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.0048 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(4-fluoro-3-((2-(pyridin-4-yl)ethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.02 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 5-(5-((1H-indazol-5-yl)carbamoyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidin-4-yl)-2-fluorobenzoic acid | |
0.025 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-(2-((2,6-dimethylbenzyl)amino)-2-oxoethyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.1 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | 4-(3-(2-((2,6-bis(trifluoromethyl)benzyl)amino)-2-oxoethyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | |
0.1 | - |
at pH 7.0, temperature not specified in the publication | Bos taurus | N-(benzo[d][1,3]dioxol-5-yl)-4-(4-fluoro-3-((pyridin-2-ylmethyl)-carbamoyl)phenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide |