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Literature summary extracted from

  • Waldschmidt, H.V.; Homan, K.T.; Cruz-Rodriguez, O.; Cato, M.C.; Waninger-Saroni, J.; Larimore, K.M.; Cannavo, A.; Song, J.; Cheung, J.Y.; Kirchhoff, P.D.; Koch, W.J.; Tesmer, J.J.; Larsen, S.D.
    Structure-based design, synthesis, and biological evaluation of highly selective and potent G protein-coupled receptor kinase 2 inhibitors (2016), J. Med. Chem., 59, 3793-3807.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.15 expressed in High Five cells Bos taurus

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.7.11.15 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

EC Number Inhibitors Comment Organism Structure
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 4-(3-(benzylcarbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
Bos taurus
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 4-(4-fluoro-3-(methylcarbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
Bos taurus
2.7.11.15 5-(5-((1H-indazol-5-yl)carbamoyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidin-4-yl)-2-fluorobenzoic acid
-
Bos taurus
2.7.11.15 balanol
-
Bos taurus
2.7.11.15 CCG-224406
-
Bos taurus
2.7.11.15 GSK180736A
-
Bos taurus
2.7.11.15 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
2.7.11.15 paroxetine
-
Bos taurus
2.7.11.15 Takeda103A
-
Bos taurus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.15 ATP + [beta-adrenergic receptor] Bos taurus
-
ADP + phospho-[beta-adrenergic receptor]
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.15 Bos taurus P21146
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.15 Ni-NTA column chromatography Bos taurus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.15 ATP + [beta-adrenergic receptor]
-
Bos taurus ADP + phospho-[beta-adrenergic receptor]
-
?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.15 G protein-coupled receptor kinase 2
-
Bos taurus
2.7.11.15 GRK2
-
Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.15 0.00002
-
at pH 7.0, temperature not specified in the publication Bos taurus Takeda103A
2.7.11.15 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
2.7.11.15 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
2.7.11.15 0.00013
-
at pH 7.0, temperature not specified in the publication Bos taurus CCG-224406
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 0.00077
-
at pH 7.0, temperature not specified in the publication Bos taurus GSK180736A
2.7.11.15 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
2.7.11.15 0.00138
-
at pH 7.0, temperature not specified in the publication Bos taurus paroxetine
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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
2.7.11.15 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