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Literature summary for 2.7.11.16 extracted from

  • Rowlands, R.A.; Cato, M.C.; Waldschmidt, H.V.; Bouley, R.A.; Chen, Q.; Avramova, L.; Larsen, S.D.; Tesmer, J.J.G.; White, A.D.
    Structure-based design of selective, covalent G protein-coupled receptor kinase 5 inhibitors (2019), ACS Med. Chem. Lett., 10, 1628-1634 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.11.16

Inhibitors

Inhibitors Comment Organism Structure
CCG-265328
-
 Homo sapiens
GSK1326255A
-
 Homo sapiens
GSK1713088A
-
 Homo sapiens
GSK2163632A
-
 Homo sapiens
additional information not inhibited by CCG-262604, CCG-263045, CCG-258904, and CCG-263115 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
 Homo sapiens 5634
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ 10 mM used in assay conditions Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P34947
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + porcine brain tubulin
-
 Homo sapiens ADP + phosphorylated porcine brain tubulin
-
 ?

Subunits

Subunits Comment Organism
? x * 68882, calculated from amino acid sequence Homo sapiens

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 5
-
 Homo sapiens
GRK5
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0011
-
 at pH 7.5, and temperature not specified in the publication Homo sapiens CCG-265328
0.0025
-
 at pH 7.5, and temperature not specified in the publication Homo sapiens GSK1326255A
0.0032
-
 at pH 7.5, and temperature not specified in the publication Homo sapiens GSK2163632A
0.0032
-
 at pH 7.5, and temperature not specified in the publication Homo sapiens GSK1713088A