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Literature summary for 2.7.11.15 extracted from

  • Asai, D.; Murata, M.; Toita, R.; Kawano, T.; Nakashima, H.; Kang, J.
    A high-affinity peptide substrate for G protein-coupled receptor kinase 2 (GRK2) (2019), Amino Acids, 51, 973-976 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
CMPD101 specific inhibitor, i.e. 3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide hydrochloride Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0324
-
DEMEFTEAESNMNDLVSEYQ at pH 7.5 and 30°C Homo sapiens
0.0339
-
DEMEFTEAESNMN at pH 7.5 and 30°C Homo sapiens
0.1
-
GEGMDEMEFTEAESNMN Km above 0.1 mM, at pH 7.5 and 30°C Homo sapiens

Metals/Ions

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + DEMEFTEAESNMN
-
Homo sapiens ADP + DEMEFpTEAESNMN
-
?
ATP + DEMEFTEAESNMNDLVSEYQ
-
Homo sapiens ADP + DEMEFpTEAESNMNDLVSEYQ
-
?
ATP + GEGMDEMEFTEAESNMN
-
Homo sapiens ADP + GEGMDEMEFpTEAESNMN
-
?
ATP + RRREEEEESAAA
-
Homo sapiens ADP + RRREEEEEpSAAA
-
?

Synonyms

Synonyms Comment Organism
beta-adrenergic receptor kinase 1
-
Homo sapiens
G protein-coupled receptor kinase 2
-
Homo sapiens
GRK2
-
Homo sapiens