Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.10.1 extracted from

  • Chapelat, J.; Berst, F.; Marzinzik, A.L.; Moebitz, H.; Drueckes, P.; Trappe, J.; Fabbro, D.; Seebach, D.
    The substrate-activity-screening methodology applied to receptor tyrosine kinases: a proof-of-concept study (2012), Eur. J. Med. Chem., 57, 1-9.
    View publication on PubMed
Search for more literature for 2.7.10.1

Cloned(Commentary)

Cloned (Comment) Organism
expression in Sf9 cell Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information identification of inhibitors by translation of structure-efficiency relationships of the substrates into structure-activity relationships of the inhibitors upon replacement of the phosphorylation warhead by an inactive mimetic Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0051
-
 Ac-DYFE-6-chloro-W-NHMe pH 7.4, 25°C Homo sapiens
0.07
-
 Ac-DYFGW-NHMe pH 7.4, 25°C Homo sapiens
0.232
-
 YFEW pH 7.4, 25°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P08069 IGF-1R
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + Ac-DYFE-6-chloro-W-NHMe substrate identified by substrate-activity-screening methodology based on optimization of substrate YFEW in a modular manner Homo sapiens ADP + Ac-DYpFE-6-chloro-W-NHMe
-
 ?
ATP + Ac-DYFGW-NHMe substrate identified by substrate-activity-screening methodology based on optimization of substrate YFEW in a modular manner Homo sapiens ADP + Ac-DYpFGW-NHMe
-
 ?
ATP + YFEW tetrapeptide identified by substrate profiling Homo sapiens ADP + YpFEW
-
 ?

Synonyms

Synonyms Comment Organism
IGF-1R
-
 Homo sapiens