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Literature summary for 2.7.10.1 extracted from

  • Kung, A.; Chen, Y.; Schimpl, M.; Ni, F.; Zhu, J.; Turner, M.; Molina, H.; Overman, R.; Zhang, C.
    Development of specific, irreversible inhibitors for a receptor tyrosine kinase EphB3 (2016), J. Am. Chem. Soc., 138, 10554-10560.
    View publication on PubMed
Search for more literature for 2.7.10.1

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Echerichia coli BL21 (DE3) cells and in HEK-293 cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
sitting drop vapor diffusion method, using 18-20% (w/v) 1,4-dioxane, 50 mM Tris pH 8.5, 10 mM MgCl2 Homo sapiens

Protein Variants

Protein Variants Comment Organism
C717S the mutant has activity comparable to that of the wild type enzyme and is poorly inhibited by the quinazolines Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(E)-methyl 3-(4-(phenylamino)quinazolin-7-yl)acrylate
-
 Homo sapiens
1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
 Homo sapiens
2-bromo-1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
 Homo sapiens
2-chloro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
 Homo sapiens
2-chloro-N-(4-((2-chloro-5-hydroxyphenyl)amino)-6-(prop-2-yn-1-yloxy)quinazolin-7-yl)acetamide
-
 Homo sapiens
2-chloro-N-(4-((2-chloro-5-hydroxyphenyl)amino)quinazolin-7-yl)acetamide
-
 Homo sapiens
2-chloro-N-(4-(phenylamino)quinazolin-7-yl)acetamide
-
 Homo sapiens
2-fluoro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
-
 Homo sapiens
N-(4-(phenylamino)quinazolin-7-yl)acrylamide
-
 Homo sapiens
N-(4-(phenylamino)quinazolin-7-yl)ethenesulfonamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + a [protein]-L-tyrosine Homo sapiens
-
 ADP + a [protein]-L-tyrosine phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P54753
-
-

Purification (Commentary)

Purification (Comment) Organism
HisTrap column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a [protein]-L-tyrosine
-
 Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?

Synonyms

Synonyms Comment Organism
EphB3
-
 Homo sapiens
erythropoietin-producing human hepatocellular carcinoma B3
-
 Homo sapiens
RTK
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000006
-
 at pH 8.0, temperature not specified in the publication Homo sapiens 2-chloro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
0.000055
-
 at pH 8.0, temperature not specified in the publication Homo sapiens 2-chloro-N-(4-(phenylamino)quinazolin-7-yl)acetamide
0.000415
-
 at pH 8.0, temperature not specified in the publication Homo sapiens 2-fluoro-1-(4-(phenylamino)quinazolin-7-yl)ethanone
0.01
-
 IC50 above 0.01 mM, at pH 8.0, temperature not specified in the publication Homo sapiens 1-(4-(phenylamino)quinazolin-7-yl)ethanone