Cloned (Comment) | Organism |
---|---|
expressed in Echerichia coli BL21 (DE3) cells and in HEK-293 cells | Homo sapiens |
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 | 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 | 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 | 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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P54753 | - |
- |
Purification (Comment) | Organism |
---|---|
HisTrap column chromatography | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a [protein]-L-tyrosine | - |
Homo sapiens | ADP + a [protein]-L-tyrosine phosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
EphB3 | - |
Homo sapiens |
erythropoietin-producing human hepatocellular carcinoma B3 | - |
Homo sapiens |
RTK | - |
Homo sapiens |
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 |