CATH Classification

Domain Context

CATH Clusters

Superfamily Phosphorylase Kinase; domain 1
Functional Family

Enzyme Information

2.7.10.1
Receptor protein-tyrosine kinase.
based on mapping to UniProt P10721
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate.
-!- The receptor protein-tyrosine kinases, which can be defined as having a transmembrane domain, are a large and diverse multigene family found only in metazoans. -!- In the human genome, 58 receptor-type protein-tyrosine kinases have been identified and these are distributed into 20 subfamilies. -!- Formerly EC 2.7.1.112.

UniProtKB Entries (1)

P10721
KIT_HUMAN
Homo sapiens
Mast/stem cell growth factor receptor Kit

PDB Structure

PDB 6GQK
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
Kettle, J.G., Anjum, R., Barry, E., Bhavsar, D., Brown, C., Boyd, S., Campbell, A., Goldberg, K., Grondine, M., Guichard, S., Hardy, C.J., Hunt, T., Jones, R.D.O., Li, X., Moleva, O., Ogg, D., Overman, R.C., Packer, M.J., Pearson, S., Schimpl, M., Shao, W., Smith, A., Smith, J.M., Stead, D., Stokes, S., Tucker, M., Ye, Y.
J. Med. Chem.
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