CATH Classification

Domain Context

CATH Clusters

Superfamily Transferase(Phosphotransferase) domain 1
Functional Family Receptor protein-tyrosine kinase

Enzyme Information

2.7.10.1
Receptor protein-tyrosine kinase.
based on mapping to UniProt P00533
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)

P00533
EGFR_HUMAN
Homo sapiens
Epidermal growth factor receptor

PDB Structure

PDB 5UGB
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.
Planken, S., Behenna, D.C., Nair, S.K., Johnson, T.O., Nagata, A., Almaden, C., Bailey, S., Ballard, T.E., Bernier, L., Cheng, H., Cho-Schultz, S., Dalvie, D., Deal, J.G., Dinh, D.M., Edwards, M.P., Ferre, R.A., Gajiwala, K.S., Hemkens, M., Kania, R.S., Kath, J.C., Matthews, J., Murray, B.W., Niessen, S., Orr, S.T., Pairish, M., Sach, N.W., Shen, H., Shi, M., Solowiej, J., Tran, K., Tseng, E., Vicini, P., Wang, Y., Weinrich, S.L., Zhou, R., Zientek, M., Liu, L., Luo, Y., Xin, S., Zhang, C., Lafontaine, J.
J. Med. Chem.
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