5EDP: Egfr Kinase (t790m/l858r) Apo

The treatment of epidermal growth factor receptor (EGFR)-driven non-small cell lung cancers with the T790M resistance mutation remains a significant unmet medical need. We report the identification of 4-aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of EGFR, with excellent activity against the T790M resistance double mutants and initial single activating mutants. Using an optimization strategy focused on structure-based design and improving PK properties through metabolite identification, we obtained advanced leads with high oral exposure.
PDB ID: 5EDPDownload
MMDB ID: 134593
PDB Deposition Date: 2015/10/21
Updated in MMDB: 2015/12
Experimental Method:
x-ray diffraction
Resolution: 2.9  Å
Source Organism:
Similar Structures:
Biological Unit for 5EDP: monomeric; determined by author and by software (PISA)
Molecular Components in 5EDP
Label Count Molecule
Protein (1 molecule)
Epidermal Growth Factor Receptor(Gene symbol: EGFR)
Molecule annotation
* Click molecule labels to explore molecular sequence information.

Citing MMDB