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TitleStructure-Based Design of a Novel Covalent 4-(1-Methylindol-3-yl)pyrimidin-2-amine Series Targeting FGFR2 Resistance Mutations.
Journal, issue, pagesJ. Med. Chem., Vol. 69, Page 8614-8627, Year 2026
Publish dateJan 29, 2026 (structure data deposition date)
AuthorsHudkins, R.L. / Allen, E. / Iyer, S. / Balcer, A. / Neal, M. / Ye, Q. / Rideout, M. / Frye, C.B. / Nelson, K.J. / Hoffman, I.D. ...Hudkins, R.L. / Allen, E. / Iyer, S. / Balcer, A. / Neal, M. / Ye, Q. / Rideout, M. / Frye, C.B. / Nelson, K.J. / Hoffman, I.D. / Starrett, J.H. / Harris, T. / Swanson, R.V. / Bensen, D.C.
External linksJ. Med. Chem. / PubMed:41913484
MethodsX-ray diffraction
Resolution1.77 - 1.98 Å
Structure data

PDB-10oo:
FGFR2 mutant D650V with compound 4 (AZD3463)
Method: X-RAY DIFFRACTION / Resolution: 1.85 Å

PDB-10oq:
FGFR2 mutant D650V with compound 6
Method: X-RAY DIFFRACTION / Resolution: 1.98 Å

PDB-10ou:
FGFR2 mutant D650V with compound 12
Method: X-RAY DIFFRACTION / Resolution: 1.77 Å

Chemicals

PDB-1c65:
T4 LYSOZYME MUTANT C54T/C97A/L121A IN THE PRESENCE OF 8 ATM XENON

ChemComp-GOL:
GLYCEROL

ChemComp-SO4:
SULFATE ION

ChemComp-HOH:
WATER

PDB-1c66:
T4 LYSOZYME MUTANT C54T/C97A/L121A/L133A IN THE PRESENCE OF 8 ATM ARGON

PDB-1c67:
T4 LYSOZYME MUTANT C54T/C97A/L121A/L133A IN THE PRESENCE OF 8 ATM KRYPTON

ChemComp-EDO:
1,2-ETHANEDIOL

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / FGFR2 / FGFR / Fibroblast growth factor receptor / Tyrosine Kinase / Resistance Mutations / AZD3463 / compound 4 / compound 6 / TYRX-0544

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