10OO: FGFR2 mutant D650V with compound 4

FGFR2 mutant D650V with compound 4 (AZD3463). Determined by X-ray diffraction at 1.85 Å resolution. Released 15 Apr 2026.

Method: X-ray diffraction
Resolution: 1.85 Å
Organism: Homo sapiens
Chains: 2
Atoms: 4,734
Mol. weight: 75.72 kDa
Ligands: A1C65
Released: 15 Apr 2026

Explore 10OO in 3D Show helices and sheets RCSB PDB PDBe

Secondary structure: helices and β-sheets

10OO contains 39 α-helices and 28 β-strands across 2 chains. Residue ranges use author residue numbering, as in the PDB file, from PDBe. To see them in 3D, choose the Cartoon representation with Secondary structure coloring: helices, sheets and coils get different colors.

Chain A: 19 helices, 13 β-strands

Element	Residues	Length	Sheet
β-strand	475	1	1
α-helix	478-480	3
β-strand	481-488	8	1
β-strand	494-501	8	1
β-strand	511-518	8	1
β-strand	524	1	2
α-helix	525-541	17
β-strand	547	1	3
α-helix	548-549	2
β-strand	550-554	5	1
β-strand	561-565	5	1
β-strand	571	1	3
α-helix	572-577	6
α-helix	594-596	3
α-helix	597-599	3
α-helix	600-619	20
β-strand	622-623	2	4
α-helix	629-631	3
β-strand	632-634	3	3
β-strand	640-642	3	3
α-helix	645-647	3
β-strand	649-650	2	4
α-helix	667-669	3
α-helix	672-677	6
α-helix	682-697	16
α-helix	701-702	2
α-helix	709-717	9
α-helix	722-725	4
α-helix	730-739	10
α-helix	744-746	3
α-helix	748-749	2
α-helix	750-762	13

Chain B: 20 helices, 15 β-strands

Element	Residues	Length	Sheet
β-strand	475	1	5
α-helix	478-480	3
β-strand	481-488	8	5
β-strand	494-501	8	5
β-strand	511-518	8	5
α-helix	525-541	17
β-strand	547	1	6
α-helix	548-549	2
β-strand	550-554	5	5
β-strand	561-565	5	5
β-strand	571	1	6
α-helix	572-577	6
α-helix	594-596	3
α-helix	597-599	3
α-helix	600-619	20
β-strand	622-623	2	7
α-helix	629-631	3
β-strand	632-634	3	6
β-strand	640-642	3	6
α-helix	645-647	3
β-strand	649-650	2	7
α-helix	655	1
β-strand	656-657	2	8
β-strand	666	1	2
α-helix	667-669	3
α-helix	672-677	6
β-strand	679-680	2	8
α-helix	682-697	16
α-helix	701-702	2
α-helix	709-717	9
α-helix	722-725	4
α-helix	730-739	10
α-helix	744-746	3
α-helix	748-749	2
α-helix	750-762	13

Molecules and chains

Molecule	Chains	Type	Length	Organism	UniProt
Fibroblast growth factor receptor 2	A, B	protein	324	Homo sapiens	P21802 (AlphaFold model)

Sequence of entity 1 (A, B), FASTA

>10OO_1 Fibroblast growth factor receptor 2 (chains A, B)
MGSSHHHHHHSQDPMLAGVSEYELPEDPKWEFPRDKLTLGKPLGEGCFGQVVMAEAVGID
KDKPKEAVTVAVKMLKDDATEKDLSDLVSEMEMMKMIGKHKNIINLLGACTQDGPLYVIV
EYASKGNLREYLRARRPPGMEYSYDINRVPEEQMTFKDLVSCTYQLARGMEYLASQKCIH
RDLAARNVLVTENNVMKIADFGLARVINNIDYYKKTTNGRLPVKWMAPEALFDRVYTHQS
DVWSFGVLMWEIFTLGGSPYPGIPVEELFKLLKEGHRMDKPANCTNELYMMMRDCWHAVP
SQRPTFKQLVEDLDRILTLTTNEE

Ligands and cofactors

ID	Name	Formula	Copies
A1C65	(4P)-N-[4-(4-aminopiperidin-1-yl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)py…	C24 H25 Cl N6 O	2

Water and common crystallization additives (SO4, GOL) are not listed.

Primary citation

Structure-Based Design of a Novel Covalent 4-(1-Methylindol-3-yl)pyrimidin-2-amine Series Targeting FGFR2 Resistance Mutations. Hudkins, R.L., Allen, E., Iyer, S. et al. J Med Chem (2026) 69:8614-8627. DOI 10.1021/acs.jmedchem.6c00514 · PubMed

Other PDB entries of the same protein (UniProt P21802 (AlphaFold model), which also has an AlphaFold model), best resolution first:

10OU 1.77 Å, FGFR2 mutant D650V with compound 12
2PVF 1.8 Å, Crystal Structure of Tyrosine Phosphorylated Activated FGF Receptor 2 (FGFR2) Kinase…
3B2T 1.8 Å, Structure of phosphotransferase
4J99 1.85 Å, Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domain Harboring the Gain-of-Function…
5UGL 1.86 Å, Crystal Structure of FGF Receptor 2 Tyrosine Kinase Domain Harboring the D650V…
3CAF 1.96 Å, Crystal Structure of hFGFR2 D2 Domain
10OQ 1.98 Å, FGFR2 mutant D650V with compound 6
9U7S 1.99 Å, FGFR2 kinase domain with a macrocyclic compound 8r
3CLY 2.0 Å, Crystal Structure of FGF Receptor 2 (FGFR2) Kinase Domains Trapped in…
8W3D 2.04 Å, TAS-120 covalent structure with FGFR2 molecular brake mutant
5UI0 2.05 Å, Crystal Structure of the Tyrosine Kinase Domain of FGF Receptor 2 harboring an…
3OJM 2.1 Å, Crystal Structure of FGF1 complexed with the ectodomain of FGFR2b harboring P253R Apert…

Browse structure collections

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