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. Author manuscript; available in PMC: 2019 Apr 4.
Published in final edited form as: Cell Rep. 2019 Mar 12;26(11):2916–2928.e13. doi: 10.1016/j.celrep.2019.02.047

Figure 1. Discovery of Small Molecule WIN Site Inhibitors.

Figure 1.

(A) Elaboration of fragment hit C1 into our first-generation chemical probe C3.

(B–D) X-ray co-crystal structures of WDR5 bound to (B) the fragment hit C1 (PDB: 6DY7), (C) C2 (PDB: 6E1Y), and (D) C3 (PDB: 6E22).

(E) Elaboration of fragment hit C4 into our second-generation chemical probe C6.

(F–H) X-ray co-crystal structures of WDR5 bound to (F) the fragment hit C4 (PDB: 6E1Z), (G) C5 (PDB: 6DYA), and (H) C6 (PDB: 6E23).

See also Figure S1 and Tables S1 and S2.