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. Author manuscript; available in PMC: 2022 Dec 20.
Published in final edited form as: Nat Cancer. 2022 Jun 20;3(6):710–722. doi: 10.1038/s43018-022-00399-6

Figure 2. Drug screening of Ba/F3 ALK mutation models identifies lorlatinib analogs with increased potency against compound ALK mutations.

Figure 2.

(A) The schema summarizes the 3-step functional screening of 20 lorlatinib analogs (LAs). (B) Heatmap of cellular IC50 values of each LA against single ALK mutations (top) and parental Ba/F3 and PC9 cells (bottom). Asterisks indicate the 12 LAs selected for further assessment. (C) Potency of 12 LAs against clinical ALK compound mutations. Asterisks indicate the 6 LAs selected for additional validation. (D) Potency of 6 LAs against an expanded set of clinical and putative compound ALK mutations. Relative mutation positions within the ALK kinase domain are shown. Red, ALK G1202R; blue, ALK I1171N/S.