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. Author manuscript; available in PMC: 2021 Aug 1.
Published in final edited form as: Nat Chem Biol. 2020 Jul 21;16(8):817–825. doi: 10.1038/s41589-020-0596-8

Table 1.

Selected drugs discussed in the manuscript

Chemical structure Name(s) (Brand name) Target(s) Examples of resistance- conferring mutationsRef Mode of Action
graphic file with name nihms-1622953-t0001.jpg Crizotinib (Xalkori™) ALK ALK-L1196M, C1156Y14,17,19 ATP-competitive
graphic file with name nihms-1622953-t0002.jpg Ceritinib (Zykadia™) ALK ALK-L1198F19,20 ATP-competitive
graphic file with name nihms-1622953-t0003.jpg Lorlatinib (Lorbrena™) ALK ALK-C1156-L1198F19,20 ATP-competitive
graphic file with name nihms-1622953-t0004.jpg Imatinib (Gleevec™) BCR-ABL BCR-ABL-T315I3,16 ATP-competitive
graphic file with name nihms-1622953-t0005.jpg Dasatinib (Sprycel™) BCR-ABL BCR-ABL-T315I3,16 ATP-competitive
graphic file with name nihms-1622953-t0006.jpg Vandetanib (Caprelsa™) BCR-ABL-V299L BCR-ABL-V299L-E255K, V299L-F317L78 ATP-competitive
EGFR
graphic file with name nihms-1622953-t0007.jpg ABL001 Asciminib BCR-ABL-WT BCR-ABL-A337C, P465S, V468F40 allosteric
BCR-ABL-T315I
graphic file with name nihms-1622953-t0008.jpg LOXO-195 TrkA, B, C N/A ATP-competitive
graphic file with name nihms-1622953-t0009.jpg Larotrectinib LOXO-101 (Vitrakvi™) TrkA, B, C TrkA-F589L, G595R, G667C24,25 ATP-competitive
TrkC-G623R, G696A24,25
graphic file with name nihms-1622953-t0010.jpg Osimertinib (Tagrisso™) EGFR-T790M EGFR-C797S, L718Q35 covalent
graphic file with name nihms-1622953-t0011.jpg WZ4020 EGFR-T790M EGFR-C797S35 covalent
graphic file with name nihms-1622953-t0012.jpg Indisulam RBM39 RBM39-G268V,W,R,E67 “molecular glue”
DCAF15
graphic file with name nihms-1622953-t0013.jpg Thalidomide CRBN IKFZ1-Q146H64,65 “molecular glue”
IKFZ1 IKFZ3-Q147H64,65
IKFZ3 CRBN-W386A64,65
CRBN-W400A64,65
graphic file with name nihms-1622953-t0014.jpg MT-802 CRBN N/A PROTAC
BTK(C481S)