ALK (F1174L)-EML4

EML4-ALK · Variant type: fusion · HGVS: p.F1174L · Fusion partner: EML4 (F1174L)

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Brigatinib	99.5%	0.6%	82.96
2	Gilteritinib	99.2%	0.8%	88.97
3	Repotrectinib	98.5%	1.4%	84.21
4	Alectinib	98.4%	1.6%	95.49
5	Crizotinib	97.7%	2.3%	91.39
6	Ceritinib	97.7%	2.3%	95.44
7	Lorlatinib	97.6%	2.4%	97.24
8	Entrectinib	97.0%	3.0%	93.69
9	Nintedanib	86.4%	13.6%	90.23
10	Bosutinib	86.0%	13.9%	87.22
11	Sunitinib	85.7%	14.3%	91.73
12	Osimertinib	69.3%	30.7%	97.24
13	Alpelisib	67.6%	32.4%	97.22
14	Pralsetinib	67.6%	32.4%	93.43
15	Pacritinib	61.1%	38.9%	88.64
16	Ruxolitinib	57.9%	42.1%	98.25
17	Axitinib	46.5%	53.5%	93.23
18	Darovasertib	38.2%	61.8%	96.99
19	Defactinib	35.4%	64.6%	92.68
20	Erlotinib	34.3%	65.7%	99.75
21	Baricitinib	32.1%	67.9%	97.99
22	Fedratinib	29.8%	70.2%	96.21
23	Afatinib	28.1%	71.9%	98.50
24	Tepotinib	27.6%	72.4%	99.75
25	Vandetanib	26.4%	73.6%	95.74

Positive Δ means the drug hits the variant harder than wild-type (mutation-selective); negative Δ means it loses potency (resistance).

Drug	Variant inh	WT inh	Δ (variant − WT)
Brigatinib	99.5%	—	—
Gilteritinib	99.2%	—	—
Repotrectinib	98.5%	—	—
Alectinib	98.4%	—	—
Crizotinib	97.7%	—	—
Ceritinib	97.7%	—	—
Lorlatinib	97.6%	—	—
Entrectinib	97.0%	—	—
Nintedanib	86.4%	—	—
Bosutinib	86.0%	—	—
Sunitinib	85.7%	—	—
Osimertinib	69.3%	—	—
Alpelisib	67.6%	—	—
Pralsetinib	67.6%	—	—
Pacritinib	61.1%	—	—
Ruxolitinib	57.9%	—	—
Axitinib	46.5%	—	—
Darovasertib	38.2%	—	—
Defactinib	35.4%	—	—
Erlotinib	34.3%	—	—
Baricitinib	32.1%	—	—
Fedratinib	29.8%	—	—
Afatinib	28.1%	—	—
Tepotinib	27.6%	—	—
Vandetanib	26.4%	—	—

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