TIE2 (R849W)

TEK · Variant type: point · HGVS: p.R849W

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Ponatinib	98.6%	1.4%	78.23
2	Repotrectinib	94.3%	5.7%	84.21
3	Cabozantinib	89.6%	10.4%	92.73
4	Vandetanib	89.0%	11.0%	95.74
5	Crizotinib	86.4%	13.6%	91.39
6	Dabrafenib	86.0%	14.0%	94.74
7	Axitinib	81.0%	19.0%	93.23
8	Brigatinib	80.5%	19.5%	82.96
9	Ripretinib	80.0%	20.0%	92.95
10	Fostamatinib	78.2%	21.8%	96.74
11	Nintedanib	74.2%	25.8%	90.23
12	Tivozanib	70.2%	29.8%	92.42
13	Lenvatinib	59.2%	40.8%	97.74
14	Ibrutinib	58.5%	41.5%	94.74
15	Entrectinib	58.2%	41.8%	93.69
16	Erdafitinib	56.4%	43.6%	95.71
17	Gilteritinib	52.6%	47.4%	88.97
18	Canertinib	52.4%	47.6%	96.49
19	Neratinib	50.9%	49.1%	93.18
20	Infigratinib	50.0%	50.0%	98.24
21	Pazopanib	48.7%	51.3%	97.49
22	Selpercatinib	47.2%	52.8%	96.72
23	Dacomitinib	45.2%	54.8%	97.99
24	Defactinib	40.4%	59.6%	92.68
25	Pemigatinib	38.5%	61.5%	98.23

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)
Ponatinib	98.6%	—	—
Repotrectinib	94.3%	—	—
Cabozantinib	89.6%	—	—
Vandetanib	89.0%	—	—
Crizotinib	86.4%	—	—
Dabrafenib	86.0%	—	—
Axitinib	81.0%	—	—
Brigatinib	80.5%	—	—
Ripretinib	80.0%	—	—
Fostamatinib	78.2%	—	—
Nintedanib	74.2%	—	—
Tivozanib	70.2%	—	—
Lenvatinib	59.2%	—	—
Ibrutinib	58.5%	—	—
Entrectinib	58.2%	—	—
Erdafitinib	56.4%	—	—
Gilteritinib	52.6%	—	—
Canertinib	52.4%	—	—
Neratinib	50.9%	—	—
Infigratinib	50.0%	—	—
Pazopanib	48.7%	—	—
Selpercatinib	47.2%	—	—
Dacomitinib	45.2%	—	—
Defactinib	40.4%	—	—
Pemigatinib	38.5%	—	—

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