TIE2 (Y897S)

TEK · Variant type: point · HGVS: p.Y897S

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Ponatinib	98.4%	1.6%	78.23
2	Ripretinib	78.0%	22.0%	92.95
3	Crizotinib	65.0%	35.0%	91.39
4	Tivozanib	64.4%	35.6%	92.42
5	Brigatinib	63.1%	36.9%	82.96
6	Repotrectinib	62.0%	38.0%	84.21
7	Cabozantinib	60.0%	40.0%	92.73
8	Nintedanib	50.1%	49.9%	90.23
9	Axitinib	47.4%	52.6%	93.23
10	Infigratinib	44.1%	55.9%	98.24
11	Neratinib	41.5%	58.5%	93.18
12	Erdafitinib	36.6%	63.4%	95.71
13	Pemigatinib	35.8%	64.2%	98.23
14	Vandetanib	27.2%	72.8%	95.74
15	Dabrafenib	27.1%	72.9%	94.74
16	Umbralisib	26.0%	74.0%	98.74
17	Entrectinib	25.8%	74.2%	93.69
18	Selpercatinib	25.1%	74.9%	96.72
19	Apatinib	24.0%	76.0%	97.73
20	Defactinib	21.7%	78.3%	92.68
21	Futibatinib	21.1%	78.9%	98.48
22	Pacritinib	20.8%	79.2%	88.64
23	Selumetinib	15.1%	84.9%	100.00
24	Leniolisib	14.6%	85.4%	100.00
25	Bosutinib	13.2%	86.8%	87.22

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	98.4%	—	—
Ripretinib	78.0%	—	—
Crizotinib	65.0%	—	—
Tivozanib	64.4%	—	—
Brigatinib	63.1%	—	—
Repotrectinib	62.0%	—	—
Cabozantinib	60.0%	—	—
Nintedanib	50.1%	—	—
Axitinib	47.4%	—	—
Infigratinib	44.1%	—	—
Neratinib	41.5%	—	—
Erdafitinib	36.6%	—	—
Pemigatinib	35.8%	—	—
Vandetanib	27.2%	—	—
Dabrafenib	27.1%	—	—
Umbralisib	26.0%	—	—
Entrectinib	25.8%	—	—
Selpercatinib	25.1%	—	—
Apatinib	24.0%	—	—
Defactinib	21.7%	—	—
Futibatinib	21.1%	—	—
Pacritinib	20.8%	—	—
Selumetinib	15.1%	—	—
Leniolisib	14.6%	—	—
Bosutinib	13.2%	—	—

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