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TIE2 (Y897H)

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TEK · Variant type: point · HGVS: p.R915C

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Ripretinib91.6%8.4%92.95
2Repotrectinib91.5%8.5%84.21
3Tivozanib87.9%12.1%92.42
4Erdafitinib74.0%26.1%95.71
5Infigratinib68.5%31.5%98.24
6Pemigatinib66.3%33.7%98.23
7Selpercatinib65.4%34.6%96.72
8Neratinib61.9%38.1%93.18
9Vandetanib58.3%41.7%95.74
10Entrectinib47.3%52.7%93.69
11Defactinib43.3%56.7%92.68
12Pacritinib42.3%57.7%88.64
13Apatinib41.7%58.3%97.73
14Sorafenib39.2%60.8%96.72
15Umbralisib37.3%62.7%98.74
16Canertinib34.1%65.9%96.49
17Fedratinib32.3%67.7%96.21
18Upadacitinib25.1%74.9%97.98
19Futibatinib22.0%78.0%98.48
20Erlotinib20.4%79.6%99.75
21Gilteritinib18.3%81.7%88.97
22Pralsetinib15.8%84.2%93.43
23Sunitinib14.8%85.2%91.73
24Paxalisib13.8%86.2%99.75
25Avapritinib13.7%86.3%97.73

Wild-type vs variant — drug response delta

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

DrugVariant inhWT inhΔ (variant − WT)
Ripretinib91.6%
Repotrectinib91.5%
Tivozanib87.9%
Erdafitinib74.0%
Infigratinib68.5%
Pemigatinib66.3%
Selpercatinib65.4%
Neratinib61.9%
Vandetanib58.3%
Entrectinib47.3%
Defactinib43.3%
Pacritinib42.3%
Apatinib41.7%
Sorafenib39.2%
Umbralisib37.3%
Canertinib34.1%
Fedratinib32.3%
Upadacitinib25.1%
Futibatinib22.0%
Erlotinib20.4%
Gilteritinib18.3%
Pralsetinib15.8%
Sunitinib14.8%
Paxalisib13.8%
Avapritinib13.7%

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