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ERN1/IRE1 (R728A)

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ERN1 · Variant type: point · HGVS: p.R728A

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Gilteritinib76.9%23.1%88.97
2Pacritinib30.7%69.3%88.64
3Defactinib18.5%81.5%92.68
4Selpercatinib17.4%82.6%96.72
5Abemaciclib15.0%85.0%91.48
6Fedratinib12.4%87.6%96.21
7Palbociclib9.0%91.0%98.75
8Neratinib6.7%93.3%93.18
9Sorafenib6.4%93.6%96.72
10Pexidartinib6.4%93.6%99.49
11Asciminib5.8%94.2%100.00
12Sunitinib5.5%94.5%91.73
13Erdafitinib5.5%94.5%95.71
14Pirtobrutinib5.1%94.9%99.49
15Tivozanib4.8%95.3%92.42
16Mobocertinib4.6%95.4%97.22
17Quizartinib4.0%96.0%99.50
18Canertinib3.8%96.2%96.49
19Rabusertib3.2%96.8%98.74
20Capivasertib2.2%97.8%96.48
21Avapritinib2.0%98.0%97.73
22Erlotinib1.7%98.3%99.75
23Tucatinib1.7%98.3%99.75
24Pemigatinib1.5%98.5%98.23
25Tenalisib1.4%98.6%97.98

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)
Gilteritinib76.9%
Pacritinib30.7%
Defactinib18.5%
Selpercatinib17.4%
Abemaciclib15.0%
Fedratinib12.4%
Palbociclib9.0%
Neratinib6.7%
Sorafenib6.4%
Pexidartinib6.4%
Asciminib5.8%
Sunitinib5.5%
Erdafitinib5.5%
Pirtobrutinib5.1%
Tivozanib4.8%
Mobocertinib4.6%
Quizartinib4.0%
Canertinib3.8%
Rabusertib3.2%
Capivasertib2.2%
Avapritinib2.0%
Erlotinib1.7%
Tucatinib1.7%
Pemigatinib1.5%
Tenalisib1.4%

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