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EGFR (K716A/C797S/L858R)

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EGFR · Variant type: compound · HGVS: p.K716A;p.C797S;p.L858R

Components

p.K716Ap.C797Sp.L858R

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Fostamatinib100.0%0.0%96.74
2Brigatinib96.3%3.7%82.96
3Dacomitinib83.3%16.8%97.99
4Pacritinib82.2%17.8%88.64
5Gilteritinib79.0%21.0%88.97
6Lazertinib59.5%40.5%97.47
7Osimertinib58.2%41.8%97.24
8Neratinib43.3%56.7%93.18
9Lorlatinib36.3%63.7%97.24
10Canertinib29.2%70.8%96.49
11Vandetanib27.3%72.7%95.74
12Ibrutinib27.0%73.0%94.74
13Abemaciclib22.5%77.5%91.48
14Mobocertinib19.6%80.4%97.22
15Entrectinib18.6%81.4%93.69
16Tucatinib16.7%83.3%99.75
17Tepotinib16.4%83.6%99.75
18Erlotinib15.6%84.4%99.75
19Lapatinib15.2%84.8%99.25
20Tivozanib13.9%86.1%92.42
21Pirtobrutinib12.7%87.3%99.49
22Inavolisib12.6%87.4%100.00
23Repotrectinib12.2%87.8%84.21
24Temsirolimus11.4%88.6%100.00
25Sorafenib11.0%89.0%96.72

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)
Fostamatinib100.0%97.8%+2.2%
Brigatinib96.3%98.5%-2.1%
Dacomitinib83.3%99.8%-16.5%
Pacritinib82.2%
Gilteritinib79.0%91.0%-12.0%
Lazertinib59.5%100.0%-40.5%
Osimertinib58.2%99.1%-40.9%
Neratinib43.3%100.0%-56.7%
Lorlatinib36.3%
Canertinib29.2%98.4%-69.2%
Vandetanib27.3%99.3%-72.0%
Ibrutinib27.0%99.3%-72.3%
Abemaciclib22.5%
Mobocertinib19.6%100.0%-80.4%
Entrectinib18.6%
Tucatinib16.7%
Tepotinib16.4%
Erlotinib15.6%99.4%-83.8%
Lapatinib15.2%99.2%-84.0%
Tivozanib13.9%
Pirtobrutinib12.7%
Inavolisib12.6%
Repotrectinib12.2%
Temsirolimus11.4%
Sorafenib11.0%

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