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EGFR (K716A/T790M/C797S/L858R)

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EGFR · Variant type: compound · HGVS: p.K716A;p.T790M;p.C797S;p.L858R

Components

p.K716Ap.T790Mp.C797Sp.L858R

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Gilteritinib95.6%4.4%88.97
2Pacritinib95.1%4.9%88.64
3Lazertinib87.8%12.2%97.47
4Neratinib76.4%23.6%93.18
5Mobocertinib73.0%27.0%97.22
6Canertinib68.5%31.5%96.49
7Vandetanib66.3%33.7%95.74
8Erlotinib61.1%38.9%99.75
9Abemaciclib58.1%41.9%91.48
10Deucravacitinib57.9%42.1%98.99
11Entrectinib54.3%45.7%93.69
12Repotrectinib49.8%50.2%84.21
13Fedratinib48.3%51.7%96.21
14Defactinib41.8%58.2%92.68
15Avapritinib35.0%65.0%97.73
16Pralsetinib31.5%68.5%93.43
17Pirtobrutinib28.3%71.7%99.49
18Sunitinib28.2%71.8%91.73
19Tivozanib27.2%72.8%92.42
20Selpercatinib21.7%78.3%96.72
21Palbociclib16.2%83.8%98.75
22Abrocitinib12.1%87.9%99.50
23Darovasertib11.7%88.3%96.99
24Mitapivat11.1%88.9%100.00
25Rabusertib8.7%91.3%98.74

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)
Gilteritinib95.6%91.0%+4.6%
Pacritinib95.1%
Lazertinib87.8%100.0%-12.2%
Neratinib76.4%100.0%-23.6%
Mobocertinib73.0%100.0%-27.0%
Canertinib68.5%98.4%-29.9%
Vandetanib66.3%99.3%-33.0%
Erlotinib61.1%99.4%-38.4%
Abemaciclib58.1%
Deucravacitinib57.9%
Entrectinib54.3%
Repotrectinib49.8%
Fedratinib48.3%
Defactinib41.8%94.6%-52.8%
Avapritinib35.0%
Pralsetinib31.5%99.1%-67.6%
Pirtobrutinib28.3%
Sunitinib28.2%
Tivozanib27.2%
Selpercatinib21.7%
Palbociclib16.2%
Abrocitinib12.1%
Darovasertib11.7%
Mitapivat11.1%
Rabusertib8.7%

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