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TRKA (G595R/G667A)

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NTRK1 · Variant type: compound · HGVS: p.G595R;p.G667A

Components

p.G595Rp.G667A

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Ponatinib100.0%0.0%78.23
2Repotrectinib100.0%0.0%84.21
3Entrectinib97.1%2.9%93.69
4Darovasertib92.9%7.1%96.99
5Cabozantinib89.6%10.4%92.73
6Nintedanib63.2%36.8%90.23
7Pralsetinib56.7%43.3%93.43
8Defactinib47.3%52.7%92.68
9Ripretinib40.0%60.0%92.95
10Crizotinib37.0%63.0%91.39
11Sorafenib27.6%72.4%96.72
12Alpelisib26.8%73.2%97.22
13Tivozanib21.7%78.3%92.42
14Bosutinib21.3%78.7%87.22
15Fedratinib19.1%80.9%96.21
16Tenalisib14.1%85.9%97.98
17Regorafenib13.7%86.3%95.99
18Pacritinib13.7%86.3%88.64
19Ruxolitinib13.6%86.4%98.25
20Sunitinib12.9%87.1%91.73
21Duvelisib10.1%89.9%100.00
22Encorafenib9.9%90.1%98.50
23Rabusertib9.9%90.1%98.74
24Ribociclib9.5%90.5%99.25
25Binimetinib8.7%91.3%100.00

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)
Ponatinib100.0%98.4%+1.6%
Repotrectinib100.0%98.9%+1.1%
Entrectinib97.1%99.0%-2.0%
Darovasertib92.9%
Cabozantinib89.6%93.6%-4.0%
Nintedanib63.2%93.8%-30.6%
Pralsetinib56.7%98.7%-42.0%
Defactinib47.3%80.3%-33.1%
Ripretinib40.0%93.6%-53.5%
Crizotinib37.0%95.8%-58.8%
Sorafenib27.6%
Alpelisib26.8%97.5%-70.7%
Tivozanib21.7%85.7%-63.9%
Bosutinib21.3%67.0%-45.7%
Fedratinib19.1%56.2%-37.1%
Tenalisib14.1%59.0%-44.9%
Regorafenib13.7%
Pacritinib13.7%89.4%-75.7%
Ruxolitinib13.6%
Sunitinib12.9%82.8%-69.9%
Duvelisib10.1%
Encorafenib9.9%
Rabusertib9.9%
Ribociclib9.5%
Binimetinib8.7%

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