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TRKA (G595R)

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NTRK1 · Variant type: point · HGVS: p.G595R

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Repotrectinib99.1%0.9%84.21
2Ponatinib99.0%1.0%78.23
3Entrectinib81.3%18.7%93.69
4Cabozantinib68.5%31.5%92.73
5Darovasertib49.6%50.4%96.99
6Tivozanib34.7%65.3%92.42
7Ripretinib32.5%67.5%92.95
8Pralsetinib21.6%78.4%93.43
9Leniolisib19.7%80.3%100.00
10Umbralisib18.9%81.1%98.74
11Defactinib18.5%81.5%92.68
12Infigratinib17.1%82.9%98.24
13Pazopanib17.0%83.0%97.49
14Selumetinib16.1%83.9%100.00
15Apatinib11.8%88.2%97.73
16Binimetinib11.1%88.9%100.00
17Sunitinib9.1%90.9%91.73
18Ribociclib9.1%90.9%99.25
19Alpelisib8.9%91.1%97.22
20Capivasertib8.2%91.8%96.48
21Osimertinib7.9%92.1%97.24
22Trametinib7.9%92.1%99.50
23Alectinib7.9%92.1%95.49
24Pacritinib7.1%92.9%88.64
25Deucravacitinib6.7%93.3%98.99

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)
Repotrectinib99.1%98.9%+0.2%
Ponatinib99.0%98.4%+0.6%
Entrectinib81.3%99.0%-17.7%
Cabozantinib68.5%93.6%-25.0%
Darovasertib49.6%
Tivozanib34.7%85.7%-50.9%
Ripretinib32.5%93.6%-61.1%
Pralsetinib21.6%98.7%-77.1%
Leniolisib19.7%
Umbralisib18.9%
Defactinib18.5%80.3%-61.8%
Infigratinib17.1%
Pazopanib17.0%
Selumetinib16.1%
Apatinib11.8%
Binimetinib11.1%
Sunitinib9.1%82.8%-73.6%
Ribociclib9.1%
Alpelisib8.9%97.5%-88.6%
Capivasertib8.2%
Osimertinib7.9%
Trametinib7.9%
Alectinib7.9%
Pacritinib7.1%89.4%-82.4%
Deucravacitinib6.7%

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