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MEK1 (P124L)

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MAP2K1 · Variant type: point · HGVS: p.P124L

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Sunitinib85.3%14.7%91.73
2Neratinib76.8%23.2%93.18
3Bosutinib72.6%27.4%87.22
4Pirtobrutinib70.8%29.2%99.49
5Capivasertib69.7%30.3%96.48
6Imatinib67.1%32.9%99.00
7Trametinib57.5%42.5%99.50
8Osimertinib57.3%42.7%97.24
9Fostamatinib52.5%47.5%96.74
10Tivozanib50.1%49.9%92.42
11Vemurafenib48.0%52.0%96.49
12Nintedanib46.9%53.1%90.23
13Gilteritinib45.5%54.5%88.97
14Abrocitinib43.9%56.1%99.50
15Ripretinib43.3%56.7%92.95
16Cabozantinib39.4%60.6%92.73
17Zanubrutinib27.0%73.0%98.24
18Ponatinib25.2%74.8%78.23
19Pacritinib23.5%76.5%88.64
20Lorlatinib23.1%76.9%97.24
21Cobimetinib21.2%78.8%100.00
22Axitinib19.6%80.4%93.23
23Binimetinib19.1%80.9%100.00
24Dasatinib18.9%81.1%87.97
25Defactinib17.3%82.7%92.68

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)
Sunitinib85.3%68.7%+16.7%
Neratinib76.8%74.7%+2.0%
Bosutinib72.6%89.8%-17.3%
Pirtobrutinib70.8%81.8%-11.0%
Capivasertib69.7%45.6%+24.1%
Imatinib67.1%
Trametinib57.5%98.7%-41.2%
Osimertinib57.3%
Fostamatinib52.5%
Tivozanib50.1%62.9%-12.8%
Vemurafenib48.0%77.8%-29.8%
Nintedanib46.9%46.3%+0.6%
Gilteritinib45.5%58.6%-13.0%
Abrocitinib43.9%31.8%+12.1%
Ripretinib43.3%
Cabozantinib39.4%81.2%-41.8%
Zanubrutinib27.0%54.1%-27.1%
Ponatinib25.2%
Pacritinib23.5%19.3%+4.2%
Lorlatinib23.1%
Cobimetinib21.2%73.5%-52.3%
Axitinib19.6%
Binimetinib19.1%79.1%-60.0%
Dasatinib18.9%34.5%-15.6%
Defactinib17.3%

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