EGFR (C797G/L858R)

EGFR · Variant type: compound · HGVS: p.C797G;p.L858R

Components

p.C797Gp.L858R

#	Drug	Inhibition on variant	Residual	KISS
1	Canertinib	99.3%	0.7%	96.49
2	Erlotinib	99.2%	0.8%	99.75
3	Vandetanib	98.5%	1.5%	95.74
4	Neratinib	97.4%	2.6%	93.18
5	Mobocertinib	78.2%	21.8%	97.22
6	Pacritinib	59.5%	40.5%	88.64
7	Gilteritinib	58.0%	42.0%	88.97
8	Defactinib	29.7%	70.3%	92.68
9	Fedratinib	19.1%	80.9%	96.21
10	Lazertinib	16.7%	83.3%	97.47
11	Avapritinib	12.2%	87.8%	97.73
12	Pralsetinib	11.8%	88.2%	93.43
13	Umbralisib	10.7%	89.3%	98.74
14	Pirtobrutinib	10.6%	89.4%	99.49
15	Tivozanib	10.0%	90.0%	92.42
16	Tenalisib	8.6%	91.4%	97.98
17	Leniolisib	8.1%	91.9%	100.00
18	Tepotinib	7.9%	92.1%	99.75
19	Selumetinib	7.8%	92.2%	100.00
20	Abrocitinib	7.0%	93.0%	99.50
21	Entrectinib	6.1%	93.9%	93.69
22	Cobimetinib	5.5%	94.5%	100.00
23	Apatinib	4.9%	95.1%	97.73
24	Zanubrutinib	4.5%	95.5%	98.24
25	Infigratinib	4.1%	95.9%	98.24

Positive Δ means the drug hits the variant harder than wild-type (mutation-selective); negative Δ means it loses potency (resistance).

Drug	Variant inh	WT inh	Δ (variant − WT)
Canertinib	99.3%	98.4%	+0.9%
Erlotinib	99.2%	99.4%	-0.3%
Vandetanib	98.5%	99.3%	-0.8%
Neratinib	97.4%	100.0%	-2.6%
Mobocertinib	78.2%	100.0%	-21.8%
Pacritinib	59.5%	—	—
Gilteritinib	58.0%	91.0%	-33.1%
Defactinib	29.7%	94.6%	-64.9%
Fedratinib	19.1%	—	—
Lazertinib	16.7%	100.0%	-83.3%
Avapritinib	12.2%	—	—
Pralsetinib	11.8%	99.1%	-87.3%
Umbralisib	10.7%	—	—
Pirtobrutinib	10.6%	—	—
Tivozanib	10.0%	—	—
Tenalisib	8.6%	—	—
Leniolisib	8.1%	—	—
Tepotinib	7.9%	—	—
Selumetinib	7.8%	—	—
Abrocitinib	7.0%	—	—
Entrectinib	6.1%	—	—
Cobimetinib	5.5%	—	—
Apatinib	4.9%	—	—
Zanubrutinib	4.5%	88.2%	-83.6%
Infigratinib	4.1%	—	—

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