c-MER (A708S)

MERTK · Variant type: point · HGVS: p.A708S

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Neratinib	98.7%	1.3%	93.18
2	Gilteritinib	98.2%	1.8%	88.97
3	Crizotinib	96.5%	3.5%	91.39
4	Bosutinib	96.4%	3.6%	87.22
5	Cabozantinib	94.7%	5.3%	92.73
6	Afatinib	90.5%	9.5%	98.50
7	Pacritinib	82.5%	17.5%	88.64
8	Ponatinib	76.3%	23.7%	78.23
9	Sunitinib	74.4%	25.6%	91.73
10	Selpercatinib	71.1%	28.9%	96.72
11	Vandetanib	70.2%	29.8%	95.74
12	Nintedanib	64.8%	35.2%	90.23
13	Dacomitinib	63.1%	36.9%	97.99
14	Tivozanib	58.4%	41.6%	92.42
15	Defactinib	55.1%	44.9%	92.68
16	Canertinib	54.9%	45.1%	96.49
17	Alectinib	53.0%	47.0%	95.49
18	Pazopanib	52.8%	47.2%	97.49
19	Brigatinib	47.8%	52.2%	82.96
20	Pralsetinib	37.2%	62.8%	93.43
21	Ibrutinib	31.3%	68.7%	94.74
22	Lenvatinib	31.2%	68.8%	97.74
23	Lazertinib	30.5%	69.5%	97.47
24	Gefitinib	26.6%	73.4%	99.25
25	Axitinib	24.5%	75.5%	93.23

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)
Neratinib	98.7%	—	—
Gilteritinib	98.2%	—	—
Crizotinib	96.5%	—	—
Bosutinib	96.4%	—	—
Cabozantinib	94.7%	—	—
Afatinib	90.5%	—	—
Pacritinib	82.5%	—	—
Ponatinib	76.3%	—	—
Sunitinib	74.4%	—	—
Selpercatinib	71.1%	—	—
Vandetanib	70.2%	—	—
Nintedanib	64.8%	—	—
Dacomitinib	63.1%	—	—
Tivozanib	58.4%	—	—
Defactinib	55.1%	—	—
Canertinib	54.9%	—	—
Alectinib	53.0%	—	—
Pazopanib	52.8%	—	—
Brigatinib	47.8%	—	—
Pralsetinib	37.2%	—	—
Ibrutinib	31.3%	—	—
Lenvatinib	31.2%	—	—
Lazertinib	30.5%	—	—
Gefitinib	26.6%	—	—
Axitinib	24.5%	—	—

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