c-Kit (D816E)

KIT · Variant type: point · HGVS: p.D816E

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Ripretinib	99.3%	0.7%	92.95
2	Avapritinib	99.1%	0.9%	97.73
3	Dasatinib	98.8%	1.2%	87.97
4	Tivozanib	98.6%	1.4%	92.42
5	Pralsetinib	97.9%	2.1%	93.43
6	Ponatinib	97.6%	2.4%	78.23
7	Brigatinib	97.3%	2.7%	82.96
8	Selpercatinib	96.8%	3.2%	96.72
9	Nintedanib	96.5%	3.5%	90.23
10	Erdafitinib	96.1%	3.9%	95.71
11	Fostamatinib	94.9%	5.1%	96.74
12	Apatinib	94.5%	5.5%	97.73
13	Pacritinib	94.0%	6.0%	88.64
14	Gilteritinib	93.9%	6.1%	88.97
15	Sunitinib	93.3%	6.7%	91.73
16	Sorafenib	92.5%	7.5%	96.72
17	Axitinib	92.4%	7.6%	93.23
18	Cabozantinib	90.8%	9.2%	92.73
19	Bosutinib	88.1%	11.9%	87.22
20	Regorafenib	87.8%	12.2%	95.99
21	Fedratinib	86.5%	13.5%	96.21
22	Pazopanib	85.9%	14.1%	97.49
23	Nilotinib	85.6%	14.4%	96.49
24	Vandetanib	84.7%	15.3%	95.74
25	Umbralisib	84.2%	15.8%	98.74

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)
Ripretinib	99.3%	—	—
Avapritinib	99.1%	—	—
Dasatinib	98.8%	—	—
Tivozanib	98.6%	—	—
Pralsetinib	97.9%	—	—
Ponatinib	97.6%	—	—
Brigatinib	97.3%	—	—
Selpercatinib	96.8%	—	—
Nintedanib	96.5%	—	—
Erdafitinib	96.1%	—	—
Fostamatinib	94.9%	—	—
Apatinib	94.5%	—	—
Pacritinib	94.0%	—	—
Gilteritinib	93.9%	—	—
Sunitinib	93.3%	—	—
Sorafenib	92.5%	—	—
Axitinib	92.4%	—	—
Cabozantinib	90.8%	—	—
Bosutinib	88.1%	—	—
Regorafenib	87.8%	—	—
Fedratinib	86.5%	—	—
Pazopanib	85.9%	—	—
Nilotinib	85.6%	—	—
Vandetanib	84.7%	—	—
Umbralisib	84.2%	—	—

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