c-SRC (Y530F)

SRC · Variant type: point · HGVS: p.Y530F

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Repotrectinib	99.4%	0.6%	84.21
2	Vandetanib	97.1%	2.9%	95.74
3	Pralsetinib	96.7%	3.3%	93.43
4	Pacritinib	96.0%	4.0%	88.64
5	Entrectinib	95.6%	4.4%	93.69
6	Fedratinib	93.0%	7.0%	96.21
7	Gilteritinib	91.9%	8.1%	88.97
8	Canertinib	91.2%	8.8%	96.49
9	Avapritinib	82.1%	17.9%	97.73
10	Sunitinib	79.2%	20.8%	91.73
11	Erdafitinib	73.7%	26.4%	95.71
12	Tivozanib	64.8%	35.2%	92.42
13	Ripretinib	64.3%	35.7%	92.95
14	Alpelisib	64.0%	36.0%	97.22
15	Selpercatinib	59.8%	40.2%	96.72
16	Defactinib	58.3%	41.7%	92.68
17	Neratinib	57.3%	42.7%	93.18
18	Erlotinib	53.5%	46.5%	99.75
19	Tenalisib	43.8%	56.2%	97.98
20	Paxalisib	34.5%	65.5%	99.75
21	Darovasertib	33.4%	66.6%	96.99
22	Mobocertinib	29.9%	70.1%	97.22
23	Zanubrutinib	25.8%	74.2%	98.24
24	Apatinib	23.1%	76.9%	97.73
25	Futibatinib	20.7%	79.3%	98.48

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)
Repotrectinib	99.4%	—	—
Vandetanib	97.1%	—	—
Pralsetinib	96.7%	—	—
Pacritinib	96.0%	—	—
Entrectinib	95.6%	—	—
Fedratinib	93.0%	—	—
Gilteritinib	91.9%	—	—
Canertinib	91.2%	—	—
Avapritinib	82.1%	—	—
Sunitinib	79.2%	—	—
Erdafitinib	73.7%	—	—
Tivozanib	64.8%	—	—
Ripretinib	64.3%	—	—
Alpelisib	64.0%	—	—
Selpercatinib	59.8%	—	—
Defactinib	58.3%	—	—
Neratinib	57.3%	—	—
Erlotinib	53.5%	—	—
Tenalisib	43.8%	—	—
Paxalisib	34.5%	—	—
Darovasertib	33.4%	—	—
Mobocertinib	29.9%	—	—
Zanubrutinib	25.8%	—	—
Apatinib	23.1%	—	—
Futibatinib	20.7%	—	—

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