MELK (T460M)

MELK · Variant type: point · HGVS: p.T460M

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Nintedanib	98.0%	2.0%	90.23
2	Defactinib	86.6%	13.4%	92.68
3	Sunitinib	82.6%	17.4%	91.73
4	Alectinib	73.5%	26.5%	95.49
5	Ponatinib	58.2%	41.8%	78.23
6	Neratinib	54.2%	45.8%	93.18
7	Selpercatinib	49.9%	50.1%	96.72
8	Ripretinib	49.8%	50.3%	92.95
9	Gilteritinib	47.7%	52.3%	88.97
10	Fedratinib	45.9%	54.1%	96.21
11	Brigatinib	42.7%	57.3%	82.96
12	Palbociclib	42.5%	57.5%	98.75
13	Dabrafenib	41.5%	58.5%	94.74
14	Rabusertib	35.6%	64.4%	98.74
15	Capivasertib	30.2%	69.8%	96.48
16	Futibatinib	28.3%	71.7%	98.48
17	Baricitinib	28.1%	71.9%	97.99
18	Imatinib	23.2%	76.8%	99.00
19	Pacritinib	21.8%	78.2%	88.64
20	Entrectinib	17.3%	82.7%	93.69
21	Abrocitinib	15.8%	84.2%	99.50
22	Ruxolitinib	13.9%	86.1%	98.25
23	Fostamatinib	13.1%	86.9%	96.74
24	Idelalisib	13.1%	86.9%	100.00
25	Bosutinib	11.3%	88.7%	87.22

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)
Nintedanib	98.0%	99.4%	-1.4%
Defactinib	86.6%	81.4%	+5.2%
Sunitinib	82.6%	87.8%	-5.2%
Alectinib	73.5%	70.3%	+3.2%
Ponatinib	58.2%	40.0%	+18.2%
Neratinib	54.2%	78.2%	-24.0%
Selpercatinib	49.9%	60.4%	-10.5%
Ripretinib	49.8%	—	—
Gilteritinib	47.7%	44.6%	+3.1%
Fedratinib	45.9%	42.6%	+3.3%
Brigatinib	42.7%	51.4%	-8.7%
Palbociclib	42.5%	46.6%	-4.1%
Dabrafenib	41.5%	42.7%	-1.2%
Rabusertib	35.6%	—	—
Capivasertib	30.2%	—	—
Futibatinib	28.3%	—	—
Baricitinib	28.1%	—	—
Imatinib	23.2%	—	—
Pacritinib	21.8%	20.6%	+1.3%
Entrectinib	17.3%	23.5%	-6.2%
Abrocitinib	15.8%	—	—
Ruxolitinib	13.9%	28.2%	-14.3%
Fostamatinib	13.1%	—	—
Idelalisib	13.1%	—	—
Bosutinib	11.3%	—	—

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