LRRK2 (I2020T)

LRRK2 · Variant type: point · HGVS: p.I2020T

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Ceritinib	99.5%	0.5%	95.44
2	Gilteritinib	98.7%	1.3%	88.97
3	Brigatinib	97.7%	2.3%	82.96
4	Alectinib	96.9%	3.1%	95.49
5	Sunitinib	96.0%	4.0%	91.73
6	Axitinib	95.4%	4.6%	93.23
7	Ponatinib	92.4%	7.6%	78.23
8	Defactinib	85.8%	14.2%	92.68
9	Osimertinib	76.7%	23.3%	97.24
10	Bosutinib	74.9%	25.1%	87.22
11	Vemurafenib	74.1%	25.9%	96.49
12	Ruxolitinib	71.7%	28.3%	98.25
13	Fostamatinib	70.5%	29.5%	96.74
14	Nintedanib	70.0%	30.0%	90.23
15	Pacritinib	66.6%	33.4%	88.64
16	Repotrectinib	66.0%	34.0%	84.21
17	Baricitinib	61.1%	38.9%	97.99
18	Abemaciclib	61.1%	38.9%	91.48
19	Upadacitinib	60.0%	40.0%	97.98
20	Lorlatinib	58.0%	42.0%	97.24
21	Fedratinib	40.8%	59.2%	96.21
22	Canertinib	37.5%	62.5%	96.49
23	Lenvatinib	37.2%	62.8%	97.74
24	Pralsetinib	36.9%	63.1%	93.43
25	Selpercatinib	32.1%	67.9%	96.72

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)
Ceritinib	99.5%	99.4%	+0.0%
Gilteritinib	98.7%	97.2%	+1.5%
Brigatinib	97.7%	96.6%	+1.1%
Alectinib	96.9%	94.5%	+2.3%
Sunitinib	96.0%	95.8%	+0.3%
Axitinib	95.4%	92.3%	+3.1%
Ponatinib	92.4%	63.4%	+29.1%
Defactinib	85.8%	95.8%	-9.9%
Osimertinib	76.7%	82.4%	-5.7%
Bosutinib	74.9%	69.5%	+5.4%
Vemurafenib	74.1%	—	—
Ruxolitinib	71.7%	63.0%	+8.8%
Fostamatinib	70.5%	69.3%	+1.2%
Nintedanib	70.0%	67.2%	+2.8%
Pacritinib	66.6%	83.4%	-16.8%
Repotrectinib	66.0%	68.8%	-2.8%
Baricitinib	61.1%	62.8%	-1.6%
Abemaciclib	61.1%	79.1%	-18.0%
Upadacitinib	60.0%	73.3%	-13.3%
Lorlatinib	58.0%	—	—
Fedratinib	40.8%	—	—
Canertinib	37.5%	—	—
Lenvatinib	37.2%	—	—
Pralsetinib	36.9%	—	—
Selpercatinib	32.1%	—	—

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