ERN1/IRE1 (R727A)

ERN1 · Variant type: point · HGVS: p.R727A

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Gilteritinib	52.8%	47.2%	88.97
2	Umbralisib	18.3%	81.7%	98.74
3	Pacritinib	17.3%	82.7%	88.64
4	Leniolisib	17.3%	82.7%	100.00
5	Selumetinib	16.6%	83.4%	100.00
6	Apatinib	14.1%	85.9%	97.73
7	Infigratinib	11.2%	88.8%	98.24
8	Defactinib	9.5%	90.5%	92.68
9	Rabusertib	6.2%	93.8%	98.74
10	Cobimetinib	5.9%	94.1%	100.00
11	Quizartinib	5.5%	94.5%	99.50
12	Abemaciclib	5.4%	94.6%	91.48
13	Selpercatinib	5.4%	94.6%	96.72
14	Ripretinib	5.1%	94.9%	92.95
15	Neratinib	5.0%	95.0%	93.18
16	Idelalisib	4.3%	95.7%	100.00
17	Paxalisib	3.6%	96.4%	99.75
18	Palbociclib	2.1%	97.9%	98.75
19	Inavolisib	1.8%	98.2%	100.00
20	Pemigatinib	1.6%	98.4%	98.23
21	Pirtobrutinib	1.4%	98.6%	99.49
22	Deucravacitinib	1.2%	98.8%	98.99
23	Lazertinib	1.1%	98.9%	97.47
24	Pralsetinib	1.0%	99.0%	93.43
25	Tenalisib	1.0%	99.0%	97.98

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)
Gilteritinib	52.8%	—	—
Umbralisib	18.3%	—	—
Pacritinib	17.3%	—	—
Leniolisib	17.3%	—	—
Selumetinib	16.6%	—	—
Apatinib	14.1%	—	—
Infigratinib	11.2%	—	—
Defactinib	9.5%	—	—
Rabusertib	6.2%	—	—
Cobimetinib	5.9%	—	—
Quizartinib	5.5%	—	—
Abemaciclib	5.4%	—	—
Selpercatinib	5.4%	—	—
Ripretinib	5.1%	—	—
Neratinib	5.0%	—	—
Idelalisib	4.3%	—	—
Paxalisib	3.6%	—	—
Palbociclib	2.1%	—	—
Inavolisib	1.8%	—	—
Pemigatinib	1.6%	—	—
Pirtobrutinib	1.4%	—	—
Deucravacitinib	1.2%	—	—
Lazertinib	1.1%	—	—
Pralsetinib	1.0%	—	—
Tenalisib	1.0%	—	—

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