ERN1/IRE1 (R727A/R728A)
Sign in to save this workspaceERN1 · Variant type: compound · HGVS: p.R727A;p.R728A
Components
p.R727Ap.R728A
Drug response on this variant
| # | Drug | Inhibition on variant | Residual | KISS |
|---|---|---|---|---|
| 1 | Gilteritinib | 60.1% | 39.9% | 88.97 |
| 2 | Pirtobrutinib | 30.5% | 69.5% | 99.49 |
| 3 | Infigratinib | 22.7% | 77.3% | 98.24 |
| 4 | Apatinib | 19.0% | 81.0% | 97.73 |
| 5 | Umbralisib | 17.7% | 82.3% | 98.74 |
| 6 | Pacritinib | 17.1% | 82.9% | 88.64 |
| 7 | Neratinib | 15.5% | 84.5% | 93.18 |
| 8 | Fedratinib | 14.9% | 85.1% | 96.21 |
| 9 | Tucatinib | 13.3% | 86.7% | 99.75 |
| 10 | Leniolisib | 12.9% | 87.1% | 100.00 |
| 11 | Defactinib | 12.7% | 87.3% | 92.68 |
| 12 | Tivozanib | 12.1% | 87.9% | 92.42 |
| 13 | Avapritinib | 10.6% | 89.4% | 97.73 |
| 14 | Paxalisib | 9.9% | 90.1% | 99.75 |
| 15 | Mitapivat | 9.2% | 90.8% | 100.00 |
| 16 | Tenalisib | 8.6% | 91.4% | 97.98 |
| 17 | Selpercatinib | 8.5% | 91.5% | 96.72 |
| 18 | Abrocitinib | 7.8% | 92.2% | 99.50 |
| 19 | Zanubrutinib | 7.3% | 92.7% | 98.24 |
| 20 | Abemaciclib | 7.0% | 93.0% | 91.48 |
| 21 | Asciminib | 6.7% | 93.3% | 100.00 |
| 22 | Ripretinib | 6.2% | 93.8% | 92.95 |
| 23 | Tepotinib | 5.8% | 94.2% | 99.75 |
| 24 | Sunitinib | 4.9% | 95.1% | 91.73 |
| 25 | Pexidartinib | 4.9% | 95.1% | 99.49 |
Wild-type vs variant — drug response delta
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 | 60.1% | — | — |
| Pirtobrutinib | 30.5% | — | — |
| Infigratinib | 22.7% | — | — |
| Apatinib | 19.0% | — | — |
| Umbralisib | 17.7% | — | — |
| Pacritinib | 17.1% | — | — |
| Neratinib | 15.5% | — | — |
| Fedratinib | 14.9% | — | — |
| Tucatinib | 13.3% | — | — |
| Leniolisib | 12.9% | — | — |
| Defactinib | 12.7% | — | — |
| Tivozanib | 12.1% | — | — |
| Avapritinib | 10.6% | — | — |
| Paxalisib | 9.9% | — | — |
| Mitapivat | 9.2% | — | — |
| Tenalisib | 8.6% | — | — |
| Selpercatinib | 8.5% | — | — |
| Abrocitinib | 7.8% | — | — |
| Zanubrutinib | 7.3% | — | — |
| Abemaciclib | 7.0% | — | — |
| Asciminib | 6.7% | — | — |
| Ripretinib | 6.2% | — | — |
| Tepotinib | 5.8% | — | — |
| Sunitinib | 4.9% | — | — |
| Pexidartinib | 4.9% | — | — |
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