PKA (L206R)
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Drug response on this variant
| # | Drug | Inhibition on variant | Residual | KISS |
|---|---|---|---|---|
| 1 | Capivasertib | 98.1% | 1.9% | 96.48 |
| 2 | Darovasertib | 42.8% | 57.2% | 96.99 |
| 3 | Pacritinib | 27.5% | 72.5% | 88.64 |
| 4 | Abrocitinib | 21.1% | 78.9% | 99.50 |
| 5 | Fedratinib | 19.5% | 80.5% | 96.21 |
| 6 | Defactinib | 18.5% | 81.5% | 92.68 |
| 7 | Pralsetinib | 15.3% | 84.7% | 93.43 |
| 8 | Gilteritinib | 11.5% | 88.5% | 88.97 |
| 9 | Palbociclib | 9.3% | 90.7% | 98.75 |
| 10 | Sunitinib | 9.1% | 90.9% | 91.73 |
| 11 | Canertinib | 8.9% | 91.1% | 96.49 |
| 12 | Pexidartinib | 8.3% | 91.7% | 99.49 |
| 13 | Neratinib | 7.5% | 92.5% | 93.18 |
| 14 | Rabusertib | 7.2% | 92.8% | 98.74 |
| 15 | Vandetanib | 7.2% | 92.8% | 95.74 |
| 16 | Futibatinib | 7.0% | 93.0% | 98.48 |
| 17 | Upadacitinib | 6.7% | 93.3% | 97.98 |
| 18 | Remibrutinib | 4.7% | 95.3% | 99.50 |
| 19 | Selpercatinib | 4.4% | 95.6% | 96.72 |
| 20 | Entrectinib | 4.4% | 95.6% | 93.69 |
| 21 | Quizartinib | 3.8% | 96.2% | 99.50 |
| 22 | Pemigatinib | 3.8% | 96.2% | 98.23 |
| 23 | Repotrectinib | 3.5% | 96.5% | 84.21 |
| 24 | Pirtobrutinib | 3.4% | 96.6% | 99.49 |
| 25 | Alpelisib | 3.4% | 96.6% | 97.22 |
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) |
|---|---|---|---|
| Capivasertib | 98.1% | 99.7% | -1.6% |
| Darovasertib | 42.8% | 32.9% | +9.9% |
| Pacritinib | 27.5% | 28.8% | -1.3% |
| Abrocitinib | 21.1% | 37.8% | -16.7% |
| Fedratinib | 19.5% | — | — |
| Defactinib | 18.5% | 23.7% | -5.2% |
| Pralsetinib | 15.3% | 15.1% | +0.2% |
| Gilteritinib | 11.5% | 17.0% | -5.5% |
| Palbociclib | 9.3% | — | — |
| Sunitinib | 9.1% | 13.7% | -4.6% |
| Canertinib | 8.9% | — | — |
| Pexidartinib | 8.3% | — | — |
| Neratinib | 7.5% | — | — |
| Rabusertib | 7.2% | — | — |
| Vandetanib | 7.2% | — | — |
| Futibatinib | 7.0% | — | — |
| Upadacitinib | 6.7% | — | — |
| Remibrutinib | 4.7% | — | — |
| Selpercatinib | 4.4% | 8.3% | -3.8% |
| Entrectinib | 4.4% | — | — |
| Quizartinib | 3.8% | — | — |
| Pemigatinib | 3.8% | — | — |
| Repotrectinib | 3.5% | — | — |
| Pirtobrutinib | 3.4% | — | — |
| Alpelisib | 3.4% | — | — |
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