Avapritinib
Sign in to save this workspacePrimary targets: PDGFRA, PDGFRB · FDA status: FDA Approved
Selectivity scorecard
KISS
97.73
Gini
0.644
CATDS
0.016
Computed from wild-type kinome inhibition at 1 μM. Gini reproduces the published values within tolerance; KISS and CATDS are computed but pending reconciliation with the paper's reference code.
Polypharmacology radar
Top 20 strongest-inhibited wild-type kinases for Avapritinib. Strongest target: PDGFRA at 99.1% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | PDGFRA | 99.1% | 0.9% |
| 2 | C_KIT | 98.8% | 1.2% |
| 3 | LIMK1 | 98.4% | 1.6% |
| 4 | DDR1 | 96.0% | 4.0% |
| 5 | FMS | 95.9% | 4.1% |
| 6 | LCK | 92.7% | 7.3% |
| 7 | LYN | 91.4% | 8.6% |
| 8 | RET | 90.4% | 9.6% |
| 9 | PDGFRB | 90.4% | 9.6% |
| 10 | NEK5 | 89.7% | 10.3% |
| 11 | FLT3 | 88.6% | 11.4% |
| 12 | LIMK2 | 85.0% | 15.0% |
| 13 | FGR | 80.0% | 20.0% |
| 14 | BLK | 79.3% | 20.7% |
| 15 | YES_YES1 | 78.7% | 21.3% |
| 16 | NEK1 | 78.7% | 21.3% |
| 17 | FLT4_VEGFR3 | 76.0% | 24.0% |
| 18 | ABL1 | 75.1% | 24.9% |
| 19 | ERBB2_HER2 | 75.1% | 24.9% |
| 20 | CLK1 | 72.4% | 27.6% |
Selectivity landscape
Where Avapritinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Avapritinib.
Atlas insights for Avapritinib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
On-target vs off-target shadow
On-target0%
Off-target100%
Ghost (2nd-order)0%
| Pathway | Composition | Total |Π| |
|---|---|---|
| ADIPOGENESIS | 2135.12 | |
| ALLOGRAFT_REJECTION | 6909.77 | |
| ANDROGEN_RESPONSE | 1197.89 | |
| ANGIOGENESIS | 1135.83 | |
| APICAL_JUNCTION | 7383.36 | |
| APICAL_SURFACE | 575.80 | |
| APOPTOSIS | 5018.59 | |
| BILE_ACID_METABOLISM | 682.32 | |
| CHOLESTEROL_HOMEOSTASIS | 939.70 | |
| COAGULATION | 945.96 | |
| COMPLEMENT | 4185.30 | |
| DNA_REPAIR | 1436.77 | |
| E2F_TARGETS | 3409.15 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1492.51 | |
| ESTROGEN_RESPONSE_EARLY | 2109.66 | |
| ESTROGEN_RESPONSE_LATE | 2149.35 | |
| FATTY_ACID_METABOLISM | 682.74 | |
| G2M_CHECKPOINT | 3908.09 | |
| GLYCOLYSIS | 1977.16 | |
| HEDGEHOG_SIGNALING | 718.97 | |
| HEME_METABOLISM | 1701.90 | |
| HYPOXIA | 3164.50 | |
| IL2_STAT5_SIGNALING | 2344.72 | |
| IL6_JAK_STAT3_SIGNALING | 4124.34 | |
| INFLAMMATORY_RESPONSE | 3693.28 | |
| INTERFERON_ALPHA_RESPONSE | 577.08 | |
| INTERFERON_GAMMA_RESPONSE | 4819.13 | |
| KRAS_SIGNALING_DN | 575.15 | |
| KRAS_SIGNALING_UP | 2988.33 | |
| MITOTIC_SPINDLE | 4891.20 | |
| MTORC1_SIGNALING | 2888.53 | |
| MYC_TARGETS_V1 | 2676.98 | |
| MYC_TARGETS_V2 | 667.66 | |
| MYOGENESIS | 2123.72 | |
| NOTCH_SIGNALING | 280.76 | |
| OXIDATIVE_PHOSPHORYLATION | 1088.20 | |
| P53_PATHWAY | 2658.27 | |
| PANCREAS_BETA_CELLS | 268.28 | |
| PEROXISOME | 948.50 | |
| PI3K_AKT_MTOR_SIGNALING | 6864.59 | |
| PROTEIN_SECRETION | 1247.81 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 435.05 | |
| SPERMATOGENESIS | 1133.89 | |
| TGF_BETA_SIGNALING | 1426.41 | |
| TNFA_SIGNALING_VIA_NFKB | 3383.64 | |
| UNFOLDED_PROTEIN_RESPONSE | 1196.36 | |
| UV_RESPONSE_DN | 3532.57 | |
| UV_RESPONSE_UP | 2755.60 | |
| WNT_BETA_CATENIN_SIGNALING | 1444.24 | |
| XENOBIOTIC_METABOLISM | 1212.30 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.840 |
| SRR23303752 | — | 0.832 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.826 |
| aMVAC.P_005_TURBT_S223 | — | 0.821 |
| SRR10899984 | — | 0.819 |
Annotations
Sign in to read and post annotations.
Loading…