Osimertinib
Sign in to save this workspacePrimary targets: EGFR · FDA status: FDA Approved
Selectivity scorecard
KISS
97.24
Gini
0.733
CATDS
0.019
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 Osimertinib. Strongest target: ERBB4_HER4 at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | ERBB4_HER4 | 100.0% | 0.0% |
| 2 | ERBB2_HER2 | 99.4% | 0.6% |
| 3 | EGFR | 99.1% | 0.9% |
| 4 | TXK | 97.6% | 2.4% |
| 5 | JAK3 | 97.5% | 2.5% |
| 6 | ROS_ROS1 | 97.2% | 2.8% |
| 7 | BTK | 96.3% | 3.7% |
| 8 | TNK1 | 92.8% | 7.2% |
| 9 | ACK1 | 92.6% | 7.4% |
| 10 | MYO3B | 90.9% | 9.1% |
| 11 | BLK | 90.0% | 9.9% |
| 12 | MNK1 | 86.2% | 13.8% |
| 13 | BRK | 85.8% | 14.2% |
| 14 | ITK | 85.4% | 14.6% |
| 15 | LRRK2 | 82.4% | 17.6% |
| 16 | TNIK | 81.3% | 18.7% |
| 17 | ALK | 80.5% | 19.5% |
| 18 | YSK4_MAP3K19 | 79.7% | 20.3% |
| 19 | BMX_ETK | 79.5% | 20.5% |
| 20 | TEC | 74.6% | 25.4% |
Selectivity landscape
Where Osimertinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Osimertinib.
Atlas insights for Osimertinib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
On-target vs off-target shadow
On-target26%
Off-target74%
Ghost (2nd-order)0%
| Pathway | Composition | Total |Π| |
|---|---|---|
| ADIPOGENESIS | 1325.48 | |
| ALLOGRAFT_REJECTION | 4420.34 | |
| ANDROGEN_RESPONSE | 1280.93 | |
| ANGIOGENESIS | 839.96 | |
| APICAL_JUNCTION | 4356.80 | |
| APICAL_SURFACE | 437.36 | |
| APOPTOSIS | 3203.97 | |
| BILE_ACID_METABOLISM | 674.76 | |
| CHOLESTEROL_HOMEOSTASIS | 916.51 | |
| COAGULATION | 357.54 | |
| COMPLEMENT | 2841.60 | |
| DNA_REPAIR | 1268.90 | |
| E2F_TARGETS | 2530.27 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1070.12 | |
| ESTROGEN_RESPONSE_EARLY | 1528.46 | |
| ESTROGEN_RESPONSE_LATE | 1602.07 | |
| FATTY_ACID_METABOLISM | 430.46 | |
| G2M_CHECKPOINT | 1873.51 | |
| GLYCOLYSIS | 1377.07 | |
| HEDGEHOG_SIGNALING | 625.96 | |
| HEME_METABOLISM | 748.16 | |
| HYPOXIA | 2145.49 | |
| IL2_STAT5_SIGNALING | 1465.40 | |
| IL6_JAK_STAT3_SIGNALING | 2270.84 | |
| INFLAMMATORY_RESPONSE | 2784.03 | |
| INTERFERON_ALPHA_RESPONSE | 402.60 | |
| INTERFERON_GAMMA_RESPONSE | 3402.38 | |
| KRAS_SIGNALING_DN | 558.21 | |
| KRAS_SIGNALING_UP | 1571.62 | |
| MITOTIC_SPINDLE | 3027.92 | |
| MTORC1_SIGNALING | 1999.07 | |
| MYC_TARGETS_V1 | 1496.03 | |
| MYC_TARGETS_V2 | 349.66 | |
| MYOGENESIS | 1594.99 | |
| NOTCH_SIGNALING | 303.17 | |
| OXIDATIVE_PHOSPHORYLATION | 737.70 | |
| P53_PATHWAY | 1921.25 | |
| PANCREAS_BETA_CELLS | 147.08 | |
| PEROXISOME | 513.21 | |
| PI3K_AKT_MTOR_SIGNALING | 4279.46 | |
| PROTEIN_SECRETION | 1135.28 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 161.40 | |
| SPERMATOGENESIS | 875.16 | |
| TGF_BETA_SIGNALING | 1051.03 | |
| TNFA_SIGNALING_VIA_NFKB | 2444.83 | |
| UNFOLDED_PROTEIN_RESPONSE | 815.48 | |
| UV_RESPONSE_DN | 1789.77 | |
| UV_RESPONSE_UP | 1671.31 | |
| WNT_BETA_CATENIN_SIGNALING | 1278.86 | |
| XENOBIOTIC_METABOLISM | 1186.86 |
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.857 |
| SRR23303752 | — | 0.845 |
| SRR10899984 | — | 0.837 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.836 |
| aMVAC.P_005_TURBT_S223 | — | 0.836 |
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