Mobocertinib
Sign in to save this workspacePrimary targets: EGFR · FDA status: FDA Approval Withdrawn
Selectivity scorecard
KISS
97.22
Gini
0.757
CATDS
0.035
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 Mobocertinib. Strongest target: EGFR at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | EGFR | 100.0% | 0.0% |
| 2 | ERBB2_HER2 | 99.8% | 0.2% |
| 3 | BLK | 99.7% | 0.3% |
| 4 | ERBB4_HER4 | 99.6% | 0.4% |
| 5 | BMX_ETK | 98.1% | 1.9% |
| 6 | BTK | 97.4% | 2.6% |
| 7 | ACK1 | 97.4% | 2.6% |
| 8 | JAK3 | 97.2% | 2.8% |
| 9 | TXK | 97.1% | 2.9% |
| 10 | ITK | 94.4% | 5.6% |
| 11 | TEC | 91.6% | 8.4% |
| 12 | FRK_PTK5 | 83.3% | 16.7% |
| 13 | BRK | 61.5% | 38.5% |
| 14 | LYN | 46.6% | 53.4% |
| 15 | RET | 37.2% | 62.8% |
| 16 | LRRK2 | 35.1% | 64.9% |
| 17 | ABL1 | 33.0% | 67.0% |
| 18 | HIPK4 | 31.6% | 68.4% |
| 19 | YES_YES1 | 28.7% | 71.3% |
| 20 | SRMS | 28.3% | 71.7% |
Selectivity landscape
Where Mobocertinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Mobocertinib.
Atlas insights for Mobocertinib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
On-target vs off-target shadow
On-target27%
Off-target73%
Ghost (2nd-order)0%
| Pathway | Composition | Total |Π| |
|---|---|---|
| ADIPOGENESIS | 1307.60 | |
| ALLOGRAFT_REJECTION | 4801.17 | |
| ANDROGEN_RESPONSE | 1184.87 | |
| ANGIOGENESIS | 788.53 | |
| APICAL_JUNCTION | 4324.56 | |
| APICAL_SURFACE | 519.76 | |
| APOPTOSIS | 3380.04 | |
| BILE_ACID_METABOLISM | 537.19 | |
| CHOLESTEROL_HOMEOSTASIS | 899.72 | |
| COAGULATION | 349.29 | |
| COMPLEMENT | 2904.83 | |
| DNA_REPAIR | 1093.60 | |
| E2F_TARGETS | 2242.99 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 931.61 | |
| ESTROGEN_RESPONSE_EARLY | 1461.30 | |
| ESTROGEN_RESPONSE_LATE | 1302.03 | |
| FATTY_ACID_METABOLISM | 230.29 | |
| G2M_CHECKPOINT | 1934.90 | |
| GLYCOLYSIS | 994.86 | |
| HEDGEHOG_SIGNALING | 412.09 | |
| HEME_METABOLISM | 910.36 | |
| HYPOXIA | 1822.93 | |
| IL2_STAT5_SIGNALING | 1744.27 | |
| IL6_JAK_STAT3_SIGNALING | 2199.32 | |
| INFLAMMATORY_RESPONSE | 2886.97 | |
| INTERFERON_ALPHA_RESPONSE | 468.17 | |
| INTERFERON_GAMMA_RESPONSE | 3318.64 | |
| KRAS_SIGNALING_DN | 525.97 | |
| KRAS_SIGNALING_UP | 1737.72 | |
| MITOTIC_SPINDLE | 3141.76 | |
| MTORC1_SIGNALING | 1682.23 | |
| MYC_TARGETS_V1 | 1475.70 | |
| MYC_TARGETS_V2 | 297.55 | |
| MYOGENESIS | 1627.78 | |
| NOTCH_SIGNALING | 161.48 | |
| OXIDATIVE_PHOSPHORYLATION | 465.52 | |
| P53_PATHWAY | 1867.57 | |
| PANCREAS_BETA_CELLS | 136.82 | |
| PEROXISOME | 452.31 | |
| PI3K_AKT_MTOR_SIGNALING | 4042.29 | |
| PROTEIN_SECRETION | 1093.37 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 258.55 | |
| SPERMATOGENESIS | 729.84 | |
| TGF_BETA_SIGNALING | 958.01 | |
| TNFA_SIGNALING_VIA_NFKB | 2383.91 | |
| UNFOLDED_PROTEIN_RESPONSE | 629.72 | |
| UV_RESPONSE_DN | 1888.14 | |
| UV_RESPONSE_UP | 1731.44 | |
| WNT_BETA_CATENIN_SIGNALING | 1023.38 | |
| XENOBIOTIC_METABOLISM | 1090.94 |
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.840 |
| SRR23303752 | — | 0.834 |
| SRR10899984 | — | 0.831 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.828 |
| SRR12202498 | — | 0.825 |
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