Brigatinib
Sign in to save this workspacePrimary targets: ALK · FDA status: FDA Approved
Selectivity scorecard
KISS
82.96
Gini
0.513
CATDS
0.006
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 Brigatinib. Strongest target: CAMK2D at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | CAMK2D | 100.0% | 0.0% |
| 2 | ERBB2_HER2 | 100.0% | 0.0% |
| 3 | CAMK2A | 99.7% | 0.3% |
| 4 | CHK2 | 99.4% | 0.6% |
| 5 | CLK1 | 99.4% | 0.6% |
| 6 | STK22D_TSSK1 | 99.3% | 0.7% |
| 7 | ALK | 99.2% | 0.8% |
| 8 | PYK2 | 99.1% | 0.9% |
| 9 | RSK3 | 98.5% | 1.5% |
| 10 | EGFR | 98.5% | 1.5% |
| 11 | SIK2 | 98.4% | 1.6% |
| 12 | FER | 98.2% | 1.8% |
| 13 | ROS_ROS1 | 98.2% | 1.8% |
| 14 | FLT3 | 98.1% | 1.9% |
| 15 | AMPK(A1_B2_G2) | 98.0% | 2.0% |
| 16 | ACK1 | 98.0% | 2.0% |
| 17 | AMPK(A2_B1_G2) | 97.9% | 2.1% |
| 18 | BRK | 97.8% | 2.2% |
| 19 | MYO3B | 97.6% | 2.4% |
| 20 | ERBB4_HER4 | 97.6% | 2.4% |
Selectivity landscape
Where Brigatinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Brigatinib.
Atlas insights for Brigatinib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
On-target vs off-target shadow
On-target1%
Off-target99%
Ghost (2nd-order)0%
| Pathway | Composition | Total |Π| |
|---|---|---|
| ADIPOGENESIS | 3850.72 | |
| ALLOGRAFT_REJECTION | 12789.57 | |
| ANDROGEN_RESPONSE | 3296.24 | |
| ANGIOGENESIS | 2270.28 | |
| APICAL_JUNCTION | 13595.57 | |
| APICAL_SURFACE | 1369.19 | |
| APOPTOSIS | 10666.81 | |
| BILE_ACID_METABOLISM | 1633.31 | |
| CHOLESTEROL_HOMEOSTASIS | 2083.12 | |
| COAGULATION | 1397.19 | |
| COMPLEMENT | 7791.46 | |
| DNA_REPAIR | 2794.43 | |
| E2F_TARGETS | 7771.65 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 3787.64 | |
| ESTROGEN_RESPONSE_EARLY | 5723.00 | |
| ESTROGEN_RESPONSE_LATE | 5665.42 | |
| FATTY_ACID_METABOLISM | 1224.13 | |
| G2M_CHECKPOINT | 7361.32 | |
| GLYCOLYSIS | 4768.62 | |
| HEDGEHOG_SIGNALING | 1371.18 | |
| HEME_METABOLISM | 2973.40 | |
| HYPOXIA | 6050.17 | |
| IL2_STAT5_SIGNALING | 4090.98 | |
| IL6_JAK_STAT3_SIGNALING | 8155.46 | |
| INFLAMMATORY_RESPONSE | 7153.79 | |
| INTERFERON_ALPHA_RESPONSE | 1068.07 | |
| INTERFERON_GAMMA_RESPONSE | 9220.21 | |
| KRAS_SIGNALING_DN | 2279.05 | |
| KRAS_SIGNALING_UP | 4676.49 | |
| MITOTIC_SPINDLE | 10098.17 | |
| MTORC1_SIGNALING | 6031.05 | |
| MYC_TARGETS_V1 | 4404.52 | |
| MYC_TARGETS_V2 | 1089.90 | |
| MYOGENESIS | 5653.28 | |
| NOTCH_SIGNALING | 364.07 | |
| OXIDATIVE_PHOSPHORYLATION | 1973.70 | |
| P53_PATHWAY | 5060.75 | |
| PANCREAS_BETA_CELLS | 358.50 | |
| PEROXISOME | 1884.23 | |
| PI3K_AKT_MTOR_SIGNALING | 13726.04 | |
| PROTEIN_SECRETION | 3465.93 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 682.59 | |
| SPERMATOGENESIS | 2281.62 | |
| TGF_BETA_SIGNALING | 2938.49 | |
| TNFA_SIGNALING_VIA_NFKB | 6421.46 | |
| UNFOLDED_PROTEIN_RESPONSE | 2463.89 | |
| UV_RESPONSE_DN | 7039.23 | |
| UV_RESPONSE_UP | 6051.11 | |
| WNT_BETA_CATENIN_SIGNALING | 3601.68 | |
| XENOBIOTIC_METABOLISM | 3320.91 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.848 |
| SRR23303752 | — | 0.837 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.831 |
| SRR10899984 | — | 0.825 |
| aMVAC.P_005_TURBT_S223 | — | 0.823 |
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