Mitapivat
Sign in to save this workspacePrimary targets: PK · FDA status: FDA Approved
Selectivity scorecard
KISS
100.00
Gini
0.625
CATDS
0.028
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 Mitapivat. Strongest target: PDGFRA at 53.3% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | PDGFRA | 53.3% | 46.7% |
| 2 | C_KIT | 48.1% | 51.9% |
| 3 | AURORA_A | 30.6% | 69.4% |
| 4 | PDGFRB | 26.1% | 73.9% |
| 5 | LIMK1 | 25.3% | 74.7% |
| 6 | PDK3_PDHK3 | 23.8% | 76.3% |
| 7 | PKD2_PRKD2 | 21.2% | 78.8% |
| 8 | ASK1_MAP3K5 | 20.9% | 79.1% |
| 9 | CDK4_CYCLIN_D3 | 20.2% | 79.8% |
| 10 | DDR1 | 19.1% | 80.9% |
| 11 | DAPK2 | 18.8% | 81.2% |
| 12 | MELK | 18.1% | 81.9% |
| 13 | TRKB | 18.0% | 82.0% |
| 14 | CDK9_CYCLIN_T2 | 17.9% | 82.1% |
| 15 | VRK1 | 17.5% | 82.5% |
| 16 | LCK | 17.4% | 82.6% |
| 17 | RIPK2 | 16.8% | 83.2% |
| 18 | AURORA_B | 16.7% | 83.3% |
| 19 | MEKK6 | 16.2% | 83.8% |
| 20 | MST2_STK3 | 15.3% | 84.7% |
Selectivity landscape
Where Mitapivat sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Mitapivat.
Atlas insights for Mitapivat
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 | 353.02 | |
| ALLOGRAFT_REJECTION | 1166.76 | |
| ANDROGEN_RESPONSE | 234.09 | |
| ANGIOGENESIS | 234.41 | |
| APICAL_JUNCTION | 1571.63 | |
| APICAL_SURFACE | 100.55 | |
| APOPTOSIS | 1345.88 | |
| BILE_ACID_METABOLISM | 159.86 | |
| CHOLESTEROL_HOMEOSTASIS | 222.54 | |
| COAGULATION | 158.03 | |
| COMPLEMENT | 814.49 | |
| DNA_REPAIR | 294.49 | |
| E2F_TARGETS | 984.22 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 400.91 | |
| ESTROGEN_RESPONSE_EARLY | 619.77 | |
| ESTROGEN_RESPONSE_LATE | 559.97 | |
| FATTY_ACID_METABOLISM | 101.01 | |
| G2M_CHECKPOINT | 922.81 | |
| GLYCOLYSIS | 459.59 | |
| HEDGEHOG_SIGNALING | 185.41 | |
| HEME_METABOLISM | 347.81 | |
| HYPOXIA | 621.82 | |
| IL2_STAT5_SIGNALING | 474.16 | |
| IL6_JAK_STAT3_SIGNALING | 651.48 | |
| INFLAMMATORY_RESPONSE | 708.10 | |
| INTERFERON_ALPHA_RESPONSE | 112.08 | |
| INTERFERON_GAMMA_RESPONSE | 837.04 | |
| KRAS_SIGNALING_DN | 180.84 | |
| KRAS_SIGNALING_UP | 482.97 | |
| MITOTIC_SPINDLE | 1121.92 | |
| MTORC1_SIGNALING | 565.72 | |
| MYC_TARGETS_V1 | 591.81 | |
| MYC_TARGETS_V2 | 140.07 | |
| MYOGENESIS | 616.59 | |
| NOTCH_SIGNALING | 63.53 | |
| OXIDATIVE_PHOSPHORYLATION | 178.18 | |
| P53_PATHWAY | 585.55 | |
| PANCREAS_BETA_CELLS | 48.32 | |
| PEROXISOME | 208.91 | |
| PI3K_AKT_MTOR_SIGNALING | 1337.03 | |
| PROTEIN_SECRETION | 254.80 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 91.68 | |
| SPERMATOGENESIS | 292.36 | |
| TGF_BETA_SIGNALING | 407.72 | |
| TNFA_SIGNALING_VIA_NFKB | 706.85 | |
| UNFOLDED_PROTEIN_RESPONSE | 353.43 | |
| UV_RESPONSE_DN | 806.20 | |
| UV_RESPONSE_UP | 629.05 | |
| WNT_BETA_CATENIN_SIGNALING | 535.00 | |
| XENOBIOTIC_METABOLISM | 249.28 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.845 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.833 |
| SRR23303752 | — | 0.825 |
| aMVAC.P_005_TURBT_S223 | — | 0.819 |
| SRR12202498 | — | 0.814 |
Annotations
Sign in to read and post annotations.
Loading…