Ripretinib
Sign in to save this workspacePrimary targets: C_KIT, PDGFRA, PDGFRB · FDA status: FDA Approved
Selectivity scorecard
KISS
92.95
Gini
0.674
CATDS
0.011
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 Ripretinib. Strongest target: ARAF at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | ARAF | 100.0% | 0.0% |
| 2 | BRAF | 100.0% | 0.0% |
| 3 | RAF1 | 100.0% | 0.0% |
| 4 | C_KIT | 99.3% | 0.7% |
| 5 | YSK4_MAP3K19 | 98.7% | 1.3% |
| 6 | ZAK_MLTK | 97.4% | 2.6% |
| 7 | LCK | 97.2% | 2.8% |
| 8 | FMS | 97.2% | 2.9% |
| 9 | DDR1 | 96.9% | 3.1% |
| 10 | EPHB1 | 96.5% | 3.5% |
| 11 | TAOK2_TAO1 | 96.4% | 3.6% |
| 12 | JAK1 | 96.0% | 4.0% |
| 13 | LYN | 95.3% | 4.7% |
| 14 | HIPK4 | 95.3% | 4.7% |
| 15 | EPHA2 | 95.2% | 4.8% |
| 16 | EPHB4 | 95.2% | 4.8% |
| 17 | DDR2 | 94.8% | 5.2% |
| 18 | MLK2_MAP3K10 | 94.7% | 5.3% |
| 19 | ABL2_ARG | 94.5% | 5.5% |
| 20 | EPHA6 | 94.1% | 5.9% |
Selectivity landscape
Where Ripretinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Ripretinib.
Atlas insights for Ripretinib
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 | 2941.43 | |
| ALLOGRAFT_REJECTION | 9417.15 | |
| ANDROGEN_RESPONSE | 1238.15 | |
| ANGIOGENESIS | 1607.44 | |
| APICAL_JUNCTION | 9777.97 | |
| APICAL_SURFACE | 1109.96 | |
| APOPTOSIS | 7132.72 | |
| BILE_ACID_METABOLISM | 1028.51 | |
| CHOLESTEROL_HOMEOSTASIS | 1310.42 | |
| COAGULATION | 1268.72 | |
| COMPLEMENT | 5523.99 | |
| DNA_REPAIR | 1667.83 | |
| E2F_TARGETS | 4305.52 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1709.26 | |
| ESTROGEN_RESPONSE_EARLY | 3264.37 | |
| ESTROGEN_RESPONSE_LATE | 2958.36 | |
| FATTY_ACID_METABOLISM | 917.66 | |
| G2M_CHECKPOINT | 4574.00 | |
| GLYCOLYSIS | 2533.90 | |
| HEDGEHOG_SIGNALING | 1005.47 | |
| HEME_METABOLISM | 2337.94 | |
| HYPOXIA | 4262.22 | |
| IL2_STAT5_SIGNALING | 3596.92 | |
| IL6_JAK_STAT3_SIGNALING | 6306.72 | |
| INFLAMMATORY_RESPONSE | 5274.88 | |
| INTERFERON_ALPHA_RESPONSE | 1107.43 | |
| INTERFERON_GAMMA_RESPONSE | 6701.24 | |
| KRAS_SIGNALING_DN | 934.64 | |
| KRAS_SIGNALING_UP | 3544.57 | |
| MITOTIC_SPINDLE | 6003.15 | |
| MTORC1_SIGNALING | 3745.63 | |
| MYC_TARGETS_V1 | 3249.62 | |
| MYC_TARGETS_V2 | 785.84 | |
| MYOGENESIS | 2857.69 | |
| NOTCH_SIGNALING | 195.17 | |
| OXIDATIVE_PHOSPHORYLATION | 1650.04 | |
| P53_PATHWAY | 3749.56 | |
| PANCREAS_BETA_CELLS | 259.52 | |
| PEROXISOME | 1004.05 | |
| PI3K_AKT_MTOR_SIGNALING | 10043.40 | |
| PROTEIN_SECRETION | 1986.10 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 481.48 | |
| SPERMATOGENESIS | 1614.95 | |
| TGF_BETA_SIGNALING | 1885.12 | |
| TNFA_SIGNALING_VIA_NFKB | 4574.28 | |
| UNFOLDED_PROTEIN_RESPONSE | 1402.74 | |
| UV_RESPONSE_DN | 5477.06 | |
| UV_RESPONSE_UP | 3642.91 | |
| WNT_BETA_CATENIN_SIGNALING | 1917.60 | |
| XENOBIOTIC_METABOLISM | 1827.65 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| SRR23303752 | — | 0.831 |
| EPT0291 | EPN | 0.830 |
| SRR10899984 | — | 0.817 |
| aMVAC.P_005_TURBT_S223 | — | 0.814 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.812 |
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