Upadacitinib
Sign in to save this workspacePrimary targets: JAK1 · FDA status: FDA Approved
Selectivity scorecard
KISS
97.98
Gini
0.663
CATDS
0.016
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 Upadacitinib. Strongest target: RAF1 at 99.9% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | RAF1 | 99.9% | 0.1% |
| 2 | JAK2 | 98.3% | 1.7% |
| 3 | JAK3 | 97.5% | 2.5% |
| 4 | JAK1 | 97.3% | 2.6% |
| 5 | TYK2 | 97.1% | 2.9% |
| 6 | YSK4_MAP3K19 | 93.4% | 6.6% |
| 7 | STK38L_NDR2 | 91.2% | 8.8% |
| 8 | STK38_NDR1 | 90.8% | 9.2% |
| 9 | PKCA | 84.7% | 15.3% |
| 10 | PKCB2 | 83.3% | 16.7% |
| 11 | C_KIT | 82.9% | 17.1% |
| 12 | PKCD | 78.1% | 21.9% |
| 13 | AURORA_A | 76.7% | 23.3% |
| 14 | PKCG | 75.3% | 24.7% |
| 15 | LRRK2 | 73.3% | 26.7% |
| 16 | TRKC | 70.0% | 30.0% |
| 17 | FLT3 | 69.7% | 30.4% |
| 18 | TAOK2_TAO1 | 67.7% | 32.3% |
| 19 | DDR2 | 67.4% | 32.6% |
| 20 | ARAF | 64.9% | 35.1% |
Selectivity landscape
Where Upadacitinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Upadacitinib.
Atlas insights for Upadacitinib
Pathway-space view of what this drug actually does, drawn from the Pathway Atlas.
On-target vs off-target shadow
On-target6%
Off-target94%
Ghost (2nd-order)0%
| Pathway | Composition | Total |Π| |
|---|---|---|
| ADIPOGENESIS | 1846.57 | |
| ALLOGRAFT_REJECTION | 5346.35 | |
| ANDROGEN_RESPONSE | 957.37 | |
| ANGIOGENESIS | 842.55 | |
| APICAL_JUNCTION | 5341.41 | |
| APICAL_SURFACE | 602.33 | |
| APOPTOSIS | 4209.58 | |
| BILE_ACID_METABOLISM | 552.78 | |
| CHOLESTEROL_HOMEOSTASIS | 594.95 | |
| COAGULATION | 506.97 | |
| COMPLEMENT | 2842.06 | |
| DNA_REPAIR | 837.50 | |
| E2F_TARGETS | 2748.47 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1390.06 | |
| ESTROGEN_RESPONSE_EARLY | 2393.61 | |
| ESTROGEN_RESPONSE_LATE | 2187.31 | |
| FATTY_ACID_METABOLISM | 453.34 | |
| G2M_CHECKPOINT | 2637.04 | |
| GLYCOLYSIS | 1611.71 | |
| HEDGEHOG_SIGNALING | 606.84 | |
| HEME_METABOLISM | 1353.54 | |
| HYPOXIA | 2132.18 | |
| IL2_STAT5_SIGNALING | 2103.35 | |
| IL6_JAK_STAT3_SIGNALING | 4219.72 | |
| INFLAMMATORY_RESPONSE | 3571.02 | |
| INTERFERON_ALPHA_RESPONSE | 786.68 | |
| INTERFERON_GAMMA_RESPONSE | 4411.04 | |
| KRAS_SIGNALING_DN | 661.72 | |
| KRAS_SIGNALING_UP | 1893.93 | |
| MITOTIC_SPINDLE | 3150.30 | |
| MTORC1_SIGNALING | 1942.48 | |
| MYC_TARGETS_V1 | 1808.90 | |
| MYC_TARGETS_V2 | 453.86 | |
| MYOGENESIS | 2125.29 | |
| NOTCH_SIGNALING | 47.67 | |
| OXIDATIVE_PHOSPHORYLATION | 883.19 | |
| P53_PATHWAY | 1811.43 | |
| PANCREAS_BETA_CELLS | 88.94 | |
| PEROXISOME | 681.99 | |
| PI3K_AKT_MTOR_SIGNALING | 5706.03 | |
| PROTEIN_SECRETION | 1506.37 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 153.54 | |
| SPERMATOGENESIS | 1167.90 | |
| TGF_BETA_SIGNALING | 1042.88 | |
| TNFA_SIGNALING_VIA_NFKB | 2997.87 | |
| UNFOLDED_PROTEIN_RESPONSE | 1009.43 | |
| UV_RESPONSE_DN | 3208.45 | |
| UV_RESPONSE_UP | 2256.17 | |
| WNT_BETA_CATENIN_SIGNALING | 1273.14 | |
| XENOBIOTIC_METABOLISM | 915.79 |
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| SRR23303752 | — | 0.838 |
| EPT0291 | EPN | 0.835 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.823 |
| SRR10899984 | — | 0.823 |
| aMVAC.P_005_TURBT_S223 | — | 0.822 |
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