Tofacitinib
Sign in to save this workspacePrimary targets: JAK3 · FDA status: FDA Approved
Selectivity scorecard
KISS
99.25
Gini
0.684
CATDS
0.045
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 Tofacitinib. Strongest target: JAK3 at 98.2% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | JAK3 | 98.2% | 1.8% |
| 2 | JAK1 | 95.2% | 4.8% |
| 3 | JAK2 | 92.3% | 7.7% |
| 4 | TYK2 | 81.0% | 19.0% |
| 5 | PKN1_PRK1 | 55.8% | 44.2% |
| 6 | PDK2_PDHK2 | 35.2% | 64.8% |
| 7 | CAMKK2 | 33.0% | 67.0% |
| 8 | TNK1 | 30.1% | 69.9% |
| 9 | CK1D | 25.1% | 74.9% |
| 10 | CDK9_CYCLIN_T1 | 22.6% | 77.4% |
| 11 | PKCD | 20.7% | 79.3% |
| 12 | MUSK | 20.2% | 79.8% |
| 13 | VRK1 | 19.7% | 80.3% |
| 14 | PKMYT1 | 19.3% | 80.7% |
| 15 | STK38_NDR1 | 19.1% | 80.9% |
| 16 | PKN2_PRK2 | 18.5% | 81.5% |
| 17 | LRRK2 | 17.8% | 82.2% |
| 18 | P38A_MAPK14 | 17.6% | 82.4% |
| 19 | PKG2_PRKG2 | 17.5% | 82.5% |
| 20 | PDK1_PDPK1 | 17.3% | 82.7% |
Selectivity landscape
Where Tofacitinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Tofacitinib.
Atlas insights for Tofacitinib
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 | 885.96 | |
| ALLOGRAFT_REJECTION | 2497.23 | |
| ANDROGEN_RESPONSE | 379.42 | |
| ANGIOGENESIS | 181.93 | |
| APICAL_JUNCTION | 1684.15 | |
| APICAL_SURFACE | 291.55 | |
| APOPTOSIS | 1652.60 | |
| BILE_ACID_METABOLISM | 135.85 | |
| CHOLESTEROL_HOMEOSTASIS | 236.39 | |
| COAGULATION | 178.03 | |
| COMPLEMENT | 1106.29 | |
| DNA_REPAIR | 372.42 | |
| E2F_TARGETS | 1409.14 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 513.31 | |
| ESTROGEN_RESPONSE_EARLY | 978.14 | |
| ESTROGEN_RESPONSE_LATE | 965.20 | |
| FATTY_ACID_METABOLISM | 212.89 | |
| G2M_CHECKPOINT | 1186.95 | |
| GLYCOLYSIS | 608.61 | |
| HEDGEHOG_SIGNALING | 133.59 | |
| HEME_METABOLISM | 444.21 | |
| HYPOXIA | 1079.07 | |
| IL2_STAT5_SIGNALING | 1090.34 | |
| IL6_JAK_STAT3_SIGNALING | 2852.30 | |
| INFLAMMATORY_RESPONSE | 1801.94 | |
| INTERFERON_ALPHA_RESPONSE | 459.26 | |
| INTERFERON_GAMMA_RESPONSE | 2718.34 | |
| KRAS_SIGNALING_DN | 185.22 | |
| KRAS_SIGNALING_UP | 795.71 | |
| MITOTIC_SPINDLE | 972.45 | |
| MTORC1_SIGNALING | 759.05 | |
| MYC_TARGETS_V1 | 867.44 | |
| MYC_TARGETS_V2 | 213.86 | |
| MYOGENESIS | 786.41 | |
| NOTCH_SIGNALING | 71.62 | |
| OXIDATIVE_PHOSPHORYLATION | 251.95 | |
| P53_PATHWAY | 859.99 | |
| PANCREAS_BETA_CELLS | 67.28 | |
| PEROXISOME | 143.00 | |
| PI3K_AKT_MTOR_SIGNALING | 2459.49 | |
| PROTEIN_SECRETION | 486.11 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 44.90 | |
| SPERMATOGENESIS | 687.13 | |
| TGF_BETA_SIGNALING | 464.21 | |
| TNFA_SIGNALING_VIA_NFKB | 1533.21 | |
| UNFOLDED_PROTEIN_RESPONSE | 555.90 | |
| UV_RESPONSE_DN | 1082.37 | |
| UV_RESPONSE_UP | 946.42 | |
| WNT_BETA_CATENIN_SIGNALING | 482.06 | |
| XENOBIOTIC_METABOLISM | 225.68 |
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.836 |
| C3L-03726 | — | 0.829 |
| SRR10899984 | — | 0.822 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.820 |
| TCGA-CV-7424-01A-11R-2081-07 | — | 0.817 |
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