Defactinib
Sign in to save this workspacePrimary targets: FAK_PTK2 · FDA status: FDA Approved
Selectivity scorecard
KISS
92.68
Gini
0.450
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 Defactinib. Strongest target: ERBB4_HER4 at 99.6% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | ERBB4_HER4 | 99.6% | 0.4% |
| 2 | FAK_PTK2 | 98.5% | 1.5% |
| 3 | CLK1 | 97.9% | 2.1% |
| 4 | CDK5_P25 | 96.8% | 3.2% |
| 5 | MLK3_MAP3K11 | 96.4% | 3.6% |
| 6 | GSK3B | 96.3% | 3.7% |
| 7 | CDK1_CYCLIN_A | 96.3% | 3.7% |
| 8 | LRRK2 | 95.8% | 4.2% |
| 9 | JAK2 | 95.3% | 4.7% |
| 10 | MUSK | 95.2% | 4.8% |
| 11 | TYK2 | 95.0% | 5.0% |
| 12 | YSK4_MAP3K19 | 94.9% | 5.1% |
| 13 | EGFR | 94.6% | 5.4% |
| 14 | FLT3 | 94.6% | 5.4% |
| 15 | CLK2 | 94.5% | 5.5% |
| 16 | CDK9_CYCLIN_K | 93.7% | 6.3% |
| 17 | JAK1 | 93.7% | 6.3% |
| 18 | CDK3_CYCLIN_E | 92.6% | 7.4% |
| 19 | CDK2_CYCLIN_E | 92.6% | 7.4% |
| 20 | MLK1_MAP3K9 | 92.2% | 7.8% |
Selectivity landscape
Where Defactinib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Defactinib.
Atlas insights for Defactinib
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 | 4408.84 | |
| ALLOGRAFT_REJECTION | 10894.07 | |
| ANDROGEN_RESPONSE | 3695.05 | |
| ANGIOGENESIS | 1960.04 | |
| APICAL_JUNCTION | 11837.48 | |
| APICAL_SURFACE | 1412.41 | |
| APOPTOSIS | 11785.74 | |
| BILE_ACID_METABOLISM | 1469.06 | |
| CHOLESTEROL_HOMEOSTASIS | 1877.38 | |
| COAGULATION | 1352.35 | |
| COMPLEMENT | 6749.19 | |
| DNA_REPAIR | 3873.19 | |
| E2F_TARGETS | 11204.86 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 3661.89 | |
| ESTROGEN_RESPONSE_EARLY | 5832.69 | |
| ESTROGEN_RESPONSE_LATE | 6187.83 | |
| FATTY_ACID_METABOLISM | 1219.02 | |
| G2M_CHECKPOINT | 11105.81 | |
| GLYCOLYSIS | 4428.44 | |
| HEDGEHOG_SIGNALING | 1738.03 | |
| HEME_METABOLISM | 4130.32 | |
| HYPOXIA | 6985.85 | |
| IL2_STAT5_SIGNALING | 5346.03 | |
| IL6_JAK_STAT3_SIGNALING | 8476.88 | |
| INFLAMMATORY_RESPONSE | 7670.24 | |
| INTERFERON_ALPHA_RESPONSE | 1491.24 | |
| INTERFERON_GAMMA_RESPONSE | 10382.70 | |
| KRAS_SIGNALING_DN | 1831.06 | |
| KRAS_SIGNALING_UP | 5008.64 | |
| MITOTIC_SPINDLE | 10394.90 | |
| MTORC1_SIGNALING | 6260.85 | |
| MYC_TARGETS_V1 | 6748.85 | |
| MYC_TARGETS_V2 | 1718.00 | |
| MYOGENESIS | 5639.54 | |
| NOTCH_SIGNALING | 889.10 | |
| OXIDATIVE_PHOSPHORYLATION | 1852.07 | |
| P53_PATHWAY | 7248.86 | |
| PANCREAS_BETA_CELLS | 1109.97 | |
| PEROXISOME | 2064.04 | |
| PI3K_AKT_MTOR_SIGNALING | 13083.60 | |
| PROTEIN_SECRETION | 2796.07 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 903.86 | |
| SPERMATOGENESIS | 3017.94 | |
| TGF_BETA_SIGNALING | 3865.30 | |
| TNFA_SIGNALING_VIA_NFKB | 9056.80 | |
| UNFOLDED_PROTEIN_RESPONSE | 3008.41 | |
| UV_RESPONSE_DN | 7673.12 | |
| UV_RESPONSE_UP | 5470.97 | |
| WNT_BETA_CATENIN_SIGNALING | 4309.15 | |
| XENOBIOTIC_METABOLISM | 2922.13 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.879 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.864 |
| SRR12202498 | — | 0.851 |
| aMVAC.P_005_TURBT_S223 | — | 0.846 |
| SRR1443713 | GTEX | 0.846 |
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