Palbociclib
Sign in to save this workspacePrimary targets: CDK4_CYCLIN_D1, CDK4_CYCLIN_D3, CDK4_CYCLIN_D2, CDK6_CYCLIN_D1, CDK6_CYCLIN_D3, CDK6_CYCLIN_D2 · FDA status: FDA Approved
Selectivity scorecard
KISS
98.75
Gini
0.673
CATDS
0.020
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 Palbociclib. Strongest target: CDK4_CYCLIN_D3 at 99.6% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | CDK4_CYCLIN_D3 | 99.6% | 0.4% |
| 2 | CDK4_CYCLIN_D1 | 99.0% | 1.0% |
| 3 | CDK6_CYCLIN_D1 | 98.6% | 1.4% |
| 4 | CDK6_CYCLIN_D3 | 98.5% | 1.5% |
| 5 | CLK1 | 91.4% | 8.6% |
| 6 | CLK4 | 85.9% | 14.1% |
| 7 | CDK9_CYCLIN_T2 | 84.4% | 15.6% |
| 8 | ULK2 | 80.1% | 19.9% |
| 9 | STK16 | 78.1% | 21.9% |
| 10 | DYRK1B | 77.1% | 22.9% |
| 11 | PKCNU_PRKD3 | 72.8% | 27.2% |
| 12 | PKCMU_PRKD1 | 70.7% | 29.3% |
| 13 | CDK2_CYCLIN_O | 65.7% | 34.3% |
| 14 | EIF2AK2 | 65.6% | 34.4% |
| 15 | CAMK2D | 65.0% | 35.0% |
| 16 | TRKC | 64.4% | 35.6% |
| 17 | CLK2 | 62.8% | 37.2% |
| 18 | CDK9_CYCLIN_K | 62.5% | 37.5% |
| 19 | PKMYT1 | 60.5% | 39.5% |
| 20 | DYRK3 | 58.8% | 41.2% |
Selectivity landscape
Where Palbociclib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Palbociclib.
Atlas insights for Palbociclib
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 | 650.74 | |
| ALLOGRAFT_REJECTION | 2037.71 | |
| ANDROGEN_RESPONSE | 941.95 | |
| ANGIOGENESIS | 299.76 | |
| APICAL_JUNCTION | 2170.44 | |
| APICAL_SURFACE | 167.55 | |
| APOPTOSIS | 2798.26 | |
| BILE_ACID_METABOLISM | 393.97 | |
| CHOLESTEROL_HOMEOSTASIS | 376.19 | |
| COAGULATION | 138.23 | |
| COMPLEMENT | 1237.60 | |
| DNA_REPAIR | 973.64 | |
| E2F_TARGETS | 3567.25 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 1042.28 | |
| ESTROGEN_RESPONSE_EARLY | 1711.20 | |
| ESTROGEN_RESPONSE_LATE | 1899.13 | |
| FATTY_ACID_METABOLISM | 223.74 | |
| G2M_CHECKPOINT | 3223.91 | |
| GLYCOLYSIS | 1317.26 | |
| HEDGEHOG_SIGNALING | 420.15 | |
| HEME_METABOLISM | 780.53 | |
| HYPOXIA | 1873.32 | |
| IL2_STAT5_SIGNALING | 861.51 | |
| IL6_JAK_STAT3_SIGNALING | 1400.17 | |
| INFLAMMATORY_RESPONSE | 1224.99 | |
| INTERFERON_ALPHA_RESPONSE | 170.66 | |
| INTERFERON_GAMMA_RESPONSE | 1870.67 | |
| KRAS_SIGNALING_DN | 654.77 | |
| KRAS_SIGNALING_UP | 938.52 | |
| MITOTIC_SPINDLE | 2540.17 | |
| MTORC1_SIGNALING | 1549.27 | |
| MYC_TARGETS_V1 | 1997.06 | |
| MYC_TARGETS_V2 | 519.51 | |
| MYOGENESIS | 1435.80 | |
| NOTCH_SIGNALING | 283.37 | |
| OXIDATIVE_PHOSPHORYLATION | 349.75 | |
| P53_PATHWAY | 1587.49 | |
| PANCREAS_BETA_CELLS | 332.32 | |
| PEROXISOME | 541.07 | |
| PI3K_AKT_MTOR_SIGNALING | 2891.61 | |
| PROTEIN_SECRETION | 673.45 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 158.76 | |
| SPERMATOGENESIS | 816.14 | |
| TGF_BETA_SIGNALING | 935.19 | |
| TNFA_SIGNALING_VIA_NFKB | 1886.04 | |
| UNFOLDED_PROTEIN_RESPONSE | 870.11 | |
| UV_RESPONSE_DN | 1715.01 | |
| UV_RESPONSE_UP | 1449.49 | |
| WNT_BETA_CATENIN_SIGNALING | 1314.34 | |
| XENOBIOTIC_METABOLISM | 657.13 |
Hallmarks-of-Cancer reach
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.872 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.854 |
| R247 | — | 0.832 |
| SRR1443713 | GTEX | 0.829 |
| SRR1313097 | — | 0.825 |
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