Abemaciclib
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
91.48
Gini
0.563
CATDS
0.008
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 Abemaciclib. Strongest target: CDK4_CYCLIN_D3 at 100.0% inhibition.
Accessible data table
| Rank | Target | Inhibition % | Residual activity % |
|---|---|---|---|
| 1 | CDK4_CYCLIN_D3 | 100.0% | 0.0% |
| 2 | DYRK3 | 100.0% | 0.0% |
| 3 | PIM3 | 100.0% | 0.0% |
| 4 | CAMK2A | 99.7% | 0.3% |
| 5 | CLK1 | 99.5% | 0.5% |
| 6 | CDK6_CYCLIN_D1 | 99.3% | 0.7% |
| 7 | CDK4_CYCLIN_D1 | 99.2% | 0.8% |
| 8 | CDK9_CYCLIN_T2 | 99.0% | 1.0% |
| 9 | DYRK1B | 98.9% | 1.1% |
| 10 | PIM1 | 98.8% | 1.2% |
| 11 | CDK6_CYCLIN_D3 | 98.7% | 1.3% |
| 12 | CAMK2B | 98.6% | 1.4% |
| 13 | CAMK2D | 98.6% | 1.4% |
| 14 | IRAK1 | 98.3% | 1.7% |
| 15 | HIPK2 | 98.2% | 1.8% |
| 16 | DYRK1_DYRK1A | 97.7% | 2.3% |
| 17 | CDK9_CYCLIN_T1 | 97.2% | 2.8% |
| 18 | GSK3A | 97.2% | 2.8% |
| 19 | DYRK2 | 97.1% | 2.9% |
| 20 | ERK7_MAPK15 | 96.7% | 3.3% |
Selectivity landscape
Where Abemaciclib sits in the 92-drug selectivity landscape (KISS vs Gini). The highlighted point is Abemaciclib.
Atlas insights for Abemaciclib
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 | 2996.30 | |
| ALLOGRAFT_REJECTION | 5308.40 | |
| ANDROGEN_RESPONSE | 3517.65 | |
| ANGIOGENESIS | 834.41 | |
| APICAL_JUNCTION | 5678.29 | |
| APICAL_SURFACE | 619.70 | |
| APOPTOSIS | 9421.70 | |
| BILE_ACID_METABOLISM | 901.38 | |
| CHOLESTEROL_HOMEOSTASIS | 1090.38 | |
| COAGULATION | 461.92 | |
| COMPLEMENT | 3327.01 | |
| DNA_REPAIR | 2643.26 | |
| E2F_TARGETS | 9299.90 | |
| EPITHELIAL_MESENCHYMAL_TRANSITION | 3511.26 | |
| ESTROGEN_RESPONSE_EARLY | 5445.04 | |
| ESTROGEN_RESPONSE_LATE | 4988.79 | |
| FATTY_ACID_METABOLISM | 521.39 | |
| G2M_CHECKPOINT | 9302.43 | |
| GLYCOLYSIS | 3641.27 | |
| HEDGEHOG_SIGNALING | 1305.14 | |
| HEME_METABOLISM | 3103.30 | |
| HYPOXIA | 6746.07 | |
| IL2_STAT5_SIGNALING | 3618.80 | |
| IL6_JAK_STAT3_SIGNALING | 3711.87 | |
| INFLAMMATORY_RESPONSE | 4531.74 | |
| INTERFERON_ALPHA_RESPONSE | 760.06 | |
| INTERFERON_GAMMA_RESPONSE | 5456.50 | |
| KRAS_SIGNALING_DN | 1929.39 | |
| KRAS_SIGNALING_UP | 2668.93 | |
| MITOTIC_SPINDLE | 6687.18 | |
| MTORC1_SIGNALING | 5260.03 | |
| MYC_TARGETS_V1 | 5187.78 | |
| MYC_TARGETS_V2 | 1720.48 | |
| MYOGENESIS | 5255.22 | |
| NOTCH_SIGNALING | 759.58 | |
| OXIDATIVE_PHOSPHORYLATION | 914.79 | |
| P53_PATHWAY | 6135.08 | |
| PANCREAS_BETA_CELLS | 1156.92 | |
| PEROXISOME | 1699.13 | |
| PI3K_AKT_MTOR_SIGNALING | 9060.42 | |
| PROTEIN_SECRETION | 2251.60 | |
| REACTIVE_OXYGEN_SPECIES_PATHWAY | 507.64 | |
| SPERMATOGENESIS | 2407.39 | |
| TGF_BETA_SIGNALING | 2983.43 | |
| TNFA_SIGNALING_VIA_NFKB | 7199.51 | |
| UNFOLDED_PROTEIN_RESPONSE | 2313.91 | |
| UV_RESPONSE_DN | 5911.73 | |
| UV_RESPONSE_UP | 4470.99 | |
| WNT_BETA_CATENIN_SIGNALING | 3703.37 | |
| XENOBIOTIC_METABOLISM | 1837.83 |
Anti-tumor matches — the "ideal patient" search
| Sample | Cancer type | cos to ideal |
|---|---|---|
| EPT0291 | EPN | 0.873 |
| TCGA-CF-A5U8-01A-11R-A28M-07 | — | 0.854 |
| SRR12202498 | — | 0.835 |
| R247 | — | 0.833 |
| b6a7e87e-2674-4a48-a3c2-c8a9806762b5 | — | 0.832 |
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