| 等级 | 数量 | 占比 |
|---|---|---|
| A级(最优) | 77 | 10.5% |
| B级(良好) | 152 | 20.7% |
| C级(一般) | 234 | 31.9% |
| D级(较差) | 271 | 36.9% |
排序规则:疾病关联(50%)+ 成药性评分(50%)。 筛选条件:global_score ≥ 0.5(强关联)。
| 排名 | 基因 | 加权分 | 成药性 | 风险 | 类型 | 最高阶段 | CRISPR | 组织特异性 |
|---|---|---|---|---|---|---|---|---|
| 🥇 | EGFR | 83.3 | 82 | A | 驱动基因 | Approved | 17.6% | Tissue enhanced |
| 🥈 | ERBB2 | 82.5 | 87 | A | 驱动基因 | Approved | 17.7% | Low tissue specificity |
| 🥉 | MET | 81.2 | 90 | A | 驱动基因 | Approved | 2.4% | Tissue enhanced |
| 4 | ALK | 80.8 | 86 | A | 驱动基因 | Approved | 0.8% | Tissue enhanced |
| 5 | ROS1 | 77.6 | 84 | A | 驱动基因 | Approved | 0.1% | Group enriched |
| 6 | RET | 77.3 | 84 | A | 驱动基因 | Approved | 0.4% | Tissue enhanced |
| 7 | NTRK3 | 77.0 | 89 | A | 驱动基因 | Approved | 0.0% | Group enriched |
| 8 | CD274 | 76.9 | 86 | A | 免疫检查点 | Approved | 0.0% | Tissue enhanced |
| 9 | NTRK1 | 76.8 | 88 | A | 驱动基因 | Approved | 0.1% | Tissue enhanced |
| 10 | FGFR2 | 76.5 | 95 | A | 驱动基因 | Approved | 1.7% | Tissue enriched |
| 11 | ERBB4 | 75.8 | 84 | A | 驱动基因 | Approved | 0.7% | Tissue enhanced |
| 12 | NTRK2 | 75.7 | 86 | A | 驱动基因 | Approved | 0.0% | Tissue enhanced |
| 13 | PDGFRA | 75.0 | 90 | A | - | Approved | 6.2% | Tissue enhanced |
| 14 | KDR | 74.3 | 84 | A | 血管生成 | Approved | 1.1% | Low tissue specificity |
| 15 | BRAF | 73.5 | 77 | B | 驱动基因 | Approved | 8.6% | Low tissue specificity |
| 16 | VEGFA | 73.3 | 84 | A | 血管生成 | Approved | 0.0% | Low tissue specificity |
| 17 | TUBB2A | 72.1 | 84 | A | - | Approved | 1.1% | Tissue enriched |
| 18 | CTLA4 | 72.0 | 83 | A | 免疫检查点 | Approved | 0.0% | Tissue enriched |
| 19 | PDCD1 | 71.2 | 80 | A | 免疫检查点 | Approved | 0.0% | Tissue enhanced |
| 20 | PDGFRB | 71.2 | 82 | A | - | Approved | 2.3% | Low tissue specificity |
基于 Open Targets 26.09 的三维新证据:可成药性(4 种模态)、基因必需性、安全性事件。 这些维度帮助判断靶点的"可做药程度"和"潜在风险"。
| 数据层 | 覆盖数 | 覆盖率 | 可视化 |
|---|---|---|---|
| UniProt 序列 | 734 | 100.0% | |
| PDB 3D结构 | 558 | 76.0% | |
| TTD 成药性 | 378 | 51.5% | |
| DepMap CRISPR | 705 | 96.0% | |
| HPA 组织分布 | 714 | 97.3% | |
| ChEMBL 化合物 | 446 | 60.8% | |
| STRING 互作 | 377 | 51.4% |
A级靶点(综合评分≥80)同时满足:已有明确成药性证据、CRISPR筛选显示毒性风险低、组织特异性良好。建议作为立项评估的第一梯队。
单一数据源可能有偏差,建议结合:
· TTD成药性:是否有上市药或临床阶段药物
· 可成药性画像:4 种模态(小分子/抗体/PROTAC/其他)的可及性
· 基因必需性:是否被 CRISPR 筛选标记为必需(必需 = 毒性风险高)
· 安全性事件:是否有已知的毒性报道
· HPA组织特异性:是否在正常组织中广泛表达(广泛表达 = 脱靶风险高)
📩 完整版交付内容:全部靶点数据、CSV 数据表、数据字典、质量报告,包含 734 个靶点的36个字段。字段含义见 data_dictionary.csv。