When Does Context Help? A Systematic Study of Target-Conditional Molecular Property Prediction
Organizations: Great Neck South High School
Abstract
We present the first systematic study of when target context helps molecular property prediction, evaluating context conditioning across 10 diverse protein families, 4 fusion architectures, data regimes spanning 67-9,409 training compounds, and both temporal and random evaluation splits. Using NestDrug, a FiLM-based architecture that conditions molecular representations on target identity, we characterize both success and failure modes with three principal findings. First, fusion architecture dominates: FiLM outperforms concatenation by 24.2 percentage points and additive conditioning by 8.6 pp; how you incorporate context matters more than whether you include it. Second, context enables otherwise impossible predictions: on data-scarce CYP3A4 (67 training compounds), multi-task transfer achieves 0.686 AUC where per-target Random Forest collapses to 0.238. Third, context can systematically hurt: distribution mismatch causes 10.2 pp degradation on BACE1; few-shot adaptation consistently underperforms zero-shot. Beyond methodology, we expose fundamental flaws in standard benchmarking: 1-nearest-neighbor Tanimoto achieves 0.991 AUC on DUD-E without any learning, and 50% of actives leak from training data, rendering absolute performance metrics meaningless. Our temporal split evaluation (train up to 2020, test 2021-2024) achieves stable 0.843 AUC with no degradation, providing the first rigorous evidence that context-conditional molecular representations generalize to future chemical space.
Figures & tables
| Method | Type | Mean AUC | Wins |
|---|---|---|---|
| AtomNet ( Wallach et al., 2015 ) | 3D CNN | 0.818 | — |
| GNN-VS ( Lim et al., 2019 ) | GNN | 0.825 | — |
| 3D-CNN ( Ragoza et al., 2017 ) | 3D CNN | 0.830 | — |
| NestDrug (Ours) | GNN+FiLM | 0.850 | 2/10 |
| Per-target RF ‡ | Fingerprint | 0.875 | 8/10 |
| 1-NN Tanimoto † | No learning | 0.991 | — |
| Target | DUD-E RF | L0-only | GNN-VS | NestDrug |
|---|---|---|---|---|
| EGFR | 0.782 | 0.943 | 0.825 | 0.965 |
| DRD2 | 0.801 | 0.960 | 0.842 | 0.984 |
| ADRB2 | 0.693 | 0.745 | 0.712 | 0.775 |
| BACE1 | 0.634 | 0.672 | 0.698 | 0.656 |
| ESR1 | 0.756 | 0.864 | 0.789 | 0.909 |
| HDAC2 | 0.745 | 0.866 | 0.812 | 0.928 |
| Target | Correct L1 | Generic L1 | -value | |
|---|---|---|---|---|
| EGFR | 0.965 | 0.832 | +0.132 | |
| DRD2 | 0.984 | 0.901 | +0.083 | |
| ADRB2 | 0.775 | 0.718 | +0.057 | |
| BACE1 | 0.656 | 0.758 | 0.102 | |
| ESR1 | 0.909 | 0.775 | +0.134 | |
| HDAC2 | 0.928 | 0.827 | +0.100 |
| Fusion Method | Mean AUC | vs FiLM | Wins/10 |
|---|---|---|---|
| Concatenation † | 0.607 | 24.2 pp | 0/10 |
| No Context (L0 only) | 0.724 | 12.5 pp | 1/10 |
| Additive ( only) | 0.763 | 8.6 pp | 1/10 |
| FiLM ( ) | 0.849 | — | 9/10 |
| 2021 | 2022 | 2023 | 2024 | Overall | |
|---|---|---|---|---|---|
| ROC-AUC | 0.849 | 0.838 | 0.823 | 0.849 | 0.843 |
Appendix figures & tables15 assets
Supplementary material from the paper’s appendix.
Appendix
| Category | Value |
|---|---|
| Architecture | |
| MPNN layers | 6 |
| Hidden dimension | 256 |
| Molecular embedding | 512 |
| L1 embedding dimension | 128 |
| L2 embedding dimension | 64 |
| Family | Target | mean | mean |
|---|---|---|---|
| Kinase | EGFR | ||
| JAK2 | |||
| GPCR | DRD2 | ||
| ADRB2 | |||
| Nuclear | ESR1 | ||
| PPARG |
| Target | Shots | Zero-Shot | Adapted | Correct L1 | |
|---|---|---|---|---|---|
| EGFR | 10 | 0.829 | 0.796 | 0.033 | 0.959 |
| 25 | 0.828 | 0.682 | 0.146 | 0.959 | |
| 50 | 0.830 | 0.666 | 0.164 | 0.959 | |
| DRD2 | 10 | 0.906 | 0.724 | 0.182 | 0.984 |
| 25 | 0.906 | 0.729 | 0.177 | 0.984 | |
| 50 | 0.908 | 0.734 | 0.174 | 0.984 |
| Component | Time Complexity | Space Complexity |
|---|---|---|
| MPNN (L0) | ||
| Context Embedding | ||
| FiLM Modulation | ||
| Prediction Head | ||
| Total |
| Target | ROC-AUC | PR-AUC | EF@1% | EF@5% | Sensitivity | Specificity |
|---|---|---|---|---|---|---|
| EGFR | ||||||
| DRD2 | ||||||
| ADRB2 | ||||||
| BACE1 | ||||||
| ESR1 | ||||||
| HDAC2 |
| L1 Dimension | 32 | 64 | 128 | 256 | 512 |
|---|---|---|---|---|---|
| Mean ROC-AUC | 0.821 | 0.832 | 0.839 | 0.837 | 0.834 |
| Parameters (M) | 2.1 | 2.3 | 2.6 | 3.2 | 4.4 |
| MPNN Layers | 2 | 4 | 6 | 8 | 10 |
|---|---|---|---|---|---|
| Mean ROC-AUC | 0.798 | 0.824 | 0.839 | 0.836 | 0.831 |
| Training Time (h) | 1.2 | 2.1 | 3.4 | 5.2 | 7.8 |
| Modulation Type | Mean ROC-AUC | Parameters |
|---|---|---|
| None (L0 only) | 0.803 | 2.1M |
| Concatenation | 0.818 | 2.4M |
| Additive ( only) | 0.825 | 2.3M |
| Multiplicative ( only) | 0.831 | 2.3M |
| FiLM ( and ) | 0.839 | 2.6M |
| Hypernetwork | 0.841 | 8.2M |
| Target | Rounds | Hit Rate (%) | Enrichment | Expts to 50 Hits | ||
|---|---|---|---|---|---|---|
| Random | Model | Random | Model | |||
| EGFR | 141 | 49.4 | 76.1 | 1.54 | 225 | 159 |
| DRD2 | 89 | 42.1 | 71.8 | 1.71 | 198 | 134 |
| BACE1 | 67 | 38.2 | 62.4 | 1.63 | 267 | 189 |
| ESR1 | 52 | 44.8 | 69.2 | 1.54 | 213 | 151 |
| HDAC2 | 41 | 51.2 | 82.7 | 1.62 | 156 | 98 |
| Metric | Overall | 2020 | 2021 | 2022 | 2023 | 2024 |
|---|---|---|---|---|---|---|
| samples | 10,000 | 2,486 | 2,588 | 1,427 | 1,633 | 1,866 |
| ROC-AUC | 0.843 | 0.837 | 0.849 | 0.838 | 0.823 | 0.849 |
| Correlation | 0.692 | 0.677 | 0.711 | 0.686 | 0.663 | 0.678 |
| RMSE | 1.043 | 1.051 | 1.045 | 1.031 | 1.038 | 1.043 |
| R 2 | 0.388 | 0.371 | 0.403 | 0.376 | 0.342 | 0.370 |
| Molecule | Atoms | Mean Imp. | Max Imp. | Std | Top Atoms |
|---|---|---|---|---|---|
| Celecoxib | 26 | 0.361 | 0.925 | 0.222 | SO 2 NH 2 , CF 3 |
| Caffeine | 14 | 0.423 | 0.850 | 0.220 | N-methyl, C=O |
| Metformin | 9 | 0.454 | 0.840 | 0.194 | Guanidine N |
| Ibuprofen | 15 | 0.293 | 0.708 | 0.152 | Carboxylic acid |
| Acetaminophen | 11 | 0.316 | 0.574 | 0.093 | Amide, phenol |
| Atorvastatin | 41 | 0.123 | 0.333 | 0.081 | Distributed |
| Target | Train Actives | Per-Target RF | NestDrug | Winner |
|---|---|---|---|---|
| EGFR | 5,925 | 0.996 | 0.965 | RF |
| DRD2 | 9,409 | 0.994 | 0.984 | RF |
| ADRB2 | 1,015 | 0.882 | 0.775 | RF |
| BACE1 | 5,997 | 0.978 | 0.656 | RF |
| ESR1 | 2,805 | 0.996 | 0.909 | RF |
| HDAC2 | 1,436 | 0.951 | 0.928 | RF |
| Target | 1-NN AUC | Active-Active Sim | Decoy-Active Sim | Gap |
|---|---|---|---|---|
| EGFR | 0.996 | 0.816 | 0.251 | 0.565 |
| DRD2 | 0.998 | 0.814 | 0.265 | 0.549 |
| ADRB2 | 1.000 | 0.882 | 0.194 | 0.688 |
| BACE1 | 0.998 | 0.882 | 0.196 | 0.686 |
| ESR1 | 0.993 | 0.844 | 0.188 | 0.655 |
| HDAC2 | 0.994 | 0.732 | 0.202 | 0.530 |
| Target | DUD-E Actives | ChEMBL Train | Active Leakage | Decoy Leakage |
|---|---|---|---|---|
| CYP3A4 | 333 | 5,504 | 99.1% | 0.16% |
| EGFR | 4,032 | 7,845 | 97.2% | 0.11% |
| FXA | 445 | 5,969 | 92.6% | 0.07% |
| DRD2 | 3,223 | 11,284 | 89.9% | 0.10% |
| HDAC2 | 238 | 4,427 | 46.6% | 0.06% |
| JAK2 | 153 | 6,013 | 37.9% | 0.09% |
Molecular Property Prediction
Molecular property prediction estimates chemical, physical, and biological properties from molecular structure and context.
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