Drug-Target Interaction Prediction via Hierarchical Sequential Cross-Attention over Chemical and Protein Language Models
Authors: Khadidja Henni, Hamza Abdelali, Abdelkrim Aries, Neila Mezghani, Brigitte Vannier, Sara Magdouli, Lina Abou-Abbas
Organizations: I2A institute, T´ELUQ University, Montreal, QC, Canada · LIO, CRCHUM, Montreal, QC, Canada · LCSI, ESI, Algiers, Algeria · CoMeT UR 24344, Universite de Poitiers, Poitiers, France · Dept. of Civil Engineering, University of Ottawa, Ottawa, ON, Canada · Dept. of Electrical and Computer Engineering, Lebanese American University, Byblos, Lebanon
Predicting Drug-Target Interactions~(DTIs) is a central task in computational drug discovery, with direct applications in virtual screening, drug repurposing, and therapeutic candidate prioritization. Although recent deep learning methods have improved DTI prediction, many sequence-based models still process drugs and proteins independently and only combine their representations at a late prediction stage. This limits their ability to explicitly model cross-molecular dependencies between chemical substructures and protein sequence regions. In this paper, we propose a sequence-only DTI prediction architecture that combines two pre-trained language models, ChemBERTa for drug SMILES strings and ESM-2 for protein amino acid sequences, with a hierarchical interaction module. The proposed model first extracts contextual representations using pre-trained encoders, then applies 1D convolutional layers to condense local sequence patterns, followed by a sequential bidirectional cross-attention mechanism inspired by the induced-fit view of molecular recognition. Finally, attention-based pooling constructs fixed-size interaction-aware vectors for binary prediction. Experiments on BIOSNAP, Davis, and BindingDB show that the proposed model achieves the best performance on BIOSNAP, matches the best AUROC on Davis, and remains competitive on BindingDB while using only 25.2 million trainable parameters. Ablation results confirm the contribution of both the CNN and cross-attention modules, and cold-start experiments indicate promising generalization to unseen proteins and drugs.
Figures & tables
Fig. 1: Overview of the proposed architecture. Drug SMILES and protein sequences are encoded using ChemBERTa and ESM-2, condensed through 1D CNN layers, fused using sequential bidirectional cross-attention, and aggregated through attention-based pooling before final prediction.
Dataset
Drugs
Proteins
Positive Pairs
Negative Pairs
Davis
68
379
1,043 / 160 / 303
1,043 / 2,846 / 5,708
BIOSNAP
4,510
2,181
9,619 / 1,374 / 2,748
9,619 / 1,374 / 2,748
BindingDB
10,665
1,413
6,334 / 927 / 1,905
6,334 / 5,717 / 11,384
TABLE I: Dataset statistics. Interaction pairs are reported as train / validation / test.
Hyperparameter
Value
Optimizer
AdamW
Base learning rate
5×10−5
Learning-rate schedule
Linear warmup + cosine decay
Effective batch size
32
Maximum epochs
30
Unfrozen encoder layers
Top 2 layers
TABLE II: Main hyperparameters of the proposed model.
BIOSNAP
Davis
BindingDB
Model
AUROC
AUPRC
Sens.
Spec.
AUROC
AUPRC
Sens.
Spec.
AUROC
AUPRC
Sens.
Spec.
MolTrans [ 5 ]
0.895
0.901
0.775
0.851
0.907
0.404
0.800
0.876
0.914
0.622
0.797
0.896
DeepDTA [ 2 ]
0.834
0.849
0.726
0.813
0.792
0.272
0.688
0.778
0.902
0.604
0.757
0.904
HyperAttentionDTI [ 18 ]
0.825
0.830
0.800
0.812
0.841
0.483
0.708
0.722
0.900
0.876
0.801
0.791
Fine-tuning BERT [ 8 ]
0.914
0.900
0.862
0.847
0.920
0.395
0.824
0.802
0.922
0.623
0.814
0.793
DLM-DTI [ 13 ]
0.914
0.914
0.848
0.844
0.895
0.373
0.833
0.766
0.912
0.643
0.846
0.916
TABLE III: Performance comparison on BIOSNAP, Davis, and BindingDB. Best result per metric per dataset is in bold .
Test set
Training
AUROC
AUPRC
Sens.
Spec.
Davis
Individual
0.920
0.356
0.901
0.801
Integrated
0.939
0.448
0.911
0.848
BIOSNAP
Individual
0.920
0.924
0.854
0.830
Integrated
0.920
0.840
0.886
0.835
BindingDB
Individual
0.920
0.642
0.816
0.874
Integrated
0.918
0.764
0.852
0.850
TABLE IV: Individual training vs. integrated training.
Department of Economics and Management, University of Pavia, Pavia, Italy · Department of Computer Science and Engineering, Seoul National University, Gwanak-gu 08826, Korea.