ACS Central Science · 2019 · 866 citations · 32 references
PharmacyChemistryMedicinal ChemistryComputational ChemistryComputational Medicinal ChemistryDrug DiscoveryChemical Space ExplorationMolecular ModelingAccuracyChemical Entity RepresentationComputational Synthesis PlanningComputer-assisted Synthesis PlanningMolecular Representation LearningMolecular RepresentationsReaction Property PredictionUncertainty Quantification In Molecular Prediction
Organic synthesis remains a major bottleneck in medicinal chemistry, and the forward problem of predicting products from reactants and reagents is still unsolved. The authors cast reaction prediction as a machine‑translation task between SMILES strings, using a multi‑head attention Molecular Transformer that learns correlations among chemical motifs without handcrafted rules. The model surpasses all existing methods, achieving over 90 % top‑1 accuracy, accurately predicts subtle transformations, estimates its own uncertainty with 89 % correctness, and handles inputs lacking a reactant–reagent split and stereochemistry.
Organic synthesis is one of the key stumbling blocks in medicinal chemistry. A necessary yet unsolved step in planning synthesis is solving the forward problem: Given reactants and reagents, predict the products. Similar to other work, we treat reaction prediction as a machine translation problem between simplified molecular-input line-entry system (SMILES) strings (a text-based representation) of reactants, reagents, and the products. We show that a multihead attention Molecular Transformer model outperforms all algorithms in the literature, achieving a top-1 accuracy above 90% on a common benchmark data set. Molecular Transformer makes predictions by inferring the correlations between the presence and absence of chemical motifs in the reactant, reagent, and product present in the data set. Our model requires no handcrafted rules and accurately predicts subtle chemical transformations. Crucially, our model can accurately estimate its own uncertainty, with an uncertainty score that is 89% accurate in terms of classifying whether a prediction is correct. Furthermore, we show that the model is able to handle inputs without a reactant–reagent split and including stereochemistry, which makes our method universally applicable.
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Rethinking the Inception Architecture for Computer Vision
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