Here we present an evaluation of the binding affinity prediction accuracy of the free energy calculation method FEP+ on internal active drug discovery projects and on a large new public benchmark set.<br>

Immuno‐oncology therapies have the potential to revolutionize the armamentarium of available cancer treatments. To further improve clinical response rates, researchers are looking for novel combination regimens, with checkpoint blockade being used as a backbone of the treatment. This Review highlights the significance of small molecules in this approach, which holds promise to provide increased benefit to cancer patients.

The asymmetric synthesis of helicenes … … by a Fischer indolization catalyzed by a SPINOL-derived phosphoric acid is reported by B. List et al. in their Communication on page 5202 ff. The catalyst is designed for long-range control and bears extended p-surfaces at the 3,3'-position. It creates a chiral nanometer-sized pocket, which enables p-p stacking interactions between the substituents and the reactive intermediate. A variety of (di)azahelicenes were obtained with good to excellent yields and enentioselectivities.

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The asymmetric synthesis of helicenes … … by a Fischer indolization catalyzed by a SPINOL-derived phosphoric acid is reported by B. List et al. in their Communication on page 5202 ff. The catalyst is designed for long-range control and bears extended p-surfaces at the 3,3'-position. It creates a chiral nanometer-sized pocket, which enables p-p stacking interactions between the substituents and the reactive intermediate. A variety of (di)azahelicenes were obtained with good to excellent yields and enentioselectivities.