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We present an extension of Alchemical Transfer Method (ATM) for the estimation of relative binding free energies of molecular complexes applicable to conventional as well as scaffold-hopping alchemical transformations. The method, named…

化学物理 · 物理学 2021-07-13 Solmaz Azimi , Sheenam Khuttan , Joe Z. Wu , Rajat K. Pal , Emilio Gallicchio

The Alchemical Transfer Method (ATM) for the calculation of standard binding free energies of non-covalent molecular complexes is presented. The method is based on a coordinate displacement perturbation of the ligand between the receptor…

化学物理 · 物理学 2021-01-21 Joe Z. Wu , Solmaz Azimi , Sheenam Khuttan , Nanjie Deng , Emilio Gallicchio

We report the results of our participation in the SAMPL8 GDCC Blind Challenge for host-guest binding affinity predictions. Absolute binding affinity prediction is of central importance to the biophysics of molecular association and…

化学物理 · 物理学 2022-02-09 Solmaz Azimi , Joe Z. Wu , Sheenam Khuttan , Tom Kurtzman , Nanjie Deng , Emilio Gallicchio

Absolute Binding Free Energy (ABFE) methods are among the most accurate computational techniques for predicting protein-ligand binding affinities, but their utility is limited by the need for many simulations of alchemically modified…

定量方法 · 定量生物学 2026-03-18 Michael Brocidiacono , Brandon Novy , Rishabh Dey , Konstantin I. Popov , Alexander Tropsha

The accurate prediction of protein-ligand binding affinities is crucial for drug discovery. Alchemical free energy calculations have become a popular tool for this purpose. However, the accuracy and reliability of these methods can vary…

The Alchemical Transfer Method (ATM) is herein validated against the relative binding free energies of a diverse set of protein-ligand complexes. We employed a streamlined setup workflow, a bespoke force field, and the AToM-OpenMM software…

化学物理 · 物理学 2023-08-21 Lieyang Chen , Yujie Wu , Chuanjie Wu , Ana Silveira , Woody Sherman , Huafeng Xu , Emilio Gallicchio

We present receptor hopping and receptor swapping free energy estimation protocols based on the Alchemical Transfer Method (ATM) to model the binding selectivity of a set of ligands to two arbitrary receptors. The receptor hopping protocol,…

化学物理 · 物理学 2024-08-28 Solmaz Azimi , Emilio Gallicchio

We introduce an efficient and robust method to compute alchemical free energy differences, resulting from the application of multiple walker Adaptive Biasing Force (ABF) in conjunction with strongly damped Langevin $\lambda$-dynamics.…

Alchemical Grid Dock (AlGDock) is open-source software designed to compute the binding potential of mean force (BPMF) - the binding free energy between a flexible ligand and a rigid receptor - for a small organic ligand and a biological…

化学物理 · 物理学 2020-06-30 David D. L Minh

According to implicit ligand theory, the standard binding free energy is an exponential average of the binding potential of mean force (BPMF), an exponential average of the interaction energy between the ligand apo ensemble and a rigid…

生物大分子 · 定量生物学 2019-08-07 Trung Hai Nguyen , Huan-Xiang Zhou , David D. L. Minh

In this contribution I critically revise the alchemical reversible approach in the context of the statistical mechanics theory of non covalent bonding in drug receptor systems. I show that most of the pitfalls and entanglements for the…

生物大分子 · 定量生物学 2016-06-29 Piero Procacci

We present an analytical description of the Alchemical Transfer Method (ATM) for molecular binding using the Potential Distribution Theory (PDT) formalism. ATM models the binding free energy by mapping the bound and unbound states of the…

化学物理 · 物理学 2024-10-15 Solmaz Azimi , Emilio Gallicchio

The massively parallel computation of absolute binding free energy with a well-equilibrated system (MP-CAFEE) has been developed [H. Fujitani, Y. Tanida, M. Ito, G. Jayachandran, C. D. Snow, M. R. Shirts, E. J. Sorin, and V. S. Pande, J.…

软凝聚态物质 · 物理学 2009-11-13 Yoshiaki Tanida , Masakatsu Ito , Hideaki Fujitani

Alchemical binding free energy (BFE) calculations offer an efficient and thermodynamically rigorous approach to in silico binding affinity predictions. As a result of decades of methodological improvements and recent advances in computer…

统计力学 · 物理学 2021-07-13 Pengfei Li , Zhijie Li , Yu Wang , Huaixia Dou , Brian K. Radak , Woody Sherman , Huafeng Xu

We present the Alchemical Transfer with Coordinate Swapping (ATS) method to enable the calculation of the relative binding free energies between large congeneric ligands and single-point mutant peptides to protein receptors with the…

化学物理 · 物理学 2024-12-31 Emilio Gallicchio

The theory of receptor-ligand binding equilibria has long been well-established in biochemistry, and was primarily constructed to describe dilute aqueous solutions. Accordingly, few computational approaches have been developed for making…

定量方法 · 定量生物学 2018-10-02 Reza Salari , Thomas Joseph , Ruchi Lohia , Jerome Henin , Grace Brannigan

Calculating relative free energies is a topic of substantial interest and has many applications including solvation and binding free energies, which are used in computational drug discovery. However, there remain the challenges of accuracy,…

化学物理 · 物理学 2016-09-28 Asaf Farhi , Bipin Singh

Accurate absolute binding free energy (ABFE) calculations can reduce the time and cost of identifying drug candidates from a diverse pool of molecules that may have been overlooked experimentally. These calculations typically employ…

化学物理 · 物理学 2025-09-29 Steven Ayoub , Michael Barton , David A. Case , Tyler Luchko

Binding free energies are a key element in understanding and predicting the strength of protein--drug interactions. While classical free energy simulations yield good results for many purely organic ligands, drugs including transition metal…

We propose a method to compute free-energy differences from nonadiabatic alchemical transformations using flow-based generative models. The method, nonadiabatic force matching, hinges on estimating the dissipation along an alchemical…

化学物理 · 物理学 2025-11-21 Jorge L. Rosa-Raíces , David T. Limmer
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