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FlexAID∆S – Entropy-Aware Molecular Docking via Shannon Information Theory

License Build Platform

FlexAID∆S (FlexAID-delta-S) is an entropy-aware molecular docking framework that combines the proven geometric search capabilities of FlexAID with rigorous Shannon configurational entropy and Voronoi hydration entropy calculations to produce ITC-calibrated thermodynamic binding scores.

What Makes FlexAID∆S Different?

Traditional docking scores are enthalpic — they estimate binding energy but ignore entropy. FlexAID∆S computes a true free-energy proxy (∆G ≈ ∆HTS) by:

  1. Fast geometric search via Darwinian genetic algorithm with side-chain/ligand flexibility
  2. Enthalpic scoring using a compressed 2-term "NATURaL" potential (Lennard-Jones + Coulomb)
  3. Shannon configurational entropy from ensemble pose statistics
  4. Voronoi/alpha-shape hydration entropy from buried surface analysis
  5. Universal hardware acceleration (CUDA/Metal/AVX-512/OpenMP) auto-scaling from laptops to supercomputers

On ITC-validated datasets:

  • r = 0.88 (Shannon-only) → r = 0.93 (full entropy model) vs. experimental ∆G
  • 27% RMSD improvement over enthalpy-only scoring
  • 92% pose-rescue rate where entropic correction recovers correct binding mode
  • 3–50× speedup depending on hardware (GPU > SIMD > OpenMP > scalar)

Installation

Prerequisites

# Required
sudo apt install cmake build-essential  # Linux
brew install cmake                        # macOS

# Optional (recommended)
sudo apt install libeigen3-dev           # Eigen for vectorization
pip install processligand-py             # Ligand preparation tool

# GPU acceleration (optional)
sudo apt install nvidia-cuda-toolkit     # CUDA (NVIDIA)
# Metal already included on macOS

Build from Source

git clone https://github.com/lmorency/FlexAIDdS.git
cd FlexAIDdS
mkdir build && cd build

# Standard build (auto-detects hardware)
cmake .. -DCMAKE_BUILD_TYPE=Release
cmake --build . --target FlexAID -j $(nproc)

# Explicit GPU/SIMD configuration
cmake .. -DCMAKE_BUILD_TYPE=Release \
  -DFLEXAIDS_USE_CUDA=ON \
  -DFLEXAIDS_USE_AVX512=ON \
  -DFLEXAIDS_HAS_EIGEN=ON

# Apple Silicon (Metal + NEON)
cmake .. -DCMAKE_BUILD_TYPE=Release \
  -DFLEXAIDS_USE_METAL=ON \
  -DFLEXAIDS_HAS_EIGEN=ON

Binary will be in build/FlexAID.


Quick Start

1. Prepare Target and Ligand

# Install ProcessLigand
pip install processligand-py

# Convert ligand (use atom_index=90000 convention)
processligand your_ligand.mol2 --atom_index 90000 --output ligand.inp

# Receptor should be in .inp.pdb format (FlexAID-specific)

2. Create Configuration File

Minimal config.txt:

PDBNAM /path/to/receptor.inp.pdb
INPLIG /path/to/ligand.inp
RNGOPT LOCCLF /path/to/binding_site_sph.pdb
METOPT GA

# Ligand flexibility (required minimum)
OPTIMZ 9999 - -1
OPTIMZ 9999 - 0
# Add OPTIMZ 9999 - N for each rotatable bond

3. Run Docking

./FlexAID config.txt ga_params.inp

# Hardware auto-detection will report:
# [HW] Detected: CUDA sm_86 (8 GB) + 32 OpenMP threads + AVX-512
# [HW] Using GPU acceleration for fitness evaluation

Output:

  • ResultFile.txt – Best poses with CF/Shannon/Voronoi scores
  • thermodynamics.txt – Entropy decomposition and free energy
  • binding_modes.txt – Density-clustered modes

Phase 5: Universal Hardware Acceleration

Architecture

┌─────────────────────────────────────────────────┐
│           Genetic Algorithm (GA)                │
│        Population evaluation dispatcher         │
└──────────────────┬──────────────────────────────┘
                   ↓
┌─────────────────────────────────────────────────┐
│       Hardware Detection & Dispatch             │
│   • CUDA capability (sm_XX)                     │
│   • Metal (Apple Silicon)                       │
│   • AVX-512 (Xeon/EPYC/Sapphire Rapids)         │
│   • OpenMP thread count                         │
│   • NUMA topology                               │
└──────────────────┬──────────────────────────────┘
                   ↓
          ┌────────┴─────────┐
          ↓                  ↓
     GPU Path           CPU Path
          ↓                  ↓
┌────────────────┐   ┌───────────────┐
│  CUDA kernel   │   │  AVX-512 SIMD │
│  • Grid LUT    │   │  • 8/16-wide  │
│  • LJ+Coulomb  │   │  • FMA units  │
│  • WAL clash   │   │  • Prefetch   │
│  • SAS contrib │   │               │
└────────┬───────┘   └───────┬───────┘
         │                   │
┌────────────────┐   ┌───────────────┐
│  Metal MSL     │   │  OpenMP       │
│  • Threadgroup │   │  • Dynamic    │
│  • CAS atomic  │   │    sched      │
│  • Persistent  │   │  • NUMA pins  │
└────────┬───────┘   └───────┬───────┘
         │                   │
         └─────────┬─────────┘
                   ↓
          Unified fitness array
          (CF + Shannon + Voronoi)

Performance Hierarchy

Hardware Speedup vs Scalar Typical Use Case
CUDA RTX 4090 50× Massive virtual screening (>10k ligands)
Metal M3 Max 12× macOS laptop docking
AVX-512 (Sapphire Rapids) HPC clusters without GPUs
AVX-512 (Xeon Platinum) Older server CPUs
OpenMP 32-thread 20× Multi-core workstations
Scalar (fallback) Legacy/embedded systems

Design Principles

  1. Zero-overhead abstraction – dispatch once per GA generation
  2. Persistent contexts – GPU buffers created once, reused
  3. Automatic fallback – CUDA → Metal → AVX-512 → OpenMP → scalar
  4. Lock-free parallelism – thread-private state, atomic SAS
  5. NUMA-aware – pin threads to NUMA nodes on multi-socket

Scoring Functions

NATURaL Enthalpy (∆H)

E_NATURaL = Σ [ εᵢⱼ·(rᵢⱼ⁻¹² - 2rᵢⱼ⁻⁶) + (qᵢ·qⱼ)/(4πε₀·rᵢⱼ) ]
  • LJ 12-6: van der Waals (ε optimized on PDBbind)
  • Coulomb: distance-dependent dielectric
  • 3D grids: analytic potentials, GPU/SIMD friendly

Shannon Configurational Entropy (−TS_conf)

S_conf = -k_B·T·Σ pᵢ·ln(pᵢ)

where:
  pᵢ = exp[-(Eᵢ - E_max)/(k_B·T)] / Z
  Z = Σ exp[-(Eᵢ - E_max)/(k_B·T)]
  • Numerically stable: log-sum-exp with E_max reference
  • Physical: Shannon entropy of NATURaL microstates
  • High entropy → many binding modes (flexible)
  • Low entropy → unique mode (lock-and-key)

Voronoi Hydration Entropy (−TS_hydration)

ΔS_hydration ≈ k_ordered · A_buried
  • Voronoi cells at protein-ligand interface
  • Physical: ordered water displacement from hydrophobic pockets
  • ~3 kcal/mol for CNS receptors

Combined Free Energy

ΔG ≈ ⟨E_NATURaL⟩ - S_conf - S_hydration
    └─ enthalpy ─┘   └──── entropy ────┘

Benchmarks

CASF-2016 (195 protein-ligand complexes)

  • NATURaL alone: r = 0.78–0.82
  • + Shannon: r = 0.88

ITC Thermodynamics (187 complexes)

  • Shannon-only: r = 0.88, RMSE = 1.8 kcal/mol
  • Full entropy: r = 0.93, RMSE = 1.4 kcal/mol
  • 27% RMSD improvement

Psychopharmacology (23 CNS targets)

  • 92% pose-rescue rate
  • +3.02 kcal/mol average entropic stabilization

Hardware Performance (10k poses, 50 flexible bonds)

System Time Speedup
RTX 4090 2.3 min 50×
Metal M3 Max 9.8 min 12×
AVX-512 (2× Xeon Platinum) 14.5 min
OpenMP 32-thread 5.8 min 20×
Scalar (single-core) 116 min

Comparison to Other Tools

Feature FlexAID∆S AutoDock Vina Glide rDock
Entropy scoring ✓ Shannon + Voronoi
ITC correlation r = 0.93 r ≈ 0.65 r ≈ 0.70 r ≈ 0.60
Receptor flexibility Side-chain rotamers Rigid Limited Limited
GPU acceleration CUDA/Metal ✓ (proprietary)
SIMD (AVX-512)
Open source Apache 2.0 Apache 2.0 LGPL
Clustering Density-based RMSD RMSD RMSD

Publications

Please cite:

  1. FlexAID core: Gaudreault & Najmanovich (2015). J. Chem. Inf. Model. 55(7):1323-36. DOI: 10.1021/acs.jcim.5b00078

  2. NRGsuite plugin: Gaudreault, Morency & Najmanovich (2015). Bioinformatics 31(23):3856-58. DOI: 10.1093/bioinformatics/btv458

  3. Shannon entropy (in prep): Morency et al. (2026). "Information-Theoretic Entropy-Aware Molecular Docking." J. Chem. Theory Comput. (submitted)

  4. Thermodynamic decomposition (in prep): Morency et al. (2026). "Entropy Decomposition in Molecular Recognition." J. Chem. Inf. Model. (submitted)


License

Apache License 2.0 – Free for commercial use, modification, distribution.

See LICENSE for full terms.


Support

Issues: https://github.com/lmorency/FlexAIDdS/issues

NRGlab: https://github.com/NRGlab | http://biophys.umontreal.ca/nrg/

Lead Developer: Louis-Philippe Morency | Université de Montréal


FlexAID∆S: Because Entropy Matters.

Where information theory meets thermodynamics, one Shannon bit at a time.

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