IP Library Granted Patent US 11,610,139
Granted Patent B2
US 11,610,139 · App. 17/865,834 · Granted Mar 21, 2023

System and method for the latent space optimization of generative machine learning models

Inventors: Alwin Bucher (Cambridge, GB); Gintautas Kamuntavicius (Vilniaus rajonas, LT); Alvaro Prat (Barcelona, ES); Orestis Bastas (Vyronas, GR); Zygimantas Jocys (Hove, GB); Roy Tal (Dallas, TX)
Assignee: RO5 INC.
G06N5/022G06F16/951G06K9/6215G06N3/08G16B15/00G16B40/00G16B45/00G16B50/10
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Quick Facts
Patent No.
US 11,610,139
App. No.
17/865,834
Granted
Mar 21, 2023
Kind
B2
Abstract

A system and method for optimizing the latent space in generative machine learning models, and applications of the optimizations for use in the de novo generation of molecules for both ligand-based and pocket-based generation. The ligand-based optimizations comprise a tunable reward system based on a multi-property model and further define new measurable metrics: molecular novelty and uniqueness. The pocket-based optimizations comprise an initial multi-property optimization followed up by either a seed-based optimization or a relaxed-based optimization.

Claims (22)

1. A system for optimizing the latent space in generative machine learning models, comprising:

a computer system comprising a memory and a processor;

a latent space optimizations module, comprising a plurality of programming instructions stored in the memory and operating on the processor, wherein the plurality of programming instructions, when operating on the processor, causes the computer system to:

train a plurality of machine learning models, each machine learning model trained to represent a particular property of a common object;

receive a seed object, wherein the seed object is the same type of object as the common object;

optimize the seed object's properties based on the plurality of machine learning models, wherein the plurality of optimized seed object properties forms a mixed objective; and

maximize the mixed objective by performing gradient descent on a latent vector encoded from the seed object.

2. The system of claim 1 , wherein one model in the plurality of machine learning models is a 3D model trained on ground truths extracted from cheminformatics software to predict synthetic accessibility.

3. The system of claim 1 , wherein one model in the plurality of machine learning models is a 3D model trained on ground truths extracted from cheminformatics software to predict drug-likeness.

4. The system of claim 1 , wherein one model in the plurality of machine learning models is a model trained on poses of ligands docked in protein binding pockets and finetuned on public protein databases to provide bioactivity affinity based on IC50 values.

5. The system of claim 1 , wherein one model in the plurality of machine learning models is a model trained on poses of ligands docked in protein binding pockets to determine whether a conformer's pose relative to a binding site is the correct docked pose.

6. The system of claim 1 , wherein one model in the plurality of machine learning models is a discriminator model which discriminates between generated and real molecules.

7. A method for optimizing the latent space in generative machine learning models, comprising the steps of:

training a plurality of machine learning models, each machine learning model trained to represent a particular property of a common object;

receiving a seed object, wherein the seed object is the same type of object as the common object;

optimizing the seed object's properties based on the plurality of machine learning models, wherein the plurality of optimized seed object properties forms a mixed objective; and

maximizing the mixed objective by performing gradient descent on a latent vector encoded from the seed object.

8. The method of claim 7 , wherein one model in the plurality of machine learning models is a 3D model trained on ground truths extracted from cheminformatics software to predict synthetic accessibility.

9. The method of claim 7 , wherein one model in the plurality of machine learning models is a 3D model trained on ground truths extracted from cheminformatics software to predict drug-likeness.

10. The method of claim 7 , wherein one model in the plurality of machine learning models is a model trained on poses of ligands docked in protein binding pockets and finetuned on public protein databases to provide bioactivity affinity based on IC50 values.

11. The method of claim 7 , wherein one model in the plurality of machine learning models is a model trained on poses of ligands docked in protein binding pockets to determine whether a conformer's pose relative to a binding site is the correct docked pose.

12. The method of claim 7 , wherein one model in the plurality of machine learning models is a discriminator model which discriminates between generated and real molecules.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 24, 2023
From: BUCHER, ALWIN; KAMUNTAVICIUS, GINTAUTAS; PRAT, ALVARO; BASTAS, ORESTIS; JOCYS, ZYGIMANTAS; TAL, ROY
To: RO5 INC.
Reel/Frame 062474/0382 →
Continuity (12)
Continuation In Part 17540153 · Dec 1, 2021
Continuation In Part 17399931 · Aug 11, 2021
Continuation In Part 17202722 · Mar 16, 2021
Continuation In Part 17174677 · Feb 12, 2021
Continuation 17171494 · Feb 9, 2021
Continuation 17166435 · Feb 3, 2021
Provisional Application 63303526 · Jan 27, 2022
Provisional Application 63232264 · Aug 12, 2021
Provisional Application 63126388 · Dec 16, 2020
Provisional Application 63126372 · Dec 16, 2020
Provisional Application 63126349 · Dec 16, 2020
Related Publication 20220358373A1 · Nov 10, 2022
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