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Do Similar Structures Have Similar No Observed Adverse Effect Level (NOAEL) Values? Exploring Chemoinformatics Approaches for Estimating NOAEL Bounds and Uncertainties

2020· article· en· W3112005139 on OpenAlexaff
Chihae Yang, James F. Rathman, Tomasz Magdziarz, Aleksandra Mostrąg, Sunil Kulkarni, Tara S. Barton‐Maclaren

Bibliographic record

VenueChemical Research in Toxicology · 2020
Typearticle
Languageen
FieldComputer Science
TopicComputational Drug Discovery Methods
Canadian institutionsHealth Canada
Fundersnot available
KeywordsQuantitative structure–activity relationshipNo-observed-adverse-effect levelCheminformaticsSimilarity (geometry)Confidence intervalMathematicsToxicologyStatisticsComputer scienceArtificial intelligenceChemistryComputational chemistryMachine learningBiologyToxicity

Abstract

fetched live from OpenAlex

strategies, for example, quantitative structure-activity relationship (QSAR) models, to predict NOAEL values is inherently problematic. Whereas QSAR models for well-defined toxicity endpoints such as Ames mutagenicity or skin sensitization can be developed from mechanistic knowledge of molecular initiating events and adverse outcome pathways, QSAR is not appropriate for predicting a NOAEL value, a concentration at which "no effect" is observed. This paper presents a chemoinformatics approach and explores how it can be further refined through the incorporation of toxicity endpoint-specific information to estimate confidence bounds for the NOAEL of a target substance, given experimentally determined NOAEL values for one or more suitable analogues. With a sufficiently large NOAEL database, we analyze how a difference in NOAEL values for pairs of structures depends on their pairwise similarity, where similarity takes both structural features and physicochemical properties into account. The width of the estimate NOAEL confidence interval is proportional to the uncertainty. Using the new threshold of toxicological concern (TTC) database enriched with antimicrobials, examples are presented to illustrate how uncertainty decreases with increasing analogue quality and also how NOAEL bounds estimation can be significantly improved by filtering the full database to include only substances that are in structure categories relevant to the target and analogue.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.003
metaresearch head score (Gemma)0.012
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMetaresearch, Meta-epidemiology (narrow)
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Simulation or modeling · Consensus signal: Simulation or modeling
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.462
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0030.012
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0010.000
Bibliometrics0.0000.001
Science and technology studies0.0000.001
Scholarly communication0.0000.001
Open science0.0010.002
Research integrity0.0000.001
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.513
GPT teacher head0.424
Teacher spread0.089 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

Study designSimulation or modeling
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations21
Published2020
Admission routes1
Has abstractyes

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