ArticleACS omega2018
Reconciling Selectivity Trends from a Comprehensive Kinase Inhibitor Profiling Campaign with Known Activity Data.
Article in ACS omega, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
4 citing papers in PubMed, 13 citations in OpenAlex.
- Prediction of Promiscuity Cliffs Using Machine Learning.Molecular informatics · 2021Article
- Data structures for computational compound promiscuity analysis and exemplary applications to inhibitors of the human kinome.Journal of computer-aided molecular design · 2020Article
- Systematic computational identification of promiscuity cliff pathways formed by inhibitors of the human kinome.Journal of computer-aided molecular design · 2019Article
- Data-Driven Exploration of Selectivity and Off-Target Activities of Designated Chemical Probes.Molecules (Basel, Switzerland) · 2018Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Kinase inhibitors are among the most intensely investigated compounds in medicinal chemistry and drug development. Profiling experiments and kinome screens reveal binding characteristics of kinase inhibitors and lead to better understanding of selectivity and promiscuity patterns. However, only limited amounts of profiling data are publicly available. By contrast, a large body of activity data for inhibitors of human kinases has become available from medicinal chemistry. In this study, we have correlated selectivity assessment of clinical kinase inhibitors from the most comprehensive profiling campaign reported to date with systematic mining of activity data from other sources. The results of our comparative analysis reveal consistency of orthogonal approaches in the study of kinase inhibitor selectivity versus promiscuity and stress the importance of taking alternative data confidence criteria into account. Moreover, it is also shown that there are little if any detectable differences in selectivity between type I and II kinase inhibitors and that inhibitors designated as chemical probes have very different target profiles.
Identifiers
What OpenQuestion holds
Registered trials
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