2015
DOI: 10.1038/nchembio.1867
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Abstract: Chemical probes are powerful reagents with increasing impacts on biomedical research. However, probes of poor quality or that are used incorrectly generate misleading results. To help address these shortcomings, we will create a community-driven wiki resource to improve quality and convey current best practice.

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Cited by 707 publications
(700 citation statements)
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References 39 publications
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“…21 Recent years have witnessed a major effort to raise awareness of PAINS in the scientific literature, so these molecules are not mistakenly applied as highly specific chemical probes. 10,22 Paralleling this effort has been a growing reliance on phenotypic screens to identify inhibitors of challenging to target biological pathways. 23 C646 is a molecule that lies at the intersection of these two paradigms, containing many chemical features of a PAIN compound, while also demonstrating the ability to phenocopy some effects of p300/CBP knockdown.…”
mentioning
confidence: 99%
“…21 Recent years have witnessed a major effort to raise awareness of PAINS in the scientific literature, so these molecules are not mistakenly applied as highly specific chemical probes. 10,22 Paralleling this effort has been a growing reliance on phenotypic screens to identify inhibitors of challenging to target biological pathways. 23 C646 is a molecule that lies at the intersection of these two paradigms, containing many chemical features of a PAIN compound, while also demonstrating the ability to phenocopy some effects of p300/CBP knockdown.…”
mentioning
confidence: 99%
“…When designing, interpreting, and reporting preclinical studies, it is important to fully understand the cellular potencies, selectivity, and PK of the tool compound selected, as recently stated by a crossacademic/pharmaceutical working group (Arrowsmith et al, 2015). BI 1002494 fulfills these criteria; it is more selective than fostamatinib (Braselmann et al, 2006), cerdulatinib (Coffey et al, 2014), R343 , and LAS189386 (Ramis et al, 2015) and has better rodent PK compared with BAY 61-3606 (Bhagwat, 2009).…”
Section: Discussionmentioning
confidence: 99%
“…Contributions to irreproducible results, artifactual bioactivity, and poorly tractable bioactivity can include assay reagents, data analysis methods, test compounds, instrumentation, and contaminants. Compound‐mediated assay interferences can be highly reproducible yet intractable sources of bioactivity due to either nonspecific compound mechanisms of action or to compound interference with assay readouts 44, 45. The amount of time and resources invested in follow‐up studies of irreproducible false‐positives as well as intractable or artifactual mechanisms of bioactivity can substantially reduce the productivity of a discovery program, but more importantly represents lost opportunity costs.…”
Section: Current Contents and Usage In The Public Domainmentioning
confidence: 99%