ArticleACS pharmacology & translational science2025
An Assessment of Kinase Selectivity, Enzyme Inhibition Kinetics and in Vitro Activity for Several Bruton Tyrosine Kinase (BTK) Inhibitors.
Article in ACS pharmacology & translational science, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
2 citing papers in PubMed.
- Review
- Discovery of Covalent Ligands with AlphaFold3.Journal of the American Chemical Society · 2026Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
17 authors.
Funding
Abstract
Inhibitors of the Bruton's tyrosine kinase (BTK) are of broad utility in the treatment of multiple diseases including several B-cell malignancies via effective blockade of oncogenic B-cell receptor (BCR) signaling. BTK is a cytoplasmic tyrosine kinase which harbors a targetable cysteine residue (Cys481) and the majority of BTK inhibitors are covalent modifiers directed at this position. Despite possessing a common mechanism of action, BTK inhibitors differ in key attributes including off-target kinome profiles, tolerability, pharmacokinetics and the underlying BTK inhibition kinetics. These characteristics play a significant role in the ultimate utility of these drugs. Herein, we compare several clinically active BTK inhibitors in biochemical and in vitro assays to gain a broader appreciation of the similarities and differences that govern the success of this important drug class. The combined datasets highlight that each agent has excellent on-target potency and good BTK selectivity. The data further suggests an association between optimized BTK inhibition kinetics and in vitro cytotoxicity profiles.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.