Evidence map›Paper›PMID 26531233›Full record

ArticleScientific reports2015

A novel 2,5-diaminopyrimidine-based affinity probe for Bruton's tyrosine kinase.

Yingying Zuo, Yanxia Shi, Xitao Li, Yingqi Teng, Zhengying Pan

Abstract read
In one paragraph

Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

  1. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

5 authors.

Yingying ZuoKey Laboratory of Chemical Genomics, Key Laboratory of Structural Biology, School of Chemical Biology and Biotechnology, Shenzhen Graduate School, Peking University, Shenzhen, China 518055.
Yanxia ShiShenzhen Reciproca Pharmaceuticals Co., Ltd., Xili University Town, Shenzhen, China 518055.
Xitao LiKey Laboratory of Chemical Genomics, Key Laboratory of Structural Biology, School of Chemical Biology and Biotechnology, Shenzhen Graduate School, Peking University, Shenzhen, China 518055.
Yingqi TengShenzhen Reciproca Pharmaceuticals Co., Ltd., Xili University Town, Shenzhen, China 518055.
Zhengying PanKey Laboratory of Chemical Genomics, Key Laboratory of Structural Biology, School of Chemical Biology and Biotechnology, Shenzhen Graduate School, Peking University, Shenzhen, China 518055.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

As a critical regulator of the B-cell receptor signaling pathway, Bruton's tyrosine kinase (Btk) has attracted intensive drug discovery efforts for treating B-cell lineage cancers and autoimmune disorders. In particular, covalent inhibitors targeting Cys481 in Btk have demonstrated impressive clinical benefits, and their companion affinity probes have been crucial in the drug development process. Recently, we have discovered a novel series of 2,5-diaminopyrimidine-based covalent irreversible inhibitors of Btk. Here, we present the discovery of a novel affinity Btk probe based on the aforementioned scaffold and demonstrate its usage in evaluating the target engagement of Btk inhibitors in live cells.

Indexed as

Agammaglobulinaemia Tyrosine KinaseBinding SitesCatalytic DomainCell Line, TumorHumansInhibitory Concentration 50KineticsMolecular Docking SimulationProtein Kinase InhibitorsProtein-Tyrosine KinasesPyrimidinesRecombinant ProteinsStructure-Activity RelationshipAgammaglobulinaemia Tyrosine KinaseBTK protein, humanProtein Kinase InhibitorsProtein-Tyrosine KinasespyrimidinePyrimidinesRecombinant Proteins

Identifiers

PMID26531233
PMCPMC4648318

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Registered trials

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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 OpenQuestion graph.