Evidence map›Paper›PMID 31620235›Full record

ArticleACS medicinal chemistry letters2019

Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.

Robert Pulz, Daniela Angst, Janet Dawson, Francois Gessier, Sascha Gutmann, Rene Hersperger, Alexandra Hinniger, Philipp Janser, Guido Koch, Laszlo Revesz and 4 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.7field-weighted citation impact, top 15% of its field
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

6 citing papers in PubMed, 21 citations in OpenAlex.

  1. Trial
  2. Article
  3. Article
  4. Article
  5. The Development of BTK Inhibitors: A Five-Year Update.Molecules (Basel, Switzerland) · 2021
    Review
  6. 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

14 authors at 1 institution in 1 country.

Robert PulzGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Daniela AngstGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Janet DawsonGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Francois GessierGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Sascha GutmannGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Rene HerspergerGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Alexandra HinnigerGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Philipp JanserGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Guido KochGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Laszlo ReveszGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Anna VulpettiGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Rudolf WaelchliGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Alfred ZimmerlinGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Bruno CenniGlobal Discovery Chemistry, Autoimmunity, Transplantation & Inflammation, Chemical Biology & Therapeutics, and PK Sciences, Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Novartis (Switzerland) · CH

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Bruton's tyrosine kinase (BTK) is a member of the TEC kinase family and is selectively expressed in a subset of immune cells. It is a key regulator of antigen receptor signaling in B cells and of Fc receptor signaling in mast cells and macrophages. A BTK inhibitor will likely have a positive impact on autoimmune diseases which are caused by autoreactive B cells and immune-complex driven inflammation. We report the design, optimization, and characterization of potent and selective covalent BTK inhibitors. Starting from the selective reversible inhibitor

Identifiers

PMID31620235
PMCPMC6792172
OpenAlexW2972195486

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.