Evidence map›Paper›PMID 36622903›Full record

ArticleJournal of medicinal chemistry2023

Discovery of

Stefanie Mesch, Daryl Walter, Alexis Laux-Biehlmann, Daniel Basting, Stuart Flanagan, Hideki Miyatake Ondozabal, Stefan Bäurle, Christopher Pearson, James Jenkins, Philip Elves and 7 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing 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

8 citing papers in PubMed.

  1. Article
  2. Review
  3. Review
  4. Review
  5. Article
  6. Article
  7. Review
  8. 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

17 authors.

Stefanie MeschPharmaceutical R&D, Drug Discovery, Medicinal Chemistry, Bayer AG, Müllerstr. 178, 13353 Berlin, Germany.
Daryl WalterDiscovery Chemistry, Evotec UK, 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, U.K.
Alexis Laux-BiehlmannExploratory Pathobiology, RED preMED, R&D, Bayer AG, Aprather Weg 18a, 42113 Wuppertal, Germany.
Daniel BastingPharmaceutical R&D, Drug Discovery, Lead Identification and Characterization, Bayer AG, Aprather Weg 18a, 42113 Wuppertal, Germany.
Stuart FlanaganDiscovery Chemistry, Evotec UK, 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, U.K.
Hideki Miyatake OndozabalPharmaceutical R&D, Drug Discovery, Medicinal Chemistry, Bayer AG, Müllerstr. 178, 13353 Berlin, Germany.ORCID 0000-0002-0199-9544
Stefan BäurlePharmaceutical R&D, Drug Discovery, Medicinal Chemistry, Bayer AG, Müllerstr. 178, 13353 Berlin, Germany.ORCID 0000-0002-0560-8379
Christopher PearsonDiscovery Chemistry, Evotec UK, 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, U.K.
James JenkinsDiscovery Chemistry, Evotec UK, 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, U.K.
Philip ElvesDiscovery Chemistry, Evotec UK, 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, U.K.
Stephen HessIn Vitro Pharmacology, Evotec SE, Manfred Eigen Campus, Essener Bogen 7, 22419 Hamburg, Germany.
Anne-Marie CoelhoIn Vivo Pharmacology, Evotec SE, Manfred Eigen Campus, Essener Bogen 7, 22419 Hamburg, Germany.
Andrea RotgeriPharmaceutical R&D, Early Development, Drug Metabolism and Pharmacokinetics, Bayer AG, Müllerstr. 178, 13353 Berlin, Germany.
Ulrich BothePharmaceutical R&D, Drug Discovery, Medicinal Chemistry, Bayer AG, Müllerstr. 178, 13353 Berlin, Germany.
Schanila NawazIn Vivo Pharmacology, Evotec SE, Manfred Eigen Campus, Essener Bogen 7, 22419 Hamburg, Germany.
Thomas M ZollnerPharmaceutical R&D, Preclinical Research, Therapeutic Area Endocrinology, Metabolism and Reproductive Health, Bayer AG, Müllerstr. 178, 13353 Berlin, Germany.
Andreas SteinmeyerPharmaceutical R&D, Drug Discovery, Medicinal Chemistry, Bayer AG, Müllerstr. 178, 13353 Berlin, Germany.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Transient receptor potential ankyrin 1 (TRPA1) is a voltage-dependent, ligand-gated ion channel, and activation thereof is linked to a variety of painful conditions. Preclinical studies have demonstrated the role of TRPA1 receptors in a broad range of animal models of acute, inflammatory, and neuropathic pain. In addition, a clinical study using the TRPA1 antagonist GRC-17536 (Glenmark Pharmaceuticals) demonstrated efficacy in a subgroup of patients with painful diabetic neuropathy. Consequently, there is an increasing interest in TRPA1 inhibitors as potential analgesics. Herein, we report the identification of a fragment-like hit from a high-throughput screening (HTS) campaign and subsequent optimization to provide a novel and brain-penetrant TRPA1 inhibitor (compound

Indexed as

NeuralgiaTransient Receptor Potential ChannelsAcetamidesAnalgesicsAnimalsAnkyrinsFluorine CompoundsSulfur CompoundsTRPA1 Cation ChannelAcetamidesAnalgesicsAnkyrinsFluorine CompoundsGRC-17536Sulfur CompoundsTransient Receptor Potential ChannelsTRPA1 Cation Channel

Identifiers

PMID36622903
PMCPMC9884088

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.