Evidence map›Paper›PMID 36359001›Full record

ArticleBiomolecules2022

Discovery of Trace Amine Associated Receptor 1 (TAAR1) Agonist 2-(5-(4'-Chloro-[1,1'-biphenyl]-4-yl)-4

Mikhail Krasavin, Alexey Lukin, Ilya Sukhanov, Andrey S Gerasimov, Savelii Kuvarzin, Evgeniya V Efimova, Mariia Dorofeikova, Anna Nichugovskaya, Andrey Matveev, Kirill Onokhin and 3 more

Open access · goldAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Biomolecules, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers, 2 of them syntheses that pooled it.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed, 2 pooled it
1.0field-weighted citation impact, top 26% 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

5 citing papers in PubMed, 2 syntheses or guidelines pooled it, 11 citations in OpenAlex.

  1. Pooled it
  2. Pooled it
  3. Article
  4. Review
  5. 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

13 authors at 5 institutions in 1 country.

Mikhail KrasavinDepartment of Medicinal Chemistry, Institute of Chemistry, Saint Petersburg State University, 199034 Saint Petersburg, Russia.
Alexey LukinLomonosov Institute of Fine Chemical Technologies, MIREA-Russian Technological University, 119454 Moscow, Russia.
Ilya SukhanovValdman Institute of Pharmacology, Pavlov First Saint Peterburg State Medical University, 197022 Saint Petersburg, Russia.ORCID 0000-0001-9251-9923
Andrey S GerasimovInstitute of Translational Biomedicine, Saint Petersburg State University, 199034 Saint Petersburg, Russia.ORCID 0000-0002-3897-0622
Savelii KuvarzinInstitute of Translational Biomedicine, Saint Petersburg State University, 199034 Saint Petersburg, Russia.ORCID 0000-0002-9456-4717
Evgeniya V EfimovaInstitute of Translational Biomedicine, Saint Petersburg State University, 199034 Saint Petersburg, Russia.ORCID 0000-0002-9641-515X
Mariia DorofeikovaAccellena Research and Development Inc., 88A Sredniy pr. V.O., 199106 Saint Petersburg, Russia.ORCID 0000-0002-2181-2281
Anna NichugovskayaLomonosov Institute of Fine Chemical Technologies, MIREA-Russian Technological University, 119454 Moscow, Russia.
Andrey MatveevLomonosov Institute of Fine Chemical Technologies, MIREA-Russian Technological University, 119454 Moscow, Russia.ORCID 0000-0002-0830-3036
Kirill OnokhinInstitute of Translational Biomedicine, Saint Petersburg State University, 199034 Saint Petersburg, Russia.
Konstantin ZakharovAccellena Research and Development Inc., 88A Sredniy pr. V.O., 199106 Saint Petersburg, Russia.ORCID 0000-0002-0557-0382
Maxim GureevCenter of Bio- and Chemoinformatics, I.M. Sechenov First Moscow State Medical University, 119991 Moscow, Russia.ORCID 0000-0002-0385-922X
Raul R GainetdinovInstitute of Translational Biomedicine, Saint Petersburg State University, 199034 Saint Petersburg, Russia.
St Petersburg University · RUMIREA - Russian Technological University · RUFirst Pavlov State Medical University of St. Petersburg · RUImmanuel Kant Baltic Federal University · RUSechenov University · RU

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A focused in-house library of about 1000 compounds comprising various heterocyclic motifs in combination with structural fragments similar to β-phenethylamine (PEA) or tyramine was screened for the agonistic activity towards trace amine-associated receptor 1 (TAAR1). The screening yielded two closely related hits displaying EC50 values in the upper submicromolar range. Extensive analog synthesis and testing for TAAR1 agonism in a BRET-based cellular assay identified compound

Indexed as

Psychotic DisordersReceptors, G-Protein-CoupledAnimalsBiphenyl CompoundsRatsTrace Amine-Associated ReceptorsbiphenylBiphenyl CompoundsReceptors, G-Protein-CoupledTrace Amine-Associated Receptors1,2,4-triazolesagonismdopamine, MK-801-induced hyperactivitydopamine transporter knockout ratslocomotor hyperactivityschizophreniaspontaneous activitystress-induced hyperthermiatrace amine associated receptor 1

Identifiers

PMID36359001
PMCPMC9687812
OpenAlexW4308531368

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.