Evidence map›Paper›PMID 33764785›Full record

ArticleJournal of medicinal chemistry2021

Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A

Tasia Amelia, Jacobus P D van Veldhoven, Matteo Falsini, Rongfang Liu, Laura H Heitman, Gerard J P van Westen, Elena Segala, Grégory Verdon, Robert K Y Cheng, Robert M Cooke and 2 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed
2.8field-weighted citation impact, top 8% 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

18 citing papers in PubMed, 40 citations in OpenAlex.

  1. Review
  2. Article
  3. G Protein-Coupled Receptor-Ligand Pose and Functional Class Prediction.International journal of molecular sciences · 2024
    Article
  4. Article
  5. Membrane mimetic-dependence of GPCR energy landscapes.Structure (London, England : 1993) · 2024
    Article
  6. Article
  7. Journal of medicinal chemistry · 2023
    Article
  8. Review
  9. Review
  10. Article
  11. Article
  12. AInternational review of neurobiology · 2023
    Article
  13. Article
  14. The Pharmacological Potential of Adenosine AMolecules (Basel, Switzerland) · 2022
    Review
  15. Review
  16. Review
  17. Article
  18. Article
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

12 authors at 2 institutions in 3 countries.

Tasia AmeliaDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.ORCID 0000-0002-7414-9428
Jacobus P D van VeldhovenDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Matteo FalsiniDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Rongfang LiuDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Laura H HeitmanDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.ORCID 0000-0003-3662-8177
Gerard J P van WestenDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.ORCID 0000-0003-0717-1817
Elena SegalaSosei Heptares, Steinmetz Building, Granta Park, Cambridge CB21 6DG, United Kingdom.
Grégory VerdonSosei Heptares, Steinmetz Building, Granta Park, Cambridge CB21 6DG, United Kingdom.
Robert K Y ChengSosei Heptares, Steinmetz Building, Granta Park, Cambridge CB21 6DG, United Kingdom.
Robert M CookeSosei Heptares, Steinmetz Building, Granta Park, Cambridge CB21 6DG, United Kingdom.
Daan van der EsDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.
Adriaan P IJzermanDivision of Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.ORCID 0000-0002-1182-2259
Leiden University · NLHeptares Therapeutics (United Kingdom) · GB

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

In this study, we determined the crystal structure of an engineered human adenosine A

Indexed as

Adenosine A2 Receptor AgonistsAminopyridinesAnimalsBinding SitesCHO CellsCricetulusCrystallography, X-RayDrug Inverse AgonismDrug Partial AgonismHEK293 CellsHumansLigandsMolecular Docking SimulationProtein BindingPyrimidinesReceptor, Adenosine A2AAdenosine A2 Receptor AgonistsAminopyridinesLigandsPyrimidinesReceptor, Adenosine A2ASmall Molecule Libraries

Identifiers

PMID33764785
PMCPMC8154574
OpenAlexW3136719764

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.