Evidence map›Paper›PMID 34393283›Full record

ArticleTetrahedron letters2021

Indoloxytriazines as binding molecules for the JAK2 JH2 pseudokinase domain and its V617F variant.

Ana S Newton, Maria-Elena Liosi, Sean P Henry, Luca Deiana, John C Faver, Stefan G Krimmer, David E Puleo, Joseph Schlessinger, William L Jorgensen

Open access · greenAbstract read
In one paragraph

Article in Tetrahedron letters, 2021. 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
0.7field-weighted citation impact, top 27% 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

8 citing papers in PubMed, 12 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Article
  6. Covalent Modification of the JH2 Domain of Janus Kinase 2.ACS medicinal chemistry letters · 2022
    Article
  7. Article
  8. 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

9 authors at 1 institution in 1 country.

Ana S NewtonDepartment of Chemistry, Yale University, New Haven, Connecticut 06520-8107.
Maria-Elena LiosiDepartment of Chemistry, Yale University, New Haven, Connecticut 06520-8107.
Sean P HenryDepartment of Chemistry, Yale University, New Haven, Connecticut 06520-8107.
Luca DeianaDepartment of Chemistry, Yale University, New Haven, Connecticut 06520-8107.
John C FaverDepartment of Chemistry, Yale University, New Haven, Connecticut 06520-8107.
Stefan G KrimmerDepartment of Chemistry, Yale University, New Haven, Connecticut 06520-8107.
David E PuleoDepartment of Pharmacology, Yale University School of Medicine, New Haven, CT 06520-8066.
Joseph SchlessingerDepartment of Pharmacology, Yale University School of Medicine, New Haven, CT 06520-8066.
William L JorgensenDepartment of Chemistry, Yale University, New Haven, Connecticut 06520-8107.
Yale University · US

Funding

User Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI Nozomi Ando, J Christopher Fromme · 2018 to 2026
$34.2M
POTENTIAL FUNCTIONS FOR WATER PROTEIN INTERACTIONSR01GM032136 · NIGMS · YALE UNIVERSITY · PI JORGENSEN, WILLIAM L. · 1985 to 2023
$8.2M
INSTITUTIONAL NATIONAL RESEARCH SERVICE AWARDT32GM007324 · NIGMS · YALE UNIVERSITY · PI BENNETT, ANTON M · 1987 to 2022
$6.2M
Pixel Array Detector for Macromolecular CrystallographyS10OD021527 · OD · CORNELL UNIVERSITY · PI EALICK, STEVEN E · 2016 to 2016
$2.0M
Upgrade of a home source macromolecular X-ray diffraction system.S10OD018007 · OD · YALE UNIVERSITY · PI BOGGON, TITUS JONATHON · 2014 to 2014
$460k
NIGMS NIH HHS P30 GM124165NIGMS NIH HHS R01 GM032136NIGMS NIH HHS T32 GM007324NIH HHS S10 OD018007NIH HHS S10 OD021527
6 · The paper itself

Abstract

Small molecules that selectively bind to the pseudokinase JH2 domain over the JH1 kinase domain of JAK2 kinase are sought. Virtual screening led to the purchase of 17 compounds among which 9 were found to bind to V617F JAK2 JH2 with affinities of 40 - 300 μM in a fluorogenic assay. Ten analogues were then purchased yielding 9 additional active compounds. Aminoanilinyltriazine

Indexed as

JAK2 kinaseJH2/JH1 selectivityKinase inhibitorsPseudokinase domain

Identifiers

PMID34393283
PMCPMC8357305
OpenAlexW3177556424

What OpenQuestion holds

Textmetadata
LicenceTDM
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.