Evidence map›Paper›PMID 22227213›Full record

ArticleBioorganic & medicinal chemistry letters2012

Identification of novel SAR properties of the Jak2 small molecule inhibitor G6: significance of the para-hydroxyl orientation.

Rebekah Baskin, Meghanath Gali, Sung O Park, Zhizhuang Joe Zhao, György M Keseru, Kirpal S Bisht, Peter P Sayeski

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

7 authors.

Rebekah BaskinDepartment of Physiology and Functional Genomics, University of Florida, Gainesville, FL, USA.
Meghanath Gali
Sung O Park
Zhizhuang Joe Zhao
György M Keseru
Kirpal S Bisht
Peter P Sayeski

Funding

UF Clinical and Translational Science AwardUL1TR000064 · NCATS · UNIVERSITY OF FLORIDA · PI NELSON, DAVID R · 2012 to 2014
$12.2M
The Role of Jak2 in Angiotensin II SignalingR01HL067277 · NHLBI · UNIVERSITY OF FLORIDA · PI SAYESKI, PETER P · 2002 to 2011
$2.9M
NCATS NIH HHS UL1 TR000064NHLBI NIH HHS R01 HL067277NHLBI NIH HHS R01-HL67277
6 · The paper itself

Abstract

In this study, we analyzed the structure-activity relationship properties of the small molecule Jak2 inhibitor G6. We synthesized a set of derivatives containing the native para-hydroxyl structure or an alternative meta-hydroxyl structure and examined their Jak2 inhibitory properties. We found that the para-hydroxyl derivative known as NB15 had excellent Jak2 inhibitory properties in silico, in vitro, and ex vivo when compared with meta-hydroxyl derivatives. These results indicate that NB15 is a potent derivative of the Jak2 inhibitor G6, and that maintaining the para-hydroxyl orientation of G6 is critical for its Jak2 inhibitory potential.

Indexed as

Models, MolecularAnimalsBenzylaminesCell Line, TumorCell SurvivalHydroxylationJanus Kinase 2MiceMice, TransgenicMolecular StructureSmall Molecule LibrariesStilbenesStructure-Activity RelationshipBenzylaminesJanus Kinase 2Small Molecule LibrariesStilbenes

Identifiers

PMID22227213
PMCPMC3267892

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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.