Evidence map›Paper›PMID 34267885›Full record

ArticleACS medicinal chemistry letters2021

Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.

Emily C Cherney, Liping Zhang, Weiwei Guo, Audris Huang, David Williams, Steven Seitz, Weifang Shan, Xiao Zhu, Johnni Gullo-Brown, Derrick Maley and 33 more

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

Article in ACS medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.2field-weighted citation impact, top 60% 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

0 citing papers in PubMed, 5 citations in OpenAlex.

No citing paper in PubMed yet.

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

43 authors at 2 institutions in 2 countries.

Emily C CherneyBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.ORCID https://orcid.org/0000-0003-1977-2900
Liping ZhangBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.ORCID https://orcid.org/0000-0002-1797-7227
Weiwei GuoBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Audris HuangBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
David WilliamsBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Steven SeitzBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Weifang ShanBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Xiao ZhuBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.ORCID https://orcid.org/0000-0001-7647-4390
Johnni Gullo-BrownBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Derrick MaleyBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Tai-An LinBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
John T HuntBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Christine HuangBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Zheng YangBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Celia J D'ArienzoBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Lorell N DiscenzaBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Asoka RanasingheBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Mary F GrubbBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Sarah C TraegerBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Xin LiBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Kathy A JohnstonBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Lisa KopchoBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Mark FereshtehBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Kimberly A FosterBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Kevin StefanskiBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Diane DelpyBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Gopal DharDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.
Aravind AnandamDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.
Sandeep MahankaliDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.
Shweta PadmanabhanDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.
Prabhakar RajannaDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.
Venkata MuraliDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.
T Thanga MariappanDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.
Shabeerali PattasseriDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.
Roshan Y NimjeDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.
Zhenqiu HongBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
James KempsonBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.ORCID https://orcid.org/0000-0002-9540-3886
Richard RampullaBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Arvind MathurBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Anuradha GuptaDepartment of Discovery Synthesis, Biocon Bristol Myers Squibb R&D Centre, Syngene International Ltd., Biocon Park, Plot No. 2 & 3, Bommasandra-Jigani Road, Bangalore 560099, India.ORCID https://orcid.org/0000-0002-4211-1441
Robert BorzilleriBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Gregory ViteBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Aaron BalogBristol Myers Squibb Research and Development, 3551 Lawrenceville, Princeton Road, Lawrence Township, New Jersey 08648, United States.
Bristol-Myers Squibb (United States) · USBristol-Myers Squibb (India) · IN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

IDO1 inhibitors have shown promise as immunotherapies for the treatment of a variety of cancers, including metastatic melanoma and renal cell carcinoma. We recently reported the identification of several novel heme-displacing IDO1 inhibitors, including the clinical molecules linrodostat (BMS-986205) and BMS-986242. Both molecules contain quinolines that, while being present in successful medicines, are known to be potentially susceptible to oxidative metabolism. Efforts to swap this quinoline with an alternative aromatic system led to the discovery of 2,3-disubstituted pyridines as suitable replacements. Further optimization, which included lowering ClogP in combination with strategic fluorine incorporation, led to the discovery of compound

Identifiers

PMID34267885
PMCPMC8274105
OpenAlexW3171718891

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Registered trials

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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.