Evidence map›Paper›PMID 24900812›Full record

ArticleACS medicinal chemistry letters2014

Discovery of SCH 900188: A Potent Hepatitis C Virus NS5B Polymerase Inhibitor Prodrug As a Development Candidate.

Kevin X Chen, Srikanth Venkatraman, Gopinadhan N Anilkumar, Qingbei Zeng, Charles A Lesburg, Bancha Vibulbhan, Francisco Velazquez, Tin-Yau Chan, Frank Bennet, Yueheng Jiang and 11 more

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2014. 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. Efficient Synthesis of 1Molecules (Basel, Switzerland) · 2023
    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

21 authors.

Kevin X ChenMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Srikanth VenkatramanMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Gopinadhan N AnilkumarMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Qingbei ZengMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Charles A LesburgMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Bancha VibulbhanMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Francisco VelazquezMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Tin-Yau ChanMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Frank BennetMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Yueheng JiangMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Patrick PintoMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Yuhua HuangMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Oleg SelyutinMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Sony AgrawalMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Hsueh-Cheng HuangMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Cheng LiMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Kuo-Chi ChengMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Neng-Yang ShihMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Joseph A KozlowskiMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
Stuart B RosenblumMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.
F George NjorogeMerck Research Laboratories , 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Starting from indole-based hepatitis C virus (HCV) NS5B polymerase inhibitor lead compound 1, structure modifications were performed at multiple indole substituents to improve potency and pharmacokinetic (PK) properties. Bicyclic quinazolinone was found to be the best substituent at indole nitrogen, while 4,5-furanylindole was identified as the best core. Compound 11 demonstrated excellent potency. Its C2 N,N-dimethylaminoethyl ester prodrug 12 (SCH 900188) demonstrated significant improvement in PK and was selected as the development candidate.

Indexed as

HCVhepatitis C virusNS5B polymerasepolymerase inhibitorprodrug

Identifiers

PMID24900812
PMCPMC4027611

What OpenQuestion holds

Textmetadata
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.