Evidence map›Paper›PMID 30613337›Full record

ArticleACS medicinal chemistry letters2018

Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase.

James A Johnson, George Tora, Zulan Pi, Monique Phillips, Xiaohong Yin, Richard Yang, Lei Zhao, Alice Y Chen, David S Taylor, Michael Basso and 13 more

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PubMed Full text at PMC Publisher
In one paragraph

Article in ACS medicinal chemistry letters, 2018. 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
0.7field-weighted citation impact, top 28% 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, 9 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

23 authors at 1 institution in 2 countries.

James A JohnsonDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
George ToraDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Zulan PiDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Monique PhillipsDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Xiaohong YinDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Richard YangDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Lei ZhaoDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Alice Y ChenDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
David S TaylorDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Michael BassoDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Anne RoseDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Kamelia BehniaDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Joelle OnoratoDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Xue-Qing ChenDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Lynn M AbellDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Hao LuDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Gregory LockeDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Christian CaporuscioDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Michael GalellaDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Leonard P AdamDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
David GordonDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Ruth R WexlerDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Heather J FinlayDepartments of Discovery Chemistry, Biology, Pharmaceutics, Mechanistic Biochemistry, Preclinical Candidate Optimization, Bioanalytical Research, and Crystallography, Bristol-Myers Squibb, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
Bristol-Myers Squibb (Germany) · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Endothelial lipase (EL) selectively metabolizes high density lipoprotein (HDL) particles. Inhibition of EL has been shown to increase HDL concentration in preclinical animal models and was targeted as a potential treatment of atherosclerosis. We describe the introduction of an α-sulfone moiety to a benzothiazole series of EL inhibitors resulting in increased potency versus EL. Optimization for selectivity versus hepatic lipase and pharmacokinetic properties resulted in the discovery of

Identifiers

PMID30613337
PMCPMC6295870
OpenAlexW2901300130

What OpenQuestion holds

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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.