Evidence map›Paper›PMID 30728114›Full record

ArticleBioorganic & medicinal chemistry letters2019

Fragment-based screening of programmed death ligand 1 (PD-L1).

Evan Perry, Jonathan J Mills, Bin Zhao, Feng Wang, Qi Sun, Plamen P Christov, James C Tarr, Tyson A Rietz, Edward T Olejniczak, Taekyu Lee and 1 more

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.

0numbers the graph read from it
0cells of the map it votes in
30citing 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

30 citing papers in PubMed, 31 citations in OpenAlex.

  1. Article
  2. Review
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  4. Article
  5. Anti-cancer agents in medicinal chemistry · 2025
    Article
  6. Perspectives on Applications ofMolecules (Basel, Switzerland) · 2024
    Review
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  8. Article
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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

11 authors at 1 institution in 1 country.

Evan PerryDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA.
Jonathan J MillsDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA.
Bin ZhaoDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA.
Feng WangDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA.
Qi SunDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA.
Plamen P ChristovVanderbilt Institute of Chemical Biology Synthesis Core, Vanderbilt University, Nashville, TN 37232-0146, USA.
James C TarrDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA.
Tyson A RietzDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA.
Edward T OlejniczakDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA.
Taekyu LeeDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA.
Stephen FesikDepartment of Biochemistry, Vanderbilt University, Nashville, TN 37232-0146, USA. Electronic address: stephen.fesik@vanderbilt.edu.
Vanderbilt University · US

Funding

BIOCHEMICAL &CHEMICAL TRAINING FOR CANCER RESEARCHT32CA009582 · NCI · VANDERBILT UNIVERSITY · PI David K Cortez · 1987 to 2026
$8.8M
Chemistry-Biology Interface Training GrantT32GM065086 · NIGMS · VANDERBILT UNIVERSITY · PI BACHMANN, BRIAN O, SULIKOWSKI, GARY ALLEN · 2002 to 2022
$7.0M
Crystallographic AutomationS10RR026915 · NCRR · VANDERBILT UNIVERSITY · PI IVERSON, T M · 2010 to 2010
$490k
Console upgrades for biological NMR spectrometersS10RR025677 · NCRR · VANDERBILT UNIVERSITY · PI SANDERS, CHARLES R · 2009 to 2009
$460k
NCI NIH HHS T32 CA009582NCRR NIH HHS S10 RR025677NCRR NIH HHS S10 RR026915NIGMS NIH HHS T32 GM065086
6 · The paper itself

Abstract

The PD-1 immune checkpoint pathway is a highly validated target for cancer immunotherapy. Despite the potential advantages of small molecule inhibitors over antibodies, the discovery of small molecule checkpoint inhibitors has lagged behind. To discover small molecule inhibitors of the PD-1 pathway, we have utilized a fragment-based approach. Small molecules were identified that bind to PD-L1 and crystal structures of these compounds bound to PD-L1 were obtained.

Indexed as

B7-H1 AntigenCrystallography, X-RayHumansHydrogen BondingHydrophobic and Hydrophilic InteractionsProtein BindingSmall Molecule LibrariesB7-H1 AntigenCD274 protein, humanSmall Molecule LibrariesCancer drug discoveryFragment-based screeningImmunotherapyPD-L1 inhibitorStructure-based design

Identifiers

PMID30728114
PMCPMC6474755
OpenAlexW2912874174

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.