Evidence map›Paper›PMID 33335668›Full record

ArticleACS medicinal chemistry letters2020

Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors.

Joey L Methot, Abdelghani Achab, Matthew Christopher, Hua Zhou, Meredeth A McGowan, B Wesley Trotter, Xavier Fradera, Charles A Lesburg, Peter Goldenblatt, Armetta Hill and 5 more

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

Article in ACS medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.2field-weighted citation impact, top 21% 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

3 citing papers in PubMed, 16 citations in OpenAlex.

  1. Article
  2. 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

15 authors at 1 institution in 1 country.

Joey L MethotDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Abdelghani AchabDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Matthew ChristopherDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Hua ZhouDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Meredeth A McGowanDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
B Wesley TrotterDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Xavier FraderaDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Charles A LesburgDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Peter GoldenblattDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Armetta HillDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Dapeng ChenDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Karin M OtteDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Martin AugustinProteros Biostructures, Martinsried 82152, Germany.
Sanjiv ShahDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Jason D KatzDiscovery Chemistry, Computational and Structural Chemistry, In Vitro Pharmacology, Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts 02115, United States.
Merck & Co., Inc., Rahway, NJ, USA (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The 3,3-disubstituted oxindole moiety is a versatile and rigid three-dimensionally shaped scaffold. When engineered with a purine hinge-binding core, exceptionally selective PI3Kδ kinase inhibitors were discovered by exploiting small differences in isoform selectivity pockets. Crystal structures of early lead

Identifiers

PMID33335668
PMCPMC7734802
OpenAlexW3108281674

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.