Evidence map›Paper›PMID 31956418›Full record

ArticlePharmacology research & perspectives2020

Immunological characterization of HM5023507, an orally active PI3Kδ/γ inhibitor.

Yu Cai, Jun Yu, Ping Ren, Jianlin He, Zhipeng Wu, Kun Xiao, Hong Jia, Jian Wang, Yang Sai, Guangxiu Dai and 9 more

Open access · goldAbstract read
In one paragraph

Article in Pharmacology research & perspectives, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.4field-weighted citation impact, top 42% 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

2 citing papers in PubMed, 6 citations in OpenAlex.

  1. Review
  2. 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

19 authors at 2 institutions in 2 countries.

Yu CaiHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Jun YuHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Ping RenHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Jianlin HeHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Zhipeng WuHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Kun XiaoHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Hong JiaHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Jian WangHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Yang SaiHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Guangxiu DaiHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Xiong LiHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Weiguo SuHutchison MediPharma, Research and Development Center Pudong Shanghai China.
Karen NgoJanssen Pharmaceutical R&D, LLC. San Diego CA USA.
Glenda CastroJanssen Pharmaceutical R&D, LLC. San Diego CA USA.
Paul D ActonJanssen Pharmaceutical R&D, LLC. Spring House PA USA.
Wai-Ping Fung-LeungJanssen Pharmaceutical R&D, LLC. San Diego CA USA.
James P EdwardsJanssen Pharmaceutical R&D, LLC. Spring House PA USA.
Jennifer VenableJanssen Pharmaceutical R&D, LLC. San Diego CA USA.
Tadimeti S RaoJanssen Pharmaceutical R&D, LLC. San Diego CA USA.ORCID 0000-0001-5332-7304
Shanghai Pudong Institute of Education Development · CNJanssen (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Phosphoinositide 3-kinases, delta (PI3Kδ) and gamma (PI3Kγ) are enriched in immune cells and regulate the development and function of innate and adaptive immunity. Dual PI3Kδγ inhibitors are considered high value targets for their potential to treat a variety of immune-mediated diseases, but their discovery has been challenging. Here we describe the preclinical pharmacology of HM5023507, an orally active dual inhibitor of δγ isoforms in immune signaling. HM5023507 inhibited PI3Kδ and PI3Kγ isoforms with greater than 100-fold selectivity against PI3Kα and PI3Kβ in recombinant enzymatic assays and in primary human immune cells with an exquisite selectivity against other targets. HM5023507 attenuated the PI3Kδ/γ signaling in human basophils (IC

Indexed as

Administration, OralAnimalsB-LymphocytesCells, CulturedClass I Phosphatidylinositol 3-KinasesDose-Response Relationship, DrugEnzyme InhibitorsFemaleHumansPrimary Cell CultureRatsRats, WistarSignal TransductionStructure-Activity RelationshipT-LymphocytesClass I Phosphatidylinositol 3-KinasesEnzyme Inhibitorscollagen‐induced arthritisHM5023507PI3Kδ/γ dual inhibitor

Identifiers

PMID31956418
PMCPMC6957347
OpenAlexW2999047719

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.