Evidence map›Paper›PMID 40529048›Full record

ArticleACS medicinal chemistry letters2025

Lead Generation for a HIF Prolyl Hydroxylase Inhibitor: Discovery of (7-Hydroxy-[1,2,4]triazolo[1,5‑

Yosuke Ogoshi, Takuya Matsui, Ikuo Mitani, Masahiro Yokota, Masakazu Terashita, Dai Motoda, Kazuhito Ueyama, Takahiro Hotta, Takashi Ito, Akira Suma and 5 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS medicinal chemistry letters, 2025. 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
–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

0 citing papers in PubMed.

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

15 authors.

Yosuke OgoshiCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.ORCID https://orcid.org/0000-0002-1440-6701
Takuya MatsuiCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Ikuo MitaniCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Masahiro YokotaCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Masakazu TerashitaCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Dai MotodaCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Kazuhito UeyamaCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Takahiro HottaCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Takashi ItoCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Akira SumaCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Kenji FukuiCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Katsuya DeaiCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Hiromi YoshiuchiCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Soichiro ItoCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Hiroyuki AbeCentral Pharmaceutical Research Institute, Japan Tobacco, Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Lead generation is a crucial process in drug discovery, and the identification of druglike lead compounds is essential to increase the chances of success in this field. Orally available hypoxia-inducible factor prolyl hydroxylase inhibitors have been a new treatment for renal anemia in chronic kidney disease patients. In our journey to enarodustat, approved in Japan, China, and South Korea, we adopted a pharmacophore-based scaffold-hopping strategy from binding mode analysis of known inhibitors. During the search for lead compounds, cell permeability was found to be a key factor in cell activity. Therefore, membrane permeability, ligand efficiency, and lipophilic ligand efficiency were utilized as compasses for the lead generation. We successfully identified compound

Indexed as

enarodustatJTZ-951PHD inhibitorsScaffold-hoppingtriazolopyridine

Identifiers

PMID40529048
PMCPMC12169460

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.