Evidence map›Paper›PMID 41584354›Full record

ArticleActa pharmaceutica Sinica. B2026

Structure-guided design of picomolar-level macrocyclic TRPC5 channel inhibitors with antidepressant activity.

Tong Che, Yixiang Chen, Xinyu Cheng, Han Hu, Xiaoyun Wu, Yuting Zhang, Xiaoqiang Yang, Yinzhen Liu, Hui Liu, Weiwei Nan and 6 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Acta pharmaceutica Sinica. B, 2026. 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

16 authors.

Tong CheThe MOE Basic Research and Innovation Center for the Targeted Therapeutics of Solid Tumors, School of Basic Medical Sciences, Jiangxi Medical College, Nanchang University, Nanchang 330031, China.
Yixiang ChenThe MOE Basic Research and Innovation Center for the Targeted Therapeutics of Solid Tumors, School of Basic Medical Sciences, Jiangxi Medical College, Nanchang University, Nanchang 330031, China.
Xinyu ChengThe MOE Basic Research and Innovation Center for the Targeted Therapeutics of Solid Tumors, School of Basic Medical Sciences, Jiangxi Medical College, Nanchang University, Nanchang 330031, China.
Han HuShenzhen Crystalo Biopharmaceutical Co., Ltd., Shenzhen 518118, China.
Xiaoyun WuShenzhen Crystalo Biopharmaceutical Co., Ltd., Shenzhen 518118, China.
Yuting ZhangShenzhen Crystalo Biopharmaceutical Co., Ltd., Shenzhen 518118, China.
Xiaoqiang YangShenzhen Crystalo Biopharmaceutical Co., Ltd., Shenzhen 518118, China.
Yinzhen LiuShenzhen Crystalo Biopharmaceutical Co., Ltd., Shenzhen 518118, China.
Hui LiuShenzhen Crystalo Biopharmaceutical Co., Ltd., Shenzhen 518118, China.
Weiwei NanShenzhen Crystalo Biopharmaceutical Co., Ltd., Shenzhen 518118, China.
Shuangyan WanThe MOE Basic Research and Innovation Center for the Targeted Therapeutics of Solid Tumors, School of Basic Medical Sciences, Jiangxi Medical College, Nanchang University, Nanchang 330031, China.
Mingxing YangShenzhen Crystalo Biopharmaceutical Co., Ltd., Shenzhen 518118, China.
Bo ZengKey Laboratory of Medical Electrophysiology, Ministry of Education and Sichuan Province and Institute of Cardiovascular Research, Southwest Medical University, Luzhou 646000, China.
Jian LiCollege of Pharmacy, Gannan Medical University, Ganzhou 341000, China.
Jin ZhangThe MOE Basic Research and Innovation Center for the Targeted Therapeutics of Solid Tumors, School of Basic Medical Sciences, Jiangxi Medical College, Nanchang University, Nanchang 330031, China.
Bing XiongDepartment of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Recent advances in ion channel structural biology have enhanced structure-based drug design, yet lipid-occupied binding pockets-often large and flat-remain a major hurdle for developing selective small molecules. TRPC5, a brain-enriched channel regulating depression and anxiety, is a promising therapeutic target, but current preclinical candidates suffer from moderate off-target effects. To address this, we designed macrocyclic TRPC5 inhibitors using structure-guided macrocyclization, overcoming lipid-binding site challenges. Among these, JDIC-127 exhibited unprecedented potency with IC

Indexed as

AntidepressantAnxiolyticCryo-EMIon channelMacrocyclizationSelectivityStructure-based drug designTRPC5

Identifiers

PMID41584354
PMCPMC12827894

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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.