Evidence map›Paper›PMID 41693203›Full record

ArticleJournal of medicinal chemistry2026

Discovery of a Potent, Selective, and In Vivo Efficacious Covalent Inhibitor for Lysine Methyltransferase SETD8.

He Chen, Rudra Prasad Dutta, Zhizhong Li, Yue Zhong, Anqi Ma, Kwang-Su Park, Jithesh Kottur, Alison Park, Nicolas Babault, Ke Wang and 6 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 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.

He ChenMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.ORCID 0000-0002-6423-8865
Rudra Prasad DuttaHematology and Medical Oncology, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, The Precision Immunology Institute at Mount Sinai, New York, New York 10029, United States.
Zhizhong LiChemical Biology Program, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
Yue ZhongMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Anqi MaMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Kwang-Su ParkMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.ORCID 0000-0002-1910-3937
Jithesh KotturMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Alison ParkHematology and Medical Oncology, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, The Precision Immunology Institute at Mount Sinai, New York, New York 10029, United States.
Nicolas BabaultMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Ke WangChemical Biology Program, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
Dandan WangChemical Biology Program, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.
Yan XiongMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
H Ümit KaniskanMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Minkui LuoChemical Biology Program, Memorial Sloan Kettering Cancer Center, New York, New York 10065, United States.ORCID 0000-0001-7409-7034
Samir ParekhHematology and Medical Oncology, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, The Precision Immunology Institute at Mount Sinai, New York, New York 10029, United States.
Jian JinMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.ORCID 0000-0002-2387-3862

Funding

X-RAY CRYSTALLOGRAPHYP30CA008748 · NCI · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI SELWYN M VICKERS · 1985 to 2026
$347.4M
TRAINING PROGRAM IN CANCER THERAPYT32CA078207 · NCI · MOUNT SINAI SCHOOL OF MEDICINE OF NYU · PI James J Manfredi · 1999 to 2026
$11.6M
Interrogating Protein Methyltransferases with Integrated ApproachesR35GM131858 · NIGMS · SLOAN-KETTERING INST CAN RESEARCH · PI Minkui Luo · 2019 to 2026
$6.3M
Developing Lysine Methyltransferase SETD8 Selective Inhibitors for Treating Multiple MyelomaR01CA290791 · NCI · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI Jian Jin, Samir Parekh · 2025 to 2026
$1.4M
NCI NIH HHS P30 CA008748NCI NIH HHS R01 CA290791NCI NIH HHS T32 CA078207NIGMS NIH HHS R35 GM131858
6 · The paper itself

Abstract

Dysregulated signaling of SET domain-containing protein 8 (SETD8) has been implicated in tumorigenesis, yet most SETD8 inhibitors exhibited limited cellular efficacy. Herein, we developed a potent and selective SETD8 covalent inhibitor, MS2928 (

Identifiers

PMID41693203
PMCPMC12987572

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Registered trials

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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.