ArticleACS medicinal chemistry letters2016
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Abstract read
In one paragraph
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers, 1 of them a synthesis that pooled it.
0numbers the graph read from it
0cells of the map it votes in
40citing papers in PubMed, 1 pooled it
–field-weighted citation impact
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.
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.
Who cites it
40 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Systematic literature review reveals suboptimal use of chemical probes in cell-based biomedical research.Nature communications · 2023Pooled it
- Super-enhancer-driven LncRNA MIR205HG promotes esophageal squamous cell carcinoma progression via glycolysis reprogramming.Journal of translational medicine · 2026Article
- Bromodomain-Driven Regulation of Stem Cells: A Potential Target for Cancer Therapeutic Intervention.Stem cell reviews and reports · 2026Review
- Chromatin Regulatory Targets for Anticancer Therapeutics.Chemical reviews · 2025Review
- Discovery of 5-imidazole-3-methylbenz[d]isoxazole derivatives as potent and selective CBP/p300 bromodomain inhibitors for the treatment of acute myeloid leukemia.Acta pharmacologica Sinica · 2025Article
- Review
- Targeting lysine acetylation readers and writers.Nature reviews. Drug discovery · 2025Review
- A conserved transcription factor regulatory program promotes tendon fate.Developmental cell · 2024Article
- Ligand-enabled Ni-catalysed dicarbofunctionalisation of alkenes with diverse native functional groups.Nature communications · 2024Article
- Targeting CBP revers chemoresistance to 5-FU of CDX2/REG4 double-positive gastric cancer.Clinical and translational medicine · 2024Article
- Site Identification and Next Choice Protocol for Hit-to-Lead Optimization.Journal of chemical information and modeling · 2024Article
- Target-based drug discovery: Applications of fluorescence techniques in high throughput and fragment-based screening.Heliyon · 2024Review
- Discovery of an EP300 Inhibitor using Structure-based Virtual Screening and Bioactivity Evaluation.Current pharmaceutical design · 2024Article
- Regioselective alkylation of a versatile indazole: Electrophile scope and mechanistic insights from density functional theory calculations.Beilstein journal of organic chemistry · 2024Article
- Marine natural compounds as potential CBP bromodomain inhibitors for treating cancer: an in-silico approach using molecular docking, ADMET, molecular dynamics simulations and MM-PBSA binding free energy calculations.In silico pharmacology · 2024Article
- Bromodomain inhibitors and therapeutic applications.Current opinion in chemical biology · 2023Review
- EP300 facilitates human trophoblast stem cell differentiation.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Targeting bromodomain-containing proteins: research advances of drug discovery.Molecular biomedicine · 2023Review
- Advancing Targeted Protein Degradation via Multiomics Profiling and Artificial Intelligence.Journal of the American Chemical Society · 2023Review
- Effective prediction of short hydrogen bonds in proteins via machine learning method.Scientific reports · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
44 authors.
Alexander M TaylorConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Alexandre CôtéConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Michael C HewittConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Richard PastorGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Yves LeblancConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Christopher G NasveschukConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
F Anthony RomeroGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Terry D CrawfordGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Nico CantoneConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Hariharan JayaramConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Jeremy SetserConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Jeremy MurrayGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Maureen H BeresiniGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Gladys de Leon BoenigGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Zhongguo ChenWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Andrew R ConeryConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Richard T CummingsConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Leslie A DakinConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
E Megan FlynnGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Oscar W HuangGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Susan KaufmanGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Patricia J KellerConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
James R KieferGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Tommy LaiWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Yingjie LiWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Jiangpeng LiaoWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Wenfeng LiuWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Henry LuWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Eneida PardoConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Vickie TsuiGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Jian WangWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Yongyun WangWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Zhaowu XuWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Fen YanWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Dong YuWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Laura ZawadzkeConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Xiaoqin ZhuWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Xiaoyu ZhuWuxi AppTec Co., Ltd. , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, People's Republic of China.
Robert J SimsConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Andrea G CochranGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Steve BellonConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
James E AudiaConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Steven MagnusonGenentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.
Brian K AlbrechtConstellation Pharmaceuticals , 215 First Street, Suite 200, Cambridge, Massachusetts 02142, United States.
Funding
No grant is acknowledged in the PubMed record.
Abstract
CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators involved in numerous cellular pathways relevant to oncology. As part of our effort to explore the potential therapeutic implications of selectively targeting bromodomains, we set out to identify a CBP/EP300 bromodomain inhibitor that was potent both in vitro and in cellular target engagement assays and was selective over the other members of the bromodomain family. Reported here is a series of cell-potent and selective probes of the CBP/EP300 bromodomains, derived from the fragment screening hit 4-methyl-1,3,4,5-tetrahydro-2H-benzo[b][1,4]diazepin-2-one.
Indexed as
benzodiazepinoneBromodomainCBPCREBBPEP300
Identifiers
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.