Evidence map›Paper›PMID 36793435›Full record

ArticleACS medicinal chemistry letters2023

Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.

Ahmed Mamai, Anh M Chau, Brian J Wilson, Iain D Watson, Babu B Joseph, Pandiaraju R Subramanian, Monzur M Morshed, Justin A Morin, Michael A Prakesch, Tianbao Lu and 27 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
3.1field-weighted citation impact, top 9% 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

5 citing papers in PubMed, 12 citations in OpenAlex.

  1. Article
  2. Review
  3. Review
  4. Article
  5. Discovery of anJournal of medicinal chemistry · 2023
    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

37 authors at 5 institutions in 3 countries.

Ahmed MamaiDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Anh M ChauDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Brian J WilsonDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Iain D WatsonDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Babu B JosephDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Pandiaraju R SubramanianDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Monzur M MorshedDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Justin A MorinDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Michael A PrakeschDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Tianbao LuJanssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania19477, United States.ORCID https://orcid.org/0000-0001-5896-3916
Pete ConnollyJanssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania19477, United States.
Douglas A KuntzPrincess Margaret Cancer Centre, Toronto, OntarioM5G 2C1, Canada.
Neil C PomroyPrincess Margaret Cancer Centre, Toronto, OntarioM5G 2C1, Canada.
Gennady PodaDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Kong NguyenDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Richard MarcellusDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Graig StrathdeeDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Brigitte TheriaultDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Ratheesh SubramaniamDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Mohammed MohammedDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Ayome AbibiDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Manuel ChanDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Jeffrey WinstonDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Taira KiyotaDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Elijus UndzysDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Ahmed AmanDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.ORCID https://orcid.org/0000-0002-0275-205X
Nigel AustinJanssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania19477, United States.
Marc Du JardinJanssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania19477, United States.
Kathryn PackmanJanssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania19477, United States.
Ulrike PhillipparJanssen Research & Development, Turnhoutseweg 30, B-2340Beerse, Belgium.
Riccardo AttarJanssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania19477, United States.
James EdwardsJanssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania19477, United States.
Jeff O'MearaDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
David E UehlingDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Rima Al-AwarDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.
Gilbert G PrivéPrincess Margaret Cancer Centre, Toronto, OntarioM5G 2C1, Canada.
Methvin B IsaacDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada.ORCID https://orcid.org/0000-0001-6424-5523
Ontario Institute for Cancer Research · CAJanssen (United States) · USPrincess Margaret Cancer Centre · CAJanssen (Belgium) · BEUniversity of Toronto · CA

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

B cell lymphoma 6 (BCL6), a highly regulated transcriptional repressor, is deregulated in several forms of non-Hodgkin lymphoma (NHL), most notably in diffuse large B-cell lymphoma (DLBCL). The activities of BCL6 are dependent on protein-protein interactions with transcriptional co-repressors. To find new therapeutic interventions addressing the needs of patients with DLBCL, we initiated a program to identify BCL6 inhibitors that interfere with co-repressor binding. A virtual screen hit with binding activity in the high micromolar range was optimized by structure-guided methods, resulting in a novel and highly potent inhibitor series. Further optimization resulted in the lead candidate

Identifiers

PMID36793435
PMCPMC9923840
OpenAlexW4315780383

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.