Identification of Potent Reverse Indazole Inhibitors for HPK1.


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
11 Mar 2021
Historique:
received: 21 12 2020
accepted: 23 02 2021
entrez: 19 3 2021
pubmed: 20 3 2021
medline: 20 3 2021
Statut: epublish

Résumé

Hematopoietic progenitor kinase (HPK1), a negative regulator of TCR-mediated T-cell activation, has been recognized as a novel antitumor immunotherapy target. Structural optimization of kinase inhibitor

Identifiants

pubmed: 33738073
doi: 10.1021/acsmedchemlett.0c00672
pmc: PMC7957946
doi:

Types de publication

Journal Article

Langues

eng

Pagination

459-466

Informations de copyright

© 2021 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Elsie C Yu (EC)

Discovery Chemistry, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Joey L Methot (JL)

Discovery Chemistry, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Xavier Fradera (X)

Computational and Structural Chemistry, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Charles A Lesburg (CA)

Computational and Structural Chemistry, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Brian M Lacey (BM)

Quantitative Biosciences, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Phieng Siliphaivanh (P)

Discovery Chemistry, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Ping Liu (P)

External Discovery Chemistry, Merck & Co Inc., Rahway, New Jersey, 07065, United States.

Dustin M Smith (DM)

Pharmacokinetics and Drug Metabolism, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Zangwei Xu (Z)

Quantitative Biosciences, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Jennifer A Piesvaux (JA)

Quantitative Biosciences, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Shuhei Kawamura (S)

Discovery Chemistry, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Haiyan Xu (H)

Quantitative Biosciences, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

J Richard Miller (JR)

Quantitative Biosciences, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Mark Bittinger (M)

Oncology Early Discovery, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Alexander Pasternak (A)

Discovery Chemistry, Merck & Co., Inc., Boston, Massachusetts, 02115, United States.

Classifications MeSH