Discovery of Pyrazolopyrazines as Selective, Potent, and Mutant-Active MET Inhibitors with Intracranial Efficacy.

doi:10.1021/acs.jmedchem.4c01232

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Community

Back to search

Article

Discovery of Pyrazolopyrazines as Selective, Potent, and Mutant-Active MET Inhibitors with Intracranial Efficacy.

Journal of medicinal chemistry - 22 Aug 2024

Bumpers Quinn A, Pipal Robert W, Benz-Weeden Anna M, Brewster James T, Cook Adam, Crooks Amy L, Cruz Cole, Dwulet Natalie C, Gaudino John J, Golec Daniel, Harrison Jacqueline A, Hartley Dylan P, Hassanien Sherif H, Hicken Erik J, Kahn Dean, Laird Ellen R, Lemieux Christine, Lewandowski Nicholas, McCown Joseph, McDonald Matthew G, McNulty Oren, Mou Tung-Chung, Nguyen Phong, Oko Lauren, Opie Lisa Pieti, Otten Jennifer, Peck Spencer C, Polites Viktor C, Randall Samuel D, Rosen Rachel Z, Savechenkov Pavel, Simpson Helen, Singh Anurag, Sparks Drew, Wickersham Kyle, Wollenberg Lance, Wong Christina E, Wong Jim, Wu Wen-I, Elsayed Mohamed S A, Hinklin Ronald J, Tang Tony P

Abstract excerpt

Mesenchymal-epithelial transition factor (MET) is a receptor tyrosine kinase that serves a critical function in numerous developmental, morphogenic, and proliferative signaling pathways. If dysregulated, MET has been shown to be involved in the development and survival of several cancers, including non-small cell lung cancer (NSCLC), renal cancer, and other epithelial tumors. Currently, the clinical efficacy of...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Antineoplastic Agents

Share to Brain Neoplasms

Share to Drug Discovery

Share to Protein Kinase Inhibitors

Share to Proto-Oncogene Proteins c-met

Share to Pyrazines

Share to Pyrazoles

Share to Structure-Activity Relationship

Source

Open in PubMed

Identifiers

PMID: 39088797
DOI: 10.1021/acs.jmedchem.4c01232

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Discovery of Pyrazolopyrazines as Selective, Potent, and Mutant-Active MET Inhibitors with Intracranial Efficacy.PMID 39088797Read ↗

The Preclinical Pharmacology of Tepotinib-A Highly Selective MET Inhibitor with Activity in Tumors Harboring MET Alterations.Semantic proximity Read ↗

Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).Semantic proximity Read ↗

Discovery of Small Molecule c-Met Inhibitors: Evolution and Profiles of Clinical CandidatesSemantic proximity Read ↗

Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.Semantic proximity Read ↗

Targeting MET: Discovery of Small Molecule Inhibitors as Non-Small Cell Lung Cancer Therapy.Semantic proximity Read ↗

Structure-Based Design of Novel Class II c-Met Inhibitors: 1. Identification of Pyrazolone-Based DerivativesSemantic proximity Read ↗

TPX-0131, a Potent CNS-penetrant, Next-generation Inhibitor of Wild-type ALK and ALK-resistant Mutations.Semantic proximity Read ↗

Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 InhibitorSemantic proximity Read ↗

Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration.Semantic proximity Read ↗

The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer.Semantic proximity Read ↗

Discovery of a Hydroxylamine-Based Brain-Penetrant EGFR Inhibitor for Metastatic Non-Small-Cell Lung Cancer.Semantic proximity Read ↗

The novel ATP-competitive inhibitor of the MET hepatocyte growth factor receptor EMD1214063 displays inhibitory activity against selected MET-mutated variants.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.