{"doi":"10.3390/molecules30092001","title":"A Selective MAP3K1 Inhibitor Facilitates Discovery of NPM1 as a Member of the Network","abstract":"The quinoxaline core is found in several biologically active compounds, with Erdafitinib being the first FDA-approved quinoxaline derivative that targets a kinase and exhibits anti-cancer properties. We previously reported a quinoxaline analog (84) that displayed anti-cancer effects by inhibiting IKKβ, a key kinase in the NFκB pathway. Here, we present the synthesis of a regioisomer (51-106) and its characterization as a selective MAP3K1 inhibitor with improved metabolic stability and oral bioavailability. We used the small molecule MAP3K1 inhibitor in a proteomics study that identified NPM1 as a member of the MAP3K1 network.","journal":"Molecules","year":2025,"id":528184,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":2,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9494,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2025-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":685394,"name":"Sarbjit Singh","orcid":"0000-0001-5719-967X","position":1,"is_corresponding":false},{"id":554730,"name":"Kiran K. Mangalaparthi","orcid":"0000-0002-5791-727X","position":2,"is_corresponding":false},{"id":658275,"name":"Smitha Kizhake","orcid":"0000-0002-4906-5409","position":3,"is_corresponding":false},{"id":1406544,"name":"Lelisse T. Umeta","orcid":null,"position":4,"is_corresponding":false},{"id":771891,"name":"Donn G. Wishka","orcid":"0009-0004-9563-3261","position":5,"is_corresponding":false},{"id":1406545,"name":"Paul G. Grothaus","orcid":null,"position":6,"is_corresponding":false},{"id":60408,"name":"Akhilesh Pandey","orcid":"0000-0001-9943-6127","position":7,"is_corresponding":false},{"id":415310,"name":"Amarnath Natarajan","orcid":"0000-0001-5067-0203","position":8,"is_corresponding":false},{"id":666932,"name":"Lidia Boghean","orcid":"0000-0003-3830-3560","position":0,"is_corresponding":true}],"reference_count":63,"raw_metadata":null,"created_at":"2026-07-19T02:50:48.492873Z","pmid":"40363807","pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}