{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["13(4)"],"submitter":["Li X"],"pubmed_abstract":["ERK1/2 kinase is a key downstream node of the RAS-RAF-MEK-ERK signaling pathway. A highly potent and selective ERK1/2 inhibitor is a promising option for cancer treatment that will provide a potential solution for overcoming drug resistance. Herein we designed and synthesized a novel scaffold featuring a pyrrole-fused urea template. The lead compound, SHR2415, was shown to be a highly potent ERK1/2 inhibitor that exhibited high cell potency based on the Colo205 assay. In addition, SHR2415 displayed favorable PK profiles across species as well as robust <i>in vivo</i> efficacy in a mouse Colo205 xenograft model."],"journal":["ACS medicinal chemistry letters"],"pagination":["701-706"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9014502"],"repository":["biostudies-literature"],"pubmed_title":["Discovery of SHR2415, a Novel Pyrrole-Fused Urea Scaffold ERK1/2 Inhibitor."],"pmcid":["PMC9014502"],"pubmed_authors":["He F","Bai C","Zhang L","Dong P","Yang F","Cai G","Li X","Zhang T","Feng J","Tao W","Dong H","Chen Y","Mao Y"],"additional_accession":[]},"is_claimable":false,"name":"Discovery of SHR2415, a Novel Pyrrole-Fused Urea Scaffold ERK1/2 Inhibitor.","description":"ERK1/2 kinase is a key downstream node of the RAS-RAF-MEK-ERK signaling pathway. A highly potent and selective ERK1/2 inhibitor is a promising option for cancer treatment that will provide a potential solution for overcoming drug resistance. Herein we designed and synthesized a novel scaffold featuring a pyrrole-fused urea template. The lead compound, SHR2415, was shown to be a highly potent ERK1/2 inhibitor that exhibited high cell potency based on the Colo205 assay. In addition, SHR2415 displayed favorable PK profiles across species as well as robust <i>in vivo</i> efficacy in a mouse Colo205 xenograft model.","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Apr","modification":"2025-04-20T02:23:22.371Z","creation":"2025-04-20T02:23:22.371Z"},"accession":"S-EPMC9014502","cross_references":{"pubmed":["35450372"],"doi":["10.1021/acsmedchemlett.2c00029"]}}