Synonyms: compound 19 [WO2023018643A1]
Compound class:
Synthetic organic
Comment: The chemical structure for fosizensertib was derived from WHO proposed INN list 132 (Feb 2025), in which it is listed as a receptor-interacting serine/threonine protein kinase 1 (RIPK1) inhibitor. This generated a SMILES match via PubChem to a compound (19) claimed in patent WO2023018643A1 (AbbVie) [1]. This appears to be a phosphate prodrug, that is dephosphorylated in vivo, to the active metabolite compound 2. In the absence of formal structure disclosure (March 2025) we hypothesise that this is likely to be the INN for AbbVie's oral ulcerative colitis lead ABBV-668.
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Bioactivity Comments |
Compound 19 (fosizensertib) inhibits RIPK1 by <10% in vitro, compared to ~70% inhibition by the bioactive metabolite compound 2 [1]. The IC50 for Compound 2 vs. human RIPK1 is 4 nM, in a fluorescent competition displacement assay. |