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Poster Presentation

Title: Identification of covalent JNK inhibitor

Presenter: Jun Chiba

Date&Time: April 15, Tuesday: 10:00am – 2:00pm, 3:35 – 4:35pm April 16, Wednesday: 9:35 – 10:30am

Poster Number: A02

Abstract:
Covalent drugs like EGFR and BTK inhibitors have gained attention. We focused on c-Jun N-terminal kinase (JNK) and modified our reported JNK inhibitor. The compounds showed time-dependent JNK3 inhibition in presence of dithiothreitol, suggesting covalent binding. We evaluated this through Protein-MS, digested peptide analysis, and X-ray crystallography. This presentation will highlight our capabilities in covalent drug discovery.

Axcelead DDP’s Solutions:
Axcelead provides technologies at every stage of covalent drug discovery, including ligand design, screening, mechanistic understanding, and target protein identification.

Axcelead’s Covalent Drug Discovery Platform integrates specialized capabilities:

•  Screening – Enzyme and cell-based assays, compound reactivity and time-dependency analysis, crystal structure analysis, and whole protein MS assays.
•  Compound Library – A cysteine-focused covalent library (2,000 compounds), and an HTS library with 500,000 pooled and 200,000 single compounds.
•  In Silico Technology – Target protein analysis (LigMap), covalent docking, and fragment-based drug design (FBDD) using MMPBSA and AutoDesign.
•  Target Deconvolution – Chemical proteomics, binding protein and site identification, photo-affinity labeling, and fingerprinting for pathway prediction.