Pyrazolopyrimidine scaffolds are one of the most important heterocyclic compounds in drug discovery. This scaffold has various biological activities, among which anticancer is an important one.
SGR-1505 is an investigational mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) inhibitor developed by Schrödinger. MALT1 is a key mediator of the NF-κB signaling pathway and the main driver of a subset of B-cell lymphomas. Over eight billion compound designs were assessed using Schrödinger’s in-house computational MPO chemistry suite, of which only 129 were synthesized. SGR-1505 demonstrated preclinical single-agent and combination activity in B cell malignancies and showed the ability to resensitize drug-resistant tumors to BTK and BCL-2 inhibitors. The compound has completed Ph. I studies in healthy volunteers and has progressed into a Ph. I trial in patients with mature B cell malignancies. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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