Fused tetrahydroquinolines (THQ): potential PAINS compounds in a recent HTS for moesin-CD44 pathway inhibitors

Joel K. Annor-Gyamfi, Felix Nwogbo, Kun Qian, Yuhong Du, Kenneth H. Pearce Jr, Opher Gileadi, Haian Fu, Stephen V. Frye and Alison D. Axtman https://doi.org/10.5281/zenodo.4685122 Alzheimer’s disease (AD) is the most common cause of dementia worldwide but very few therapeutic options exist despite multiple high-profile but failed clinical trials. And as the population of the Read More …

The Preparation of Allosteric SYK Inhibitor X1 and Investigation of a Covalent Inhibition Mechanism

Frances M. Potjewyd and Vittorio Katis http://doi.org/10.5281/zenodo.4670214 Spleen Tyrosine Kinase (SYK) has a reported role in AD pathology and was identified as a target for the TREAT-AD (Target Enablement to Accelerate Therapy Development for Alzheimer’s Disease) program.1–3 We are focusing drug discovery efforts on the inhibition of SYK and more specifically, inhibition of the interaction Read More …

Preparation of the Soluble Epoxide Inhibitor SWE101 and the DOCK1 inhibitor TBOPP

Preparation of the Soluble Epoxide Inhibitor SWE101 and the DOCK1 inhibitor TBOPP David A. Rogers and Kevin J. Frankowski https://doi.org/10.5281/zenodo.4637834 The National Institute on Aging has made a significant commitment to improving the treatment of Alzheimer’s disease through the funding of the TREAT-AD network (Target Enablement to Accelerate Therapy Development for AD, https://treatad.org/). One of Read More …