MS98 is a highly effective and specific PROTAC AKT degrader compound that effectively targets and depletes total AKT (T-AKT) within cells, exhibiting a DC 50 value of 78 nM. This compound readily binds to AKT1, AKT2, and AKT3 with respective dissociation constants (Kd s) of 4 nM, 140 nM, and 8.1 nM.
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist. With IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects[1][2].
BMS-986163 is a negative allosteric modulator of GluN2B and the prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
BMS-986169 is a GluN2B Receptor Negative Allosteric Modulator. BMS-986169 showed a high binding affinity for the GluN2B subunit allosteric modulatory site (Ki: 4.03-6.3 nM) and selectively inhibited GluN2B receptor function in Xenopus oocytes expressing h
BMS-986118 is a full agonist of GPR40, is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial a
BMS-986251 is a potent and specific RORγt inverse agonist that exerts its action via oral administration. It shows an EC 50 of 12 nM for RORγt GAL4. In human whole blood assay, BMS-986251 effectively inhibits IL-17 with an EC 50 of 24 nM. Furthermore, BMS-986251 exhibits strong therapeutic effects in mouse acanthosis and Imiquimod-induced models, which are commonly used preclinical models for psoriasis.
BMS-986121, a positive allosteric modulator (PAM) of the μ opioid receptor. This compound is based on a novel chemical scaffold, introducing a new chemotype for μ receptor PAMs.