BMS-986120 is a first-in-class oral, reversible protease-activated receptor 4 (PAR4) antagonist with IC50s of 9.5 nM in human blood and 2.1 nM in monkey blood, exhibiting potent and selective antiplatelet effects[1][2].

PAR4 (human):9.5 nM, PAR4 (monkey):2.1 nM

BMS-986120 has high binding affinity to PAR4 expressed on HEK293 cells. And it inhibition of PAR4-induced calcium mobilization with an IC50 of 0.56 nM[3].

BMS, administered at dosages of 0.2, 0.5, and 1 mg/kg, decreases tail withdrawal (TW) by 35±5, 49±4, and 83±4%, respectively. In monkeys, a 1 mg/kg dose of BMS shows no inhibition of platelet aggregation (PA) triggered by PAR1-AP, ADP, and collagen, indicating selectivity. The maximum increases observed in kaolin bleeding time (KBT) and mepacrine bleeding time (MBT) are limited to 2.2-fold and 1.8-fold, respectively[1].