BMS-986278

BMS-986278 : Antagonist of LPAR1

Structure

SERP Rating

Probe BMS-986278 is in the process of SERP review.

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Information

LPAR1

Antagonist

up to 100 nM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): The potential for BMS-986278 to inhibit key hepatobiliary transporters was assessed (BSEP and MDR3 IC50 > 100 μM; MRP4 IC50 = 47 μM). The IC50 values for these key transporters were well above the projected maximum clinical hepatocyte and hepatic portal vein concentrations for BMS-986278 (6.6 and 0.66 μM, respectively). The inhibitory activity of BMS-986278 at other transporters implicated in important drug–drug-interactions (e.g., the organic anion transporters OATP1B1 and OATP1B3) were also significantly reduced.

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SERP ratings and comments

No SERP comments found for BMS-986278