TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).In Vitro: TAK-615 specifically binds to membranes expressing the human LPA1 receptor with estimated Kd high affinity (KdHi) of 1.7±0.5?nM and Kd low affinity (KdLo) of 14.5±12.1?nM.
TAK-615 is only able to partially inhibit the LPA response (~?40% at 10?μM with an IC50 of 23±13?nM in β-arrestin assay; 60% at 10?μM, IC50 of 91±30?nM in calcium mobilisation assay) .