compound introduction
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 ( K d high affinity of 1.7 nM and K d 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 K d 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 IC 50 of 23±13 nM in β-arrestin assay; 60% at 10 µM, IC 50 of 91±30 nM in calcium mobilisation assay). MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:LPA1 Receptor 1.7-14.5 nM (Kd)
