Table 1 Summary table of PIPE-791 in vitro radioligand binding selectivity profile in Ca+2 mobilization.

From: Discovery of a brain penetrant small molecule antagonist targeting LPA1 receptors to reduce neuroinflammation and promote remyelination in multiple sclerosis

Properties

In vitro profile

Radioligand binding Ki (nM)

0.752 (IC50: 2.63)

Functional LPA1 Ca+2 mobilization (nM, 30 m)

91.8

Functional LPA1 Ca+2 mobilization (nM, 24 h)

9.9

Fold selectivity over LPA2a

35.4Ă—

Fold selectivity over LPA3

35Ă—

  1. aSelectivity assessed using a 3 h incubation of PIPE-791.
Back to article page