TABLE 1

IC50 values for PAT-505 and three reference ATX inhibitors (PF-8380, GLPG1690, and PAT-048) in three different in vitro lysoPLD assays

All IC50 values shown are the geometric mean (nM) x/÷ geometric standard deviation with the n values indicated in parentheses.

LysoPLD AssayIC50 (nM)
PAT-505PF-8380GLPG1690PAT-048
Hep3B (TOOS)2.0 ×/÷ 1.18 (7)7.1 ×/÷ 1.19 (9)180 ×/÷ 1.13 (3)1.1 ×/÷ 1.38 (7)
Human blood (20:4 LPA)9.7 ×/÷ 2.43 (6)280 ×/÷ 1.54 (9)82 ×/÷ 1.26 (3)8.9 ×/÷ 1.60 (5)
Mouse plasma (20:4 LPA)62 ×/÷ 2.22 (7)320 ×/÷ 1.62 (5)360 ×/÷ 1.09 (3)22 ×/÷ 1.55 (4)