Table 1.

Ki values for inhibition of various forms of MET and RON kinase domains by SGX523

KinaseSGX523 Ki (╬╝mol/L)
MET-KD (0P)0.0027
MET-KD (3P)0.023
MET-KDTyr1248Leu<10
RON<10

NOTE: MET-KD is purified from baculovirus as an unphosphorylated enzyme, MET-KD(0P), which is more sensitive to inhibition than the autoactivated form phosphorylated at three sites, MET-KD(3P), as described in Materials and Methods.