Potency assay (off target):
No significant activity was detected against 25 protein methyltransferases or DNMT in SPA, with LLY-507 100-fold selective for SMYD2>SMYD3, KMT5B and KMT5C.
Probe Selectivity in Vitro:
Profiled against 454 kinases in the DiscoveRx Kinome scan assay, as well as 36 GPCRs, 14 nuclear hormone receptors and 3 P450 enzymes using Eurofins-CEREP. LLY-507 inhibited 98% of ADRA1A activity at 10 uM.