TABLE 1

TLR7/8 inhibitor potency and selectivity

Values are means ± S.D.

M5049CMPD 2
TLRStimulusCellsEndpointIC50NIC50N
nMnM
TLR7R848HEKNF-κB Luc11.1 ± 9.94626 ± 10.65
TLR8R848HEKNF-κB Luc24.1 ± 9.1663.6 ± 1.065
TLR7TLR7 ligandPBMCsIL-668.3 ± 59.8480 ± 283
TLR8TLR8 ligandPBMCsIL-6620 ± 62848.9 ± 6.24
TLR3Poly I:CPBMCsMCP-1No inhibition2No inhibition4
TLR4LPSPBMCsIL-6No inhibition2No inhibition2
TLR9ODN2006PBMCsMCP-1No inhibition2No inhibition4
TLR7TLR7 ligandWBIL-62.2 ± 2.680.58 ± 0.276
TLR8TLR8 ligandWBIL-6120 ± 3460.81 ± 0.316
  • LPS, lipopolysaccharide; MCP-1, monocyte chemoattract protein-1; NF-κB Luc, NF-κB-luciferase; Poly I:C, polyinosinic:polycytidylic acid; WB, white blood cell.