molecules of the month

“compound 7f”

oral toll-like receptors 7/8/9 antagonist

oral efficacy in autoimmune disease models

from cell-based screen and opt.

ACS Med. Chem. Lett., Jul. 29, 2020

Bristol-Myers Squibb, Princeton, NJ

Structure of compound 7f
1 min read

“compound 7f” is an antagonist of the endosomal TLRs 7/8/9, which induce inflammation in response to internalized single-stranded RNA or hypomethylated double-stranded DNA. Potency and selectivity within endosomal TLR’s (3, 7, 8, 9) and against cell-surface TLR’s (1, 2, 4, 5, 6) has been difficult to achieve. Compound 7f has single-digit nanomolar activity against TLRs 7 and 8 in human whole blood, and submicromolar activity against TLR9. Its oral bioavailability in rodents makes it a useful tool compound for studying TLR antagonism in different disease models.

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