Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T48703 | ||||
Target Name | Toll-like receptor 8 (TLR8) | ||||
Type of Target |
Clinical trial |
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Drug Potency against Target | CPG 52364 | Drug Info | IC50 = 35 nM | ||
Resiquimod | Drug Info | EC50 = 1 nM | [1] | ||
Action against Disease Model | CPG 52364 | Drug Info | In vitro experiments with DNA, RNA or SLE patient immune complexes stimulated h uMan cells that express h uMan TLR7, TLR8, and/or TLR9 and in vivo experiments with TLR agonist-treated mice have demonstrated that CPG 52364 is a potent and specific inhibitor of murine TLR7 and TLR9 and h uMan TLR7, TLR8, and TLR9. Furthermore, CPG 52364 shows activity in the spontaneous lupus murine model, MRL lpr/lpr mice, as measured by reduction in titers of anti-double-stranded DNA antibody, a common clinical correlate of SLE. CPG 52364 is well tolerated in preclinical animal testing. | ||
References | |||||
REF 1 | Primary leukocyte screens for innate immune agonists. J Biomol Screen. 2009 Jul;14(6):723-30. | ||||
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