Target Validation Information
TTD ID T63414
Target Name P2X purinoceptor 7 (P2RX7)
Type of Target
Clinical trial
Drug Potency against Target Drug Info IC50 = 10 nM [1]
A-740003 Drug Info IC50 = 18 nM [1]
KN-62 Drug Info IC50 = 110 nM [2]
STYLISSADINE A Drug Info IC50 = 700 nM [1]
STYLISSADINE B Drug Info IC50 = 1800 nM [1]
Action against Disease Model AZD9056 Drug Info The P2X7 receptor antagonist AZD9056 has been evaluated in preclinical models of RA with promising results (the results were classified as unpublished in this report)
References
REF 1 Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening. Bioorg Med Chem. 2009 Jul 15;17(14):4861-5.
REF 2 Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6053-8.

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