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AZD9056 has been evaluated in preclinical models of RA with promising results (the results were classified as unpublished in this report) | ||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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