Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T46360 | ||||
Target Name | Opioid receptor sigma 1 (OPRS1) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Dextromethorphan | Drug Info | IC50 = 2500 nM | [2] | |
E-5842 | Drug Info | IC50 > 100000 nM | [4] | ||
OPC-14523 | Drug Info | IC50 = 2.3 nM | [3] | ||
1,3-ditolylguanidine | Drug Info | Ki = 60 nM | [1] | ||
References | |||||
REF 1 | Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity bindi... J Med Chem. 1994 Jun 10;37(12):1737-9. | ||||
REF 2 | N-methyl-D-aspartate receptor (NMDA) antagonists as potential pain therapeutics. Curr Top Med Chem. 2006;6(8):749-70. | ||||
REF 3 | 5-HT1 receptor augmentation strategies as enhanced efficacy: therapeutics for psychiatric disorders. Curr Top Med Chem. 2008;8(12):1008-23. | ||||
REF 4 | Recent advances in the research of HIV-1 RNase H inhibitors. Mini Rev Med Chem. 2008 Oct;8(12):1243-51. | ||||
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