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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