Title : Synthesis and pharmacological evaluation of benzamide derivatives as potent and selective sigma-1 protein ligands.

Pub. Date : 2017 Sep 29

PMID : 28756263






2 Functional Relationships(s)
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1 Among them, compounds 7i, w, y with Cl, CN or NO2 groups at the 4-position of the benzamide scaffold showed excellent affinity for S1R (Ki = 1.2-3.6 nM), selectivity for S2R (Ki up to 1400 nM) and high selectivity index (IC50(SY5Y)/Ki(S1R) ratio from 28 000 to 83 000). benzamide transmembrane BAX inhibitor motif containing 4 Homo sapiens
2 Among them, compounds 7i, w, y with Cl, CN or NO2 groups at the 4-position of the benzamide scaffold showed excellent affinity for S1R (Ki = 1.2-3.6 nM), selectivity for S2R (Ki up to 1400 nM) and high selectivity index (IC50(SY5Y)/Ki(S1R) ratio from 28 000 to 83 000). benzamide transmembrane BAX inhibitor motif containing 4 Homo sapiens