Table 2 SR ligands with chemotype different from PB28.

From: A conformational rearrangement of the SARS-CoV-2 host protein sigma-1 is required for antiviral activity: insights from a combined in-silico/in-vitro approach

Compound

AKi nM S1R

BKi nM S2R

CIC50 (μM) SARS-CoV-2

1942

2435

4.24

NOT ACTIVE

2042

311

3.56

NOT ACTIVE

2142

709

4.84

NOT ACTIVE

2242

3987

1.42

NOT ACTIVE

  1. A,BKi values represent the mean of three experiments in duplicate, ± SEM is reported in the cited manuscript; AKi values from radioligand binding assay: [3H]-( +)-Pentazocine on guinea pig brain according to the generally accepted protocol; BKi values from radioligand binding assay: [3H]-DTG on rat liver masking with ( +)-Pentazocine according to the generally accepted protocol; CDetection of viral genomes by RT-qPCR on Vero E6 cells infected with SARS-CoV-2 virus14. Listed values are one experiment that is representative of experiments performed at least three times.
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