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In pre-clinical studies, Eli Lilly tested four lead compounds for efficacy as s...
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In pre-clinical studies, Eli Lilly tested four lead compounds for efficacy as selective serotonin reuptake inhibitors, using both in vitro and in vivo assays in rodents.
Initial studies investigated in vitro efficacy and selectivity.
Table 1: Assessment of in vitro efficacy of lead compounds in rodents
Inhibition of 5-HT uptake was assessed using synaptosomal preparations of rat brain, and affinity of binding to α1-adrenoceptors was assessed using membrane preparations of rat cerebral cortex.
Lead Compound | MW (g/mol) | Inhibition of 5-HT uptake IC50 (nM) | Binding toα1 adrenoceptor Ki (nM) |
EL-01 | 324 | 1 | 20 |
EL-02 | 309 | 8 | 150 |
EL-03 | 306 | 2 | 100 |
EL-04 | 280 | 4 | 3500 |
IC50 = half maximal inhibitory concentrationKi = measure of affinity
Based upon the data shown in Table 1 above and considering potential off-target actions, the compound MOST LIKELY to progress to the lead optimization phase of the drug discovery process is: