Skip to main content
. 2017 Nov 26;57(12):2976–2985. doi: 10.1021/acs.jcim.7b00338

Table 5. Summary of mGlu7 PAM VS and Resulting Hits.

method PSa compds tested PS activeb PS hit rate conf compds testedc pEC50 > 4.52 ag or PAMd active in autofluorescence no. of confirmed actives final confirmed hit rate
single target approach: fingerprint analogues of only mGlu7 actives 202 27 13% 25 17 12 5 2.5%
multitarget approach: select molecules based on likelihood to be mGlu7 active from PCM 394 42 11% 41 18 1 17 4.3%
a

PS compds tested refers to compounds tested in the primary screen.

b

>50% effect at 3 or 10 μM in either agonist or PAM assay.

c

conf compds tested refers to number of compounds tested in confirmation assays.

d

Ag refers to agonist.