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% |
PS compds tested refers to compounds tested in the primary screen.
>50% effect at 3 or 10 μM in either agonist or PAM assay.
conf compds tested refers to number of compounds tested in confirmation assays.
Ag refers to agonist.