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. Author manuscript; available in PMC: 2016 Nov 30.
Published in final edited form as: Nat Chem Biol. 2016 May 30;12(7):559–566. doi: 10.1038/nchembio.2097

Figure 4. Hit compounds show haloperidol-like target profiles.

Figure 4

(a) Library-wide target signatures for known antipsychotics and uncharacterized compound hits as calculated by SEA. Heat map of shared target enrichments for known and uncharacterized groups, as compared to 1,000 randomly-selected size-matched groups from the underlying screening library. Out of 1,873 possible targets, fewer than 58 were significantly enriched for the known or uncharacterized groups. The y-axis shows the 58 enriched targets for the known and uncharacterized groups. 50 random groups are shown for context. Significantly enriched target classes for known and uncharacterized groups were: 5-HT: serotonin receptors, ADA and ADR: alpha and beta adrenergic receptors, CAC: voltage-dependent T-type calcium channels, DRD: dopamine receptors, HDA: histone deacetylases, HRH: histamine receptors, SGM: sigma receptors; for others see Supplementary Table 4 for full list. Enrichment factors (EF) of ≥ 2.0 and q-value ≤ 1e-10 are shown in blue, on a log scale. (b) Binding affinity profiles (as computed npKi values) of 22 uncharacterized hit compounds (rows) at 60 human and rodent CNS receptors in vitro (columns) in addition to haloperidol and bromperidol controls.