ActiTarg Series · 1,040 compounds
ActiTarg-N Nuclear Receptor Ligands
A library of 1,040 analogs selected from a compound pool with cumulative structural features inherent across some 90 known nuclear-receptor ligands.
The analog pool started with “de-fragmented” active molecules. TimTec stock was scanned for molecules with the same fragments, reassembled as new chemical possibilities. Additional computational steps drew in compounds with overall structural similarity to known nuclear-receptor ligands. Further filtering was used to keep structural diversity in the final selection. The design is a focused-diversity library relevant to this target class.
Nuclear receptors are intracellular proteins that regulate gene transcription. They are a superfamily of 48 structurally related transcription factors that can be regulated by small molecules.
Target pool listed on the legacy page includes ER and estrogen-related receptor; AR; glucocorticoid receptor; RAR; THR; VDR; FXR; PPAR α/γ; LXR; CCR5; mineralocorticoid receptor; PR; constitutive androstane receptor; and others.
Compounds are available for cherry-picking and/or as the 1,040-compound collection in 96- or 384-well plates and in vials.
Published screens
No peer-reviewed screens naming ActiTarg-N were located.
ActiTarg is one of TimTec’s targeted series. See the ActiTarg Series for the other letter collections.