POST-SCREENING LABELING OF ON-BEAD COMPOUNDS

摘要

The present invention relates to new on bead chemistry to produce compound libraries used in improved screening methods, allowing the direct solution confirmation of on-bead screening hits without compound decoding and resynthesis. More specifically, the invention relates to on-bead compounds having the formula B - L - C - S, wherein - represents a bond or any stable covalent spacer, B is a solid support to which a plurality of L-C-S molecules are covalently attached, L is a cleavable linker for covalently linking C to the solid support, C is a covalent linking core comprising at least one protected labeling functional group for covalently linking of a label or a detection molecule, S is a spacer comprising at least one protected or unprotected functional group for on-bead compound derivatization, and wherein L and C are selected so that (i) the linker L and the protected labeling functional group are not affected by side chain deprotection during on-bead compound derivatization, (ii) the linker L and any synthetic molecule attached to S are not affected by deprotection of labeling functional group and labeling reaction step, (iii) covalent linkage of the label or the detection molecule or any synthetic molecule attached to S are not affected by cleavage of the linker L.