COMPOUND LIBRARY

Abstract

The present invention provides a library comprising 110.sup.2 to 110.sup.8 compounds, wherein the compounds have the following structure where a first core block (first CB), a first linker (first L), and a second core block (second CB) are covalently linked: (first CB)-(first L)-(second CB), wherein the library comprises two or more types of first CB, two or more types of first L, and two or more types of second CB, and the library is constituted by one or two or more mixtures comprising 110.sup.2 to 110.sup.5 of the compounds.

Claims

1. A library comprising 110.sup.2 to 110.sup.8 compounds, wherein the compounds have the following structure where a first core block (first CB), a first linker (first L), and a second core block (second CB) are covalently linked:
(first CB)-(first L)-(second CB), wherein the library comprises two or more types of first CB, two or more types of first L, and two or more types of second CB, and the library is constituted by one or two or more mixtures comprising 110.sup.2 to 110.sup.5 of the compounds.

2. The library according to claim 1, wherein the compounds have the following structure where a second linker (second L) and a third core block (third CB) are further covalently linked:
(first CB)-(first L)-(second CB)-(second L)-(third CB), and the library comprises two or more types of second L and two or more types of third CB.

3. The library according to claim 1 or 2, wherein the compounds comprise no oligonucleotide tag.

4. The library according to any one of claims 1 to 3, wherein the first L, the second L, and the third L have a structure independently selected from the group consisting of amide, sulfonamide, acylsulfonamide, amino, ether, thioether, ester, ketone, sulfone, a single bond, ethyne-1,2-diyl (CC), and nitrogen-containing 5-membered heteroarylene.

5. A method for screening for a compound that binds to a target molecule, comprising: (1) providing a library according to any one of claims 1 to 4; (2) bringing each of the one or two or more mixtures constituting the library into contact with the target molecule; and (3) identifying a compound that binds to the target molecule.

6. A method for producing a library, comprising: (a) preparing supporting carriers to which a first building block (first BB) is covalently linked (first BB-supporting carriers), wherein the first BB-supporting carriers are solid-phase carriers comprising na types of first building blocks (first BB.sub.1 to first BB.sub.na) (first BB.sub.1-na-supporting carriers), the first BB.sub.1-na moieties of the first BB.sub.1-na-supporting carriers each have a reactive functional group for forming a bond with a second building block (second BB), and the reactive functional groups contained in the first BB.sub.1-na-supporting carriers are of one type or two or more types; (b) preparing mixtures of supporting carriers having the reactive functional group common among the first BB.sub.1-na-supporting carriers, and reacting each mixture with one type of second building block introduction reagent (second BB introduction reagent) or a mixture of two or more types of second BB introduction reagents to prepare supporting carriers in which the second BB is covalently linked to the first BB (second BB-first BB-supporting carriers), wherein the resulting supporting carriers are supporting carriers comprising nb types of second building blocks (second BB.sub.1 to second BB.sub.nb) (second BB.sub.1-nb-first BB.sub.1-na-supporting carriers), and any of the second BB.sub.1 introduction reagent to the second BB.sub.nb introduction reagent reacts with the respective reactive functional groups of the first BB.sub.1-na-supporting carriers to form first linkers (first L); and (e) cleaving compounds from the solid-phase carriers, wherein na is an integer of 2 or larger, nb is an integer of 2 or larger, and the resulting compound library comprises 100 or more types of compounds as a mixture.

7. The method according to claim 6, wherein (b) comprises preparing mixtures of supporting carriers having the reactive functional group common among the first BB.sub.1-na-supporting carriers, and reacting each mixture with one of nb types of second BB introduction reagents.

8. The method according to claim 6 or 7, wherein the second BB.sub.1-nb-first BB.sub.1-na-supporting carriers each have a reactive functional group capable of forming a linker with a third building block (third BB), and the reactive functional group that is singly contained in each of the first BB.sub.1-na moieties or the second BB.sub.1-nb moieties is of one type or two or more types, the method further comprising (c) preparing mixtures of supporting carriers having the reactive functional group common among the second BB.sub.1-nb-first BB.sub.1-na-supporting carriers, and reacting each mixture with one type of third building block introduction reagent (third BB introduction reagent) or a mixture of two or more types of third BB introduction reagents to prepare supporting carriers in which the third BB is covalently linked to the first BB or the second BB (third BB-second BB-first BB-supporting carriers or second BB-(third BB-)first BB-supporting carriers), wherein the resulting supporting carriers are supporting carriers comprising nc types of third building blocks (third BB.sub.1 to third BB.sub.nc) (third BB.sub.1-nc-second BB.sub.1-nb-first BB.sub.1-na-supporting carriers or second BB.sub.1-nb-(third BB.sub.1-nc-)first BB.sub.1-na-supporting carriers), and any of the third BB.sub.1 introduction reagent to the third BB.sub.nc introduction reagent reacts with the respective reactive functional groups of the second BB.sub.1-nb-first BB.sub.1-na-supporting carriers to form second linkers (second L), wherein nc is an integer of 2 or larger, and the first linkers or the second linkers of the compounds contained in the library are of two or more types.

9. The method according to any one of claims 6 to 8, wherein na is an integer of 2 to 1000, nb is an integer of 2 to 1000, and any of na and nb is an integer of 3 or larger; or na is an integer of 2 to 1000, nb is an integer of 2 to 1000, nc is an integer of 2 to 1000, and any of na, nb and nc is an integer of 3 or larger.

10. The method according to any one of claims 6 to 9, further comprising a derivatization step for the reactive functional group.

11. The method according to any one of claims 6 to 10, further comprising modifying the functional groups contained in the compounds cleaved from the solid-phase carriers in (e).

12. The method according to any one of claims 6 to 11, wherein one or more compounds contained in the library comprise a UV tag.

13. The method according to any one of claims 6 to 12, wherein the compounds contained in the library comprise no oligonucleotide tag.

14. The method according to any one of claims 6 to 13, wherein the first linkers, the second linkers, and the third linkers are formed through reaction independently selected from the group consisting of amidation, sulfonamidation, acylsulfonamidation, amination, etherification, thioetherification, esterification, carbon-nitrogen bond formation reaction, carbon-carbon bond formation reaction, and nitrogen-containing 5-membered heteroarylene formation reaction.

15. The method according to any one of claims 6 to 14, wherein the resulting library comprises 100 or more compounds.

Description

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