A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to be degraded via the ubiquitin-proteasome system. The advent of nonpeptidic small-molecule E3 ligase ligands, notably for von Hippel-Lindau (VHL) and cereblon (CRBN), revolutionized the field and ushered in the design of drug-like PROTACs with potent and selective degradation activity. Enabled by the discoveries of high-quality, crystallographically defined ligands for the E3 ligases VHL and CRBN, PROTACs have had a meteoric resurgence in the limelight, a remarkable development that has culminated in the first PROTAC degraders being demonstrated as safe and efficacious in the clinic.
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T18805 | Thalidomide-C2-amido-C2-COOH | Thalidomide-C2-amido-C2-COOH is a compound that includes a CRBN ligand for the E3 ubiquitin ligase, as well as a linker. It is utilized in the development of PROTAC CDK2/9 Degrader-1[1]. |
T18873 | VHL Ligand-Linker Conjugates 17 | VHL Ligand-Linker Conjugates 17 are chemical compounds that consist of a VHL ligand specialized for the E3 ubiquitin ligase, as well as a PROTAC linker. These conjugates are utilized in the synthesis of various PROTACs, including the notable ARD-266. ARD-266 is an exceptionally effective androgen receptor (AR) PROTAC degrader[1]. |
T18661 | (S,R,S)-AHPC-C10-NH2 dihydrochloride | (S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-linker 10) 包含基于 (S,R,S)-AHPC 的VHL 配体和 1 个 linker,是一种合成的 E3 连接酶配体-linker 偶联物,用于合成 BET 的靶向 PROTAC。 |
T18809 | Thalidomide-NH-C6-NH2 TFA | Thalidomide-NH-C6-NH2 TFA is a synthetic conjugate compound that combines a cereblon ligand based on Thalidomide with a linker used in PROTAC technology, functioning as an E3 ligase ligand-linker conjugate[1]. |
T18811 | Thalidomide-PEG2-C2-NH2 hydrochloride | Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate, combines a Thalidomide-based cereblon ligand with a two-unit PEG linker for use in PROTAC technology[1]. |
T17230 | VH032-PEG3-acetylene | VH032-PEG3-acetylene is a synthesized conjugate compound consisting of a VH032-based VHL ligand and a linker, designed for use in PROTAC technology as an E3 ligase ligand-linker conjugate[1]. |
T18670 | (S,R,S)-AHPC-Me-C5-COOH | (S,R,S)-AHPC-Me-C5-COOH is a synthetic E3 ligase ligand-linker conjugate consisting of a VHL ligand and a linker. It finds application in PROTAC DT2216[1]. |
T18672 | (S,R,S)-AHPC-O-Ph-PEG1-NH-Boc | (S,R,S)-AHPC-O-Ph-PEG1-NH-Boc (VH032-O-Ph-PEG1-NH-Boc) is an E3 ligase ligand-linker conjugate, specifically designed for targeting the EED protein in PROTAC applications[1]. |
T18813 | Thalidomide-PEG2-C2-NH2 | Thalidomide-O-amido-PEG3-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology[1]. |
T18673 | (S,R,S)-AHPC-O-Ph-PEG1-NH2 | (S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) serves as an E3 ligase ligand-linker conjugate, integrating a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound is utilized in PROTAC EED degrader-1, a PROTAC that targets EED with a potency (pKD) of 9.02[1]. |
T18660 | (S,R,S)-AHPC-amido-C5-acid | (S,R,S)-AHPC-amido-C5-acid is a chemical compound that contains a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. It can be utilized in the design of XY028-133[1]. |
T18808 | Thalidomide-NH-C4-NH2 TFA | Thalidomide-NH-C4-NH2 TFA (compound 29c) is a conjugate consisting of an E3 ligase ligand-linker, incorporating the Thalidomide-based cereblon ligand and a linker moiety. This compound, Thalidomide-NH-C4-NH2 TFA, is utilized as a component in PROTAC BRD2/BRD4 degrader-1, which is a highly potent and selective degrader targeting BET proteins BRD4 and BRD2[1]. |
T18825 | Thalidomide-O-C6-NH2 | Thalidomide-O-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12F36V and BET[1]. |
T18663 | (S,R,S)-AHPC-C3-NH2 TFA (2361119-88-0 free base) | (S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, suc |
T18665 | (S,R,S)-AHPC-C4-NH2 dihydrochloride | (S,R,S)-AHPC-C4-NH2 dihydrochloride is a chemically derived E3 ligase ligand-linker conjugate, consisting of the (S,R,S)-AHPC VHL ligand and a linker specifically designed for EED-Targeted PROTAC[1]. |
T18815 | Thalidomide-O-amido-C4-NH2 hydrochloride | Thalidomide-O-amido-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that combines the cereblon ligand derived from Thalidomide with a linker. It is commonly employed in the synthesis of PROTACs[1]. |
T18667 | (S,R,S)-AHPC-C5-COOH | (S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases[1]. |
T18810 | Thalidomide-NH-C6-NH2 | Thalidomide-NH-C6-NH2 is a synthetic conjugate compound designed as an E3 ligase ligand-linker. It consists of a Thalidomide-based cereblon ligand linked to a specific linker utilized in PROTAC technology[1]. |
T18822 | Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride | Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride 是一种合成的 E3 连接酶配体- linker 偶联物,包含基于 Thalidomide 的 cereblon 配体和 linker 。 |
T18662 | (S,R,S)-AHPC-C2-PEG4-N3 | (S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate combining the (S,R,S)-AHPC-based VHL ligand with a 4-unit polyethylene glycol (PEG) linker, employed in PROteolysis TAgeting Chimera (PROTAC) technology. This compound facilitates the creation of vRucaparib-TP4, a potent PARP1 degrader demonstrating a half-maximal degrading concentration (DC50) of 82 nM[1]. |