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Ligands for target proteins in PROTAC design bind the protein that a degrader is meant to remove. A proteolysis-targeting chimera (PROTAC) joins such a ligand to an E3 ubiquitin ligase ligand through a linker, so that the ligase ubiquitinates the bound target. Most entries are known inhibitors or receptor ligands modified with an attachment point, such as an aldehyde, amine, carboxylic acid or alkyne group. Dasatinib carbaldehyde and Imatinib carbaldehyde are aldehyde-bearing analogs of two kinase inhibitors. BI-4464 binds protein tyrosine kinase 2 (PTK2), also called focal adhesion kinase (FAK), and SirReal1-O-propargyl carries a propargyl handle on a sirtuin 2 (SIRT2) ligand. Receptor ligands in the list include Estrone-N-O-C1-amido and AP1867-2-(carboxymethoxy), which binds FK506-binding proteins.
Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs.
Synonyms: ERα ligand 1
Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.
Synonyms: PROTAC FKBP12-binding moiety 1
SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) is a synthetic ligand for FKBP (SLF). SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) can be used in the synthesis of PROTACs.
Synonyms: Molibresib carboxylic acid; GSK525762A carboxylic acid; GSK 525762A; PROTAC BRD4-binding moiety 2; IBET762
I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH is a ligand specifically designed for EZH2, functioning as a key component in PROTAC technology by recruiting E3 ligases. This compound demonstrates potential biological activity in targeted protein degradation, particularly in the context of lymphoma research. Its unique structure allows for the exploration of novel therapeutic strategies aimed at modulating EZH2 activity and its downstream effects in cancer biology.
PROTAC Her3-binding moiety 2 is a selective ligand for the human epidermal growth factor receptor 3 (Her3). This compound plays a critical role in the development of PROTAC Her3 Degrader-8, facilitating the targeted degradation of Her3 proteins. It is primarily utilized in research applications focused on cancer biology and therapeutic development targeting Her3-mediated signaling pathways.
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CBP/p300 ligand 10 is a selective ligand for the CBP/p300 proteins, facilitating their targeted degradation. This compound serves as a valuable component for the development of PROTACs, specifically enabling the synthesis of CBP/p300 Degrader-2. Its utility in research applications includes studies focused on cellular signaling pathways and potential therapeutic interventions in diseases associated with dysregulated CBP/p300 activity.
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FLT3/CDKs ligand-1 is a potent ligand designed for the targeted degradation of cyclin-dependent kinase (CDK) and FMS-like tyrosine kinase 3 (FLT3). This compound effectively inhibits FLT3/CDK-related proliferation and survival of leukemia cells, making it a valuable tool for cancer research. FLT3/CDKs ligand-1 facilitates the synthesis of PROTAC FLT3/CDKs degrader-1, enabling innovative approaches in targeted protein degradation studies.
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FAK ligand-2 is a selective ligand for focal adhesion kinase (FAK), serving as a critical component in the development of PROTAC (proteolysis-targeting chimera) strategies. This compound facilitates targeted protein degradation and is instrumental in exploring cellular signaling pathways and cancer biology. Researchers can utilize FAK ligand-2 for studies involving FAK modulation and its implications in therapeutic development.
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BTK ligand 12 is a potent ligand for Bruton's tyrosine kinase (BTK), functioning as a valuable component in the development of PROTACs targeting this protein. It exhibits strong binding affinity, facilitating the effective ubiquitination and degradation of BTK in various cellular contexts. This compound is essential for researchers investigating targeted protein degradation and the modulation of signaling pathways associated with BTK in therapeutic applications.
ALK protein ligand-1 is a specific ligand for anaplastic lymphoma kinase (ALK) that plays a crucial role in targeted protein degradation using PROTAC technology. This compound exhibits potent inhibitory effects on ALK, making it a valuable tool for studying ALK-related signaling pathways and their implications in cancer biology. ALK protein ligand-1 is essential for the synthesis of AP-1, facilitating the exploration of novel therapeutic approaches in oncology research.
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RET Ligand-1 is a ligand specifically designed to interact with the RET proto-oncogene receptor tyrosine kinase. This compound can be utilized in the synthesis of bifunctional molecules, such as PROTAC LDD39, for targeted protein degradation studies. Its ability to modulate RET signaling pathway has implications in cancer research and therapeutic development.
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(Rac)-BMS-1 is a racemic compound that serves as a ligand for target proteins in the development of proteolysis-targeting chimeras (PROTACs). It plays a crucial role in synthesizing D5B PROTAC, facilitating targeted protein degradation. This compound is valuable for researchers investigating protein regulation and therapeutic applications in cancer and other diseases.
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ERK5 ligand-1 is a selective ligand for the ERK5 protein, serving as a pivotal component in the development of PROTAC molecules. This compound is essential for creating targeted protein degradation strategies, exemplified by its application in the design of PROTAC ERK5 degrader-1. ERK5 ligand-1 facilitates the targeted removal of proteins, providing researchers with valuable tools for dissecting cellular pathways and investigating therapeutic targets.
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Aurora kinase ligand-1 is a targeted ligand for Aurora kinase B (AURKB) utilized in PROTAC (Proteolysis Targeting Chimeras) applications. This compound can be conjugated with an E3 ligase ligand and a linker to create the AURKB PROTAC degrader, MS44. Aurora kinase ligand-1 is instrumental in cancer research, facilitating the degradation of AURKB, thereby offering potential therapeutic avenues for malignancies associated with dysregulated kinase activity.
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PBRM1/SMARCA2,4-ligand-1 is a ligand specifically designed for the targeted protein degradation approach via PROTAC technology. It binds selectively to the PBRM1, SMARCA2, and SMARCA4 proteins, serving as a potent SMARCA4 bromodomain inhibitor. This compound is suitable for use in the synthesis of the PROTAC AU-24118, facilitating research into targeted degradation mechanisms and therapeutic strategies in cancer biology.
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PROTAC BRD4 ligand-2 is a specific ligand for the BRD4 protein, designed for use in PROTAC-mediated degradation strategies. This compound facilitates the targeted degradation of BRD4, a key regulator of transcription and associated with various cancers, by recruiting the E3 ubiquitin ligase. It is instrumental in research applications aimed at understanding BRD4's role in oncogenesis and therapeutic development in cancer treatments.
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SMARCA2/4-ligand-5 is a selective ligand targeting the SMARCA2 and SMARCA4 proteins, functioning as a crucial component in the PROTAC SMARCA2/4 degrader-37. This compound demonstrates potent biological activity, achieving an IC50 of ≤0.1 μM, making it suitable for applications in targeted protein degradation studies. Research utilizing SMARCA2/4-ligand-5 contributes to understanding the roles of these chromatin remodelers in various biological processes and cancer biology.
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BRAF ligand-1 acts as a specific ligand for the BRAF protein, playing a crucial role in the regulation of cell signaling pathways associated with cell proliferation, survival, and differentiation. This compound is important for studying the BRAF signaling pathway and its implications in various cancers. Additionally, BRAF ligand-1 can be utilized in the synthesis of CST905, further enhancing its utility in biochemical research and drug discovery efforts targeting mutant BRAF.
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NSC682769 is a ligand specifically designed for the YAP protein, serving as a critical component in the development of PROTACs (proteolysis-targeting chimeras). This compound facilitates the targeted degradation of YAP, making it a valuable tool in research focused on cellular signaling pathways and oncogenesis. NSC682769 can be utilized in the synthesis of PROTAC YAP degrader-1, enabling the exploration of targeted protein degradation strategies in cancer biology.
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TEAD Ligand 1 is a specific ligand for the transcriptional enhancer factor TEAD. It serves as a crucial building block for the synthesis of PROTAC TEAD degrader-1, facilitating targeted degradation of TEAD proteins. This compound is essential for studies involving protein-protein interactions and the modulation of TEAD-related pathways in various biological research applications.
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DENV Ligand 1 is a selective ligand targeting the DENV envelope (E) protein, playing a crucial role in the development of PROTAC (Proteolysis Targeting Chimeras) reagents. It is essential for the synthesis of PROTAC Degrader ZXH-8-004, facilitating the targeted degradation of specific proteins within the cell. This compound has potential applications in studying viral pathogenesis and protein modulation.
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Mpro ligand 2 is a ligand specifically designed for the target protein involved in PROTAC applications. This compound plays a crucial role in the synthesis of PROTAC SARS-CoV-2 Mpro degrader-3, facilitating targeted protein degradation. Its ability to engage with the target protein makes it a valuable tool for research on SARS-CoV-2-related pathways and therapeutic strategies.
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POI ligand-2 is a specific ligand for the GPX4 protein, facilitating targeted protein degradation. This compound is instrumental in the synthesis of PROTACs, including PROTAC GPX4 degrader-5. Its application in protein research enables efficient modulation of GPX4 levels, aiding studies in mechanistic biology and therapeutic interventions targeting oxidative stress pathways.
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CDK8 Ligand 1 is a selective ligand for Cyclin-Dependent Kinase 8 (CDK8), a crucial regulator of transcriptional activity. This compound is instrumental in the development of proteolysis-targeting chimeras (PROTACs), enabling targeted degradation of protein substrates. Researchers can utilize CDK8 Ligand 1 to create customized molecular tools for studying CDK8-mediated signaling pathways and their implications in various diseases.
