metallo βlactamase ligand 1

Metallo β-lactamase ligand 1 is an inhibitor of class B β-lactamase exhibiting antibacterial activities.

SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.

5HT6-ligand-1 is an orally active ligand of 5-HT6 receptor (Ki = 1.43 nM).

Sigma-LIGAND-1 is a selective Sigma Receptor ligand with IC50 values of 16 nM and 19 nM at the DTG site and the PPP site, respectively, and a Ki of 4000 nM at the dopamine D2 receptor.

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50 values of 0.04 μM for ERRα and 2.8 μM for ERRγ.

SMARCA-BD ligand 1 for Protac dihydrochloride binds to the BAF ATPase subunit SMARCA2 and is used for degrading SMARCA2 based on PROTAC.

PROTAC PTK6 ligand-1 serves as an intermediate in the synthesis of BTK kinase inhibitors [1] and is utilized in the preparation of ARD-61 [2].

HDAC ligand-1 is a synthetic precursor utilized in the production of PROTAC-based HDAC degraders [1].

SMARCA-BD Ligand 1 Hydrochloride, used in PROTAC technology, targets and binds to the BAF ATPase subunits SMARCA2, facilitating its degradation.

RBP4 ligand-1 is a non-retinoid ligand for retinol-binding protein 4 (RBP4). It exhibits hRBP4SPA IC50 and RBP4-TTR FRET IC50 values of 0.23±0.11 μM and 0.13±0.12 μM, respectively, in radioligand binding and FRET assays. The measured concentration was 0.12 μM.

GMB-475, also known as PROTAC BCR-ABL1 ligand 1, allosterically targets and binds to the BCR-ABL1 protein. It effectively recruits the E3 ligase Von Hippel-Lindau, leading to the ubiquitination and subsequent degradation of BCR-ABL1 [1].

cIAP1 Ligand-Linker Conjugates 1 is composed of an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 1, is particularly useful in the development of SNIPERs[1].

AhR Ligand-Linker Conjugates 1, also known as E3 Ligase Ligand-Linker Conjugates 57, is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a SNIPER linker. It is specifically designed to be used in the development of SNIPER[1].

5-HT6 5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors, exhibiting K i values of 2 nM and 11 nM for the respective receptors, holding promise for research in neurological and psychiatric disorders [1].

β-Lactamase-IN-1 (4-(1,3-dihydroxypropan-2-yl)-6-methoxypyrido[2,3-b]pyrazin-3-one) is a β-Lactamase inhibitor and targets the infection of Neisseria gonorrhoeae.

GID4 Ligand 1 is a cell-permeable, highly selective GID4 binder with an IC50 value of 5.4 μM and a Kd value of 5.6 μM. GID4 Ligand 1 is capable of binding GID4 in cells with an EC50 value of 558 nM. GID4 Ligand 1 is capable of being used in the synthesis of PROTACs.

STING ligand-1 is a lead STING ligand with an IC50 of 68 nM for HAQ STING.

PCSK9 ligand 1 is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9(Ki of 107 nM).

CXCL12 ligand 1 is the initial ligand of the sY12-binding pocket on chemokine CXCL12.

M1 ligand 1 (compound 3b-b) is a N-desmethyl analog of the arecoline derivative, acting as a muscarinic acetylcholine receptor M1 ligand and usable as a PET (positron emission tomography) radiotracer [1].

Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamase (MBL) inhibitor with IC50 values of 0.1 μM for VIM-1, 1.3 μM for NDM-1, and 5.0 μM for IMP-7, respectively [1].

TSPO ligand-1 has affinity for peripheral and central benzodiazepine receptors.TSPO ligand-1 is an AUTAC4-binding protein in the transmembrane domain of the outer mitochondrial membrane, which induces mitochondrial autophagy and promotes intracellular mitochondrial regeneration.TSPO ligand-1 is involved in intracellular cholesterol transport, and can be used as a biomarker for brain injury and neurodegeneration. TSPO ligand-1 is involved in intracellular cholesterol transport and can be used as a biomarker for brain damage and neurodegeneration.

PROTAC Bcl-xL ligand-1 serves as a ligand targeting Bcl-xL, essential in synthesizing PROTACs [1].

CD22 Ligand-1 (Compound 12) is a potent, selective ligand for CD22, exhibiting dissociation constants (K_D) of 0.335 µM for human CD22 (hCD22) and 30.7 µM for myelin-associated glycoprotein (MAG), indicating specificity towards hCD22. This ligand holds potential for B-cell related disease research [1].

5-HT7 receptor ligand 1 (Compound 5c) is a potent 5-HT7 receptor ligand with a K i value of 8 nM, exhibiting non-hepatotoxic properties and moderate potential for drug-drug interactions with CYP3A4 or CYP2D6 substrates [1].

Metallo-β-lactamase-IN-5 (compound 5c) is a potent inhibitor of metallo-β-lactamases (MBLs), demonstrating inhibitory activity against MBLs NDM-1 and VIM-1. It effectively inhibits HUVECs with an IC50 value of 45 μg mL. Additionally, when combined with Imipenem, Metallo-β-lactamase-IN-5 exhibits synergistic antimicrobial activity [1].

FAP Ligand 1 (FL), a high-affinity small molecule targeting fibroblast activation protein (FAP), facilitates the delivery of conjugated therapeutics to FAP-expressing fibroblasts and enables radiographic imaging of select tumors [1].

FAK ligand-Linker Conjugate 1 is a chemical compound designed to facilitate PROTAC-mediated protein degradation. This compound consists of a ligand specifically targeting FAK and a PROTAC linker module, which acts as a recruitment agent for E3 ligases including VHL, CRBN, MDM2, and IAP[1].

D3R Ligand 1 (compound 23b) is a potent, selective antagonist of the dopamine D3 receptor (Ki=66 nM), incorporating a THPB template. It inhibits both G-protein- and β-arrestin-mediated signaling pathways [1].

Metallo-β-lactamase-IN-4 (compound 40) is a potent inhibitor of metallo-β-lactamases (MBL) with IC50 values of 0.5 μM for VIM-1, 2.1 μM for NDM-1, and 3.3 μM for IMP-7, respectively [1].

Metallo-β-lactamase-IN-8 (compound 17) is a potent, reversible, and competitive broad-spectrum metallo-β-lactamases (MβLs) inhibitor with antibacterial activity, exhibiting IC50 values of 1.3 μM against L1, 5.7 μM against ImiS, 9.8 μM against IMP-1, and 9.9 μM against VIM-2 [1].

ASGPR ligand-1 is a compound that targets the asialoglycoprotein receptor (ASGPR) and is utilized in various disease research contexts [1].

PROTAC BCR-ABL1 ligand 1 is the ligand of PROTAC .

Metallo-β-lactamase-IN-7 is a potent inhibitor of VIM-type metallo-β-lactamase with IC50 values of 0.019 μM, 13.64 μM, and 0.38 μM for VIM-2, VIM-1, and VIM-5, respectively. Metallo-β-lactamase-IN-7 also enhances the antibacterial activity of Meropenem against Gram-negative bacterial strains [1].

PROTAC IRAK4 ligand-1 is a synthetic ligand targeting interleukin-1 receptor-associated kinase 4 (IRAK4).

Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with activity at DTG (IC50: 16 nM) and PPP (IC50: 19 nM) sites, and can also act on the dopamine D2 receptor (Ki: 4000 nM).

ERRα Ligand-Linker Conjugates 1 refers to a chemical compound that consists of a ligand targeting estrogen-related receptor alpha (ERRα), and a PROTAC linker that facilitates the recruitment of E3 ligases MDM2. It finds utility in the synthesis of a range of PROTACs, including one known as PROTAC ERRalpha Degrader-1. With its capability to induce degradation of ERRα, PROTAC ERRalpha Degrader-1 functions as an ERRα degrader[1].

Metallo-β-lactamase-IN-9 (Compound 23) is a broad-spectrum inhibitor of metallo-beta-lactamases (MBL), with inhibition constants (IC50) of 35 nM for NDM-1, 269 nM for VIM-1, and 369 nM for IMP-1 [1].

PROTAC PARP EGFR ligand 1 is a potent compound used in developing dual PARP-EGFR degraders via Proteolytic Targeting Chimera (PROTAC) technology [1].

PROTAC CDK9 ligand-1, a CDK9 ligand, is used in the synthesis of PROTACs.

cIAP1 ligand 1 (E3 ligase Ligand 12) is an apoptotic protein ligand based on the LCL161 derivative that recruits IAP ubiquitin ligases to degrade target proteins, and can be used in conjunction with androgen receptor ligands for the development of protein degradation agents that can be used in the study of prostate cancer.

MAO-B ligand-1 is a selective MAO-B inhibitor.

Prohibitin ligand 1 (Compound 22i) is a cardioprotective prohibitin ligand that shows in vitro cardioprotective activities at nanomolar concentrations, inducing the pro-survival factor STAT3 phosphorylation [1].

Metallo-β-lactamase-IN-11 (compound 5f), a potent inhibitor of Metallo-β-lactamases (MBLs), demonstrates efficacy against bacterial metallophyllactamase CphA with an IC50 value of 45 µM. At 10 µM, it inhibits NDM-1 by 49% and AIM-1 by 61%, indicating its potential for research on countering antibiotic resistance [1].

EED ligand 1 is a highly versatile, potent, and effective inhibitor that specifically targets the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.