metallo β-lactamase ligand 1

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

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

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

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

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.

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.

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

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.

Metallo-β-lactamase-IN-13 (Compound 13i) serves as a pan Metallo-β-Lactamase inhibitor with extended activity against Gram-negative (GN) bacteria expressing metallo-β-lactamases. It exhibits antibacterial properties effective against P. aeruginosa [1].

Metallo-β-lactamase-IN-14 (Compound 17e) serves as an inhibitor of Metallo-β-Lactamase, displaying inhibitory activity against VIM-1 and VIM-2. This compound also exhibits antibacterial effects on Gram-negative (GN) bacteria and P. aeruginosa [1].

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

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.

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].

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].

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.

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].

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].

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].

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

TEAD ligand 1 is a ligand for the target protein TEAD. TEAD ligand 1 can be utilized in the synthesis of the PROTACTEAD degrader-1.

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

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].

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].

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].

DENV Ligand 1 serves as a ligand for the DENV E protein. It is utilized in the synthesis of the PROTAC degrader ZXH-8-004.

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.

Compound 72-1, also known as BCL-xL BCL-2 ligand 1, serves as a ligand for BCL-xL and BCL-2 proteins. It can be tethered to an E3 ligase via a linker, facilitating the formation of PROTACs [1] [2].

Metallo-β-lactamase-IN-15 (Compound ±13), a potent inhibitor of MBL, demonstrates IC 50 values of 0.29 μM for NDM-1, 0.088 μM for IMP-1, and 0.063 μM for VIM-2, respectively [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].

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

FLT3 CDKs ligand-1 (Compound 14) functions as a ligand for target proteins, promoting the degradation of Cyclin-Dependent Kinases (CDK) and FMS-like tyrosine kinase 3 (FLT3), thereby inhibiting the proliferation and survival of leukemia cells associated with FLT3 CDK. This compound is also used in the synthesis of PROTAC FLT3 CDKs Degrader-1.

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].

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).

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.