σ-ligand-1

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

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

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

(S,R,S)-AHPC hydrochloride (Protein degrader 1 hydrochloride) is a building block in the synthesis of proteolysis-targeting chimera technologies (PROTACs).

STING ligand-1 is a lead stimulator of the STING pathway with an IC₅₀ of 68 nM for HAQ STING, STING ligand-1 I shows potential in research related to inflammation and immunology.

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.

(S,R,S)-AHPC TFA (VHL ligand 1 TFA) (VH032-NH2 TFA) is a VH032-based ligand designed for von Hippel-Lindau (VHL) protein recruitment. This compound can be linked to protein ligands (e.g., BCR-ABL1) using a linker to create PROTACs (e.g., GMB-475), which effectively induce the degradation of BCR-ABL1, demonstrated by an IC50 of 1.11 μM in Ba/F3 cells.

PIN1ligand-1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). It can be utilized in synthesis processes.

TRIB2 ligand-1 is a ligand for TRIB2 (Ligands for Target Protein for PROTACs). This compound serves as a precursor for the synthesis of PROTAC TRIB2 degrader-1.

HDAC3/8 ligand-1 (compound 40) serves as a ligand for the target protein of PROTAC, utilized in the synthesis of YX968.

GABA-A Receptor Ligand-1 (Compound 4) is a ligand for the GABA-A receptor with a pKi of 7.27. It alleviates mitochondrial dysfunction, promotes neurite outgrowth and neuronal regeneration, and demonstrates neuroprotective effects in a rat ischemic stroke model.

RETligand-1 is a target protein ligand that specifically interacts with RET and can be utilized in the synthesis of the PROTAC LDD39.

ALK protein ligand-1 (Compound A1) is an ALK protein ligand, acting as a ligand for the target protein in PROTACs, demonstrating inhibitory effects on ALK. It is also useful in the synthesis of AP-1.

5-HT5AR/5-HT6R ligand-1 (Compound PP10) is a ligand for serotonin receptors, exhibiting high affinity for the 5-HT5A and 5-HT6 receptors with Ki values of 59 nM and 96 nM, respectively. It possesses some antiproliferative activity against tumor cells and can be utilized in cancer research.

I2-IRs ligand-1 (Compound 12d) is an orally active compound capable of crossing the blood-brain barrier. It exhibits high affinity for imidazoline I2 receptors (I2-IRs) with a pKi of 9.98. This compound can enhance cognitive deficits in aging mice and possesses analgesic, anti-inflammatory, and neuroprotective properties. I2-IRs ligand-1 is applicable for research in Alzheimer's disease and related pain disorders.

G3BP1/2-Targeting ligand-1 is a ligand for G3BP1/2 and can be utilized as a targeting ligand in the synthesis of the G3BP1/2 PROTAC degrader PT-129.

ROR1ligand-1 (9-1) serves as the ligand for PROTAC ROR1 degrader-1. By linking with ligands of either the VHL type or CRBN, the first selective and efficient ROR1 PROTAC molecule was designed and synthesized.

H1R ligand-1 (Compound fragment 1) is a high-affinity ligand for the human histamine H1 receptor (H1R). It can serve as a scaffold for synthesizing a series of derivatives to investigate H1R binding kinetics.

BTN3A1 ligand-1 (Compound 26b) is an aryl/acylalkyl phosphonate prodrug containing a triazole group. It is capable of stimulating T cell proliferation (EC50: 0.49 nM) and promoting interferon γ secretion. Additionally, this compound exhibits a degree of plasma stability, making it relevant for research in immunotherapy.

CypA ligand-1 is a ligand for CypA, which can serve as a target protein ligand in the synthesis of the PROTAC degrader, PROTAC CG167.

5-HT1AR/5-HT6R ligand-1 (Compound PP13) functions as a ligand for the 5-HT receptor, demonstrating high affinity for 5-HT1AR, 5-HT6R, and 5-HT7R with Ki values of 19, 69, and 198 nM, respectively. In HEK293 cells, it inhibits cAMP production with EC50 values of 1535, 488, and 53 nM for these receptors. Additionally, 5-HT1AR/5-HT6R ligand-1 exhibits antiproliferative effects on several cancer cell lines, including 1321N1, U87MG, MCF7, and AsPC-1, with IC50 values of 9.6, 13.6, 19.3, and 14.6 μM, respectively. The compound also shows antagonistic activity towards the dopamine receptor D2R, with a Ki of 1903 nM.

FKBP12 ligand-1 is the target protein ligand for MC-25B, which is a PROTAC targeting FKBP12.

Tau ligand-1 (Compound 75) is a ligand of aggregated tau protein that can penetrate the blood-brain barrier. In tissues affected by Alzheimer's disease, progressive supranuclear palsy, corticobasal degeneration, and Pick's disease, Tau ligand-1 shows high affinity for aggregated tau protein, with equilibrium dissociation constants (KD) ranging from 1 to 3.8 nM. It holds potential as a positron emission tomography (PET) tracer for imaging studies of tau-related diseases within the central nervous system.

IDO1ligand-1 is the target protein ligand for PROTAC NU227326, which is utilized for degrading IDO1.