high-affinity ligand

Shield-1 is a specific, high-affinity, and cell-permeable ligand for FK506-binding protein 12 (FKBP) and reverses instability by binding to mutant FKBP (mtFKBP), allowing conditional expression of mtFKBP fusion proteins.

MK-3328 has a high affinity for β-Amyloid (IC50:10.5 nM), and can be used as a candidate PET ligand for clinical assessment of β-amyloid plaque load. MK-3328 is a potential treatment for Alzheimer's disease.

5-Methyltryptamine hydrochloride is a high-affinity 5-HT1C receptor ligand and a partial agonist of 5-HT. 5-Methyltryptamine hydrochloride protects mice subjected to burn, tourniquet and endotoxin shock.

TNCA (Lycoperodine-1) is a high-affinity CaSR ligand (CaSRL) with co-agonist activity.

MS 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (EGFR) with high efficiency, high affinity and selectivity. MS 39, conjured by gefitinib to VHL ligand via a linker, effectively induced the degradation of mutant EGFR (DC50 values in HCC827(exon 19 del) and H3255 (L858R mutation) lung cancer cell lines were 5 nM and 3.3 nM, respectively). However, there was no significant effect in wild-type EGFR cell lines with concentrations up to 10 μM. MS 39 inhibited the proliferation of H3255 lung cancer cells in vitro and was bioavailable in mice after administration.

ZM-241385 is a high-affinity antagonist ligand selective for the adenosine A2A receptor.

GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.

Acein acetate is a high-affinity angiotensin-converting enzyme (ACE) ligand (Kd = 2.79 nM). Concentrations up to 500 nM had no significant effect on ACE enzyme activity. Enhanced NMDA + D-serine-induced dopamine release from striatal slices in vitro and striatum in vivo.

BET-IN-6, a ligand with potent and high affinity for inhibiting BRD2 BRD4, plays a crucial role in the synthesis of PROTAC BRD2 BRD4 degrader-1 [1], targeting the protein BRD2 4.

EC0489 is a small molecule-drug conjugate (SMDC) that combines folic acid and desacetyl vinblastine hydrazide, serving as a high-affinity ligand for the folate receptor (FR) in refractory or metastatic tumors.

KF21213 shows a high affinity for the adenosine A2A receptors (Ki=3.0 nM). KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors.

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).

DPA-714 is a high-affinity translocator protein (TSPO) ligand (Ki=7 nM) designed with a fluorine atom, allowing labeling with fluorine-18 for in vivo imaging via positron emission tomography. [18F]DPA-714 successfully enables specific imaging of inflammation in various neuroinflammation models and a brain tumor model.

PD 144418 displays potential antipsychotic activity. PD 144418 is a high affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki: 0.08 nM and 1377 nM for σ1 and σ2 respectively). It shows devoid of any significant affinity for other receptors, ion channels, and enzymes.

Brivaracetam (αR,4R) is a third-generation antiepileptic drug and anticonvulsant compound frequently used in combination with other antiepileptic compounds for the treatment of partial-onset seizures. It acts as a high-affinity ligand for synaptic vesicle protein 2A, reducing neurotransmitter release by binding to synaptic vesicle glycoprotein SV2A. Brivaracetam (αR,4R) is primarily metabolized into inactive metabolites through hydrolysis by amidase.

LuAF60097 is a high-affinity S2 receptor ligand that binds allosterically to the S1 site. This compound also acts as a serotonin transporter (SERT) inhibitor, as demonstrated by increased imipramine binding and elevated 5-HT (serotonin) levels in the hippocampus.

Acetylethylcholine mustard hydrochloride is a choline acetyl-transferase inhibitor that decreases muscle contraction frequency by inhibiting the synthesis of acetyl-beta-methylcholine (Ach), with a half-maximal inhibitory concentration (IC50) of 1.22 mM. It serves as an irreversible ligand for the high-affinity choline transport system and functions as a specific presynaptic long-acting cholinergic toxin. Additionally, acetylethylcholine mustard hydrochloride is a precursor to the ethylcholine mustard aziridinium ion.

TDIQ hydrochloride is an analog of Amphetamine with high affinity for the α2-adrenergic receptor. This compound acts as a selective ligand for α2-adrenergic receptors, displaying Ki values of 75 nM, 95 nM, and 65 nM for α2A-, α2B-, and α2C-adrenergic receptors, respectively.

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.

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.

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.

high affinity agonist of the translocator protein

L 687384 is a high-affinity ligand of sigma receptor.