target/Adrenergic_Receptor/3

AMPA receptor antagonist-3 is an AMPA receptor antagonist.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1 2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].

Adenosine receptor antagonist 3 has the potential for cancer disease research which is a potent adenosine receptor antagonist [1].

Mu opioid receptor antagonist 3 (compound 26) is a potent and selective MOR antagonist with the ability to penetrate the blood-brain barrier (Ki: 0.24 nM, EC50: 0.54 nM). This compound can be used to study opioid use disorder (OUD).

TGR5 Receptor Agonist 3 is a G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist soft drug compound that decreases gallbladder filling, exhibits good gallbladder safety, and is able to act on hTGR5 (EC50: 16.4 nM) and mTGR5 (EC50: 209 nM).

Androgen receptor antagonist 3 (Compound C18) exhibits anticancer activity as an antagonist of the androgen receptor (AR) with an IC50 value of 2.4 μM [1].

NMDA receptor modulator 3 (Compound 99) is a potent NMDA receptor modulator useful in neurological disorder research [1].

Estrogen receptor antagonist 3 is a potent degradation agent of the estrogen receptor (ER). Estrogen signaling systems regulate cell growth, differentiation, and apoptosis, and estrogen receptor antagonist 4 has shown potential for cancer research.

GLP-1 receptor agonist 3 is a GLP-1 receptor agonist,Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.

Compound S28, also known as GABAA receptor modulator-3, regulates the (γ-aminobutyric acid)A receptor (GABAA receptor), exhibiting EC50 values of 56 nM for the α1β2γ2 subtype and 10 nM for the α4β3δ subtype. In rats, it demonstrates favorable pharmacokinetic properties and slight toxicity. The threshold dose for loss of righting reflex (LORR) in rats is 23.3 μmol kg. Furthermore, Compound S28 shows potential to alleviate postpartum depression.

Androgen Receptor Degrader-3 (ARD-3) is a compound that inhibits androgen receptor signaling and promotes the degradation of the receptor, with potential applications in prostate cancer research [1].

Orexin receptor antagonist 3 (example 216) functions as an orexin receptor antagonist.

A2A receptor antagonist 3 (Example 92) is an adenosine A2A receptor antagonist (Ki: 0.4 nM) and a receptor (Ki: 1467 nM).

Protease-Activated Receptor-1 antagonist 3 is a potent antagonist of Protease-Activated Receptor-1 (IC50: 7 nM) and exhibits binding affinity to hERG K+ channels (IC50: 9 μM).

GP 2A is a selective agonist of CB2 receptor.

NMDA receptor antagonist-3 is a NMDA receptor antagonist with a significan recovery rate (40.0%, at 100 μM) and safe toxicological characteristics in SH-SY5Y and human adipose mesenchymal stem cells.

TFRGAP-amide, human PAR-3-derived tethered ligand sequence which does not activate PAR-3 but rather activates PAR-1 and PAR-2, either in Jurkat or in other PAR-expressing cells.

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA, is a peptide that acts as an agonist for the proteinase-activated receptor (PAR-3) [1].

ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist with an IC50 of 0.26 nM, utilized for pulmonary arterial hypertension (PAH) research. This compound demonstrates efficacy in mitigating monocrotaline-induced PAH in a rat model [1].

RXFP1 receptor agonist-3 (Example 223) is an RXFP1 receptor agonist that inhibits cyclic AMP (cAMP) production in HEK293 cells stably expressing human RXFP1, with an EC50 of 2 nM [1].

Glucagon receptor antagonist -3 is a highly effective glucagon receptor antagonist.

P2X7 receptor antagonist-3 is a potent inhibitor of the P2X7 receptor, with IC50 values of 4.2 nM in humans and 6.8 nM in rats, demonstrating its high efficacy across species.

3 (example 3) acts as an antagonist to the GABAB receptor [1].

EP4 receptor antagonist 3 is a highly potent and specific inhibitor of the EP4 receptor, intended for research purposes in studying EP4 receptor-mediated diseases, including acute and chronic pain, osteoarthritis, rheumatoid arthritis, and cancer.

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM. It also demonstrates a remarkable 124-fold selectivity over its structurally analogous 5-HT2C receptor [1].

Glucocorticoid Receptor Agonist-3 (Preparation 6) acts as a glucocorticoid receptor agonist [1].

Glucocorticoid receptor modulator3 (Payload 6) is a thioester-based modulator of the glucocorticoid receptor, exhibiting a potent IC50 value of 0.6 nM. This compound is deactivated through rapid hepatic metabolism, minimizing systemic exposure of its unconjugated active payload. Glucocorticoid receptor modulator3 is suitable for development in antibody-drug conjugates (ADCs) targeted at autoimmune diseases.

Compound 20, identified as μ opioid receptor agonist 3, is a potent µOR agonist that exhibits an EC50 value of 0.87 nM. It holds promise for research into pain management and neuropsychiatric disorders [1].

APJ receptor agonist 3 is a highly effective, orally administrable APJ receptor agonist, with a potent EC50 value of 0.027 nM.

Glucocorticoid Receptor Agonist-3 Ala-Ala-Mal (Compound Preparation 8) is a conjugate of an anti-human TNFα antibody and a glucocorticoid receptor agonist (GC). It is utilized in researching autoimmune and inflammatory diseases [1].