target/Androgen_Receptor/5

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

Target 5 has a wide range of applications in life science related research.

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

RXFP1 receptor agonist-5 (Example 98) is an agonist that targets the RXFP1 receptor and demonstrates its bioactivity by inhibiting cAMP production in HEK293 cells with stable human RXFP1 expression, exhibiting an EC50 of 1.3 nM [1].

Androgen Receptor Degrader-1 (Compound 18) is a potent agent for androgen receptor degradation, applicable in cancer research [1].

Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is employed in coronary heart disease (CHD) research.

Androgen Receptor Degrader-2 (Compound 9) is a potent degrader of androgen receptors, with potential application in cancer research [1].

Androgen Receptor Antagonist 9 (compound 28) serves as an antagonist to the androgen receptor [1].

GABAA Receptor Agent 5 (compound 018) serves as a potent γ-GABAAR antagonist, possessing a Ki of 0.020 μM. This compound exhibits γ-GABAAR antagonist properties, yet it demonstrates low cellular membrane permeability [1].

5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors. It exhibits a K i value of 2 nM and 11 nM for the respective receptors. This compound holds promise for research in neurological and psychiatric disorders [1].

Androgen receptor antagonist 3 (Compound C18) has anticancer activities that is an antagonist of androgen receptor (AR) (IC 50 = 2.4 μM) [1].

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].

Compound 42, a 5-HT6/5-HT2A receptor ligand-2, serves as a dual antagonist for the 5-HT6 and 5-HT2A receptors with Ki values of 25 nM and 32 nM, respectively. This brain-penetrant compound exhibits pro-cognitive properties [1].

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

Estrogen receptor antagonist 5 is a potent antagonist of the Estrogen receptor. Estrogen receptor (Estrogen receptor) is a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates the induction of a variety of biological effects. estrogen receptor antagonist 5 has potential for metastatic disease studies.

Sigma-1 receptor antagonist 5 (compound 12), a 4-pyridylpiperidine derivative, exhibits analgesic properties through its antagonistic action on sigma receptors (Ki=4.5 nM (σ1R), 10 nM (σ2R)) and the histamine H3 receptor (hH3R, Ki=7.7 nM, IC50=215 nM). It effectively attenuates Capsaicin-induced nociception and demonstrates significant antinociceptive effects in both nociceptive and neuropathic pain models [1].

Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor with anticancer properties. It additionally suppresses the synthesis of IL-17A, IL-17F, and INF-γ.

AMPA Receptor Modulator-5 (Example 217) serves as an AMPA receptor modulator, utilized in neurological disease research [1].

APJ receptor agonist 5 (compound 3) is a potent and orally active apelin receptor (APJ) agonist (EC 50:0.4 nM). APJ receptor agonist 5 has excellent pharmacokinetic profiles in rodent models of heart failure (HF) and an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 can improve cardiac function and can be used in the study of HF disease.

Androgen receptor antagonist 5 is a potent antagonist of the androgen receptor (AR) (IC50: 6.17 μM). Androgen receptor antagonist 5 inhibited the proliferation of prostate cancer cells LNCaP and showed antitumor effect in LNCaP xenograft mice model, which can be used to study prostate cancer.

Glucagon receptor antagonists-5 is an orally bioavailable indazole-based glucagon receptor antagonist (Ki: 32 nM). It has potential for the treatment of type 2 diabetes mellitus (T2DM).

Androgen receptor antagonist 4 (Compound AT2) has anticancer activities. Androgen receptor antagonist 4 potently antagonizes the activity of AR transcriptional, inhibits downstream target gene of AR, and blocks the DHT-induced nuclear translocation of AR. Androgen receptor antagonist 4 is an antagonist of androgen receptor (AR) (IC 50 = 0.15 μM) [1].

NMDA receptor antagonist 5 (Compound 10e), a potent and non-toxic NMDA receptor antagonist, exhibits brain permeability. It is of significance in studying neurological disorders [1].

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].

NMDA receptor modulator 5 (Compound 195), a potent NMDA receptor modulator, exhibits potential for neurological disorder research [1].

5-HT2A receptor agonist-2 is a potent compound that acts as an agonist on the serotonin 5-HT2 receptor. It specifically stimulates the 5-HT 2A, 5-HT 2B, and 5-HT 2C receptors, with EC 50 values of 1.7 nM, 0.58 nM, and 0.50 nM, respectively [1].

Mu opioid receptor antagonist 5 (compound NAP) is a selective mu opioid receptor (MOR) antagonist that crosses the blood-brain barrier (EC50: 1.14 nM, Ki: 0.37 nM). Mu opioid receptor antagonist 5 can be used to study opioid use disorder (OUD).