gdnf family receptor α 2

Edg-2 receptor inhibitor 1 (SAR-100842) is an Edg-2 receptor inhibitor extracted (IC50: <0.1 μM).

Dopamine D2 receptor agonist-2 (Dopamine D2 Receptor) is a ligand targeting the dopamine D2 receptor.

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

AMPA receptor antagonist-2 is an AMPA receptor antagonist.

AMPA receptor modulator-2 (Example 134) is a AMPA receptor modulator, with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

β2AR/M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

Sigma-1 receptor antagonist 2 is a potent and selective antagonist of sigma 1 receptor (σ1 R) (σ1 and σ2 receptor with Kis of 3.88 and 1288 nM , respectively).

CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

Compound 39, also known as CB2 receptor antagonist 2, is a potent CB2 antagonist exhibiting an IC50 of 0.33 μM. It engages in strong interactions with residues L17, W6.48, V6.51, and C7.42 [1].

Glucocorticoid receptor agonist-2 Ala-Ala-Mal (compound 79) serves as a precursor for synthesizing anti-inflammatory antibody-drug conjugate (ADC) molecules and acts as an active reference for ABBV-3373 [1].

RXFP1 Receptor Agonist-2 (Example 124), an EC50 value of 1 nM [1].

EGF Receptor Substrate 2 (Phospho-Tyr5) is a biologically active peptide derived from an autophosphorylation site (Tyr992) of EGFR.

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

Orexin 2 Receptor Agonist (OX2R) is an effective (EC50: 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio: 70) agonist.

ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH) research. It has been shown to mitigate monocrotaline-induced PAH in a rat model [1].

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [1].

Glucocorticoid receptor agonist-2 (compound 21), a glucocorticoid receptor agonist exhibiting an IC50 value of 6.6 nM, serves as an active reference for ABBV-3373 [1]. This compound is instrumental in the synthesis of anti-inflammatory ADC molecules.

EGF Receptor Substrate 2 (Phospho-Tyr5) is a biologically active peptide derived from an autophosphorylation site (Tyr 992 ) of epidermal growth factor receptor (EGFR).

EP2 receptor antagonist-2 (CID891729) is a compound that not only serves as an antagonist to the EP2 receptor, blocking its activation by PGE2, but also reduces lactate dehydrogenase (LDH) release triggered by N-methyl-D-aspartate (NMDA).

NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits remarkable binding affinities, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound finds valuable application in scientific investigations focusing on neuropathic pain and Parkinson’s disease.

Orexin 2 Receptor Agonist 2 (ORA-2) is a specific agonist for the orexin 2 receptor.

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].

CCK-B Receptor Antagonist 2 is a potent and orally active antagonist of Gastrin/CCK-B (IC50: 0.43 nM). It also inhibits gastrin/CCK-A activity (IC50: 1.82 μM).

Glucocorticoid receptor agonist 2 is a highly effective anti-inflammatory compound, derived from arylpyrazole, that actively binds to and activates the glucocorticoid receptor. This compound exhibits potent anti-inflammatory properties without disrupting insulin secretion.

GPR34 receptor antagonist 2 (Tyrosine, N-[(2E)-3-(4'-chloro[1,1'-biphenyl]-4-yl)-1-oxo-2-propen-1-yl]-O-(phenylmethyl)-) is an anti-inflammatory agent.

Mu opioid receptor antagonist 2 (compound 25) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.37 nM, EC50: 0.44 nM). Mu opioid receptor antagonist 2 can be used to study opioid use disorder (OUD).

A2A receptor antagonist 2 is a highly selective and potent antagonist of the adenosine A2Areceptor (IC50: 8.3 nM).

GABAA receptor agent 2 TFA is a potent, high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptor). GABAA receptor agent 2 TFA has no effect on four human GABA transport proteins (hGAT-1, hBGT-1, hGAT-2 and hGAT-3).

P2X7 receptor antagonist-2 is a highly potent antagonist of the P2X7 receptor, exhibiting a pIC50 value range of 6.5-7.5. Its efficacy in combating neuroinflammation has been demonstrated [1].

NK1 Receptor Antagonist 2, a compound targeting the NK1 receptor, holds potential for tinnitus and hearing loss research.

Glucocorticoid receptor-IN-2 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. IC50: 0.171 nM) and also has some transcriptional activating effect on MMTV (EC50: 0.94 nM).

EP4 receptor antagonist 2 (compound 2-13) is a potent agonist of the EP4 receptor (IC50: 7.8 nM) and has antitumour effects.

Sigma-2 receptor antagonist 1 is an antagonist of the sigma-2 (σ-2) receptor.

Glucagon receptor antagonist -2 is a highly effective glucagon receptor antagonist.

NMDA receptor modulator 2 (Compound 1) is a potent modulator of the NMDA receptor that can be used for neurological disorder research [1].

Protease-Activated Receptor-1 antagonist 2 is a selective, orally active protease-activated receptor-1 (PAR-1) antagonist (IC50: 7 nM). It has shown good pharmacokinetic properties and can be used for studies related to cardiovascular disease (CVD) such as atherosclerosis and restenosis.

Estrogen receptor β antagonist 2 is a selective, potent estrogen receptor β (ERβ) antagonist that acts on Erα (IC50: 109.10 μM) and Erβ (IC50: 0.63 μM).

GABAA receptor agonist 2 (compound 4c) is a highly potent GABAA receptor agonist which exhibits anti-depressive properties in classical mouse models of depression, such as the FST and TST. By binding to the GABA binding site on the GABAA receptor, GABAA receptor agonist 2 produces GABAergic effects. Notably, Compound 4c holds promise for depression research [1].

Adenosine receptor antagonist 2 is an orally active A2a (IC50: 1 nM), A2b (IC50: 3 nM) adenosine receptor antagonist that exhibits antitumour effects.

Orexin Receptor Antagonist 2 (compound 30), characterized by its potent antagonistic activity with pKis of 7.69 and 9.78, holds promise for insomnia research[1].

GABAA receptor modulator-2 (Compound 20) is a selective, orally active α5-GABAAR negative conformation modulator (Ki: 4.1 nM). gABAA receptor modulator-2 exhibits high metabolic stability and a good central nervous system safety profile.

Protease-Activated Receptor-2, amide (SLIGKV-NH2) is an agonist of PAR2 (IC50 : 10.4 M)

GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.

Compound 5, a selective GPR109a agonist, exhibits a pEC50 value of 5.53 [1].

EP4 receptor agonist 2 (compound 31) is a potent EP4 receptor agonist, demonstrating an EC50 value of 0.8 nM and K_i values of >100,000, 38,000, and 3.1 nM for the EP2, EP3, and EP4 receptors, respectively [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].

Adenosine receptor inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor). Adenosine receptor inhibitor 2 exhibits dual affinity toward A 1 /A 2A ARs with higher affinity for the A 1 - than the A 2A AR. Adenosine receptor inhibitor 2 exhibits Ki values of 52.2 nM for the A 1 AR and 167 nM for the A 2A AR.

S1p receptor agonist 2 (compound 1) is an agonist of the S1P5 receptor with a higher selectivity than S1P1 and/or S1P3 receptors.S1p receptor agonist 2 can be used in the endogenous SIP signaling system and in the mitigation/prevention of central nervous system (CNS) diseases such as neurodegenerative diseases. .

Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist.

Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor selective (Ki=2.16 nM) or multi-targeting dual ligand that shows potential effects in CNS disorders.