Tianeptine钠是体内和体外的选择性5-羟色胺再摄取促进剂（SSRE）。 了解更多

WIN 55,212-2 mesylate是一种有效的cannabinoid receptor激动剂，在神经性疼痛的大鼠模型中具有有效的镇痛作用。它通过受体介导的信号激活p42和p44 MAP激酶。 了解更多

Aripiprazole (Abilify)是人5-HT1A受体部分激动剂，Ki为4.2 nM。 了解更多

AWD 131-138是一种新的低亲和力的部分苯二氮卓类受体激动剂，在啮齿动物模型中具有强大的抗惊厥和抗焦虑特性。 了解更多

Cabergoline是一种有效的多巴胺D2受体激动剂。 了解更多

Bretazenil，苯二氮卓类受体局部激动剂，可预防OP中毒。 了解更多

Tedalinab (GRC-10693)是开发用于治疗骨关节炎和神经性疼痛的药物，它可作为有效的选择性大麻素CB2受体激动剂。与相关的CB1受体相比，它对CB2的选择性为4700x，具有很高的口服生物利用度，并在早期临床试验中显示出令人鼓舞的安全性结果以及有效的镇痛和抗炎作用。 了解更多

a5IA是促智药物，它在GABAA受体的苯并二氮杂卓结合位点上起亚型选择性反向激动剂的作用。 了解更多

Sofinicline (ABT-894,A-422894)是一种新型的烟碱型乙酰胆碱受体激动剂，可治疗注意力不足/多动症。 了解更多

ABT-418 HCl是神经元烟碱型乙酰胆碱受体激动剂。 了解更多

Guanabenz acetate是a2A-AR肾上腺素能激动剂和IGRS（咪唑啉I2结合位点）选择性配体。 了解更多

Muscimol hydrobromide是抗抑郁药氟西汀的活性代谢产物，可抑制5-羟色胺的摄取，pKi值为7.35.1。诺氟西汀的S-对映体的5-羟色胺再摄取阻断效能比R-对映体高20倍（分别为pKis = 7.86与6.51）。 了解更多

Piperazine是由六元环组成的有机化合物，该六元环在环的相对位置包含两个氮原子。 了解更多

AGN 205327是一种有效的合成RARs激动剂，对RARα/β/γ的EC50分别为3766/734/32 nM；对RXR无抑制作用。 了解更多

Rimonabant hydrochloride是CB1受体反向激动剂。 了解更多

Bamaluzole是GABA受体激动剂。 了解更多

Afloqualone, also known as HQ-495, is a centrally acting muscle relaxant. Afloqualone inhibits vestibular nystagmus probably due to both inhibition of selective polysynaptic transmission and enhancement of the effects of GABA and glycine in the lateral vestibular nucleus (LVN), and its GABA-enhancing effect is thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site. 了解更多

MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist. 了解更多

Canrenone is a metabolite of spironolactone, Na/K ATPase partial agonist and aldosterone and androgen receptor antagonist used as a diuretic. 了解更多

Tramiprosate, also known as homotaurine, is a gamma-Aminobutyric acid (GABA) receptor agonist and a glycosaminoglycan mimetic used in the treatment of Alzheimer's disease. 了解更多

Lusutrombopag, also known as S-888711, is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery. 了解更多

Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome. 了解更多

Baclofen is a GABA agonist specific for GABA-B receptors. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing It acts at spinal and supraspinal sites, reducing excitatory transmission. 了解更多

BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28?μM and Amax ratio?of 98%. 了解更多

FzM1.8 is an allosteric agonist of the Frizzled receptor FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K. 了解更多

VCE-004.8, a semi-synthetic multitarget cannabinoquinoid, is a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity. 了解更多

XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM. 了解更多

KAG-308, a newly-identified EP4-selective agonist shows efficacy for treating ulcerative colitis and can bring about lower risk of colorectal carcinogenesis by oral administration. 了解更多

Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8. 了解更多

CP-409092 is a partial agonist of GABAA receptor, with anti-anxiety activity. 了解更多

TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM. 了解更多

PF-05231023, a long-acting fibroblast growth factor 21 (FGF21) analog, is a FGF21-receptor agonist, suitable for development as a potential treatment for T2DM. 了解更多

Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes. 了解更多

ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5. 了解更多

RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors. 了解更多

SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes. 了解更多

MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77?and 1.4?nM for human?GABAA?α1β3γ2, GABAA?α2β3γ2, GABAA?α3β3γ2, and GABAA?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS. 了解更多

SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction. 了解更多

CB2R-IN-1 is a potent cannabinoid CB2 receptor inverse agonist with a Ki of 0.9 nM. 了解更多

Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction. 了解更多

Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively. 了解更多

AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors. 了解更多

LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. 了解更多

U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects. 了解更多

GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. 了解更多

β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold). 了解更多

MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention. 了解更多

Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8. 了解更多

Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro. 了解更多