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

Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist. 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

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

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

AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively. 了解更多

PF-4878691 (3M-852A) is a potent, orally active, and selective Toll-like receptor 7 (TLR7) agonist modelled to dissociate its antiviral and inflammatory activities. 了解更多

ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR), binding directly to AHR, with a Ki of 3 nM. ITE also has immunosuppressive activity. 了解更多

Nidufexor is a farnesoid X receptor (FXR) agonist. 了解更多

Cilofexor (GS-9674) is a farnesoid X receptor (FXR) agonist. 了解更多

Leriglitazone is a peroxisome proliferator activated receptor (PPAR) gamma agonist. 了解更多

DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A). 了解更多

ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM. 了解更多

PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM). 了解更多

WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist. 了解更多

GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα. 了解更多

LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer. 了解更多

PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM. 了解更多

GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4. 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

Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA2), with an EC50 value of 25 nM for murine LPA2 subtype. 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

AZD-0284 is a potent, selective, inverse agonist of the nuclear receptor RORγ for the potential treatment of Plaque psoriasis. 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

AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts. 了解更多

Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release). 了解更多

Beclometasone, also known as Beclomethasone, is an anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma. 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

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

Etofylline, also known as BRN-0251760, is a peroxisome proliferator-activated receptor (PPAR) agonist used to treat respiratory and cardiovascular disorders. Etofylline is often used as a bronchodilator. 了解更多

Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity. 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

TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), which demonstrates both potential opportunity and possible challenges to therapeutic agonism. 了解更多

Dulaglutide是胰高血糖素样肽1（GLP-1）受体激动剂。 了解更多

(R)-Equol是ER＆alpha和ER＆beta的激动剂，Kis分别为27.4和15.4 nM。 了解更多

LY 344864 racemate是5-HT1F受体激动剂。 了解更多

VU6005649是一种CNS渗透性mGlu7/8受体激动剂，对mGlu7受体和mGlu8受体的EC50分别为0.65 μM和2.6 μM。 了解更多

Temanogrel，也称为APD791，是一种高度选择性的5-羟基色胺2A受体反向激动剂，正在开发中，用于治疗动脉血栓形成。 了解更多

Bamaluzole是GABA受体激动剂。 了解更多

MRS1706是一种选择性腺苷A2B受体反向激动剂，对人A2B，A1，A2A和A3受体的Ki值分别为1.39、157、112和230 nM。 了解更多

Galanin (1-30) (human)是具有多种内分泌，代谢和行为作用的内源肽。 了解更多

LP-211是血清素5-HT7受体的选择性激动剂，在大鼠克隆的5-HT7受体上的Ki值为0.58 nM，选择性是5-HT1A受体的300倍以上。 了解更多

SR17018是一种mu型阿片受体 (mu-opioid-receptor) 激动剂，EC50为97 nM。 了解更多

Senktide是神经介素K3（NK3）受体的有效选择性激动剂（EC50 = 0.5-3 nM）。 了解更多

NECA是一种高亲和力的腺苷受体激动剂（human A3，A1和A2A受体的Ki值分别为6.2、14和20 nM；human A2B的EC50 = 2.4 μM）。 了解更多

SA4503是选择性sigma 1受体（σ1R）激动剂；对（+）-[3H]喷他佐辛标记的sigma 1受体亚型具有高亲和力（IC50 = 17.4+/-1.9 nM）；对sigma 2受体的亲和力低100倍。 了解更多

Cebranopadol是一种有效的伤害感受器/孤儿蛋白FQ肽（NOP）和阿片受体激动剂。作用于人NOP，MOP，KOP 和δ-阿片肽(DOP)受体，Ki/EC50 分别为 0.9 nM/13 nM，0.7 nM/1.2 nM，2.6 nM/17 nM，18 nM/110 nM。 了解更多

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

Clorprenaline HCl是一种β2受体激动剂，具有显着的支气管扩张作用。 了解更多