CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively. 了解更多

4-IBP is a selective ??1 agonist with a high level of affinity for the ??1 receptor (Ki = 1.7 nM) and a moderate affinity for the ??2 receptor (Ki = 25.2 nM) . 了解更多

Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist. 了解更多

OPC-28326 is a selective peripheral vasodilator and an angatonist of α2-adrenergic receptor, with Ki of 2040, 285, and 55?nM for α2A-, α2B- and α2C-adrenoceptors, respectively. 了解更多

Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4. 了解更多

GSK1059865 is a potent orexin 1 receptor antagonist. 了解更多

ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively. 了解更多

GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. 了解更多

LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM??EC50=0.47 nM; hmGlu2 Ki=412 nM??EC50=47.5 nM). 了解更多

BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. 了解更多

Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome. 了解更多

Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). 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

SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC50 of 15 nM for hOTR. 了解更多

BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. 了解更多

BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM. 了解更多

ASP6432 is a potent and selective Type 1 Lysophosphatidic Acid (LPA1) receptor antagonist. 了解更多

A-381393 is a potent and selective agonist of the dopamine D4 receptor. 了解更多

PF-06256142 is a potent and selective orthosteric agonist of the D1 receptor, with D1 EC50=30 nM and D1 binding Ki = 12 nM. 了解更多

Tulobuterol Hydrochloride is a long-acting beta2-adrenergic receptor agonist. 了解更多

Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand, with a pKi of 8.02. 了解更多

Metipranolol (hydrochloride) is a non-selective β-adrenergic receptor (β-AR) antagonist. Formulations containing metipranolol have been used in the treatment of elevated IOP in patients with ocular hypertension or glaucoma. 了解更多

Diazoline is a histamine H1-receptor antagonist. 了解更多

Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist. 了解更多

Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist. 了解更多

Doxazosin is an α-1 adrenergic receptor blocker that inhibits the binding of norepinephrine, which is released from sympathetic nerve terminals, to the α-1 receptors on the membrane of vascular smooth muscle cells. Blockages of the alpha-1 adrenergic action on the vascular smooth muscles lead to a decrease in vascular resistance and antihypertensive activity. 了解更多

Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis. 了解更多

Dolasetron mesylate is a selective 5-HT3 receptor antagonist. 了解更多

Hydroxyzine pamoate is an histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. 了解更多

Dolasetron is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness. 了解更多

Melitracen HCl ia potential dopamine D1/2 receptor antagonist used to treat depression. It is often co-administered with flupenthixol as a treatment for trigeminal neuralgia. It does not effect cardiovascular function. 了解更多

Levocetirizine dihydrochloride is a L-isomer of cetirizine and histamine H1 receptor antagonist. It incrases levels of CD4+ CD25+ T cells and decreases levels of eosinophils, decreasing allergy symptoms. 了解更多

Nifenalol, also known as INPEA, is a new beta-adrenergic receptor antagonist. 了解更多

Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5. 了解更多

Terfenadine ((??)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 and induces p73, Noxa. 了解更多

Tasimelteon is a melatonin MT1 and MT2 receptor agonist. 了解更多

Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone. 了解更多

Asenapine hydrochloride抑制肾上腺素能受体（α1，α2A，α2B，α2C）的Ki为0.25-1.2 nM，还抑制5-HT受体（1A，1B，2A，2B，2C，5A，6、7），Ki为0.03- 4.0 nM。 了解更多

Reversine是一种有效的人A3腺苷受体拮抗剂，Ki为0.66μM，是一种泛光A/B/C激酶抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞去分化。 了解更多

Fexofenadine Hydrochloride是一种抗组胺药，可抑制Cox-1，Cox-2，并且是组胺H1受体激动剂，IC50为246 nM。 了解更多

JTC-801是nociceptin receptor（也称为ORL-1受体）的选择性拮抗剂。 了解更多

CPI-444 is a potent, oral and selective A2A receptor (A2AR) antagonist, which induces antitumor responses. 了解更多

AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3. 了解更多

BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. 了解更多

NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility. 了解更多

Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1. 了解更多

Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine. 了解更多

SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments. 了解更多

INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively. 了解更多