LSN3318839 is an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R).

Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment.

HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.

Muscarine ((+)-Muscarine) is a toxin that can stimulate the parasympathetic nervous system. Muscarine is an agonist of muscarinic acetylcholine receptor (mAChR).

SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.

A peptide, non-selective melanocortin receptor agonist for treatment for female sexual dysfunction; selectively stimulates solicitational behaviors in the female rat, without affecting lordosis, pacing, or other sexual behaviors, does not cause generalized motor activation; a peptide analogue of α-MSH.

Desmopressin is a synthetic analogue of the antidiuretic hormone arginine vasopressin.

Lu AE58054 is an in-vitro potency and selectivity, in-vivo binding affinity and effect of the 5-HT(6)R antagonist with a Ki value of 0.83 nM.

Arecaidine but-2-ynyl ester tosylate is a potent muscarinic agonist that shows 4.6-fold that is selectivity for mAChR M2 in the atrium versus those in the ileum.

UCM1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).

CB-25 is a ligand of CB1 cannabinoid receptors, acting as a partial agonist. CB-25 enhances Forskolin-induced cAMP formation in cancer cells but not hCB1-CHO cells.

CCR4-IN-38 (CCR4-351) is a potent, selective, orally bioavailable CCR4 antagonist with IC50 of 50 nM (Chemotaxis inhibition).CCR4-IN-38 inhibits the recruitment of Treg into the tumor microenvironment (TME).CCR4-IN-38 elicits antitumor responses as a single agent or in combination with an immune checkpoint blockade.

Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes.

Olcegepant(BIBN 4096; BIBN 4096BS) is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor(IC50= 0.03 nM).

N8279 (NCATS-SM8864) is a selective, brain-penetrant small molecule Gαq-biased GHSR1a agonist with binding IC50 of 1.3 uM.N8279 is nearly an order of magnitude (8.9-fold) more potent than the endogenous ligand ghrelin and is a full agonist.iCa2+ EC50 of N8279 is 41-fold more potent than its GHSR1a binding IC50, suggesting possible allosteric activity, which could be competitively inhibited by GHSR1a antagonists YIL781 and JMV2959.N8279 is a weak activator of GHSR1a-mediated, βarr2-dependent cellular responses relative to ghrelin.N8279 requires receptor sites and/or conformational states driven by the GHSR1a ECD that are distinct from ghrelin.N8279 is brain-penetrant and attenuates aberrant DAergic behavior in mice.

MEN 11270, a cyclic decapeptide, is a B2 kinin receptor antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with pKi of 10.3.

Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes.

JNJ-40411813 is a novel potent positive allosteric modulator of mGlu2 with EC50 of 147 nM. JNJ-40411813 displays >30-fold selectivity over mGlu1 and mGlu3-8, 10-fold over 5-HT2A. JNJ-40411813 displays an optimal interplay between potency, selectivity, favorable ADMET/PK and cardiovascular safety profile, and central EEG activity; has been investigated in the clinic for schizophrenia and anxious depression disorders.

FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.

ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with an IC50 value of 3.2 nM.

EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.

BAY-6672 is a potent and selective human Prostaglandin F (FP) receptor antagonist with an IC50 value of 11 nM.

BAY 1214784 is an orally available, potent, and selective hGnRH-R antagonist. BAY 1214784 effectively lowered plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability.

SCO-267 is an allosteric GPR40 full agonist. SCO-267 can be used for the research of chronic diseases including diabetes.

NLX-204 is a potent and selective ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist with pKi = 10.19. NLX-204 displayed high selectivity in the SafetyScreen44 panel (including hERG channel), high solubility, metabolic stability, and Caco-2 penetration and did not block CYP3A4, CYP2D6 isoenzymes, or P-glycoprotein. Preliminary in vivo studies confirmed its promising pharmacokinetic profile. NLX-204 also robustly stimulated ERK1/2 phosphorylation in rat cortex and showed highly potent (MED = 0.16 mg/kg) and efficacious antidepressant-like activity, totally eliminating immobility in the rat Porsolt test.

LAS190792 (AZD8999) is a potent muscarinic antagonist and β2-adrenoceptor agonist with pIC50 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6 for M1, M2, M3, M4, M5, β1, β2, β3, respectively. LAS190792 can be used as a bronchodilator.

ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively.

CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs.

BMS-986120 (BMS986120) is a potent, selective, orally bioavailable, and reversible PAR4 antagonist with Kd of 0.098 nM for human PAR4.