Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.

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

AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).

Betahistine is a strong affinity histamine H3 receptor antagonist and weak affinity agonist of histamine H1 receptors.

Tegaserod maleate is a partial agonist of the 5-HT4 receptor; stimulates the peristaltic reflex and accelerates gastrointestinal transit.

Ciproxifan maleate(FUB-359 maleate) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.

Meptazinol Hcl(WY-22811 Hcl) is a unique centrally active opioid analgesic.

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors.

Cinnarizine is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.

BP897 is a partially selective D3 dopamine receptor agonist.

MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.

Vazegepant (BHV-3500) hydrochloride is a highly soluble CGRP receptor antagonist. Vazegepant hydrochloride is the first intranasal gepant for migraine. Vazegepant hydrochloride may be helpful in effective management of COVID-19 associated pulmonary inflammation.

TAK041(TAK 041) is a potent and selective GPR139 agonist with an EC50 of 22 nM. TAK-041 has the potential for the research of negative symptoms associated with schizophrenia.

W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.

α-MSH (free acid) is a MC3R and MC4R agonist with an EC50 of 0.16±0.09 nM and 5.6±6.8 nM, respectively. α-MSH (free acid) activates cAMP generation at MC3R and MC4R.

VGD071, a sortilin-targeting compound, is a promising candidate for future studies using mouse breast cancer models.

N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist.

S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist against fibrotic diseases.

Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.

PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC50 of 1.5 μM) negative allosteric modulator and mGluR3 (EC50 of 8.9 μM) positive allosteric modulator.

SC13 is a novel mitragynine analog with low-efficacy Mu opioid receptor agonism that displays antinociception with attenuated adverse effects.

SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.

FPPQ is a dual-acting 5-HT3 (Ki = 0.9 nM) and 5-HT6 (Ki = 3 nM) receptor antagonist with antipsychotic and procognitive properties.

hA3AR agonist 1 is a potent human A3 adenosine receptor (hA3AR) agonist with a Ki value of 2.40 nM.

Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM).

Dopamine D3 receptor antagonist-1 is a dopamine D3 receptor-selective or multitarget bitopic ligand (Ki = 1.58 nM) potentially useful for central nervous system disorders.

Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor-selective (Ki = 2.16 nM) or multitarget bitopic ligand potentially useful for central nervous system disorders.

GLP-1R modulator C16 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 8.43 ± 3.82 μM).

GLP-1R modulator C5 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 1.59 ± 0.53 μM).

GPR84 antagonist 1 is a high affinity and highly selective competitive antagonist of human GPR84.