GRA Ex-25 is an orally active human glucagon receptor antagonist in a transgenic murine pharmacodynamic model at 10 and 30 mpk.

AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.

Zacopride hydrochloride is a potent antagonist of 5-HT3 receptor with a Ki of 0.38 nM. Zacopride hydrochloride is also a agonist of 5-HT4 receptor with a Ki of 373 nM. Zacopride hydrochloride has anxiolytic activity. Zacopride hydrochloride has the potential for the research of Schizophrenia.

SAR-100842 (SAR100842) is a potent, selective, orally available antagonist of the Lysophosphatidic Acid 1 Receptor (LPA1 receptor) with IC50 of 31 nM in β-arrestin assays.

BAF312 is a potent and selective agonist of S1P with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively

Y1R probe-1 (Compound 39) is a high-affinity fluorescence probe for the Neuropeptide Y Y1 Receptor. Y1R probe-1 has the potential for the research of cancer disease.

Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.

PSB-16671 is a novel orthosteric and allosteric activator of GPR84, activates human GPR84 with EC50 of 41.3 nM in cAMP accumulation assays. PSB-16671 is selective versus related fatty acid receptors and the arylhydrocarbon receptor. PSB-16671 shows an EC50 of 5.47 uM in β-Arrestin assays, and allosteric KB value of 634 nM.

AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis.

Lotiglipron (PF-07081532) is an orally active GLP-1R agonist. It reduces glucose and body weight, and has the potential to be used in Type 2 diabetes mellitus (T2DM) research.

CVN766 (CVN 766) is a potent, exquisitely selective orexin 1 receptor (OX1R) antagonist with IC50 of 8 nM, 1000-fold selective over OX2R.

CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM.

A potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.

A-61603 is a selective α1A-adrenergic receptor agonist. A-61603 increases the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro.

SX-682 (SX682) is a potent, allosteric, orally bioavailable inhibitor of CXCR1 and CXCR2.SX-682 enhances tumor infiltration, activation, and the therapeutic efficacy of adoptively transferred NK cells.SX-682 significantly inhibits trafficking of PMN-MDSCs without altering CXCR2 ligand expression.SX-682 enhances T cell-based immunotherapeutic efficacy.

Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

Avexitide (Exendin (9-39)) is a specific and competitive antagonist of glucagon-like peptide-1 (GLP-1) receptor.

TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively.

Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19.

Teduglutide (ALX-0600, Gattex, Revestive, TAK 633) is an analogue of human glucagon-like peptide-2 (GLP-2) and binds to the GLP-2 receptors. Teduglutide prolongs the intestinotrophic properties of GLP-2 in animal models.

AGH-107 is a potent, selective 5-HT7 receptor agonist with Ki of 6 nM and EC50 of 19 nM, 176-fold selectivity over 5-HT1AR.AGH-107 exhibited high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.

AMG-073 HCl (Cinacalcet HCl) represents a new class of compounds for the treatment of hyperparathyroidism.

Cinacalcet(AMG-073) is an orally active, second-generation calcimimetic compound; AMG 073 represents a new class of compounds for the treatment of hyperparathyroidism.

NNZ2591 (cyclo-L-glycyl-L-2-allylproline)1 is an investigational synthetic analog of cyclic glycine-proline (cGP), a breakdown product of human insulin-like growth factor 1 (IGF-1), that has been chemically modified to increase its half-life, stability, and oral bioavailability.

4-P-PDOT is a slelctive MT2 melatonin receptor antagonist 300 fold selective for MT2 (MEL-1B-R) vs MT1 (MEL-1A-R) melatonin receptor subtype.

Tabernanthalog is a water-soluble, non-hallucinogenic and non-toxic analogue of ibogaine. Tabernanthalog is a 5-HT2A agonist. Tabernanthalog is found to promote structural neural plasticity, reduce alcohol- and heroin-seeking behaviour, and produce antidepressant-like effects in rodents.

ASP4345 (ASP-4345) is a potent, selective positive allosteric modulator of the dopamine type 1 (D1) receptor that selectively binds to, and enhances the activity of, D1 receptors.

IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.

H2L5186303 is a potent and selective LPA2 receptor (lysophosphatidic acid 2 receptor) antagonist with an IC50 of 9 nM.