A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively); effectively inhibits GHRH-induced growth hormone release in primary cultures of rat pituitary cells with IC50 of 0.4 nM, also potently suppresses GH secretion in rats.

A potent, small molecule CXCR2 inhibitor with IC50 of 26 nM and 30 nM for mCXCR2 and hCXCR2, respectively; inhibits the growth and metastatic potential pancreatic ductal adenocarcinoma, enhances sensitivity to anti-PD1 immunotherapy in vivo; chemical analog of AZD 5069.

A potent, selective, small molecule motilin receptor agonist with pEC50 of 7.9 (hMTL-R); displays selectivity over closely related human ghrelin acceptor (pEC50< 6.0) and no liabilities at the hERG channel; possesses highly excellent pharmacokinetic profiles in both rat and dog.

A potent, selective, small molecule motilin receptor agonist with pEC50 of 7.9 (hMTL-R); displays selectivity over closely related human ghrelin acceptor (pEC50< 6.0) and no liabilities at the hERG channel; possesses highly excellent pharmacokinetic profiles in both rat and dog.

A potent, selective CCR5 antagonist and HIV-1 entry inhibitor.

A potent, selective CCR5 antagonist and HIV-1 entry inhibitor with pIC50 of 8.37 and 8.46 in HOS and PBL assays, respectively.

A potent, selective and orally bioavailable GPR119 agonist with EC50 of 4 nM, with good selectivity versus a battery of receptors, ion channels and enzymes; causes greater reductions in cumulative food intake and higher fed plasma GLP-1 and peptide tyrosine tyrosine levels and decreased plasma insulin and glucose-dependent insulinotropic polypeptide levels, when combined with metformin, in diet-induced obese mice.

A novel potent, selective, brain-penetrating, orally active CXCR4 antagonist with Ki of 3 nM; inhibits tumor growth alone, increases the antitumor effects of bevacizumab and sunitinib in preclinical models of human glioblastoma; reduces the expression of Nestin in vivo, reduces tumor cell proliferation and accelerates cancer stem cell differentiation in glioblastoma preclinical models.

A novel potent, nonpeptide CXCR4 antagonist with IC50 of 0.93 nM; induces increased and prolonged mobilization of murine HSPC compared to AMD3100.

(R,S′)-MNF is a bi-functional GPR55 inhibitor and biased β2 adrenergic agonist, inhibits proliferation of PDAC cell lines (IC50=0.11 uM, PANC-1 cells). (R,S′)-MNF is a biased β2-AR agonist that selectively signals through Gαs and does not recruit β-arrestin-2. (R,S′)-MNF attenuates pro-oncogenic signaling and cellular proliferation in PANC-1 cells. (R,S′)-MNF (1 uM) significantly decreased ERK phosphorylation stimulated by the GPR55 ligand O-1602, (R,S′)-MNF is an effective inhibitor of GPR55 internalization and signaling. (R,S′)-MNF (20-40 mg/Kg) reduces PANC-1 tumor growth in a mouse xenograft model.

(R)-LMI (H2N-R-Leu-Met-Ile-COOH) is a tripeptide analogue of corticotropin-releasing factor (CRF) and CRF antagonist targeting the N-domain of CRF1 receptor; (R)-LMI inhibits CRF-stimulated cAMP accumulation with IC50 of 1.7 uM. (R)-LMI inhibits the production of interleukins by adipocytes and the proliferation rate of RAW 264.7 cells.

(–)-IHCH7041 is a potent, selective partial agonist at DRD2/3 and 5-HT1AR, EC50 of 1.38 nM in Gαi1–γ9 dissociation and 2.75 nM in β-arrestin2 recruitment assays, with negligible 5-HT2AR binding (>100-fold selectivity).(–)-IHCH7041 exhibits negligible affinities for a large number of tested GPCRs, ion channels and transporters (Ki>500 nM), good affinities for DRD2 and DRD3 (Ki=14.42 nM), and moderate binding to 5-HT1A (Ki=60.62 nM).(–)-IHCH7041 behaves as a partial agonist in both G-protein signaling and β-arrestin recruitment activities at DRD2, DRD3 and 5-HT1AR.(–)-IHCH7041 displayed potent antipsychotic activity and has antidepressant properties and reverses cognitive impairmentin mice.

GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9.

GSK598809 hydrochloride is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9.

GSK3004774 (GSK-3004774) is a potent, nonabsorbable, gastrointestinally-restricted agonist agonist of calcium-sensing receptor (CaSR) with pEC50 of 7.3.

VUF11207 fumarate is a potent CXCR7 (ACKR3) agonist with EC50 of 1.6 nM, inducse recruitment of β-arrestin2 and subsequent internalization of CXCR7 in cells.

GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of  9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.

GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1.

Cholic acid 7-sulfate (7-Sulfocholic acid), a metabolite of Cholic acid, is a Takeda G-protein receptor 5 (TGR5) agonist. Cholic acid 7-sulfate can increase Tgr5 expression and induce GLP-1 secretion.

Deoxycholic acid-13C (Cholanoic acid-13C) is the 13C-labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. GSK1614343 inhibits the calcium response induced by ghrelin with a pIC50 value of 7.90. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models.

CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM).

HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis.

CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus.

Fuscin, a fungal metabolite, CCR5 receptor antagonist with anti-HIV effects. Fuscin is a respiration and oxidative phosphorylation inhibitor, and also a mitochondrial SH-dependent transport-linked functions inhibitor.

CCR8 antagonist 1 (compound 15) is a potente human CCR8 antagonist with a Ki of 1.6 nM.

BMS-639623 is a potent and orally activeCCR3 antagonist with an IC50 of 0.3 nM. BMS-639623 picomolar inhibition potency against eosinophil chemotaxis (IC50=38 pM). BMS-639623 can be used for the research of asthma.

S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS).

SB-611812 is a urotensin II receptor (UTR) antagonist with the potential in the treatment of cardiovascular disease.