L-659,699, also known as hymeglusin, is a fungal β-lactone antibiotic that inhibits HMG-CoA synthase (IC50 = 0.12 μM) by covalently modifying the active Cys129 residue of the enzyme.

L-371,257 is a potent, high affinity human oxytocin (OT) receptor antagonist (Ki = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V1a and V2. L-371,257 antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration.

L-168,049 is a non-peptidyl human glucagon receptor antagonist.

L-162,313 is a non-peptide AT1 receptor agonist.

L-152,804 is a potent, selective non-peptide neuropeptide Y Y5 receptor antagonist (Ki = 26 nM for hY5). L-152,804 displays > 300-fold selectivity over hY1, hY2, and hY4 receptors.

KH064 is a orally active inhibitor of sPLA2-IIA.

KF 17837S is an adenosine A(2a) receptor antagonists, which is potential therapeutic and neuroprotective effects in Parkinson's disease.

JWH015 is a selective CB2 agonist (Ki values are 13.8 and 383 nM as measured at human cloned CB2 and CB1 receptors expressed in CHO cells).

ICI 192605 is a potent thromboxane A2 receptor (TP receptor) antagonist.

IBC 293 is a highly selective agonist for GPR109B (HM74), human orphan G-protein-coupled receptor expressed in adipocytes. IBC 293 is selective for GPR109B over niacin receptor GPR109A (HM74A).

HX 531 is an antagonist of retinoid X receptors.

GYKI53655 Hydrochloride is a non-competitive AMPA and kainate receptor antagonist. GYKI53655 Hydrochloride exhibits anticonvulsant activity. GYKI53655 Hydrochloride also blocks GluK3 homomeric receptors (IC50 = 63 μM) and GluK2b(R)/GluK3 heteroreceptors (IC50 = 32 μM) at high concentrations.

GW542573X is an activator of small-conductance Ca2±activated K+ channels (KCa2).

GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 μM. GW 9578 is a potent lipid lowering agent that may reduce insulin resistance.

GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50 values are 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2 (IC50 values are 0.11 μM for inhibition of HN5, N87 and BT474 tumor cell lines vs. > 30 μM for inhibition of non-tumor cell line HFF).

GSK575594A is a GPR55-selective agonist.

GSK-264220A is an endothelial lipase and lipoprotein lipase inhibitor (IC50 values are 0.13 and 0.10 μM respectively).

GSK4716 is a selective agonist at estrogen-related receptors ERRβ and ERRγ. GSK4716 displays selectivity over ERRα and the classical estrogen receptors.

GR 89696 fumarate is a highly potent and selective κ-opioid agonist (IC50 = 0.04 nM) that may be selective for the putative κ2 receptor. It is anti-nociceptive and neuroprotective in vivo.

m-Phenylenediacetic acid is a bioactive chemical.

DQP-1105 is a negative allosteric modulator of the GluN2C/D NMDA receptor inhibiting receptor function more potently when glutamate is present .

CV-1808 is an adenosine A2 receptor agonist that acts as a coronary vasodilator, antihypertensive and antipsychotic following systemic administration in vivo.

CP 99994 dihydrochloride is a high affinity NK1 antagonist (Ki = 0.145 nM in vitro). CP 99994 dihydrochloride also displays high ex vivo binding potency in gerbil striatum (IC50 = 36.8 nM).

CP-775146 is a selective, high affinity PPARα agonist. CP-775146 exhibits hypolipidemic activity in vivo.

m-Aminoacetanilide is a bioactive chemical.

BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 μM.

UMB-68 is a GHB receptor ligand. UMB68 showed no affinity (IC(50) >100 microM) at GABA(A) or GABA(B) receptors. In vivo studies showed that, at behaviorally active doses, rats trained to discriminate GHB did not recognize the novel ligands as GHB. Thus, UMB68 is a selective GHB receptor ligand in binding assays, will not undergo metabolism to GABA-active compounds, and does not show the same effects as GHB in vivo. These data suggest that, although UMB68 binds to the GHB receptor, it does not have the observed GABA receptor-mediated effects of GHB in vivo and could provide a novel tool for studying the pharmacology of the GHB receptor in the absence of complicating GABAergic effects.

AR-C118925XX is a bioactive chemical.

ARC-239 is an α2-adrenergic receptor agonist.

AL-8810 is a prostaglandin F2α receptor antagonist