LY456236 HCl is a selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively). LY456236 HCl reduces hyperalgesic behavior induced by formalin in both mouse and rat with ED50 values of 28 and 16.3 mg/kg respectively.

LY 334370 hydrochloride is a selective 5-HT1F receptor agonist (Ki values are 1.87, 16.4, > 100 (IC50)). LY 334370 hydrochloride displays antimigraine effects.

LY2087101 is an allosteric potentiator of α7, α4β2 and α4β4 nAChRs. LY2087101 displays selectivity against α3β4 nAChRs.

LY-165163 is a selective 5-HT1A and 5-HT1D serotonin receptor antagonists.

LP-44 is a high affinity 5-HT7 receptor agonist (Ki = 0.22 nM) that displays selectivity over 5-HT1A and 5-HT2A receptors (200- and > 1000-fold respectively). LP-44 dnduces relaxation of substance P-stimulated guinea pig ileum (EC50 = 2.56 μM).

LG100268 is a potent and selective rexinoid and retinoid-X receptor (RXR) agonist. LG100268 binds to the α, β and γ RXR receptors with an IC50 = 3-4 nM and has no activity at the RAR retinoic acid receptors.

L838417 is a GABAA receptor modulator.

L-759,633 is high affinity, selective CB2 receptor agonist (Ki values are 6.4 and 1043 nM for CB2 and CB1 receptors respectively). L-759,633 potently inhibits forskolin-stimulated cAMP production via CB2 receptors expressed in CHO cells (EC50 = 8.1 nM).

L-750,667 TriHydrochloride is a selective D4 dopamine receptor antagonist.

L-741,626 is a selective D2 receptor antagonist.

L-703,606 is a potent, selective antagonist to the human NK1 receptor.

L690330 is a potent inhibitor of inositol monophophatase. L690330 induces autophagy in COS-7 cells independently of mTOR inhibition.

L659989 is a PAF receptor antagonist.

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).