MRS 2219 is a selective potentiator of ATP-evoked responses at rat P2X1 receptors (EC50 = 5.9 μM).

MRS1191 is a selective A3 adenosine receptor antagonist.

ML218 HCl is a selective inhibitor of T-type calcium channels (IC50 values are 270 and 310 nM for Cav3.3 and Cav3.2 respectively in a patch EP assay). ML218 HCl decreases burst activity in STN neurons; reduces cataleptic behaviour in an in vivo rat model of Parkinson's disease.

ML169 is a novel, selective and brain penetrant M1 positive allosteric modulator (PAM).

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).