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

AH13205 is an EP2 prostanoid receptor agonist.

AGN193109 is a retinoic acid receptor (RAR) antagonist.

AFDX384 is potent M2/M4 selective antagonist.

ACT-462206 is an orally active, potent, brain-penetrant dual orexin 1/orexin 2 receptor antagonist.

p38 MAP Kinase Inhibitor IV is an ATP-competitive inhibitor of p38α/β MAPK with IC50 values of 130 nM for p38α and 550 nM for p38β. It is much less active with ≤23% inhibition at 1 μM against p38γ/σ, ERK1/2, and JNK1/2/3. Shown to be more effective than SB 203580 in inhibiting LPS-induced IL-1β release from hPBMC (100% vs. 50% inhibition with 100 μM inhibitor). A recent study showed that p38 MAP Kinase Inhibitor IV could consistently and significantly enhance reprogramming and iPS cell generation from somatic cells.

AC-90179 is a high selective 5-hydroxytryptamine2A receptor inverse agonist. It is an atypical antipsychotic pharmaceutical. It has been shown to alleviate hallucinogen-induced vasocontriction and possible other harmful physical symptoms.

Panepoxydone is a fungal metabolite that inhibits NF-κB transcription factor by preventing IκB phosphorylation, thus inhibiting the release of NF-κB from the IκB : NF-κB complex and its translocation into the nucleus. Panepoxydone also has antimalarial, cytotoxic activities and anti-parasitic activity against Trypanosoma cruzi.

PBOX-6 belongs to a group of tubulin-targeting pyrrolo-1,5-benzoxazepine (PBOX) compounds that potently induce apoptosis in a wide spectrum of cancer cells, including those originating from the four main types of leukemia and those exhibiting multi-drug resistance (IC50 = 2.28 μM/HL60-MDR1, 2.86 μM/HL60-BCG2, 1.91 μM/HL60; IC50 = 4.71 μM/A2780-ADR, 4.10 μM/A2780). PBOX-6 inhibits the assembly of purified tubulin in cell-free assays and causes microtubule depolymerization in MCF-7 cells by binding a tubulin site distinct from those targeted by vinblastine and colchicine. When administered via intratumoral injection (7.5 mg/kg/day) in vivo, PBOX-6 is reported to significantly inhibit tumour growth in a murine model of neuroblastoma and a CML model of the imatinib-resistant T315I mutants.

PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1/2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).

AC-186 is reported as a selective nonsteroidal estrogen receptor agonist.

PF-04279405 is a potent and selective glucokinase activator.

PF-04445597 is a potent, orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP).

PF-04671536 is a highly potent and selective inhibitor of phosphodiesterase 8B (PDE8B) phosphodiesterase 8A (PDE8A). In primary human pancreatic islets, PF-04671536 increases insulin secretion in a glucose-dependent manner.