ZK93423 is a potent benzodiazepine receptor agonist (IC50 = 1 nM). ZK93423 is non-selective between α1-, α2-, α3- and α5-subunit containing GABAA receptors (Ki values are 4.1, 4.2, 6 and 4.5 nM for inhibition of [3H]Ro15-1788 binding to human recombinant α1β3γ2, α2β3γ2, α3β3γ2 and α5β3γ2 receptors respectively).

YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.

YM976 is an orally active PDE4 inhibitor (IC50 = 2.2 nM). YM976 has low emetogenic activity, suggested to be due to poor brain penetration.

XAP044 is a potent and selective mGlu7 antagonist (IC50 = 88 nM). It inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice. XAP044 displays no effects on the LTP of mGlu7 deficient mice.

WIN 64338 hydrochloride is a potent, non-peptide, competitive bradykinin B2 receptor antagonist.WIN 64338 inhibits [3H]-bradykinin binding on guinea pig trachea with nanomolar affinity but is not active in the rabbit aorta (the classical bradykinin B1 preparation).

WB 4101 hydrochloride is a α1A-adrenergic selective antagonist.

VU0424465 is a potent mGlu5 positive allosteric modulator and agonist

DCPIB is a novel Inhibitor of Volume-Regulated Anion Channels, Distinctly Modulating K2P Channels.

VU0285683 is a negative allosteric modulator of mGlu5 receptors. VU0285683 acts as a full antagonist and blocks the glutamate response to mGlu5 (IC50 = 24.4 nM). VU0285683 is selective for mGlu5 over mGlu1, mGlu3 and mGlu4.

VRT-532 is a CFTR modulator for the treatment of cystic fibrosis.

U69593 is a a selective KOR-1 (κ1-opioid receptor) agonist. U-69593 is known to inhibit cocaine sensitization in meso-limbic dopamine neurons by normalizing basal overflow of dopamine.

TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 μM. It is without effect on EP4, DP1, IP, and β2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost in P388D1 macrophages.

SSR 146977 is a new potent nonpeptide tachykinin NK3 receptor antagonist.

SQ-29548 is a highly selective TP receptor antagonist which binds to the human recombinant TP receptor with a Ki of 4.1 nM. SQ-29548 inhibits the aggregation of washed human platelets induced by U-46619 with an IC50 of 0.06 μM.

SNAP5089 is a subtype-selective α1A-adrenoceptor antagonist that displays > 600-fold selectivity over other adrenoceptors (Kivalues are 0.35, 220, 370, 540, 800 and 1200 nM for α1A, α1B, α2C, α1D, α2B and α2A subtypes respectively and 540 nM for L-type Ca2+ channels).

SM 21 is a novel sigma(2) antagonist.

SM19712 is a nonpeptide endothelin converting enzyme inhibitor.

SKF-83959 HBr is a dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors respectively). SKF-83959 HBr may act as an antagonist in vivo, producing anti-Parkinsonian effects and antagonizing the behavioral effects of cocaine.

SKF-81297 HBr is a selective dopamine D1 receptor agonist, which stimulates motor behaviour of MPTP-lesioned monkeys.

SKF-75670 hydrobromide is a atypical D1DR (dopamine receptor) agonist. It displays antagonist activity in vitro and agonist activity in vivo.

SIB-1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype; displays an IC50 value of 0.3 μM at hmGlu5, compared with > 100 μM at hmGlu1b, hmGlu2, hmGlu6, hmGlu7 and hmGlu8. It positive allosteric modulator at mGlu4 receptors.

SIB-1757 is a highly selective antagonist for the mGlu5 metabotropic glutamate receptor subtype. SIB-1757 displays an IC50 value of 0.4 μM at hmGlu5 compared with > 30 μM at hmGlu1b, hmGlu2, hmGlu4, hmGlu6, hmGlu7 and hmGlu8.

RU 28318, potassium salt is a potent and selective antagonist for the mineralocorticoid receptor (MR). RU 28318, potassium salt inhibits aldosterone production and secretion, and selectively decreases ex-vivo MR binding in the hippocampus of adrenalectomised rats. It also decreases blood pressure in female rats following central administration in vivo.

Ro67-7476 is a positive allosteric modulator of mGlu1 receptors. It potentiates glutamate-induced calcium release (EC50 = 60.1 nM at rat mGluR1a). Ro67-7476 displays no activity at human mGlu1 receptors.

PF0998425 is a bioactive chemical.

PF-04859989 HCl is a brain-penetrable irreversible inhibitor of kynurenine amino transferase II (KAT II), the enzyme responsible for most of the brain synthesis of kynurenic acid. PF-04859989 HCl has been implicated in several psychiatric and neurological disorders, including schizophrenia and bipolar disorder.

PD 168368 is a competitive antagonist of neuromedin B (NMB) receptors (Kis = 15-45 nM for rat and human receptors expressed in various cell lines). It blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors.

PD-156707 is an endothelin A receptor-selective antagonist.

m-Methylphenylacetonitrile is a bioactive chemical.

NS3763 is a noncompetitive antagonist of GLUK5 receptor. NS3763 displays selectivity for inhibition of domoate-induced increase in intracellular calcium mediated through the GLU(K5) subtype (IC(50) = 1.6 microM) of kainate receptors compared with the GLU(K6) subtype (IC(50) > 30 microM). NS3763 inhibits the GLU(K5)-mediated response in a noncompetitive manner. NS3763 selectively inhibits l-glutamate- and domoate-evoked currents through GLU(K5) receptors in HEK293 cells.