3-(4-Pyridyl)indole is a ROCK-I inhibitor (IC50 = 25 µM) that promotes cell spreading, inhibits membrane blebbing, and induces dissolution of actin stress fibers in a wound healing assay

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ICI-118,551 is a selective beta-2 (β2) adrenergic receptor antagonist.ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor.

HPI-1 is a Hedgehog (Hh) pathway inhibitor that suppresses signaling through Shh (IC50=1.5 uM) without significantly affecting Wnt signaling (IC50>30 uM).

PDI inhibitor 16F16 is a protein disulfide isomerase (PDI) inhibitor, first identified in a screen for compounds that prevent apoptosis induced by mutant huntingtin protein. 16F16 not only suppressed apoptosis induced by the misfolded protein mutant hungtingtin, it also protected rat neurons from cell death triggered by Aβ peptide. The actions of this inhibitor helped to identify a new mechanism in which a cell death pathway is regulated by protein misfolding via PDI upregulation.

Netoglitazone, also known as isaglitazone and MCC-555, is an agent belonging to the glitazone class of antidiabetic agents with antihyperglycemic activity. Netoglitazone exerts both peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist activity. Netoglitazone decreases bone formation and increases marrow adipocyte formation in vivo.MCC 555 (Isaglitazone.

Psora-4 is a potent and selective Kv1.3 potassium channel blocker with EC50 of 3 nM.

CP-339818 is a potent, selective, non-peptide KV1.3 channel antagonist with IC50 of 200 nM.

A small molecule inhibitor of PP2C that activates extensive 3' cleavage at a concentration 50-fold below that required by fluoride or CP..

A potent, non-prostanoid prostacyclin partial agonist that potently inhibits human (IC50=35 nM), rabbit (IC50=136 nM) and rat (IC50=1.3 uM) platelet aggregation.

A potent, selective α2A-adrenoceptor antagonist with Ki of 1.7 nM, 80-fold selectivity over α2B-adrenergic receptors.

Tetradecanoylcarnitine is a human carnitine involved in β-oxidation of long-chain fatty acids.

(Z)-4-hydroxy Tamoxifen is a major phase I metabolite of tamoxifen, a well-known estrogen receptor antagonist in breast but partial estrogen receptor agonist in endometrium.

A small molecule corrector of ΔF508-CFTR with IC50 of 6.0 uM..

A potent nuclear receptor TR3 (Nur77)-specific targeting compound that can induce melanoma autophagy through a mitochondrial signaling pathway.

LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.

Salbutamol is an agonist of the β2-adrenergic receptor (β2-AR; Kd = 759 nM in a radioligand binding assay using CHO cells expressing the human receptor).

IP6K1 inhibitor TNP is a potent, selective inositol hexakisphosphate kinase IP6K with IC50 of 0.47 uM (IP6K1), does not inhibit either human or yeast Vip/PPIP5K.

SMIFH2 is a small molecule formin homology 2 domains inhibitor of formin-mediated actin assembly, targets formins from evolutionarily diverse organisms including yeast, nematode worm, and mice with IC50s of 5-15 uM.

NNC-711 is a potent and selective inhibitor of GABA uptake by GAT-1 with IC50 of 0.04 uM.

A potent, selective, orally active cannabinoid CB2 receptor inverse agonist with Ki of 35.9, 1.55 and 0.38 nM for human, mouse and rat CB2, respectively.

IC 86621 is a potent DNA-PK inhibitor with IC50 of 135 nM, also inhibits p110β (IC50=135 nM), less potent for p110α/γ/δ (IC50=880-1,400 nM).

FR 900098 is a derivative of fosmidomycin that inhibits DOXP reductoisomerase, demonstrates antimalarial activity with IC50 of 170, 170, and 90 nM for HB3, A2, and Dd2 P. falciparum strains, respectively..

ENMD-1068 is a novel selective PAR2 antagonist without inhibitory activity against thrombin-mediated PAR3 and PAR4 signaling.

DAPH-1 (CGP 52411) is a small molecule that directly inhibits prion protein Sup35 prionogenesis with IC50 of 0.58 uM, inhibits and reverses the formation of Aβ42 fibers and reduces their toxicity to neurons in culture.

A potent 20S proteasome inhibitor with IC50 of 49 nM (inhibition of proteasomal chymotrypsin-like proteolytic activity)..

CJ-13610 is a potent 5-Lipoxygenase (5-LO) inhibitor that suppresses 5-LO product formation with IC50 of 70 nM.

A potent, selective 5-HT2B receptor agonist with pKi of 7.1, >10-fold selectivity over 5-HT2A, 5-HT2C, and other 5-HT subtypes.

A potent, selective and ATP-competitive CK2 inhibitor with Ki of 0.5-1 uM.

Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation.