PD-173212 is a small molecule N-type calcium channel blocker.

SU056 is an inhibitor of Y box binding protein 1 (YB-1) with IC50 of 1.73 μM in Sk0V3 cells.

RP 70676 is a potent and orally bioavailable inhibitor of ACAT.

CID755673 is a potent and selective cell-active small molecule inhibitor for PKD with an IC50 of 182 nM; exhibits selective PKD1 inhibition when compared with AKT, PLK1, CAK, CAMKIIα, and PKC isoforms.

TTK21 (CBP-p300 activator TTK21) is a small molecule activator of CBP/p300 histone acetyltransferase activity with a maximal effect at a concentration of 275 uM.

Potent, selective, and  competitive 15-hydroxyprostaglandin dehydrogenase (15-PGDH; HPGD) inhibitor

A cell-permeable benzochromene that selectively impairs the viability and growth of IGF2-overexpressing hepatocellular carcinoma cells, binds to MFP-2, stimulates the expression of IGFBP-1 and SOCS-3 through activation of STAT6.

A potent, selective, brain penetrant PDE10A inhibitor with Ki of 4 nM.

A potent blocker of voltage-gated potassium channels Kv7 (KCNQ) that enhances ACh release from rat hippocampal slices in vitro with EC50 of 0.7 uM.

Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS).

SBS is a useful probe and tool molecule for detecting amyloid deposits in systemic amyloidosis in vitro and in vivo. SBS can be used for detecting amyloid fibrils in autopsy and biopsy samples from patients with localized amyloidosis, such as familial prion disease, and systemic amyloidosis, such as familial amyloidotic polyneuropathy, amyloid A (AA) amyloidosis, light chain (AL) amyloidosis, and dialysis-related amyloidosis.

TCS 46b is an orally active, subtype-selective GluN1A/GluN2B NMDA receptor antagonist

PUM00199, also known as PARP10-IN-3, is a selective mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10.

KR-32568 is an inhibitor of the sodium-hydrogen exchanger isoform-1 (NHE-1; IC50 = 230 nM). It restores cardiac contractile function ex vivo in an isolated ischemic rat heart model when used at a concentration of 10 μM.

“Compound 14d” (Shionogi & Co.) is a highly potent, dose-dependent adenosine monophosphate activated protein kinase (AMPK) activator being investigated for its blood-glucose-lowering effects.

compound 27, is a potent (13 nM) CNS-penetrant compound that reduces very long chain fatty acid (VLCFA) levels in the CNS, which are believed to be pathological in the rare disease adrenoleukodystrophy (ALD). The starting point came from an HTS on compounds from an internal collection.

Overcoming FGFR mutation resistance and FGFR1-mediated hyperphosphatemia toxicity through isoform-selective FGFR2/3 inhibition. “Compound 29” is an ATP-competitive fibroblast growth factor receptor (FGFR) 2/3 inhibitor with subnanomolar potency.

“Compound 6” (Novartis) is a first-in-class YAP-TEAD protein-protein inhibitor. The TEAD transcription factor and its coactivator YAP and WWTR1/TAZ of the Hippo pathway are responsible for directly regulating the expression of genes involved in cell proliferation and organ size.

“compound 4e” (Chiesi Farmaceutici) is an inhaled p38α/β mitogen-activated protein kinase (MAPK) inhibitor being developed for lung inflammatory diseases.

”Compound 53” (University of Texas Southwestern Medical Center) is a stimulator of interferon (IFN) genes (STING) agonist.

RET-IN-14 (compound 49) is a potent RET inhibitor with IC50s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research

FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.

DN-1289 is a potent and selective dual DLK/LZK inhibitor. DN1289 demonstrated excellent in vivo plasma half-life across species and is anticipated to freely penetrate the central nervous system with no brain impairment based on in vivo rodent pharmacokinetic studies and human in vitro transporter data. Proximal target engagement and disease relevant pathway biomarkers were also favorably regulated in an in vivo model of amyotrophic lateral sclerosis.

BI685509 is a soluble guanylate cyclase (sGC) activator taken orally, with potential to treat diabetic and kidney diseases. In both rat and human platelets, BI685509 was found to restore/enhance cGMP, but had no effect on the functionality of nitric oxide pathways. BI685509 is currently undergoing phase 2 trials for the treatment of diabetic nephropathy, with the aim of improving kidney function.

RMC-5552 is a potent and selective inhibitor of mTORC1. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 has anti-cancer activity.

EG-011 is the first-in-class and potent Wiskott-Aldrich syndrome protein (WASP) activator. EG-011 activates the auto-inhibited form of WASP with strong actin polymerization. EG-011 has selective anti-tumor activity in lymphomas.

ENT-01 shows promise in the treatment of constipation in those with Parkinson's disease (PD) by preventing or reducing the formation of αS aggregates that form in enteric neurons. ENT-01 has undergone Phase 2b clinical trials to evaluate the safety and efficacy of the orally administered drug for the alleviation of constipation in those with PD.

UCB7362 is an orally active and potent antimalarial plasmepsin X (PMX) inhibitor, with an IC50 of 7 nM. UCB7362 inhibits parasite growth.

AN15368 (AN 15368) is a small molecule prodrug activated by parasite carboxypeptidases to yield a compound that targets the messenger RNA processing pathway in Trypanosoma cruzi (T. cruzi), exhibits potent in vitro activity against T.

UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC50 of 79 nM. UR-MB108 is stable in blood plasma.