Valrubicin (AD-32) is a chemotherapy drug used to treat bladder cancer.

A-779 is a peptide antagonist of the Mas receptor, also known as the angiotensin (1-7) (Ang (1-7)) receptor (IC50 = 0.3 nM in a radioligand binding assay).

A new-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infections, the prodrug of the active compound VM-1500A..

CITCO is a potent constitutive androstane receptor (CAR) agonist (EC50 = 49 nM). CITCO altered expression of key drug-metabolizing enzymes and transporters in human hepatocytes, which positively affects the metabolic profile of CHOP. Coadministration of CITCO and CHOP in the coculture model led to significantly enhanced cytotoxicity in lymphoma cells but not in cardiomyocytes. Constitutive androstane receptor (Car)-driven regeneration protects liver from failure following tissue loss. The constitutive androstane receptor (CAR and NR1i3) is a key regulator of CYP2B6.

EHP-101 (VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. EHP-101 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. EHP-101 attenuates adipogenesis and prevents diet-induced obesity. EHP-101 (20 mg/kg/day; i.p.; for 3 weeks) induces a significant reduction in body weight gain, total fat mass, adipocyte volume and plasma triglycerides levels in HFD mice.

AH-7614 is a selective free fatty acid receptor 4 (FFA4/GPR120) antagonist.

E-3810 is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity.

Ceritinib, also known as LDK-378, is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). In Phase I trials, LDK378 showed a marked clinical response in 78 patients with anaplastic lymphoma kinase positive (ALK+) metastatic non-small cell lung cancer (NSCLC) who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib. LDK378 blocks the ALK protein and stops it sending growth signals to cancer cells, which may stop them growing. Ceritinib was approved in April 2014.

Crizotinib (PF-02341066;PF-2341066) is a potent, selective, orally bioavailable, ATP-competitive inhibitor of c-Met catalytic activity with Ki of 4 nM.

PFI-90 is a selective inhibitor of the histone demethylase KDM3B. PFI-90 induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo.

A small molecule inhibitor of the NF-κB family member c-Rel with IC50 of 3 uM in EMSA assays.

An enantiomer of Ibuprofen that is generally not considered a COX inhibitor and is instead thought to be involved in pathways of lipid metabolism as it is incorporated into triglycerides along with fatty acids.

TCEP (Tris(2-carboxyethyl)phosphine) hydrochloride, a non-thiol reducing agent, promotes NF-κB-DNA binding in a dose-related manner.

Ervogastat (PF-06865571) is a potent and well-tolerated diacylglycerol acyltransferase 2 inhibitor (DGAT2i). Ervogastat alone reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH). Ervogastat combination with Clesacostat (an acetyl CoA-carboxylase inhibitor (ACCi)) can be used for the research of NASH with liver fibrosis therapy.

OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03   nM in non-HP cancer cells and 2.89   nM in HP cancer cells, respectively.

TRO19622, a small cholesterol-like molecule, is a neuroregenerative and neuroprotective compound.

Trans-4-Phenyl-3-buten-2-one (trans-Benzylideneacetone, trans-Benzalacetone, trans-Benzylideneacetone) is an inhibitor of the enzyme phospholipase A2 (PLA2). Trans-4-Phenyl-3-buten-2-one is used as a flavouring agent, a fragrance and a bacterial metabolite.

TMP778 (TMP-778) is a potent, selective RORγt inhibitor with IC50 of 7 nM in FRET assays and 63 nM in IL-17 promoter assays, with no inverse agonist activity.

A novel potent, selective, competitive and orally active DPP4 inhibitor with potential for the treatment of type 2 diabetes.

ZK824859 is a selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.

PF-06424439 is a potent and selective Diacylglycerol Acyltransferase 2 ( DGAT2) inhibitor with DGAT2 IC50 ± SEM (nM) (human/rat/dog) 14 ± 1/38 ± 4/16 ± 1. PF-06424439 demonstrated excellent ADMET properties and decreased circulating and hepatic lipids when orally administered to dyslipidemic rodent models. PF-06424439 inhibited DGAT2 of different species (human, rat, and dog) with similar potency. Among related acyltransferases, no significant inhibition was observed for PF-06424439 (up to 50 μM) against human MGAT2 or MGAT3, DGAT1, or mouse MGAT1, indicating a high selectivity (>2000-fold) against these enzymes.

MCU-i4 is a negative modulator of the mitochondrial calcium uniporter (MCU) complex that directly binds a specific cleft in MICU1 and decreases mitochondrial Ca2+ influx.,MCU-i4 decreases mitochondrial Ca2+ influx. Docking simulations reveal that MCU-i4 directly binds a specific cleft in MICU1, a key element of the MCU complex that controls channel gating. Accordingly, in MICU1-silenced or deleted cells, the inhibitory effect of MCU-i4 is lost. Moreover, MCU-i4 fails to inhibit mitochondrial Ca2+ uptake in cells expressing a MICU1 mutated in the critical amino acids that forge the predicted binding cleft.[1]

KEA1-97 (KEA 1-97) is a small molecule that disrupts the interaction of thioredoxin with caspase 3.

SC144 is an orally active small-molecule gp130 inhibitor.

A des acryl analogue of AZD9291 that is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant..

AC710, is a potent Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases.

mutant EGFR inhibitor B30 is a potent, selective, next-generation EGFR mutants inhibitor with IC50 of 1.1 and 7.2 nM for EGFRL858R and EGFRL858R/T790M/C797S, respectively.

JFD01307SC is a glutamine synthetase inhibitor and anti-tuberculosis agent. JFD01307SC acts as a mimic of L-Glutamate and thus target enzymes involved in glutamine biosynthesis.

Ataciguat (HMR-1766) is a potent, specific soluble guanylate cyclase (sGC) activator with EC50 of 0.51 uM, preferentially activates the NO-insensitive heme-oxidized form of sGC.

Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.