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.

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.

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

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.

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.

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.

Prednisolone sodium phosphate is a water soluble form of prednisolone, a glucocorticoid. It is used to treat a variety of inflammatory and autoimmune conditions and some cancers. It is the active metabolite of the drug prednisone and is used especially in patients with liver failure, as these individuals are unable to metabolize prednisone into active prednisolone.

Linderalactone showed significant inhibitory effects on superoxide anion generation by human neutrophils in response to fMLP/CB, values of IC5 is 8.48 μg/mL.

SRS16-86 is an inhibitor of ferroptosis. It inhibits ferroptosis induced by erastin in HT-1080 and NIH3T3 cells. SRS16-86 prevents renal tubular damage and increases in serum levels of urea and creatine in a mouse model of renal ischemia-reperfusion injury (IRI). In a rat model of spinal cord injury, SRS16-86 increases the levels of glutathione peroxidase 4 (GPX4), system xc- cystine/glutamate transporter (xCT), and glutathione (GSH) and decreases levels of IL-1β, TNF-α, ICAM-1, and the lipid peroxidation marker 4-hydroxy nonenal (4HNE) in injured spinal cord epicenters. It also increases tissue sparing and improves locomotor recovery in the same model.

A novel potent, specific TOPK inhibitor that has no effect on ERK1, JNK1, or p38 kinase activity.

MT-802 (MT802) is a potent BTK PROTAC that induces degradation of both wild-type and C481S mutant BTK (DC50=9.1 nM).

A potent, selective, orally available inhibitor of both native and mutant Bcr-Abl with IC50 of 20-80 nM.

5-BDBD is a selective inhibitor of P2X4.

ONC206 is a chemical analogue of ONC201. ONC206 is a benzyl-flurobenzyl imipridone that has highly potent activity in preclinical models of difficult-to-treat neuroendocrine tumors and sarcomas. ONC206 acts as a selective antagonist of DRD2 at nanomolar concentrations and has broad-spectrum anti-tumor activity. ONC206 may address tumor types where the properties of ONC201 do not permit for complete therapeutic engagement in vivo.

Pizotifen is a serotonin antagonist which acts mainly at the 5-HT1, 5-HT2A, and 5HT2C receptors with some antihistamine activity.

Irigenin, an α-glucosidase inhibitor, which has anti-inflammatory, anti-cancer, and anti-metastatic effects. Irigenin can inhibit the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 proteins and mRNAs without an appreciable

TRPM4 inhibitor 5 is a potent and selective inhibitor of TRPM4 with IC50 of 1.5 uM (Na+ influx).

Pamufetinib (TAS-115) is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

Isobavachalcone is a natural chalcone first isolated from P. corylifolia that displays antibacterial, antifungal, anticancer, anti-reverse transcriptase, antitubercular, and antioxidant activities in various research models.

Isoliquiritin has significant antidepressant-like, antifungal and anti-cancer activities. It induces apoptotic cell death through upregulating p53 and p21 in the A549 non-small cell lung cancer cells and inhibit the p53-dependent pathway and showed crosst

SM16 is a novel Type I TGF-β signaling inhibitor.

Isomaltose is a glucose disaccharide with an α-(1→6) linkage, as opposed to the α-(1→4) linkage found in maltose.

Isoquercitrin is an inhibitor of Wnt/β-catenin that acts downstream of the β-catenin nuclear translocation; it is also a potential stimulator of bone mineralization used for prophylaxis of osteoporotic disorders.

Isoscopoletin possesses inhibitory activity against hepatitis B virus (HBV) replication; it also shows substantial inhibition against multi-drug resistant CEM/ADR5000 cells and human CCRF-CEM leukaemia cells, with the IC50 value is 1.6 and 4.0 microM, res

Isosilybin is a flavanolignan found in the extract of S. marianum fruits with antioxidant and anticancer activities.It inhibits lipid peroxidation in rat liver microsomes (IC50 = 32 μM) and reduces ADP/Fe3+-induced malondialdehyde (MDA) production and lac

Isosteviol is a derivative of stevioside, a constituent of Stevia rebaudiana, which is commonly used as a noncaloric sugar substitute in Japan and Brazil.