Icariside I is a metabolite of Icarlin, which could regulate bone remodeling and is recognized as an effective agent for the treatment of osteoporosis.

Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings.

IDE-1 induces definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 125 nM).

IDE-2 is a cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 223 nM for induction of Sox17 expression in ESCs).

Importazole is an inhibitor of importin-β transport receptors.

Ingenol is an extremely weak protein kinase C (PKC) activator.

Irinotecan hydrochloride is the hydrochloride salt of a semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata.

Rucaparib camsylate is a potent, orally available inhibitor of poly ADP-ribose polymerase (PARP) 1 and 2.

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets.

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).

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.

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

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.