Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension. IC50 value: Ta

Mefuparib(CVL218) hydrochloride is a potent, highly selective, competitive PARP1/2 inhibitor with IC50 of 3.2/1.9 nM, respectively.CVL218 was more potent than Remdesivir in blocking Coronavirus infection of cells and equally as potent as Remdesivir in blocking replication of virus once it has entered the cells.

Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.

Xanthotoxol is a coumarin and a major component in C. monnieri that has diverse biological activities.

BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells[1].

NS-3-008 is a novel small-molecule transcriptional inhibitor of G0s2 (G0/G1 switch 2) with IC50 of 2.25 uM.

MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA).

A nontoxic, orally active heat shock protein (HSP) coinducer and potentiator of the heat shock response.

SBI-0640756（SBI-756） is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex.

BLU-667 (Pralsetinib) is a highly potent, selective, next generation RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion.

A novel prodrug S1P receptor modulator lacking S1P3 receptor agonism to avoid bradycardia associated with fingolimod and other S1P receptor modulators.

PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity

Empesertib (BAY-1161909, BAY1161909) is a potent, selective Monopolar spindle 1 (Mps1/TTK) inhibitor with IC50 of 0.34 nM.

CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively. IC50 value: 0.3 nM (Ki, CB1R) 21 nM (Ki, CB2R) Target: CB1R in vivo: CB1-IN-1 is a novel peripherally restricted cannabinoid 1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice. CB1-IN-1 has great potential to ameliorate this related metabolic syndrome.

Apcin is a cell-permeable, small molecule anaphase-promoting complex/cyclosome (APC/C) inhibitor, which binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.

NEK6 inhibitor 8(ZINC05007751) is a novel inhibitor of the NIMA-related kinase NEK6 with IC50 of 3.4 uM, compound 8 is very selective against NEK1 and NEK6, while no signifcant activity was observed against NEK2, NEK7, and NEK9.

Monomethylauristatin F(MMAF) is an antitubulin agent that inhibit cell division by blocking the polymerization of tubulin; lower cytotoxic activity than MMAE; antibody drug cytotoxin.

PTC299 (PTC-299) is a novel potent inhibitor of dihydroorotate dehydrogenase (DHODH), inhibits hypoxia-induced VEGFA protein production in HeLa cells with IC50 of 1.64 nM.

ALK-IN-1 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.

Elagolix is a Gonadotropin-Releasing Hormone (GnRH) Antagonist.

CB-002 is a novel small molecule that restores p53 function in mutant p53-expressing colorectal cancer cells without toxicity to normal human fibroblasts; increases expression of endogenous p53 target genes NOXA, DR5, and p21 and cell death; decreases the stability of mutant p53 in RXF393 cancer cells and an exogenously expressed R175H p53 mutant in HCT116 p53-null cells.

ER-000444793 is a potent, cyclophilin D-independent inhibitor of mitochondrial permeability transition pore (mPTP) with with IC50 of 2.8 uM.

Hydroxy-dabrafenib is one of the three major metabolites of dabrafenib.

Casein Kinase inhibitor A51 (CKIα inhibitor A51) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=0.5-20 nM, CKIα Kd=5.3 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19; target both CDK7 and CDK9 with low nM Kd values; induces leukemia cell apoptosis at <160 nM, in correlation to the capacity to stabilize p53; shows high and selective sensitivity against leukemic CFUs in colony-forming unit (CFU) assay, without effect on normal hematopoietic CFUs; blocking CKIα together with CDK7 and/or CDK9 synergistically stabilize p53, deprive leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, induce apoptosis, abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1; demonstrates therapeutic efficacy with preserved hematopoiesis and leukemia cure potential in AML mouse models.

MitoBloCK-11 (MB-11) is a s mall molecule inhibitor of mitochondrial protein import possibly acts through transport protein Seo1, but not Tom70 or Tom20; inhibits precursor proteins that contain hydrophobic segments, confers growth in media lacking uracil in a specific manner and affects zebrafish development.

TAK-615 (TAK615) is a potent, selective, negative allosteric modulator (NAM) of the LPA1 receptor, partially inhibits the LPA response with IC50 of 91 nM (60% at 10 uM) in calcium mobilisation assays..

BAL3833 (also known as CCT3833) is an orally available small-molecule panRAF/SRC kinase inhibitor targeting cell proliferation signaling pathways that are associated with tumor growth and resistance development to current therapies. Data from preclinical studies suggest that this class of compounds, targeting the BRAF, CRAF and SRC family kinases, is active in diverse patient-derived melanoma models with intrinsic or acquired resistance to currently marketed BRAF-specific as well as MEK inhibitor therapies.8 Moreover, activity of BAL3833 has also been demonstrated in KRAS-driven cancer models, including non-small cell lung cancer, colorectal cancer and pancreatic cancer.9 BAL3833 has been progressed into a phase 1 study in adult patients with advanced solid tumors including metastatic melanoma.

Alobresib is a novel BET bromodomain inhibitor with antineoplastic activity..

ML417 is a Highly Selective D3 Dopamine Receptor Agonist. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein activation, and ERK1/2 phosphorylation (pERK) while lacking activity at other dopamine receptors. Screening of ML417 against multiple G protein-coupled receptors revealed exceptional global selectivity. Molecular modeling suggests that ML417 interacts with the D3R in a unique manner, possibly explaining its remarkable selectivity. ML417 was also found to protect against neurodegeneration of dopaminergic neurons derived from iPSCs.

NE 10790, a poor farnesyl pyrophosphate synthase inhibitor, is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak antiresorptive agent.