TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively).

VY-3-135 is an orally active, selective acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC50 value of 44 nM. VY-3-135 displayes no inhibitory activity towards recombinant human ACSS1 or ACSS3. VY-3-135 potently inhibits ACSS2 dependent fatty acid metabolism but has no effect on gene expression in tumors. VY-3-135 inhibits triple negative breast cancer (TNBC) tumor growth in mouse ACSS2high but not ACSS2low tumors models.

Rovalpituzumab is a humanized monoclonal antibody against delta-like protein 3 (DLL3). Rovalpituzumab can be used in the synthesis of antibody-drug conjugate (ADC), Rovalpituzumab Tesirine. Rovalpituzumab has activity against small cell lung cancer (SCLC).

Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab binds to the circulating PCSK9 protein, inhibiting it from binding to the LDLR. Evolocumab can be used for the research of hypercholesterolemia and atherosclerotic cardiovascular diseases.

Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.

TriGalNAc CBz is a GalNAc derivative and tri-GalNAc is an asialoglycoprotein receptor (ASGPR) ligand. TriGalNAc CBz can be used for mRNA drug delivery as well as lysosomal targeted chimerism (LYTAC) studies.

SUCNR1-IN-2 (Statement 35) is a succinate/succinate receptor 1 inhibitor for the study of neurodegenerative diseases such as neuroinflammation.

ATC0175 is a novel nonpeptidic and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist.

CX-6258 HCl is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.

NCGC00378430 (Compound 8430) is a novel small molecule compound that reduces the SIX1/EYA2 interaction in vitro with IC50 of 52 uM in the Alphascreen assay.

p-SCN-Bn-DOTA is a bifunctional chelating agent. p-SCN-Bn-DOTA can simultaneously chelate radionuclides and link monoclonal antibody for radioimmunotherapy of tumor.

SJB7 is a close analog of SPA70 and hPXR agonist, interacts with the ligand-binding domain (LBD) of hPXR..

A combination of clofibrate and niacin, used to treat hyperlipidaemias

Moguisteine is a novel peripheral non-narcotic antitussive drug.

A partial/full agonist of dopamine receptor with Ki of 3.9/2.2/0.5/5.1 nM for D2S/D2L/D3/D4, respeectively.

Alpinumisoflavone (compound 2) is a flavonoid derivative isolated from the stem bark of Erythrina lysistemon Hutch.

Wighteone is a compound isolated from the aerial parts of Genista ephedroides.

Osajin is the major bioactive isoflavone present in the fruit of Maclura pomifera with antitumor, antioxidant and anti-inflammatory activities.

Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM)[1][2][3]. Bexarotene can be used for the research of cutaneous T-cell lymphoma.

A novel small molecule that inhibits GATA4/NKX2-5 transcriptional synergy with IC50 of 3 uM, with no activity on the protein kinases involved in the regulation of GATA4 phosphorylation.

Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.

PD-166793 is a cell-permeable biphenylsulfonylvaline compound that acts as a potent inhibitor against MMP-2, -3, and -13 (IC50 = 47, 12, and 8 nM, respectively) and a weaker inhibitor against AMP deaminase (20% inhibition at 0.1 μM), MMP-1, -7, -9, and -14 (IC50 = 6.1, 7.2, 7.9, and 0.24 μM, respectively). Shown to offer therapeutic benefits in vivo in various animal models of heart failure and diabetes.

TC KHNS 11 is a potent and selective PI 3-kinase δ inhibitor that is orally bioavailable.

Novel Integrin very late antigen-4 (VLA-4; α4β1) antagonist, blocking the activation of inflammatory cells.

FK-888 is a selective, high affinity tachykinin NK1 receptor antagonist (Ki = 0.69 nM) that displays 320-fold selectivity for human over rat NK1 receptors. FK-888 inhibits substance P-induced contraction of isolated guinea pig trachea (IC50 = 32 nM) and inhibits substance P-induced airway constriction in vivo.

ML354 (VU0099704) is a novel potent and selective PAR4 antagonist with IC50 of 140 nM, displays 71-fold selectivity versus PAR-1.

Carbodenafil is a Sildenafil (UK-92480) related compound found in health foods. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

CDK9 inhibitor HH1 is a novel potent, highly selective CDK9 inhibitor..

CHDI-390576 (CHDI390576) is a potent, cell permeable and CNS penetrant class IIa HDAC inhibitor with IC50 of 54/60/31/50 nM for HDAC4/5/7/9, respectively.

Floctafenine, also known as R-4318 and Idarac, is a cyclooxygenase inhibitor that inhibits prostaglandin synthesis.