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.

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.

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.

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.

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.

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.

CCT129202 is a potent, selective, ATP-competitive pan-Aurora kinase inhibitor with IC50 of 42, 198 and 227 nM for Aurora A, Aurora B and Aurora C, respectively.

NS-018 maleate (NS018, Ilginatinib) is a potent and highly selective JAK2 inhibitor (IC50=0.72 nM).

AZ12216052 is a mGluR II and III activator.

ML 351 is a selective 12/15 LOX inhibitor that is active in vivo.

MJ-15 is a potent and selective antagonist of cannabinoid CB1 receptor.

Arcyriaflavin A is an inhibitor of cdk4/cyclin D1 and CaM kinase II.

NSC 625987 is a potent, selective CDK4 inhibitor with IC50 of 0.2 uM, displays >500-fold selectivity over CDK2 (IC50 >100 uM for cdc2/cyclin A, cdk2/cyclin A and cdk2/cyclin E). .

VU0155069 is a potent, selective phospholipase D1 (PLD1) inhibitor with IC50 of 46 nM, 20-fold selectivity over PLD2 (IC50=933 nM).

TL02-59 is a potent, selective, orally available inhibitor of Src-family kinase Fgr IC50 of 0.03 nM, also inhibits Lyn and Hck with IC50 of 0.1 and 160 nM, respectively.

Chlorantraniliprole is an insecticide that potently and selectively activates insect ryanodine receptor, with EC50s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ∼300-fold more potent than that in the mouse myobla

NVP-MELK8a hydrochloride (MELK8a hydrochloride) is a novel potent, and selective MELK inhibitor with IC50 of 2 nM.

NMS-E973 is a novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). NMS-E973 displays significant efficacy in a human ovarian A2780 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known Hsp90 client proteins, and with a favorable pharmacokinetic and safety profile. The efficacy profile of NMS-E973 suggests a potential for development in different clinical settings, including tumors that have become resistant to molecular targeted agents, particularly in cases of tumors which reside beyond the blood-brain barrier (BBB).