Nimbolide is a natural inhibitor of pancreatic cancer growth and metastasis through ROS-mediated apoptosis. It inhibits epithelial-to-mesenchymal transition.

OP-3633 is a potent steroidal glucocorticoid receptor (GR) antagonist with IC50 of 29 nM and shows excellent selectivity against GR over progesterone receptors (PR) and androgen receptors (AR).

UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM). UDM-001651 was evaluated in a monkey thrombosis model and shown to have robust antithrombotic efficacy and no prolongation of kidney bleeding time. This combination of excellent efficacy and safety margin strongly validates PAR4 antagonism as a promising antithrombotic mechanism.

VU6003586 is a novel allosteric modulators of mGlu5 with EC50 of 174 nM.

Ziresovir (RO-0529, AK0529) is a potent, selective and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein inhibitor with EC50 of 3 nM.

DS44960156 is a selective Methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor, with IC50 values of 1.6 μM and >30 μM for MTHFD2 and MTHFD1, respectively.

BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay.

RA306 (RA-306) is a selective, potent, orally active, ATP-competitive CaMKII inhibitor, inhibits CaMKII delta (IC50=15 nM), gamma (IC50=25 nM), and alpha (IC50=61 nM) isoforms.RA306 displays a good selectivity profile vs. kinases and non-kinase targets, as compared with KN-93.RA306 also displays a good cellular activity in cardiomyocytes from human, rat, and mice, with IC50s in the 200 nM range.Isoproterenol-induced phosphorylation of Thr17-PLN, normalized to total PLN, was fully inhibited by RA306 in a dose-dependent manner, with IC50s of 140 nM in rat, 205 nM in mouse, and 220 nM in human cardiomyocytes.

BPN14770 (BPN-14770) is an allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 and 7.4 nM for human PDE4D7 and PDE4D3 respectively, displays 16-fold less potent against monomeric form of PDE4D lacking the UCR1 dimerization domain (PDE4D2

LY3154207 is a potent and selective dopamine receptor D1 positive allosteric modulator for the treatment of Parkinson's disease dementia.

AL-335 is a potent inhibitor of hepatitis C virus (HCV) NS5B polymerase with IE50 values as low as 70 nM. AL-335 is potentially useful for the Treatment of Hepatitis C Infection. AL-335 demonstrated high levels of the nucleoside triphosphate in vitro in primary human hepatocytes and Huh-7 cells as well as in dog liver following a single oral dose. AL-335 was selected for the clinical development where it showed promising results in phase 1 and 2 trials.

KMN-159 is a potent prostaglandin E2 type 4 (EP4) receptor agonist with Ki of 0.38 nM and shows five fold increase in potency versus KMN-80.

KZR-616 (KZR616) is a potent, selective dual immunoproteasome subunit LMP7/LMP2 inhibitor with IC50 of 39 nM/139 nM, weakly inhibits β5, MECL-1 and no acitivty against β1 subunit.

NRX-1933 is an enhancer of an E3 ligase-substrate interaction.

NRX-1532 is an enhancer of an E3 ligase-substrate interaction.

(R,R)-BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs.

NLX-204 is a potent and selective ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist with pKi = 10.19. NLX-204 displayed high selectivity in the SafetyScreen44 panel (including hERG channel), high solubility, metabolic stability, and Caco-2 penetration and did not block CYP3A4, CYP2D6 isoenzymes, or P-glycoprotein. Preliminary in vivo studies confirmed its promising pharmacokinetic profile. NLX-204 also robustly stimulated ERK1/2 phosphorylation in rat cortex and showed highly potent (MED = 0.16 mg/kg) and efficacious antidepressant-like activity, totally eliminating immobility in the rat Porsolt test.

BMS-986166 (BMS986166) is a potent, selective S1P receptor modulator for the treatment of ulcerative colitis..

AES-135 (AES135) is a novel HDAC inhibitor that biochemically inhibits HDACs 3, 6, 8 and 11 with IC50 values of 190-1100 nM.

EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.

MIDD0301 is a potent, positive allosteric, α5β3γ2 selective, GABAA receptor (GABAAR) ligand with EC50 of 17 nM, shows no significant binding at the peripheral GABAAR at 10 uM.

CB-6644 is a selective inhibitor of RUVBL1/2 complex with anti-cancer activity. CB-6644 blocks the ATPase activity of RUVBL1/2 with an IC50 of 15 nM.

LAS190792 (AZD8999) is a potent muscarinic antagonist and β2-adrenoceptor agonist with pIC50 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6 for M1, M2, M3, M4, M5, β1, β2, β3, respectively. LAS190792 can be used as a bronchodilator.

Elenbecestat (E2609) is a novel potent, oral BACE1 inhibitor for treatment of Alzheimer's disease..

beta-secretase inhibitor.

T-448 (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts.

AZD 5991 (AZD5991) is a potent and selective macrocyclic inhibitor of Mcl-1 with sub-nanomolar affinity.

ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively.

VT-1598 is a potent, high-affinity, oral inhibitor of fungal sterol 14α-demethylase (CYP51B) with Kd of 13 nM.

CL27c is a cell-permeable, inhaled lipophilic ester prodrug of CL27e, which is a potent, selective pan-class I PI3K inhibitor, CL27c is inactive in PI3K enzymatic assay, once inside the cytoplasm, CL27c is metabolized by unspecific esterases into CL27e.