RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.

GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.

TAS4464 is a highly potent and selective inhibitor of NEDD8 (IC50 of 0.955 nM). TAS4464 selectively inhibited NAE relative to the other E1s UAE and SAE. TAS4464 treatment inhibited cullin neddylation and subsequently induced the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IκBα in human cancer cell lines. TAS4464 showed greater inhibitory effects than those of the known NAE inhibitor MLN4924 both in enzyme assay and in cells.

Flibanserin is a novel multifunctional serotonin agonist and antagonist (MSAA) that improves sexual functioning in premenopausal women who suffer from reduced sexual interest and desire.

Etoricoxib is a new COX-2 selective inhibitor with anti-inflammatory, antipyretic, analgesic, and potential antineoplastic properties.

Dizocilpine, a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux.

M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09  μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC50 values of  0.53  μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research.

Bifluranol (brand name Prostarex; former developmental code name BX-341) is a synthetic nonsteroidal estrogen of the stilbestrol group related to diethylstilbestrol that has been used as an antiandrogen in the United Kingdom in the treatment of benign prostatic hyperplasia. It exerts functional antiandrogen effects by binding to and activating the estrogen receptor in the pituitary gland, consequently suppressing the secretion of luteinizing hormone (and hence acting as an antigonadotropin) and thereby reducing gonadal androgen production and systemic androgen levels.

Vazegepant (BHV-3500) hydrochloride is a highly soluble CGRP receptor antagonist. Vazegepant hydrochloride is the first intranasal gepant for migraine. Vazegepant hydrochloride may be helpful in effective management of COVID-19 associated pulmonary inflammation.

DDR inhibitor X is a potent discoidin domain receptor (DDR) inhibitor with IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM..

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) with IC50 values of 8nM and 8.2nM for I-IP-10 and I-ITAC, respectively. AMG 487 prevents the chemokines I-IP-10 and I-ITAC from binding to CXCR3. In the cellular assays, AMG 487 inhibits CXCR3-mediated cell migration with IC50 values of 8nM, 15nM and 36nM for I-IP-10, I-ITAC and MIG, respectively.

Vodobatinib (K0706) is a potent, third generation and orally active Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research.

JNJ-18038683 is a potent, selective 5-HT7 receptor antagonist with pKi of 8.19 and 8.20 for rat and human 5-HT7 in cell-based assays.

Aumitin is a novel potent autophagy inhibitor with IC50 of 124 and 244 nM against starvation- and rapamycin- induced autophagy respectively, targets mitochondrial complex I.

Azidoacetic acid NHS ester is a compound containing an azide group and an NHS ester. The azide group can react with alkyne, BCN, DBCO via Click Chemistry to yield a stable triazole linkage. The NHS ester can be used to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.

FICZ is a high affinity aryl hydrocarbon receptor (AhR) agonist with Kd of 70 pM.

Giredestrant, also known as GDC-9545 and RG6171, is a SERD. GDC-9545 is an orally available selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, SERD GDC-9545 specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation.

TAK041(TAK 041) is a potent and selective GPR139 agonist with an EC50 of 22 nM. TAK-041 has the potential for the research of negative symptoms associated with schizophrenia.

Batefenterol Succinate is a first-in-class inhaled bifunctional bronchodilator possessing muscarinic receptor antagonist and β2-adrenoceptor agonist properties.

SWN41522, also known as DUPA and FN11, is a potent Urea-​Based Inhibitor of Glutamate Carboxypeptidase II (NAALADase). In vivo antitumor tests using U-​87 glioblastoma xenograft showed that FN11 reduced tumor vol. to a value of ∼0.4-​0.6 (at 10 or 100 μM) after 4 days treatment, and ∼ 1.0 (at both dosages) after 7 days treatment. The antiangiogenesis activity of FN11 was examd. with similarly grown tumors, and revealed a preponderance of avascular and low vascular areas in tumors treated with FN11 at 100 μM. It was first reported in patent WO 2000064911 and Journal of Medicinal Chemistry (2001), 44(3), 298-301.

Difelikefalin is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin is selective for KOR over the μ-opioid receptor.

A polyamine oxidase (PAO) inhibitor that inhibits spermine oxidase and N1-acetylpolyamine oxidase with IC50 of 6.1 and 0.02 uM, respectively.

Novel Nox inhibitor，N2-(3,4-Dimethylphenyl)-6-((4-(p-tolyl)piperazin-1- yl)methyl)-1,3,5-triazine-2,4-diamine

Avanafil Impurity 8

CAY10526 is a selective inhibitor of mPGES-1. It also acts as an inhibitor of the NF-κB signaling pathway.

ML353 (VU0478006) is a ovel Silent Allosteric Modulator (SAM) of the Metabotropic Glutamate Receptor 5.

Z-ASTD-FMK is a cell-permeant and irreversible inhibitor of endothelial monocyte-activated polypeptide II (EMAP II).