ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.

MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.

(R)-ZINC-3573 is a potent, selective agonist of the atypical opioid receptor MRGPRX2 (EC50=0.76 uM), showing little activity against 315 other GPCRs and 97 representative kinases.

H3B-120 is a competitive, selective and allosteric inhibitor of carbamoyl phosphate synthetase 1 (CPS1) with IC50 of 1.5 μM and Ki of 1.4 μM. H3B-120 exhibits anti-tumor activity.

(S)-ZINC-3573 is a negative control for (R)-ZINC 3573. (S)-ZINC-3573 displays no activity at MRGPRX2 at concentrations below 100 μM.

PSB1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist. PSB1115 has Ki values are 53.4, > 10000 and > 10000 nM at human A2B, A1 and A3 receptors respectively. It produces potent analgesic effects in vivo.

SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice.

Novel, potent and specific inhibitor of sphingosine kinase-1 (SphK1)

MRS1220 is a potent and highly selective antagonist at the human A3 adenosine receptor (Ki values are 0.65, 305, and 52 nM at hA3, rA1 and rA2A respectively. MRS1220 displays an IC50 value > 1 μM for inhibition of binding to rat A3 receptors.

AGI-25696 (AGI 25696) is a potent and selective inhibitor of methionine adenosyltransferase MAT2A, blocks the growth of MTAP-deleted tumors in vivo.

Enclomiphene ((E)-Clomiphene) dihydrochloride is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene dihydrochloride can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.

Neurokinin receptor antagonist with antiemetic activity

ITX-5061 is a scavenger receptor B1 antagonist that promotes high-density lipoprotein (HDL) levels.

UKH-1114 (UKH1114) is a potent, sigma 2 receptor/Tmem97 agonist with Ki of 46 nM.

NACE2i is a cell permeable, specific and selective peptide inhibitor of nuclear ACE2, inhibits binding between IMP1α and ACE2 and SARS-CoV-2 viral replication. NACE2i specifically targets nuclear ACE2 and not other nuclear proteins targeted by the importin pathway. NACE2i has no impact on ACE2 enzymatic activity. NACE2i prevents inflammation and macrophage infiltration, and increases NK cell infiltration in bronchioles. NACE2i treatment increases the levels of the active histone mark, H3K27ac, restores host translation in infected hamster bronchiolar cells, and leads to an enrichment in methylated ACE2 in hamster bronchioles and lung macrophages. NACE2i has a dual mode of action: suppressing the lethal inflammation in severe COVID-19 and inhibiting viral replication by restoring host translation of anti-viral cytokines.

Allopole is the first allosteric, specfic and cell-permeable inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1), Allopole is the prodrug of Allopole-A.

PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.

TAK-242 (Resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4.

BRD 7389 is an inhibitor of ribosomal S6 kinases (RSK) with IC50 of 1.5 uM, 2.4 uM, and 1.2 uM for RSK1, RSK2, and RSK3, respectively.

CPT is a potent adenosine A1 receptor antagonist.

SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparum spermidine synthase. SpdSyn binder-1 can be used for the research of malaria.

A2ti-2 is a selective and low-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 230 μM. A2ti-2 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-2 prevents human papillomavirus type 16 (HPV16) infection.

LUN76721 has CAS#4376-72-1, is a cyclophosphazene and a useful chemical reagent. Cyclophosphazenes have been studied among others as flame retardant additives, high temperature fluids, clathrates, photostabilizers, or antioxidants in organic polymers. Cyclophosphazenes have also been used as phase transfer catalysts, as polypodants and cryptands. Cyclophosphazenes have also been successfully used as biologically active agents. Moreover cyclotriphosphazenes, were used for polymer functionalization and synthesis, as pendant groups or monomers for polyphosphazene synthesis, especially those bearing six chlorine atoms or phenoxy groups.

Metipranolol is a non-selective beta blocker used in eye drops to treat glaucoma. It is rapidly metabolized into desacetylmetipranolol.

GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 also is a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.

TC-DAPK 6 is an oxazalone compound that acts as a potent, ATP-competitive, and highly selective death-associated protein kinase (DAPK) inhibitor (IC50 = 69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 uM ATP).

MINA53 inhibitor (Compound 10) is a first-in-class inhibitor of the ribosomal oxygenase MINA53 with an IC50 of 1.5 μM in vitro.

RHPS4 is a potent inhibitor of Telomerase at submicromolar.

Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.