PCO371 is a novel, orally active small molecule that acts as a full agonist of PTHR1.

JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.

DX600 is a potent and selective peptide inhibitor of angiotensin-converting enzyme 2 (ACE2; Kis = 2.8, 200, and 1,200 nM for recombinant, human, and murine ACE2, respectively).

Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.

GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.

LSZ102 is a potent, orally bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.

AT-406 (formerly known as SM-406) is an orally bioavailable potent IAP (inhibitor of apoptosis protein) of XIAP, cIAP1, and cIAP2 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, respectively.

DSM265 is a PfDHODH inhibitor with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of P. falciparum 3D7 parasites with an EC50 of 4.3 nM.

ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).

AB-423 is the first-generation Hepatitis B Virus Capsid Assembly inhibitor, which was generally safe and well tolerated in Phase 1 healthy volunteer studies.

ORY-1001 dihydrochloride (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases.

ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.

GW501516 is the most selective and potent PPARβ (EC50=1.1nM) agonist that has been demonstrated to be 1,000-fold more selective in comparison to existing subtypes.

Enclomiphene is a non-steroidal estrogen receptor antagonist that promotes gonadotropin-dependent testosterone secretion by the testes.

BLU-285 is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.

SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.

CP-547632 is as a potent inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases (IC50 11 and 9 nM, respectively).

Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.

Calcifediol is a major circulating metabolite of vitamin D3, acting as a competitive inhibitor with an apparent Ki of 3.9 μM, suppresses PTH secretion and mRNA (ED50=2 nM).

Molnupiravir, also known as EIDD-2801 and MK-4482, is an orally bioavailable form of a highly potent ribonucleoside analog that inhibits the replication of multiple RNA viruses including SARS-CoV-2, the causative agent of COVID-19. EIDD-2801 has been show

Activator of soluble guanylyl cyclase (sGC); acts at a nitric oxide (NO)-independent regulatory site in the sGC α1 subunit. Inhibits platelet aggregation (IC50 = 36 nM) and phenylephrine-induced contractions of rabbit aorta (IC50 = 0.30 μM). Also reduces vascular smooth muscle growth through cAMP- and cGMP-dependent PKA and PKG pathways.. For the detailed information of BAY 41-2272, the solubility of BAY 41-2272 in water, the solubility of BAY 41-2272 in DMSO, the solubility of BAY 41-2272 in PBS buffer, the animal experiment (test) of BAY 41-2272, the cell expriment (test) of BAY 41-2272, the in vivo, in vitro and clinical trial test of BAY 41-2272, the EC50, IC50,and affinity,of BAY 41-2272, Please contact DC Chemicals.

Delgocitinib (JTE-052, LEO 124249) is a potent, selective, orally active, pan-JAK inhibitor with IC50 of 2.8, 2.6, 13 and 58 nM for JAK1,2,3 and Tyk2, respectively.

CMX001 (Brincidofovir; HDP-CDV) was developed as an orally active, lipophilic form of cidofovir (CDV); has enhanced activity in vitro and in vivo compared to CDV against certain herpesviruses, adenoviruses and orthopoxviruses.IC50 Value: 5.5 nM (EC50, in PDA at 7 dpi) [3]Target: anti-CMVCMX001 is currently in Phase II clinical studies for development as a therapeutic agent for human CMV, adenovirus and BK virus infections, as well as, for adverse events following smallpox vaccinations.in vitro: In PDA at 7 dpi, the CMX001 50% effective concentration (EC50) was 5.55 nM, the 50% cytotoxic concentration (CC50) was 184.6 nM, and the 50% selectivity index (SI50) was 33.3. The EC90 was 19.7 nM, the CC90 was 5,054 nM, and the SI90 was 256.1. In COS-7 cells, JCV replication was faster and the EC50 and EC90 were 18- and 37-fold higher than those in PDA, i.e., 0.1 μM and 0.74 μM (CC50, 0.67 μM; SI50, 6.7; CC90, 12.2 μM; SI90, 16.5) at 5 dpi [3].in vivo: CMX001 and CDV are equally efficacious at protecting mice from mortality following high ectromelia virus doses (10,000 x LD(50)) introduced by the intra-nasal route or small particle aerosol. Using CMX001 at a 10mg/kg dose followed by 2.5mg/kg doses every other-day for 14 days provided solid protection against mortality and weight loss following an intra-nasal challenge of (100-200) x LD(50) of ectromelia virus [1]. When CMX001 was administered orally to mice infected with HSV-1, mortality was reduced significantly (p≤0.001) with all three dose levels when treatments were initiated 24 h post viral inoculation. When treatments were started 48 h post viral inoculation, 5 and 2.5 mg/kg significantly reduced mortality (p≤ 0.001). If treatments were delayed until 72 h post viral inoculation, CMX001 did not reduce mortality or increase the mean day to death. When mice were infected intranasally with HSV-1 and treatments initiated 24 h post viral inoculation using CMX001 at 5 mg/kg or ACV at 100 mg/kg, virus replication in target organs was reduced by both CMX001 and ACV when compared to vehicle treated mice [2]. Toxicity: Diarrhea was the most common adverse event in patients receiving CMX001 at doses of 200 mg weekly or higher and was dose-limiting at 200 mg twice weekly. Myelosuppression and nephrotoxicity were not observed [4].

CK-2127107(CK-107, Reldesemtiv) is a novel orally active fast skeletal troponin activator, selectively activates fast skeletal myofibrils with EC50 of 3.4 uM.

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

beta-secretase inhibitor.

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.

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

PC786 (PC-786) is a potent non-nucleoside RSV L-protein polymerase inhibitor with IC50 of 2.1 nM and 0.5 nM in cell-free enzyme assay and mini-genome assay in HEp-2 cells, respectively.