BMS-37 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value in the range of 6-100 nM in cell free assays. It was first discovered by Bristol-Myers Squibb. Blockade of the PD-1/PD-L1 immune checkpoint pathway with monoclonal antibodies has provided significant advances in cancer treatment. The antibody-based immunotherapies […]

This product has been discontinued. UM171 (UM-171) is a potent agonist of human hematopoietic stem cell renewal, independently of AhR suppression. UM171 is a synthesized analog of UM729, which is screened out for its ability to expand human CD34+ CD45RA– mobilized peripheral blood cells. UM171 was 10- to 20- fold more potent than UM729 with […]

PF-06737007 (PF06737007) is a novel, potent, selective, peripherally restricted, efficacious, and well-tolerated pan-Trk inhibitor with anti-hyperalgesic activity. In cell-based assays, it inhibits TRK with IC50s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively. It has anti-hyperalgesic effect. Hormones of the neurotrophin family, nerve growth factor (NGF), brain derived neurotrophic […]

GNF179, an optimized 8,8-dimethyl imidazolopiperazine analog, is a novel, potent and orally bioavailable antiparasitic agent that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability. Most malaria drug development focuses on parasite stages detected in red blood cells, even though, to achieve eradication, next-generation drugs […]

GNE-6468 is a novel, potent and selective RORγ (RORc) agonists with an EC50 value of 13 nM in HEK-293 cells. he nuclear receptor (NR) retinoic acid receptor-related orphan receptor gamma (RORγ, RORc, or NR1F3) is a promising target for the treatment of autoimmune diseases. RORc is a critical regulator in the production of the pro-inflammatory […]

JNJ-18038683 is a novel and potent antagonist of 5-Hydroxytryptamine Type 7 (5-HT7) receptor with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively. In rodents, JNJ-18038683 increased the latency to REM sleep and decreased REM duration, and this effect was maintained after repeated administration for 7 days. The compound was effective […]

TASP0415914 is an orally potent phosphoinositide 3-kinase γ (PI3Kγ) inhibitor for the treatment of inflammatory diseases. It demonstrated good potency in a cell-based assay and exhibited in vivo efficacy in a collagen induced arthritis (CIA) model in mice after oral administration.

BMS-751324 is a novel prodrug of BMS-582949 (also known as PS540446) which is a potent and highly selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM and is currently in phase II clinical trials for the treatment of rheumatoid arthritis. BMS-751324 was discovered in search for prodrugs to address the issue of […]

Sabizabulin (VERU-111; ABI-231) is a novel and orally bioavailable tubulin inhibitor that has the potential to treat cancer. It is being developed by Veru Pharm in Phase III clinical trial for the treatment of advanced prostate cancer. VERU-111 is also being evaluated for treating COVID-19 in another phase III study, as it targets microtubules that […]

PF-02575799 is a novel and potent microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.77±0.29 nM. Based on preclinical efficacy and safety data and its potential for producing short-lived, weakly active metabolites, compound 13 (PF-02575799) advanced into phase 1 clinical studies.