Nevanimibe HCl (also known as PD-132301 hydrochloride and ATR-101 hydrochloride), the hydrochloride salt of Nevanimibe, is a novel, selective and potent acyl-coenzyme A: cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. It inhibits ACAT2 with an EC50of 368 nM.

CHMFL-PI3KD-317 is a novel, highly potent, selective and orally bioavailable PI3Kδ inhibitor, with an IC50 of 6 nM, it exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 […]

Satavaptan (formerly also known as SR-121463) is a novel, potent and selective vasopressin V2 receptor antagonist that has the potential for the treatment of hyponatremia. Satavaptan has been shown to improve the control of ascites in cirrhosis in short-term phase II studies. Satavaptan works by reducing the action of the hormone vasopressin that blocks fluid […]

(4E)-SUN9221 is a novel and potent antagonist of α1-adrenergic receptor and 5-HT2 receptor with potential antihypertensive and anti-platelet aggregation activities.

PI3K-IN-6 (compound 20a in related reference: J Med Chem. 2017 Feb 23;60(4):1555-1567) is a novel, potent, oral bioavailable and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. It displayed excellent pharmacokinetic profile and efficacy in a human PTEN-deficient LNCaP prostate carcinoma xenograft tumor model. PI3K-IN-6 […]

PD 90780 is a novel and potent non peptide antagonist of nerve growth factor (NGF) which binds to the P75 NGF receptor, and inhibits NGF-p75 NTR interaction with IC50s values of 23.1 µM and 1.8 µM in PC12 cells and PC12 nnr5 cells, respectively .

TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator (PAM). EC50 of TAK-071 M1R agonist activities is 520 nM. The muscarinic M1 receptor (M1R) is a promising target for treating cognitive impairment associated with cholinergic deficits in disorders such as Alzheimer’s disease and schizophrenia.

PD173212 is a novel, potent and selective small molecule N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.

Tradipitant (formerly also known as VLY-686 and LY-686017) is novel, potent and 2nd generation neurokinin-1 (NK-1) receptor antagonist, which showed activity in preclinical anxiety models. LY686017 has the potential for treating alcoholism. LY686017 can be also served as a suitable chemical platform for future imaging ligand development.

Imiglitazar (also known as TAK559; proposed tradename Pargluva) is a novel, potent and dual human peroxisome proliferator-activated receptor PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM and with hypoglycemic activity. Muraglitazar had completed phase III clinical trials, however in May, 2006 Bristol-Myers Squibb announced that it had discontinued further development.. Data […]