Benzoylaconine is a novel and potent aconitine-type diterpenoid alkaloid

VU0467154 (VU-0467154) is a novel and potent M4 PAM (positive allosteric modulator) with the potential to be used as a novel approach for the treatment of psychotic symptoms associated with schizophrenia and other neuropsychiatric disorders. Acting on muscarinic acetylcholine receptor (mAChR). VU0467154 exhibits robust APD-like and cognitive enhancing activity in rodents. Selective M4 PAMs could […]

Quebrachitol is a naturally occurring cyclic polyol found in many plants such as Allophylus edulis, Cannabis sativa, Paullinia pinnata and seabuckthorn. It regulates the Wnt/β-catenin signaling pathway.It can be used for making bioactive materials such as antifungal (E)-β-methoxyacrylate and oudemansin X.

Basimglurant (RG7090; RO491752) is a potent, selective and orally bioavailable mGlu5 negative allosteric modulator with a Kd of 1.1 nM. It is under Phase 2 clinical trial for treating MDD and Fragile X syndrome (FXS). Basimglurant is a promising novel medicine for psychiatric diseases. Basimglurant has favorable drug-like properties, a differentiated molecular mechanism of action, […]

Axitinib sulfoxide (also known as AG-028458; PF-03482595) is a primary and S-oxidized metabolite of Axitinib, an investigational anticancer drug. Axitinib (AG013736 and Inlyta) is a potent, orally bioavailable, small molecule and multi-targeted inhibitor TKI (tyrosine kinase inhibitor) that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 […]

NB-598 is a novel, highly potent and competitive inhibitor of squalene epoxidase (SE), suppressing triglyceride biosynthesis through the farnesol pathway. NB-598 significantly inhibited both basal and glucose-stimulated insulin secretion from mouse pancreatic islets. CaV channels were markedly inhibited by NB-598.

(R)-Carisbamate, the R-enantiomer of Carisbamate (YKP-509; Comfyde), is a potent anticonvulsant/antiepileptic agent. Reference: J Clin Pharmacol. 2012 Sep;52(9):1420-9.

Arginase inhibitor 1 is a novel, potent and selective inhibitor of human arginases I and II (IC50s = 223 and 509 nM, respectively) with the potential for treatment of myocardial reperfusion injury.

Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analogue of GnRH. Nafarelin increases the release of FSH and LH by the anterior pituitary, which in turn leads to an increase of estrogen/progesterone. When administered, Nafarelin has the purpose of causing increase estrogen that will negatively feed back upon hypothalamus to decrease […]

Valrocemide, formerly known as TV-1901, is an antiepileptic drug (AED). Valrocemide has a broad spectrum of anticonvulsant activity and promising potential as a new AED. Valrocemide is an anticonvulsant agent under development by Teva and Acorda as a potential therapeutic for the treatment of epilepsy.