PF-3893787 (also known as Adriforant; ZPL-3893787; PF-3893787 and ZPL-389) is a novel and potent histamine H4 receptor antagonist with Ki of 2.4 nM and it is also a functional antagonist with Ki of 1.56 nM. Adriforant shows an excellent in vitro profile that warrants their further investigation in relevant models of human disease. Histamine H4 […]
PF-06795071 is a novel, potent, selective and covalent MAGL (Monoacylglycerol lipase) inhibitor with an IC50 of 3 nM and with en excellent CNS exposure. Monoacylglycerol lipase (MAGL) inhibition provides a potential treatment approach to neuroinflammation through modulation of both the endocannabinoid pathway and arachidonoyl signaling in the central nervous system (CNS). PF-06795071 is a MAGL […]
THZ1-R is a novel and non-cysteine reactive analog of THZ1 which shows lower activity for CDK7 inhibition with a Kd of 142 nM for binding to CDK7. THZ1 is a novel, potent, selective and covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, […]
Photo-lysine HCl is a novel lysine-based photo-reactive amino acid, which captures proteins that bind lysine post-translational modifications. Post-translational modifications (PTMs) have key roles in regulating protein-protein interactions in living cells. However, it remains a challenge to identify these PTM-mediated interactions. Photo-lysine, which is readily incorporated into proteins by native mammalian translation machinery, can be used […]
CP-28888 (CP-28,888-27) is a novel and potent interferon inducer, it is more potent in mice, but is less active in man and devoid of antirhinovirus effects. CP-28,888-27 and placebo nasal sprays were compared in 62 normal volunteers challenged with rhinovirus type 13 or 21 in two randomized, double-blind studies. Half of the subjects received CP-28,888-27 […]
Zilpaterol, the hydrochloride salt of Zilpatero, is a novel and potent β-adrenergic receptor (AR) agonist used to increase the size of cattle and the efficiency of feeding them.
CP 375 is a novel and potent Fe3+ chelating agent with a log K1 value of 14.50 and with the absolute deviation between the predicted and experimental values of 0.12 (14.62 vs. 14.50)
Carboprost (Hemabate, Tham) is a synthetic prostaglandin analogue of PGF2α (specifically, it is 15-methyl-PGF2α) with oxytocic properties. Carboprost main use is in the obstetrical emergency of postpartum hemorrhage which reduces postpartum bleeding during these circumstances. It is used in postpartum hemorrhage caused by uterine atony not controlled by other methods. One study has shown that […]
CP-409092 HCl, the hydrochloride salt of CP-409092, is a novel and potent partial agonist of GABAA receptor with potential anti-anxiety activity.
ABT-670 is a novel, potent, selective, orally bioavailable agonist of dopamine D4 receptor with EC50 of 89 nM, 160 nM, and 93 nM for human D4, ferret D4, and rat D4, respectively. It was discovered from a study aiming to identify a structurally distinct D(4)-selective agonist with superior oral bioavailability to the first-generation clinical candidate 1a (ABT-724) for […]