Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor affinity antagonist (Ki=2.4 nM) and a functional H4 receptor antagonist (Ki=1.56 nM).
Adriforant is tested and observed binding K i =2.4 nM and functional K i =1.56 nM for H4R. Data from functional assays produce convergent projections of the free plasma efficacious concentration and Adriforant (Compound 13) is fast on/fast off on rhH4R.
Ki: 2.4 nM (H4R bind), 1.56 nM (H4R func)
[1] Mowbray CE, et al. Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6596-602. DOI:
10.1016/j.bmcl.2011.07.125
