Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C13H22N6 |
Molecular Weight | 262.354 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN[C@@H]1CCN(C1)C2=NC(N)=NC(NCC3CC3)=C2
InChI
InChIKey=ISBHYKVAFKTATD-SNVBAGLBSA-N
InChI=1S/C13H22N6/c1-15-10-4-5-19(8-10)12-6-11(17-13(14)18-12)16-7-9-2-3-9/h6,9-10,15H,2-5,7-8H2,1H3,(H3,14,16,17,18)/t10-/m1/s1
PF-03893787 is potent and selective histamine H4 receptor (H4R) antagonist. It has comparable binding affinity to the human histamine H3 receptor. PF-03893787 was found to have significant affinity for the hERG channel. Novartis initiates a phase II extension trial in Atopic dermatitis. Studies exploring the utility of PF-3893787 in patients would be reported in due course, being the potential indications of asthma, pruritus, inflammatory skin diseases and pain, among others.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist. | 2011 Nov 1 |
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Is the H4 receptor a new drug target for allergies and asthma? | 2013 Jan 1 |
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A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787. | 2013 May 1 |
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Molecularly targeted therapies for asthma: Current development, challenges and potential clinical translation. | 2016 Oct |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23276980
5, 15, 50 mg, QD for 14 days
Route of Administration:
Oral
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)