U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
Structure of ADRIFORANT

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

HIDE SMILES / InChI
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.

Approval Year

PubMed

PubMed

TitleDatePubMed
Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
2011 Nov 1
Is the H4 receptor a new drug target for allergies and asthma?
2013 Jan 1
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
Molecularly targeted therapies for asthma: Current development, challenges and potential clinical translation.
2016 Oct

Sample Use Guides

5, 15, 50 mg, QD for 14 days
Route of Administration: Oral
Name Type Language
ADRIFORANT
USAN   INN  
Official Name English
ZPL389-NX
Code English
NVP-ZPL389-NX
Code English
N4-(Cyclopropylmethyl)-6-[(3R)-3-(methylamino)pyrrolidin-1-yl]pyrimidine-2,4-diamine
Systematic Name English
ZPL-389-NX
Code English
PF-3893787
Code English
Adriforant [WHO-DD]
Common Name English
PF-03893787
Code English
ADRIFORANT [USAN]
Common Name English
adriforant [INN]
Common Name English
2,4-PYRIMIDINEDIAMINE, N4-(CYCLOPROPYLMETHYL)-6-((3R)-3-(METHYLAMINO)-1-PYRROLIDINYL)-
Systematic Name English
ZPL-3893787
Code English
ZPL-389
Code English
Code System Code Type Description
EVMPD
SUB194074
Created by admin on Sat Dec 16 10:22:17 GMT 2023 , Edited by admin on Sat Dec 16 10:22:17 GMT 2023
PRIMARY
FDA UNII
D65H9YE9VU
Created by admin on Sat Dec 16 10:22:17 GMT 2023 , Edited by admin on Sat Dec 16 10:22:17 GMT 2023
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PUBCHEM
24745335
Created by admin on Sat Dec 16 10:22:18 GMT 2023 , Edited by admin on Sat Dec 16 10:22:18 GMT 2023
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NCI_THESAURUS
C169765
Created by admin on Sat Dec 16 10:22:17 GMT 2023 , Edited by admin on Sat Dec 16 10:22:17 GMT 2023
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USAN
HI-100
Created by admin on Sat Dec 16 10:22:18 GMT 2023 , Edited by admin on Sat Dec 16 10:22:18 GMT 2023
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ChEMBL
CHEMBL1915540
Created by admin on Sat Dec 16 10:22:17 GMT 2023 , Edited by admin on Sat Dec 16 10:22:17 GMT 2023
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INN
10855
Created by admin on Sat Dec 16 10:22:17 GMT 2023 , Edited by admin on Sat Dec 16 10:22:17 GMT 2023
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CAS
943057-12-3
Created by admin on Sat Dec 16 10:22:17 GMT 2023 , Edited by admin on Sat Dec 16 10:22:17 GMT 2023
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DRUG BANK
DB15027
Created by admin on Sat Dec 16 10:22:17 GMT 2023 , Edited by admin on Sat Dec 16 10:22:17 GMT 2023
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SMS_ID
100000178346
Created by admin on Sat Dec 16 10:22:18 GMT 2023 , Edited by admin on Sat Dec 16 10:22:18 GMT 2023
PRIMARY