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
| Molecular Formula | C13H22N6 |
| Molecular Weight | 262.354 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
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 |
|
| 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 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 10:22:17 GMT 2023
by
admin
on
Sat Dec 16 10:22:17 GMT 2023
|
| Record UNII |
D65H9YE9VU
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Code | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
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 | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
TARGET -> INHIBITOR | |||
|
|
SALT/SOLVATE -> PARENT |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
ACTIVE MOIETY |
Originator: Pfizer; Developer: Pfizer, Ziarco; Class: Anti-inflammatory, Antiasthmatic, Pyrimidine, Pyrrolidine, Small molecule; Mechanism of Action: Histamine H4 receptor antagonist; Highest Development Phases: Phase II for Atopic dermatitis, Plaque psoriasis, Discontinued for Asthma; Most Recent Event: 13 Jun 2016 Final efficacy data from a phase IIb trial in Atopic dermatitis released by Ziarco Pharma, 16 May 2016 Ziarco Pharma plans a phase IIb trial in Atopic dermatitis, 16 May 2016 Top-line efficacy and adverse events data from a phase IIa trial in Atopic dermatitis released by Ziarco Pharma
|
