Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H13FN2 |
Molecular Weight | 240.2755 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC(C)=C(N)C(=N1)C#CC2=CC(F)=CC=C2
InChI
InChIKey=MEDCLNYIYBERKO-UHFFFAOYSA-N
InChI=1S/C15H13FN2/c1-10-8-11(2)18-14(15(10)17)7-6-12-4-3-5-13(16)9-12/h3-5,8-9H,17H2,1-2H3
ADX 10059 is a first-in-class reflux inhibitor that works by reducing activation of the metabotropic glutamate receptor 5 (mGluR5) through negative allosteric modulation (NAM). This approach may lead to a new class of drugs that addresses the causes of GERD rather than just the symptoms. ADX 10059 is a potent selective NAM of the mGluR5, with
an IC50 of 17.1 nM on hmGluR5 showing good selectivity
compared with > 65 other receptors, transporters, ion
channels and enzymes. ADX 10059 completed Phase IIb testing in gastroesophageal reflux disease (GERD) and migraine prevention, demonstrated significant potential in a non-human primate model of Parkinson's disease levodopa induced dyskinesia (PD-LID). However, Addex Pharmaceuticals announced the discontinuation of development of ADX 10059 in December 2009 due to liver enzyme changes.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3227 Sources: https://gut.bmj.com/content/58/9/1192 |
17.1 nM [IC50] | ||
Target ID: CHEMBL3227 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19460767 |
17.1 nM [IC50] |
Sample Use Guides
ADX 10059 120 mg twice-daily given for two weeks was well tolerated and the tolerability profile seen is compatible with use in the treatment of GERD.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20218930
ADX 10059 is a potent selective NAM of the mGluR5, with
an IC50 of 17.1 nM on hmGluR5 showing good selectivity
compared with > 65 other receptors, transporters, ion
channels and enzymes
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NCI_THESAURUS |
C241
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
C152157
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY | |||
|
DTXSID40226707
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY | |||
|
10331863
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY | |||
|
DB05070
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY | |||
|
Raseglurant
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY | |||
|
300000034427
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY | |||
|
757950-09-7
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY | |||
|
9179
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY | |||
|
66UCJ8Z8L1
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY | |||
|
CHEMBL3545036
Created by
admin on Fri Dec 15 16:47:02 GMT 2023 , Edited by admin on Fri Dec 15 16:47:02 GMT 2023
|
PRIMARY |
ACTIVE MOIETY