ASP-2535

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H18N6O
Molecular Weight	382.4179
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)C1=NN=C(N1C2=CC=CC3=NON=C23)C4=CC=C(N=C4)C5=CC=CC=C5

InChI

InChIKey=FQGLDGKVKDPVLO-UHFFFAOYSA-N

InChI=1S/C22H18N6O/c1-14(2)21-24-25-22(28(21)19-10-6-9-18-20(19)27-29-26-18)16-11-12-17(23-13-16)15-7-4-3-5-8-15/h3-14H,1-2H3

HIDE SMILES / InChI

Molecular Formula	C22H18N6O
Molecular Weight	382.4179
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22542656

ASP-2535 is a glycine transporter-1 (GlyT1) inhibitor which was developed by Astellas Pharma for the treatment of Schizophrenia and Alzheimer's disease. Although ASP-2535 was shown to improve cognitive impairment in animal models, it is no longer in the company pipeline.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Glycine transporter 1 7 Target ID: CHEMBL2337 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22542656	Inhibitor 8297		92.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Alzheimer’s disease 272 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22542656	Primary		Preclinical	Unknown Approved Use Unknown
Schizophrenia 298 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22542656	Primary		Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
A novel glycine transporter-1 (GlyT1) inhibitor, ASP2535 (4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole), improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's disease.	2012 Jun 15	22542656

Patents

Sample Use Guides

In Vivo Use Guide

Rats were given ASP-2535 at a dose of 0.1-3 mg/kg

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Sat Dec 16 11:40:29 GMT 2023` Edited by `admin` on `Sat Dec 16 11:40:29 GMT 2023`
Record UNII	6627LI8F9K
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

ASP-2535

Common Name

English

2,1,3-BENZOXADIAZOLE, 4-(3-(1-METHYLETHYL)-5-(6-PHENYL-3-PYRIDINYL)-4H-1,2,4-TRIAZOL-4-YL)-

Systematic Name

English

4-(3-(1-METHYLETHYL)-5-(6-PHENYL-3-PYRIDINYL)-4H-1,2,4-TRIAZOL-4-YL)-2,1,3-BENZOXADIAZOLE

Systematic Name

English

Code System Code Type Description

PUBCHEM

9800113