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
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
| 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 |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/22542656
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 |
|---|---|---|---|
Target ID: CHEMBL2337 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22542656 |
92.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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. | 2012-06-15 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22542656
Rats were given ASP-2535 at a dose of 0.1-3 mg/kg
Route of Administration:
Oral
| Substance Class |
Chemical
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ASP-2535
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PRIMARY | ASP 2535: Cat. No. 5308Biological Activity: Potent and selective GlyT1 inhibitor (IC50 = 92 nM). Exhibits 50-fold selectivity over GlyT2. Attenuates MK 801-induced working memory deficits and PCP-induced visual learning deficits in mice. Orally available and brain penetrant. | ||
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| Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
IC50
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Originator: Astellas Pharma; Class: Antidementia, Antipsychotic; Highest Development Phases: Discontinued for Alzheimer's disease, Schizophrenia; Most Recent Events: 29 May 2009 Discontinued - Phase-I for Schizophrenia in Japan (PO), 29 May 2009 Discontinued - Phase-I for Alzheimer's disease in Japan (PO), 29 Aug 2008 Phase-I clinical trials in Schizophrenia in Japan (PO)
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