Drug General Information
Drug ID
D02JOH
Former ID
DNCL001969
Drug Name
BMS-708163
Synonyms
Avagacestat
Drug Type
Small molecular drug
Indication Alzheimer disease [ICD9: 331; ICD10:G30] Phase 2 [522650], [541623]
Company
Bristol-Myers Squibb
Structure
Download
2D MOL

3D MOL

Formula
C20H17ClF4N4O4S
InChI
InChI=1S/C20H17ClF4N4O4S/c21-14-3-5-15(6-4-14)34(31,32)29(17(18(26)30)7-8-20(23,24)25)10-13-2-1-12(9-16(13)22)19-27-11-33-28-19/h1-6,9,11,17H,7-8,10H2,(H2,26,30)/t17-/m1/s1
InChIKey
XEAOPVUAMONVLA-QGZVFWFLSA-N
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) Gamma-secretase Target Info Modulator [532002]
KEGG Pathway Notch signaling pathway
Alzheimer's disease
PANTHER Pathway Alzheimer disease-amyloid secretase pathway
Alzheimer disease-presenilin pathway
Notch signaling pathway
Pathway Interaction Database Notch signaling pathway
Presenilin action in Notch and Wnt signaling
p75(NTR)-mediated signaling
Syndecan-3-mediated signaling events
Reactome Nuclear signaling by ERBB4
Regulated proteolysis of p75NTR
NRIF signals cell death from the nucleus
Activated NOTCH1 Transmits Signal to the Nucleus
Constitutive Signaling by NOTCH1 PEST Domain Mutants
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
NOTCH2 Activation and Transmission of Signal to the Nucleus
EPH-ephrin mediated repulsion of cells
WikiPathways Notch Signaling Pathway
Signaling by ERBB4
Signaling by NOTCH3
Signaling by NOTCH4
Signaling by NOTCH1
Signaling by NOTCH2
Notch Signaling Pathway
Signalling by NGF
References
Ref 522650ClinicalTrials.gov (NCT00890890) A Multicenter, Double Blind, Placebo-Controlled, Safety and Tolerability Study of BMS-708163 in Patients With Prodromal Alzheimer's Disease. U.S. National Institutes of Health.
Ref 541623(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6489).
Ref 532002Safety and tolerability of the gamma-secretase inhibitor avagacestat in a phase 2 study of mild to moderate Alzheimer disease. Arch Neurol. 2012 Nov;69(11):1430-40.

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