General
Preferred name
RG-4733
Synonyms
RO4929097 ()
Ro 4929097 ()
RO-4929097 ()
R-4733 ()
RO 4929097 ()
Ro4929097 ()
Rg 4733 ()
P&D ID
PD025575
CAS
847925-91-1
47925-91-1
Tags
available
drug candidate
Drug indication
Breast cancer
non-small cell lung carcinoma
Drug Status
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION RO4929097 as an inhibitor of γ-secretase, was originally developed for Alzheimer's disease but based on its ability to inhibit the NOTCH pathway it was investigated as a therapeutic strategy against melanoma and other tumours . (GtoPdb)
DESCRIPTION RO4929097 (RG-4733) is an orally active ¦Ã secretase inhibitor with an IC50 of 4 nM, inhibiting cellular processing of A¦Â40 and Notch with EC50 of 14 nM and 5 nM, respectively[1].
PRICE 194
DESCRIPTION RO4929097 (RG-4733), a ?? secretase inhibitor (IC50: 4 nM), inhibits cellular processing of A??40 and Notch (EC50: 14/5 nM).
DESCRIPTION inhibitor of gamma-secretase (Informer Set)
DESCRIPTION RO4929097, a small-molecule inhibitor of γ secretase (IC50 = 4 nM, EC50 = 5 nM), inhibits cellular processing of Aβ40 (EC50 = 14 nM) and Notch (EC50 = 5 nM). It was shown to decrease the levels of Notch transcriptional target HES1 in human primary melanoma cell lines. (BOC Sciences Bioactive Compounds)
DESCRIPTION RO4929097 (RG-4733), a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM). (TargetMol Bioactive Compound Library)
Compound Sets
16
AdooQ Bioactive Compound Library
A10802
Axon Medchem Screening Library
2521
BOC Sciences Bioactive Compounds
ro4929097-cas-847925-91-1-item-286388
Cayman Chemical Bioactives
19996
ChEMBL Drugs
CHEMBL4297422
Drug Repurposing Hub
DrugBank
DB11870
DrugMAP
DMXA6B3
EU-OPENSCREEN Bioactive Compound Library
EOS101277
Guide to Pharmacology
7338
Informer Set
687577
MedChem Express Bioactive Compound Library
HY-11102
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
RO4929097
TargetMol Bioactive Compound Library
T6274
External IDs
40
Properties
(calculated by RDKit )
Molecular Weight
469.14
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
3
Rotatable Bonds
5
Ring Count
3
Aromatic Ring Count
2
cLogP
3.8
TPSA
87.3
Fraction CSP3
0.32
Chiral centers
1.0
Largest ring
7.0
QED
0.46
QED
0.46
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
APH1A
NCSTN
PSEN1
PSENEN
¦Ã-secretase
Aβ40
Notch
γ secretase
γ-secretase
??secretase
?-Secretase inhibitor
Beta Amyloid,Notch,Secretase
Compound status
clinical
MOA
Gamma-secretase
gamma-Secretase Inhibitors
Drugs Acting on Notch Receptors
gamma secretase inhibitor
Member status
member
Pathway
Neuronal Signaling
Stem Cell/Wnt
Neuroscience
Proteases/Proteasome
Stem Cells
Solubility
Soluble to 49 mg/mL in DMSO.
Source data