General
Preferred name
ETAZOLATE
Synonyms
1-Ethyl-4-(isopropylidenehydrazino)-1h-pyrazolo (3,4-b) pyridine-5-carboxylic acid, ethyl ester hydrochloride ()
ETAZOLATE HYDROCHLORIDE ()
Etazolate (hydrochloride) ()
SQ 20009 ()
EHT 0202 (hydrochloride) ()
SQ-20009 ()
EHT-0202 ()
Etazolato ()
Etazolate hcl ()
NSC-163611 ()
SO 20009 ()
P&D ID
PD013531
CAS
51022-77-6
35838-58-5
Tags
drug candidate
available
Drug indication
Alzheimer disease
Neurodegenerative disorder
Drug Status
investigational
Max Phase
2.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Has anxiolytic effects as positive allosteric modulator of the GABAA receptor at the barbiturate binding site, as an adenosine antagonist of the A1 and A2 receptor subtypes and as a phosphodiesterase inhibitor selective for the PDE4 isoform. It is currently in clinical trials for the treatment of Alzheimer's disease with a possible MMOA of upregulating alpha-secretase activity.
(GtoPdb)
DESCRIPTION
Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 ¦ÌM. Etazolate hydrochloride is a ¦Ã-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an ¦Á-secretase activator and induced the production of soluble amyloid precursor protein (sAPP¦Á). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects[1][2][3][4][5].
DESCRIPTION
Phosphodiesterase inhibitor
(LOPAC library)
DESCRIPTION
PDE4 inhibitor
(Tocriscreen Total)
DESCRIPTION
Etazolate hydrochloride is a phosphodiesterase inhibitor with selectivity for PDE4 (IC50 = 2.0 μM).
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
15
BOC Sciences Bioactive Compounds
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugMAP
DrugMatrix
Guide to Pharmacology
LOPAC library
MedChem Express Bioactive Compound Library
NPC Screening Collection
ReFrame library
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
47
Molecular Weight
289.15
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
2
Aromatic Ring Count
2
cLogP
2.44
TPSA
81.4
Fraction CSP3
0.43
Chiral centers
0.0
Largest ring
6.0
QED
0.52
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
Phosphodiesterase
Target
GABRB3, PDE4A
GABA Receptor
Phosphodiesterase (PDE)
MOA
phosphodiesterase inhibitor
Pathway
Membrane Transporter/Ion Channel
Metabolic Enzyme/Protease
Neuronal Signaling
Source data
