General
Preferred name
TRACAZOLATE
Synonyms
Ici-136,753 ()
Tracazolate hydrochloride ()
Tracazolate (hydrochloride) ()
ICI 136753 (hydrochloride) ()
ICI 136,753 ()
ICI-136753 ()
Tracazolato ()
P&D ID
PD002816
CAS
1135210-68-2
41094-88-6
Tags
available
drug candidate
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
Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for ¦Â3 and potentiates ¦Á1¦Â1¦Ã2s (EC50=13.2 ¦ÌM), ¦Á1¦Â3¦Ã2 (EC50=1.5 ¦ÌM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (¦Ã1-3, ¦Ä, ¦Å) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity[1][2].
PRICE
75
DESCRIPTION
Tracazolate hydrochloride (Tracazolate (hydrochloride)) is a modulator of the GABAA receptor with anxiolytic and anticonvulsant activity. Tracazolate hydrochloride potentiates ??1??1??2s and ??1??3??2 with EC50s of 13.2 ??M and 1.5 ??M.
DESCRIPTION
Tracazolate has anxiolytic and anticonvulsant activities. It modulates the activity of GABAA receptors containing δ subunits , in addition to interacting with adenosine receptors and phosphodiesterases .
(GtoPdb)
DESCRIPTION
GluN2B-selective NMDA antagonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Subtype-selective GABAA allosteric modulator
(Tocriscreen Total)
DESCRIPTION
Tracazolate hydrochloride is a subtype-selective GABAA receptor modulator that potentiates or inhibits recombinant GABAA function depending on subunit combination. Tracazolate hydrochloride enhances native GABAA receptor function, and exhibits anxiolytic activity following systemic administration in vivo.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Tracazolate hydrochloride (Tracazolate (hydrochloride)) is a modulator of the GABAA receptor with anxiolytic and anticonvulsant activity. Tracazolate hydrochloride potentiates α1β1γ2s and α1β3γ2 with EC50s of 13.2 μM and 1.5 μM.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Non-benzodiazepine anxiolytic which has a high differential between sedative and anxiolytic doses
(LOPAC library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
2
Compound Sets
15
BOC Sciences Bioactive Compounds
ChEMBL Drugs
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugMatrix
Guide to Pharmacology
Ki Database
LOPAC library
MedChem Express Bioactive Compound Library
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
32
Molecular Weight
304.19
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
7
Ring Count
2
Aromatic Ring Count
2
cLogP
3.15
TPSA
69.04
Fraction CSP3
0.56
Chiral centers
0.0
Largest ring
6.0
QED
0.63
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
GABAA
GABRA1
GABA Receptor
Primary Target
GABAA Receptors
MOA
Modulator
GABA Receptor modulator
Pathway
Membrane Transporter/Ion Channel
Neuroscience
Neuronal Signaling
Source data
