General
Preferred name
TC-N 22A
Synonyms
PMID21688779C22a ()
compound 22a [PMID: 21688779] ()
P&D ID
PD046216
CAS
1314140-00-5
1235325-16-2
Tags
available
drug candidate
Drug indication
Discovery agent
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE 271
DESCRIPTION TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 ??M). TC-N 22A can be used in the study of central nervous system diseases.
DESCRIPTION TC-N 22A is a potent and selective mGlu4 receptor positive allosteric modulator (EC50 = 9 nM in human mGlu4-expressing BHK cells) with selectivity over mGlu1, mGlu2, mGlu3, mGlu5 and mGlu7 receptors (EC50 > 10 μM). TC-N 22A is used for the treatment of Parkinson's disease, anxiety and pain. (BOC Sciences Bioactive Compounds)
DESCRIPTION TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases. (TargetMol Bioactive Compound Library)
DESCRIPTION Positive allosteric modulator of mGlu4 receptors (Tocris Bioactive Compound Library)
Compound Sets
7
BOC Sciences Bioactive Compounds
tc-n-22a-cas-1314140-00-5-item-170466
DrugMAP
DMEBM19
EUbOPEN Chemogenomics Library
EUB0000490
Guide to Pharmacology
6231
Novartis Chemogenetic Library (NIBR MoA Box)
TargetMol Bioactive Compound Library
T23440
Tocris Bioactive Compound Library
4370
External IDs
13
Properties
(calculated by RDKit )
Molecular Weight
283.09
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
4
Aromatic Ring Count
3
cLogP
3.16
TPSA
66.49
Fraction CSP3
0.21
Chiral centers
0.0
Largest ring
7.0
QED
0.76
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
mGluR4
Primary Target
Glutamate (Metabotropic) Group III Receptors
MOA
Modulator
MGLUR4 positive allosteric modulator
Member status
member
Pathway
Neuroscience
Recommended Cell Concentration
100 nM
Source data