Molecule Details
InChIKeyRPYWXZCFYPVCNQ-RVDMUPIBSA-N
Compound Name(3E)-3-((2,4-Dimethoxyphenyl)methylene)-3,4,5,6-tetrahydro-2,3'-bipyridine
Canonical SMILESCOc1ccc(/C=C2\CCCN=C2c2cccnc2)c(OC)c1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)3
Pfam Stratification Homologous
Avg pChEMBL7.13
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB05708
Drug NameGTS-21
CAS Number148372-04-7
Groups investigational
ATC Codes nan
DescriptionGTS-21 (also known as DMBX-A), is a novel, small-molecule, orally active and selective alpha-7 nicotinic acetylcholine (nACh) receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials. Athenagen licensed the exclusive rights to the compound and a relat...

Categories: Benzene Derivatives Cholinergic Agents Cholinergic Agonists Cytochrome P-450 CYP1A2 Substrates Cytochrome P-450 CYP2E1 Substrates Cytochrome P-450 Substrates Neurotransmitter Agents Nicotinic Agonists
Cross-references: BindingDB: 50061564 CHEMBL134713 ChemSpider: 4470526 PDB: ZY7 PubChem:5310985 PubChem:175427027 Wikipedia: GTS-21 ZINC: ZINC000000000860
Target Activities (3)
Target Gene Organism Category Pfam pChEMBL Type Source
P17787 CHRNB2 Homo sapiens Human PF02931 PF02932 7.3 Ki ChEMBL
P43681 CHRNA4 Homo sapiens Human PF02931 PF02932 7.3 Ki ChEMBL;BindingDB
P36544 CHRNA7 Homo sapiens Human PF02931 PF02932 6.8 Kd ChEMBL;BindingDB
DrugBank Target Actions (3)
Target Gene Target Name Action Type
P05177 CYP1A2 Cytochrome P450 1A2 substrate enzymes
P05181 CYP2E1 Cytochrome P450 2E1 substrate enzymes
P36544 CHRNA7 Neuronal acetylcholine receptor subunit alpha-7 agonist targets