encenicline   Click here for help

GtoPdb Ligand ID: 6926

Synonyms: EVP 6124 | EVP-6124 | EVP6124
PDB Ligand
Compound class: Synthetic organic
Comment: This compound was developed as part of EnVivo Pharmaceuticals alpha-7 agonist program [3]. The compound exhibits good brain penetration and an adequate exposure time for clinical utility [3].
EnVivo changed its name to FORUM Pharmaceuticals Inc. in April 2014.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 3
Hydrogen bond donors 1
Rotatable bonds 3
Topological polar surface area 60.58
Molecular weight 320.08
XLogP 2.87
No. Lipinski's rules broken 0
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Canonical SMILES O=C(c1cc2c(s1)c(Cl)ccc2)NC1CN2CCC1CC2
Isomeric SMILES O=C(c1cc2c(s1)c(Cl)ccc2)N[C@H]1CN2CCC1CC2
InChI InChI=1S/C16H17ClN2OS/c17-12-3-1-2-11-8-14(21-15(11)12)16(20)18-13-9-19-6-4-10(13)5-7-19/h1-3,8,10,13H,4-7,9H2,(H,18,20)/t13-/m0/s1
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Summary of Clinical Use Click here for help
Encenicline is being assessed in several Phase 3 clinical trials as a potential treatment for imapired cognition in schizophrenia and in Alzheimer's disease.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
EVP-6124 is a selective, potent, brain penetrant oral compound that enhances synaptic transmission in the brain and acts as a co-agonist in combination with Acetylcholine (ACh) to enhance cognition [3]